JP2021080270A - Composition comprising xanthophyll and processed trapaceae plant - Google Patents
Composition comprising xanthophyll and processed trapaceae plant Download PDFInfo
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- JP2021080270A JP2021080270A JP2021023833A JP2021023833A JP2021080270A JP 2021080270 A JP2021080270 A JP 2021080270A JP 2021023833 A JP2021023833 A JP 2021023833A JP 2021023833 A JP2021023833 A JP 2021023833A JP 2021080270 A JP2021080270 A JP 2021080270A
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Abstract
Description
本発明は、1)キサントフィル又はその塩及びヒシ属植物の加工物を含有する新規の組成物、2)ヒシ属植物の加工物を含有する新規の眼科用組成物、及び3)ルテイン又はその塩を含有する眼科用組成物の新規用途に関する。本発明の組成物は、視機能低下等の予防及び/又は改善並びに眼疾患等の予防及び/又は治療に使用できる。 The present invention relates to 1) a novel composition containing xanthophyll or a salt thereof and a processed product of a Trapa plant, 2) a novel ophthalmic composition containing a processed product of a Trapa plant, and 3) lutein or a salt thereof. Relevant to new uses of ophthalmic compositions containing The composition of the present invention can be used for prevention and / or improvement of visual function deterioration and the like and prevention and / or treatment of eye diseases and the like.
パソコン、インターネット、スマートフォン等の普及に伴い、目の疲れ(眼疲労)やそれに伴う全身的な疲労(眼精疲労)を訴える人が増加している。また、老視、白内障、緑内障、加齢性黄斑変性、糖尿病網膜症等の、加齢や眼疾患に伴う視機能低下は、QOL(Quality of Life)を著しく低下させる原因となることから、深刻な社会問題となっている。そのため、目又は目に起因するトラブル(眼精疲労、眼の老化、それらに起因する各種疾患)を訴える人が年々増加しており、視機能を維持し、目又は目に起因するトラブルを予防又は改善するサプリメントや目又は目に起因するトラブルを治療する医薬のニーズも増大している。 With the widespread use of personal computers, the Internet, smartphones, etc., an increasing number of people are complaining of eye fatigue (eye strain) and associated systemic fatigue (eye strain). In addition, deterioration of visual function associated with aging and eye diseases such as presbyopia, cataract, glaucoma, age-related macular degeneration, and diabetic retinopathy is serious because it causes a significant decrease in QOL (Quality of Life). It has become a social problem. Therefore, the number of people who complain of troubles caused by eyes or eyes (eye strain, aging of eyes, various diseases caused by them) is increasing year by year, and the visual function is maintained to prevent troubles caused by eyes or eyes. There is also an increasing need for supplements that improve or medicines that treat eyes or eye problems.
特に、老視は、加齢やパソコン、インターネット、スマートフォン等のITツールの長時間にわたる極度の使用等に伴う、水晶体の老化(水晶体の混濁(白濁)、硬化等)により、水晶体の弾性が失われる等して、目のピント調節機能がそこなわれ、目の疲れ、かすみ、肩こり等の自覚症状を伴う目又は目に起因する代表的なトラブルの一つである。 In particular, presbyopia loses its elasticity due to aging of the crystalline lens (opacity (white turbidity), hardening, etc.) of the crystalline lens due to aging and extreme use of IT tools such as personal computers, the Internet, and smartphones for a long period of time. It is one of the typical troubles caused by eyes or eyes with subjective symptoms such as tired eyes, haze, and stiff shoulders due to impaired eye focus adjustment function.
キサントフィルは、カロテノイド由来の色素であり、ルテイン、アスタキサンチン、ゼアキサンチン、メソゼアキサンチン等を含む化合物が知られている。また、これらキサントフィルは、ヒトの体内で生合成ができないので、ヒトはキサントフィルを食物等から摂取する必要がある。さらに、キサントフィルは、眼の調節機能障害や眼精疲労を改善することも知られている(特許文献1)。 Xanthophyll is a carotenoid-derived pigment, and compounds containing lutein, astaxanthin, zeaxanthin, mesozeaxanthin, and the like are known. In addition, since these xanthophylls cannot be biosynthesized in the human body, humans need to ingest xanthophylls from food or the like. Furthermore, xanthophyll is also known to improve accommodation dysfunction and eye strain of the eye (Patent Document 1).
ルテインは、緑黄色野菜に多く含まれるカロテノイドの一種であり、体内の主要なカロテノイドの一つである。ルテインは抗酸化作用を有するが、加齢や紫外線等により消費されるので、日々の食事やサンテルタックス(登録商標)20等のサプリメントを通して継続的に摂取する必要がある(非特許文献1)。さらに、体内のルテインが不足すると白内障、加齢黄斑変性、ドライアイといった様々な眼のトラブルを引き起こす可能性も指摘されている。 Lutein is a type of carotenoid that is abundant in green and yellow vegetables, and is one of the major carotenoids in the body. Although lutein has an antioxidant effect, it is consumed by aging, ultraviolet rays, etc., so it is necessary to take it continuously through daily meals and supplements such as Santeltax (registered trademark) 20 (Non-Patent Document 1). Furthermore, it has been pointed out that lack of lutein in the body may cause various eye problems such as cataract, age-related macular degeneration, and dry eye.
アスタキサンチンは、サケ、イクラ、カニ、エビ、マダイ等に多く含まれるカロテノイドの一種である。アスタキサンチンは、ヘマトコッカス藻が生合成する色素であり、このアスタキサンチンも抗酸化作用を有する。また、アスタキサンチンは、眼精疲労、ブドウ膜炎等の眼炎症性の疾患の改善に有用であることが知られており、多数のサプリメントや化粧品に配合されている。 Astaxanthin is a type of carotenoid that is abundant in salmon, salmon roe, crab, shrimp, red sea bream and the like. Astaxanthin is a pigment biosynthesized by Haematococcus algae, and this astaxanthin also has an antioxidant effect. In addition, astaxanthin is known to be useful for improving eye inflammatory diseases such as eyestrain and uveitis, and is incorporated into many supplements and cosmetics.
ゼアキサンチンは、ルテインと同様にカロテノイドの一種であり、βカロテンに似た脂溶性の物質で、ルテインの構造異性体である。また、ゼアキサンチンはルテインと同様に黄斑に多く存在するという事から、ゼアキサンチンもルテインと同様に黄斑を保護する働きがあるといわれている。 Zeaxanthin, like lutein, is a type of carotenoid, a fat-soluble substance similar to β-carotene, and a structural isomer of lutein. In addition, since zeaxanthin is abundant in the macula like lutein, it is said that zeaxanthin also has a function of protecting the macula like lutein.
メソゼアキサンチンは、ルテインの代謝物質であり、ゼアキサンチンの立体異性体である。また、メソゼアキサンチンはゼアキサンチンと同様の働きがあるといわれている。 Mesozeaxanthin is a metabolite of lutein and is a stereoisomer of zeaxanthin. In addition, mesozeaxanthin is said to have the same function as zeaxanthin.
ヒシ属植物の果皮を熱水抽出したヒシ属植物の抽出物、特にトウビシ抽出物は、ヒシエキスと呼ばれ糖化抑制作用を有することが知られている(特許文献2)。糖化作用により生じる終末糖化産物(AGEs:Advanced Glycation End−products)は、コラーゲン、エラスチン等の生体タンパク質の変性と機能低下を引き起こすことで、様々な老化現象や疾病の発現に関与することも知られている。この糖化作用を抑制することで、生体の老化、特に皮膚の老化の予防が期待されるため、トウビシ抽出物は化粧品等に配合されている。 It is known that an extract of a trapa genus plant obtained by hot water extraction of the peel of a trapa genus plant, particularly a trapa extract, is called a trapa extract and has a saccharification inhibitory effect (Patent Document 2). Advanced glycation end products (AGEs) produced by saccharification are also known to be involved in the development of various aging phenomena and diseases by causing denaturation and functional deterioration of biological proteins such as collagen and elastin. ing. By suppressing this saccharification action, it is expected to prevent the aging of the living body, particularly the aging of the skin. Therefore, the Tobishi extract is blended in cosmetics and the like.
紫外線は波長が10〜400nmの不可視光線の電磁波であり、その波長が280nm未満のものはUV−C、280〜315nmのものはUV−B、315〜400nmのものはUV−Aと呼ばれる。また、紫外線は殺菌消毒、体内でのビタミンDの合成、生体に対する血行、新陳代謝の促進等の有用な作用を有するが、一方でDNA損傷による皮膚がんの誘発、肌のシミの生成、各組織の老化の加速、眼障害等の原因となることも広く知られている。また、パソコン、インターネット、スマートフォン等のITツールからも紫外線が放射されることが知られている。 Ultraviolet rays are invisible electromagnetic waves having a wavelength of 10 to 400 nm, those having a wavelength of less than 280 nm are called UV-C, those having a wavelength of 280 to 315 nm are called UV-B, and those having a wavelength of 315 to 400 nm are called UV-A. In addition, ultraviolet rays have useful effects such as sterilization and disinfection, synthesis of vitamin D in the body, blood circulation to the living body, and promotion of metabolism, but on the other hand, they induce skin cancer due to DNA damage, generate skin stains, and each tissue. It is also widely known that it causes accelerated aging and eye damage. It is also known that ultraviolet rays are emitted from IT tools such as personal computers, the Internet, and smartphones.
しかしながら、キサントフィル又はその塩とヒシ属植物の加工物を組み合わせて使用すること、例えば、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物が、1)紫外線照射により誘発される角膜等の上皮細胞死を抑制すること、2)糖尿病モデルラットの水晶体の混濁(白濁)を抑制すること、3)糖尿病モデルラットの網膜の損傷を抑制又は改善すること、は知られていない。 However, the use of xanthophylls or salts thereof in combination with processed products of Trapa plants, for example, compositions containing xanthophylls or salts thereof and processed products of Trapa plants, 1) cornea induced by ultraviolet irradiation, etc. It is not known to suppress the epithelial cell death of the trapa, 2) to suppress the opacity (white turbidity) of the crystalline lens of the diabetic model rat, and 3) to suppress or improve the damage to the retina of the diabetic model rat.
また、ヒシ属植物の加工物を単独で使用すること、例えば、ヒシ属植物の加工物を含有する組成物が、1)紫外線照射により誘発される角膜等の上皮細胞死を抑制すること、2)糖尿病モデルラットの水晶体の混濁(白濁)を抑制すること、3)糖尿病モデルラットの網膜の損傷を抑制又は改善すること、も知られていない。 In addition, the use of a processed product of the genus Trapa alone, for example, a composition containing the processed product of the genus Trapa suppresses 1) suppression of epithelial cell death of the cornea and the like induced by ultraviolet irradiation, and 2) It is also not known to suppress the opacity (white turbidity) of the crystalline lens of the diabetic model rat, and 3) to suppress or improve the damage to the retina of the diabetic model rat.
さらに、ルテイン又はその塩を単独で使用すること、ルテイン又はその塩を含有する組成物が、紫外線照射により誘発される角膜等の上皮細胞死を抑制することは知られていない。 Furthermore, it is not known that lutein or a salt thereof is used alone, and that a composition containing lutein or a salt thereof suppresses epithelial cell death such as cornea induced by ultraviolet irradiation.
本発明が解決しようとする課題は、1)キサントフィル又はその塩及びヒシ属植物の加工物を含有する新規の組成物及びその眼科用途、2)ヒシ属植物の加工物を含有する新規の眼科用組成物、並びに3)ルテイン又はその塩を含有する眼科用組成物の新規用途を提供することである。 The problems to be solved by the present invention are 1) a novel composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa and its ophthalmic use, and 2) a new ophthalmic use containing a processed product of the genus Trapa. To provide new uses for compositions, as well as 3) ophthalmic compositions containing lutein or salts thereof.
本発明者らは、ルテイン及びヒシエキスの組み合わせ、ヒシエキス単独、又はルテイン単独を使用することによって、角膜上皮細胞死を効果的に抑制すること、水晶体の白濁(混濁)を抑制すること、及び網膜の損傷を抑制または改善することを見出した。すなわち、キサントフィル又はその塩及びヒシ属植物の加工物の組み合わせ、ヒシ属植物の加工物、又はルテイン又はその塩が、眼を構成する角膜、水晶体、網膜等に作用して、視機能低下及びそれに伴う自覚症状の予防、治療又は改善することを見出だして、本発明を完成させた。 By using a combination of lutein and Hishi extract, Hishi extract alone, or lutein alone, we can effectively suppress corneal epithelial cell death, suppress cloudiness (opacity) of the crystalline lens, and retina. It has been found to suppress or ameliorate damage. That is, a combination of xanthophyll or a salt thereof and a processed product of Trapa, a processed product of Trapa, or lutein or a salt thereof acts on the cornea, lens, retina, etc. constituting the eye to reduce visual function and the like. The present invention has been completed by finding prevention, treatment or amelioration of the accompanying subjective symptoms.
すなわち、本発明は、以下に関する。
項1−1.キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物。
項1−2.キサントフィルがルテイン、アスタキサンチン、β−クリプトキサンチン、ゼアキサンチン、メソゼアキサンチン、カンタキサンチン、カプサンチン及びフコキサンチンからなる群より選択される少なくとも一つである、項1−1に記載の組成物。
項1−3.キサントフィルがルテイン、アスタキサンチン、ゼアキサンチン及びメソゼアキサンチンからなる群より選択される少なくとも一つである、項1−1又は1−2に記載の組成物。
項1−4.ヒシ属植物の加工物がツノナシビシ、ヒメビシ、ヒシ、トウビシ、トラパ・ナタンス、オニビシからなる群より選択される少なくとも一つのヒシ属植物の加工物である、項1−1〜1−3のいずれか一項に記載の組成物。
項1−5.ヒシ属植物の加工物がヒシ属植物の果皮の粉砕物又は抽出物である、項1−1〜1−4のいずれか一項に記載の組成物。
項1−6.ヒシ属植物の加工物がヒシ属植物の加工物の総重量に対して、ポリフェノールを0.1〜80重量%で含有する、項1−1〜1−5のいずれか一項に記載の組成物。
項1−7.ルテイン又はその塩とトウビシの加工物を含有する組成物。
項1−8.トウビシの加工物がトウビシの果皮の粉砕物及び/又は抽出物である、項1−7に記載の組成物。
項1−9.トウビシの加工物がトウビシの加工物の総重量に対して、ポリフェノールを0.1〜80重量%で含有する、項1−7又は1−8に記載の組成物。
項1−10.組成物が経口又は非経口用である、項1−1〜1−9のいずれか一項に記載の組成物。
項1−11.組成物が飲食品又は医薬用である、項1−1〜1−10のいずれか一項に記載の組成物。
項1−12.組成物がサプリメント用である、項1−1〜1−11のいずれか一項に記載の組成物。
項1−13.組成物が眼科用である、項1−1〜1−12のいずれか一項に記載の組成物。
項1−14.組成物がソフトカプセル、ハードカプセル、液剤、ゼリー、グミ、錠剤又は散剤である、項1−1〜1−13のいずれか一項に記載の組成物。
項1−15.視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための、項1−1〜1−14のいずれか一項に記載の組成物。
項1−16.視機能低下が眼の疲労、眼の老化又は眼のピント調節機能の低下である、項1−15に記載の組成物。
項1−17.視機能低下が加齢、紫外線、血行不良、乾燥、活性酸素及び/又は炎症により誘発される視機能低下である、項1−15又は1−16に記載の組成物。
項1−18.自覚症状が肩、首筋、背中又は腰のこりである、項1−15に記載の組成物。
項1−19.眼疾患の予防及び/又は治療のための、項1−1〜1−14に記載の組成物。
項1−20.眼疾患が加齢、紫外線、血行不良、乾燥、活性酸素及び/又は炎症により誘発される眼疾患である、項1−19に記載の組成物。
項1−21.眼疾患が眼精疲労、白内障、加齢黄斑変性、糖尿病網膜症、網膜色素変性症、中心性漿液性脈絡網膜症、緑内障、ブドウ膜炎、老視、近視、ドライアイ、翼状片及び炎症性眼疾患からなる群より選択される、項1−19又は1−20に記載の組成物。
項1−22.角膜障害の予防、改善及び/又は治療のための、項1−1〜1−14のいずれか一項に記載の組成物。
項1−23.角膜障害が紫外線により誘発される角膜障害である項1−22に記載の組成物。
項1−24.水晶体変性の予防、改善及び/又は治療のための、項1−1〜1−14のいずれか一項に記載の組成物。
項1−25.水晶体変性が水晶体の混濁又は硬化である項1−24に記載の組成物。
項1−26.眼調節機能の低下の予防、改善及び/又は治療のための、項1−1〜1−14のいずれか一項に記載の組成物。
項1−27.眼調節機能がピント調節機能である、項1−26に記載の組成物。
項1−28.網脈絡膜障害の予防、改善及び/又は治療のための、項1−1〜1−14のいずれか一項に記載の組成物。
項1−29.網脈絡膜障害が網膜の損傷である、項1−28に記載の組成物。
項1−30.キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする視機能低下及びそれに伴う自覚症状の予防及び/又は改善剤。
項1−31.キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする眼疾患の予防及び/又は治療剤。
項1−32.キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする角膜障害の予防、改善及び/又は治療剤。
項 1−33.角膜障害が紫外線により誘発される角膜損傷である項1−32に記載の組成物。
項1−34.キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする水晶体変性の予防、改善及び/又は治療剤。
項1−35.水晶体変性が水晶体の混濁又は硬化である項1−34に記載の予防、改善及び/又は治療剤。
項1−36.キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする眼調節機能の低下の予防、改善及び/又は治療剤。
項1−37.眼調節機能がピント調節機能である項1−36に記載の予防、改善及び/又は治療剤。
項1−38.キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする網膜障害の予防、改善及び/又は治療剤。
項1−39.網膜障害が網膜の損傷である、項1−38に記載の予防、改善及び/又は治療剤。
なお、項1−1〜1−39を適宜選択して、組み合わせた発明も本発明の範囲である。
That is, the present invention relates to the following.
Item 1-1. A composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-2. Item 2. The composition according to Item 1-1, wherein the xanthophyll is at least one selected from the group consisting of lutein, astaxanthin, β-cryptoxanthin, zeaxanthin, mesozeaxanthin, canthaxanthin, capsanthin and fucoxanthin.
Item 1-3. Item 2. The composition according to Item 1-1 or 1-2, wherein the xanthophyll is at least one selected from the group consisting of lutein, astaxanthin, zeaxanthin and mesozeaxanthin.
Item 1-4. Any one of Items 1-1 to 1-3, wherein the processed product of Trapa japonica is a processed product of at least one Trapa plant selected from the group consisting of Trapa incisa, Trapa incisa, Trapa japonica, Trapa natans, and Trapa natans. The composition according to
Item 1-5.
Item 1-6. Item 2. The composition according to any one of Items 1-1 to 1-5, wherein the processed product of the genus Trapa contains 0.1 to 80% by weight of polyphenol based on the total weight of the processed product of the genus Trapa. Stuff.
Item 1-7. A composition containing lutein or a salt thereof and a processed product of Tobishi.
Item 1-8. Item 2. The composition according to Item 1-7, wherein the processed product of Tobishi is a pulverized product and / or extract of the peel of Tobishi.
Item 1-9. Item 2. The composition according to Item 1-7 or 1-8, wherein the processed Tobishi product contains 0.1 to 80% by weight of polyphenol based on the total weight of the processed Tobishi product.
Item 1-10.
Item 1-11. Item 2. The composition according to any one of Items 1-1 to 1-10, wherein the composition is for food or drink or pharmaceutical use.
Item 1-12.
Item 1-13. Item 2. The composition according to any one of Items 1-1 to 1-12, wherein the composition is for ophthalmology.
Item 1-14. Item 2. The composition according to any one of Items 1-1 to 1-13, wherein the composition is a soft capsule, a hard capsule, a liquid preparation, a jelly, a gummies, a tablet or a powder.
Item 1-15.
Item 1-16. Item 2. The composition according to Item 1-15, wherein the decrease in visual function is eye fatigue, aging of the eye, or decrease in the ability to adjust the focus of the eye.
Item 1-17.
Item 1-18. Item 2. The composition according to Item 1-15, wherein the subjective symptom is stiff shoulders, nape of the neck, back or lower back.
Item 1-19. Item 2. The composition according to Item 1-1 to 1-14, for the prevention and / or treatment of eye diseases.
Item 1-20. Item 2. The composition according to Item 1-19, wherein the eye disease is an eye disease induced by aging, ultraviolet rays, poor circulation, dryness, active oxygen and / or inflammation.
Item 1-21. Eye diseases include eye strain, cataract, age-related luteal degeneration, diabetic retinopathy, retinitis pigmentosa, central serous chorioretinopathy, glaucoma, vegetation inflammation, presbyopia, myopia, dry eye, pterygium and inflammatory Item 2. The composition according to Item 1-19 or 1-20, which is selected from the group consisting of eye diseases.
Item 1-22.
Item 1-23. Item 2. The composition according to Item 1-22, wherein the corneal disorder is an ultraviolet-induced corneal disorder.
Item 1-24.
Item 1-25. Item 2. The composition according to Item 1-24, wherein the lens denaturation is opacity or hardening of the lens.
Item 1-26.
Item 1-27. Item 2. The composition according to Item 1-26, wherein the eye accommodation function is an accommodation accommodation function.
Item 1-28.
Item 1-29. The composition according to Item 1-28, wherein the retinal choroidal disorder is retinal damage.
Item 1-30. An agent for preventing and / or ameliorating visual dysfunction and associated subjective symptoms, which is characterized by combining xanthophyll or a salt thereof with a processed product of the genus Trapa.
Item 1-31. A prophylactic and / or therapeutic agent for eye diseases, which comprises combining xanthophyll or a salt thereof with a processed product of the genus Trapa.
Item 1-32. A prophylactic, ameliorating and / or therapeutic agent for corneal disorders, which comprises combining xanthophyll or a salt thereof with a processed product of the genus Trapa.
Item 1-33. Item 3. The composition according to Item 1-32, wherein the corneal disorder is UV-induced corneal damage.
Item 1-34. A prophylactic, ameliorating and / or therapeutic agent for lens degeneration, which comprises combining xanthophyll or a salt thereof with a processed product of the genus Trapa.
Item 1-35. The prophylactic, ameliorating and / or therapeutic agent according to Item 1-34, wherein the lens degeneration is opacity or hardening of the lens.
Item 1-36. A prophylactic, ameliorating and / or therapeutic agent for the deterioration of accommodation function, which is characterized by combining xanthophyll or a salt thereof with a processed product of the genus Trapa.
Item 1-37. Item 3. The prophylactic, ameliorating and / or therapeutic agent according to Item 1-36, wherein the accommodation function is an accommodation function.
Item 1-38. A prophylactic, ameliorating and / or therapeutic agent for retinal disorders, which comprises combining xanthophyll or a salt thereof with a processed product of the genus Trapa.
Item 1-39. The prophylactic, ameliorating and / or therapeutic agent according to Item 1-38, wherein the retinal disorder is retinal damage.
The invention in which items 1-1 to 1-39 are appropriately selected and combined is also within the scope of the present invention.
また、本発明は、以下に関する。
項1−40.キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物であって、視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための該組成物の使用。
項1−41.視機能低下及びそれに伴う自覚症状の予防、改善及び/又は治療の方法であって、キサントフィル又はその塩及びヒシ属植物の加工物の有効量を投与することを含む方法。
項1−42.キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物であって、眼疾患の予防及び/又は治療のための該組成物の使用。
項1−43.眼疾患の予防、改善及び/又は治療の方法であって、キサントフィル又はその塩及びヒシ属植物の加工物の有効量を投与することを含む方法。
項1−44.キサントフィル又はその塩及びヒシ属植物の加工物を含有するメイラード反応抑制剤。
項1−45.キサントフィル又はその塩及びヒシ属植物の加工物を含有する抗酸化剤。
項1−46.キサントフィル又はその塩及びヒシ属植物の加工物を含有する活性酸素消去剤。
項1−47.キサントフィル又はその塩及びヒシ属植物の加工物を含有する光毒性抑制剤。
項1−48.光が紫外線である項1−47に記載の光毒性抑制剤。
項1−49.キサントフィル又はその塩及びヒシ属植物の加工物を含有する上皮細胞死抑制剤。
項1−50.上皮細胞が角膜上皮細胞である項1−49に記載の上皮細胞死抑制剤。
項1−51.キサントフィル又はその塩及びヒシ属植物の加工物を含有する水晶体変性抑制剤。
項1−52.水晶体変性が水晶体の混濁又は硬化である項1−51に記載の水晶体変性抑制剤。
項1−53.キサントフィル又はその塩及びヒシ属植物の加工物を含有する老化防止剤。
項1−54.キサントフィル又はその塩及びヒシ属植物の加工物を含有する炎症改善剤。
項1−55.キサントフィル又はその塩及びヒシ属植物の加工物を含有する網脈絡膜の損傷抑制剤。
項1−56.網脈絡膜が網膜である項1−55に記載の網脈絡膜の損傷抑制剤。
なお、項1−1〜1−56を適宜選択して、組み合わせた発明も本発明の範囲である。
The present invention also relates to the following.
Item 1-40. Use of a composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa for the prevention and / or improvement of visual dysfunction and associated subjective symptoms.
Item 1-41. A method for preventing, ameliorating and / or treating visual dysfunction and associated subjective symptoms, which comprises administering an effective amount of xanthophyll or a salt thereof and a processed product of a Trapa plant.
Item 1-42. Use of a composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa, for the prevention and / or treatment of eye diseases.
Item 1-43. A method of preventing, ameliorating and / or treating an eye disease, which comprises administering an effective amount of xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-44. A Maillard reaction inhibitor containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-45. An antioxidant containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-46. An active oxygen scavenger containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-47. A phototoxicity inhibitor containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-48. Item 4. The phototoxicity inhibitor according to Item 1-47, wherein the light is ultraviolet light.
Item 1-49. An epithelial cell death inhibitor containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-50. Item 4. The epithelial cell death inhibitor according to Item 1-49, wherein the epithelial cells are corneal epithelial cells.
Item 1-51. A lens denaturation inhibitor containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-52. Item 5. The lens degeneration inhibitor according to Item 1-51, wherein the lens degeneration is opacity or hardening of the lens.
Item 1-53. An anti-aging agent containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-54. An anti-inflammatory agent containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-55. A reticulochoroidal damage inhibitor containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
Item 1-56. Item 3. The agent for suppressing damage to the retina choroid according to Item 1-55, wherein the retina is the retina.
The invention in which items 1-1 to 1-56 are appropriately selected and combined is also within the scope of the present invention.
また、本発明の別の態様は、以下に関する。
項2−1.ヒシ属植物の加工物を含有する眼科用組成物。
項2−2.ヒシ属植物の加工物がツノナシビシ、ヒシ、トウビシ、トラパ・ナタンス及びオニビシからなる群より選択される少なくとも一つのヒシ属植物の加工物である、項2−1に記載の眼科用組成物。
項2−3.ヒシ属植物の加工物がヒシ属植物の果皮の粉砕物又は抽出物である、項2−1又は2−2のいずれか一項に記載の眼科用組成物。
項2−4.ヒシ属植物の加工物がヒシ属植物の加工物の総重量に対して、ポリフェノールを0.1〜80重量%で含有する、項2−1〜2−3のいずれか一項に記載の眼科用組成物。
項2−5.トウビシの加工物を含有する眼科用組成物。
項2−6.トウビシの加工物がトウビシの果皮の粉砕物及び/又は抽出物である、項2−5に記載の眼科用組成物。
項2−7.トウビシの加工物がトウビシの加工物の総重量に対して、ポリフェノールを0.1〜80重量%で含有する、項2−5又は2−6に記載の眼科用組成物。
項2−8.眼科用組成物が経口又は非経口用である、項2−1〜2−7のいずれか一項に記載の眼科用組成物。
項2−9.眼科用組成物が飲食品又は医薬用である、項2−1〜2−8のいずれか一項に記載の眼科用組成物。
項2−10.眼科用組成物がサプリメント用である、項2−1〜2−9のいずれか一項に記載の眼科用組成物。
項2−11.眼科用組成物がソフトカプセル、ハードカプセル、液剤、ゼリー、グミ、錠剤又は散剤である、項2−1〜2−10のいずれか一項に記載の眼科用組成物。
項2−12.視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための、項2−1〜2−11のいずれか一項に記載の眼科用組成物。
項2−13.視機能低下が眼の疲労、眼の老化又は眼のピント調節機能の低下である、項2−12に記載の組成物。
項2−14.視機能低下が加齢、紫外線、血行不良、乾燥、活性酸素及び/又は炎症により誘発される視機能低下である、項2−12又は2−13に記載の組成物。
項2−15.自覚症状が肩、首筋、背中又は腰のこりである、項2−12に記載の組成物。
項2−16.眼疾患の予防及び/又は治療のための、項2−1〜項2−11に記載の眼科用組成物。
項2−17.眼疾患が加齢、紫外線、血行不良、乾燥、活性酸素及び/又は炎症により誘発される、項2−16に記載の眼科用組成物。
項2−18.眼疾患が、眼精疲労、白内障、加齢黄斑変性、糖尿病網膜症、網膜色素変性症、中心性漿液性脈絡網膜症、緑内障、ブドウ膜炎、老視、近視、ドライアイ、翼状片及び炎症性眼疾患からなる群より選択される、項2−16又は2−17に記載の眼科用組成物。
項2−19.角膜障害の予防、改善及び/又は治療のための、項2−1〜2−11のいずれか一項に記載の眼科用組成物。
項2−20.角膜障害が紫外線により誘発される角膜障害である項2−19に記載の眼科用組成物。
項2−21.水晶体変性の予防、改善及び/又は治療のための、項2−1〜2−10のいずれか一項に記載の眼科用組成物。
項2−22.水晶体変性が水晶体の混濁又は硬化である項2−21に記載の眼科用組成物。
項2−23.眼調節機能低下の予防、改善及び/又は治療のための、項2−1〜2−11のいずれか一項に記載の眼科用組成物。
項2−24.眼調節機能がピント調節機能である、項2−23に記載の眼科用組成物。
項2−25.網脈絡膜障害の予防、改善及び/又は治療のための、項2−1〜2−11のいずれか一項に記載の眼科用組成物。
項2−26.網脈絡膜障害が網膜の損傷である、項2−25に記載の眼科用組成物。
項2−27.ヒシ属植物の加工物を含有する視機能低下及びそれに伴う自覚症状の予防及び/又は改善剤。
項2−28.ヒシ属植物の加工物を含有する眼疾患の予防及び/又は治療剤。
項2−29.ヒシ属植物の加工物を含有する角膜障害の予防、改善及び/又は治療剤。
項2−30.角膜障害が紫外線により誘発される角膜障害である項2−29に記載の予防、改善及び/又は治療剤。
項2−31.ヒシ属植物の加工物を含有する水晶体変性の予防、改善及び/又は治療剤。
項2−32.水晶体変性が水晶体の混濁又は硬化である項2−31に記載の予防、改善及び/又は治療剤。
項2−33.ヒシ属植物の加工物を含有する眼調節機能の低下の予防、改善及び/又は治療剤。
項2−34.眼調節機能がピント調節機能である項2−33に記載の予防、改善及び/又は治療剤。
項2−35.ヒシ属植物の加工物を含有する網脈絡膜障害の予防、改善及び/又は治療剤。
項2−36.網脈絡膜障害が網膜の損傷である項2−35に記載の予防、改善及び/又は治療剤。
なお、項2−1〜2−36を適宜選択して、組み合わせた発明も本発明の範囲である。
In addition, another aspect of the present invention relates to the following.
Item 2-1. An ophthalmic composition containing a processed product of the genus Trapa.
Item 2-2. Item 2. The ophthalmic composition according to Item 2-1. The processed product of Trapa japonica is a processed product of at least one Trapa japonica plant selected from the group consisting of Trapa japonica, Trapa japonica, Trapa japonica, Trapa natans and Trapa natans chinensis.
Item 2-3. Item 2. The ophthalmic composition according to any one of Items 2-1 or 2-2, wherein the processed product of the Trapa plant is a pulverized product or an extract of the pericarp of the Trapa plant.
Item 2-4. Item 2. Ophthalmology according to any one of Items 2-1 to 2-3, wherein the processed product of the genus Trapa contains 0.1 to 80% by weight of polyphenol based on the total weight of the processed product of the genus Trapa. Composition for.
Item 2-5. An ophthalmic composition containing a processed Tobishi product.
Item 2-6. Item 2. The ophthalmic composition according to Item 2-5, wherein the processed product of Tobishi is a pulverized product and / or extract of the peel of Tobishi.
Item 2-7. Item 2. The ophthalmic composition according to Item 2-5 or 2-6, wherein the processed Tobishi product contains 0.1 to 80% by weight of polyphenol based on the total weight of the processed Tobishi product.
Item 2-8. Item 2. The ophthalmic composition according to any one of Items 2-1 to 2-7, wherein the ophthalmic composition is oral or parenteral.
Item 2-9. Item 2. The ophthalmic composition according to any one of Items 2-1 to 2-8, wherein the ophthalmic composition is for food and drink or pharmaceuticals.
Item 2-10. Item 2. The ophthalmic composition according to any one of Items 2-1 to 2-9, wherein the ophthalmic composition is for a supplement.
Item 2-11. Item 2. The ophthalmic composition according to any one of Items 2-1 to 2-10, wherein the ophthalmic composition is a soft capsule, a hard capsule, a liquid preparation, a jelly, a gummies, a tablet or a powder.
Item 2-12.
Item 2-13. Item 2. The composition according to Item 2-12, wherein the deterioration of visual function is eye fatigue, aging of the eye, or deterioration of the accommodation function of the eye.
Item 2-14. Item 2. The composition according to Item 2-12 or 2-13, wherein the visual dysfunction is a visual dysfunction induced by aging, ultraviolet rays, poor circulation, dryness, active oxygen and / or inflammation.
Item 2-15. Item 2. The composition according to Item 2-12, wherein the subjective symptom is stiff shoulders, nape of the neck, back or lower back.
Item 2-16. Item 2. The ophthalmic composition according to Item 2-1 to Item 2-11 for prevention and / or treatment of eye diseases.
Item 2-17. Item 2. The ophthalmic composition according to Item 2-16, wherein the eye disease is induced by aging, ultraviolet rays, poor circulation, dryness, active oxygen and / or inflammation.
Item 2-18. Eye diseases include eye strain, cataracts, age-related luteal degeneration, diabetic retinopathy, retinitis pigmentosa, central serous chorioretinopathy, glaucoma, glaucoma, presbyopia, myopia, dry eyes, pterygium and inflammation. Item 2. The ophthalmic composition according to Item 2-16 or 2-17, which is selected from the group consisting of glaucoma.
Item 2-19.
Item 2-20. Item 2. The ophthalmic composition according to Item 2-19, wherein the corneal disorder is an ultraviolet-induced corneal disorder.
Item 2-21.
Item 2-22. Item 2. The ophthalmic composition according to Item 2-21, wherein the lens degeneration is opacity or hardening of the lens.
Item 2-23.
Item 2-24. Item 2. The ophthalmic composition according to Item 2-23, wherein the accommodation function is an accommodation function.
Item 2-25.
Item 2-26. Item 2. The ophthalmic composition according to Item 2-25, wherein the retinal choroidal disorder is retinal damage.
Item 2-27. A preventive and / or ameliorating agent for visual dysfunction and associated subjective symptoms containing a processed product of the genus Trapa.
Item 2-28. A preventive and / or therapeutic agent for eye diseases containing a processed product of the genus Trapa.
Item 2-29. A preventive, ameliorating and / or therapeutic agent for corneal disorders containing a processed product of the genus Trapa.
Item 2-30. The prophylactic, ameliorating and / or therapeutic agent according to Item 2-29, wherein the corneal disorder is an ultraviolet-induced corneal disorder.
Item 2-31. A prophylactic, ameliorating and / or therapeutic agent for lens degeneration containing a processed product of the genus Trapa.
Item 2-32. Item 2. The preventive, ameliorating and / or therapeutic agent according to Item 2-31, wherein the lens degeneration is opacity or hardening of the lens.
Item 2-33. A prophylactic, ameliorating and / or therapeutic agent for a decrease in accommodation function containing a processed product of the genus Trapa.
Item 2-34. Item 2. The prophylactic, ameliorating and / or therapeutic agent according to Item 2-33, wherein the accommodation function is an accommodation function.
Item 2-35. A prophylactic, ameliorating and / or therapeutic agent for reticulochoroidal disorders containing a processed product of the genus Trapa.
Item 2-36. The prophylactic, ameliorating and / or therapeutic agent according to Item 2-35, wherein the retinal choroidal disorder is retinal damage.
The invention in which items 2-1 to 2-36 are appropriately selected and combined is also within the scope of the present invention.
また、本発明は、以下に関する。
項2−37.ヒシ属植物の加工物を含有する眼科用組成物であって、視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための該組成物の使用。
項2−38.視機能低下及びそれに伴う自覚症状の予防、改善及び/又は治療の方法であって、ヒシ属植物の加工物の有効量を投与することを含む方法。
項2−39.ヒシ属植物の加工物を含有する眼科用組成物であって、眼疾患の予防及び/又は治療のための該組成物の使用。
項2−40.眼疾患の予防、改善及び/又は治療の方法であって、ヒシ属植物の加工物の有効量を投与することを含む方法。
項2−41.ヒシ属植物の加工物を含有する眼におけるメイラード反応抑制剤。
項2−42.ヒシ属植物の加工物を含有する眼における抗酸化剤。
項2−43.ヒシ属植物の加工物を含有する眼における活性酸素消去剤。
項2−44.ヒシ属植物の加工物を含有する眼における光毒性抑制剤。
項2−45.光が紫外線である、項2−44に記載の光毒性抑制剤。
項2−46.ヒシ属植物の加工物を含有する上皮細胞死抑制剤。
項2−47.上皮細胞が角膜上皮細胞である項2−46に記載の上皮細胞死抑制剤。
項2−48.ヒシ属植物の加工物を含有する水晶体変性抑制剤。
項2−49.水晶体変性が水晶体の混濁又は硬化である、項2−48に記載の水晶体変性抑制剤。
項2−50.ヒシ属植物の加工物を含有する眼における老化防止剤。
項2−51.ヒシ属植物の加工物を含有する眼炎症改善剤。
項2−52.ヒシ属植物の加工物を含有する網脈絡膜の損傷抑制剤。
項2−53.網脈絡膜が網膜である項2−52に記載の網脈絡膜の損傷抑制剤。
なお、項2−1〜2−53を適宜選択して、組み合わせた発明も本発明の範囲である。
The present invention also relates to the following.
Item 2-37. Use of an ophthalmic composition containing a processed product of the genus Trapa for the prevention and / or amelioration of visual dysfunction and associated subjective symptoms.
Item 2-38. A method for preventing, ameliorating and / or treating visual dysfunction and associated subjective symptoms, which comprises administering an effective amount of a processed product of the genus Trapa.
Item 2-39. Use of an ophthalmic composition containing a processed product of the genus Trapa for the prevention and / or treatment of eye diseases.
Item 2-40. A method of preventing, ameliorating and / or treating an eye disease, which comprises administering an effective amount of a processed product of the genus Trapa.
Item 2-41. A Maillard reaction inhibitor in the eye containing a processed product of the genus Trapa.
Item 2-42. Antioxidants in the eye containing processed products of the genus Trapa.
Item 2-43. An active oxygen scavenger in the eye containing a processed product of the genus Trapa.
Item 2-44. A phototoxicity inhibitor in the eye containing a processed product of the genus Trapa.
Item 2-45. Item 2. The phototoxicity inhibitor according to Item 2-44, wherein the light is ultraviolet light.
Item 2-46. An epithelial cell death inhibitor containing a processed product of the genus Trapa.
Item 2-47. Item 2. The epithelial cell death inhibitor according to Item 2-46, wherein the epithelial cells are corneal epithelial cells.
Item 2-48. A lens denaturation inhibitor containing a processed product of the genus Trapa.
Item 2-49. Item 2. The lens degeneration inhibitor according to Item 2-48, wherein the lens degeneration is opacity or hardening of the lens.
Item 2-50. An anti-aging agent in the eye containing a processed product of the genus Trapa.
Item 2-51. An eye inflammation improving agent containing a processed product of the genus Trapa.
Item 2-52. An agent for suppressing damage to the reticulochoroid containing a processed product of the genus Trapa.
Item 2-53. Item 2. The agent for suppressing damage to the retina choroid according to Item 2-52, wherein the retina is the retina.
The invention in which items 2-1 to 2-53 are appropriately selected and combined is also within the scope of the present invention.
更に、本発明の別の態様は、以下に関する。
項3−1.ルテイン又はその塩を含有する角膜上皮細胞死抑制剤。
項3−2.紫外線により誘発される角膜上皮細胞死である、項3−1に記載の角膜上皮細胞死抑制剤。
項3−3.紫外線がUV−Bである、項3−1又は3−2に記載の角膜上皮細胞死抑制剤。
項3−4.ルテイン又はその塩を含有する眼科用組成物であって、紫外線により誘発される視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための眼科用組成物。
項3−5.ルテイン又はその塩を含有する眼科用組成物であって、紫外線により誘発される眼疾患の予防及び/又は治療のための眼科用組成物。
項3−6.ルテイン又はその塩を含有する眼科用組成物であって、紫外線により誘発される角膜障害の予防及び/又は治療のための眼科用組成物。
項3−7.眼科用組成物が経口又は非経口用である、項3−4〜3−6に記載の眼科用組成物。
項3−8.眼科用組成物が飲食品又は医薬用である、項3−4〜3−7に記載の眼科用組成物。
項3−9.眼科用組成物がサプリメント用である、項3−4〜3−8のいずれか一項に記載の眼科用組成物。
項3−10.眼科用組成物がソフトカプセル、ハードカプセル、液剤、ゼリー、グミ、錠剤又は散剤である、項3−4〜3−9のいずれか一項に記載の眼科用組成物。
項3−11.視機能低下が眼の疲労、眼の老化、又は眼のピント調節機能の低下である、項3−4に記載の眼科用組成物。
項3−12.自覚症状が肩、首筋、背中又は腰のこりである、項3−4に記載の眼科用組成物。
項3−13.眼疾患の予防及び/又は治療のための、項3−5に記載の眼科用組成物。
項3−14.眼疾患が、眼精疲労、白内障、加齢黄斑変性、ブドウ膜炎、老視、近視、ドライアイ、翼状片及び炎症性眼疾患からなる群より選択される、項3−5に記載の眼科用組成物。
項3−15.角膜障害が角膜上皮細胞障害である、項3−6に記載の眼科用組成物。
なお、項3−1〜3−15を適宜選択して、組み合わせた発明も本発明の範囲である。
Furthermore, another aspect of the present invention relates to the following.
Item 3-1. A corneal epithelial cell death inhibitor containing lutein or a salt thereof.
Item 3-2. Item 3. The corneal epithelial cell death inhibitor according to Item 3-1 which is UV-induced corneal epithelial cell death.
Item 3-3. Item 3. The corneal epithelial cell death inhibitor according to Item 3-1 or 3-2, wherein the ultraviolet rays are UV-B.
Item 3-4. An ophthalmic composition containing lutein or a salt thereof for preventing and / or ameliorating ultraviolet-induced visual dysfunction and associated subjective symptoms.
Item 3-5. An ophthalmic composition containing lutein or a salt thereof for the prevention and / or treatment of ultraviolet-induced eye diseases.
Item 3-6. An ophthalmic composition containing lutein or a salt thereof for the prevention and / or treatment of ultraviolet-induced corneal disorders.
Item 3-7. Item 3. The ophthalmic composition according to Item 3-4 to 3-6, wherein the ophthalmic composition is oral or parenteral.
Item 3-8. Item 3. The ophthalmic composition according to Item 3-4 to 3-7, wherein the ophthalmic composition is for food or drink or medicine.
Item 3-9.
Item 3-10.
Item 3-11. Item 3. The ophthalmic composition according to Item 3-4, wherein the deterioration of visual function is eye fatigue, aging of the eye, or deterioration of the accommodation function of the eye.
Item 3-12. Item 3. The ophthalmic composition according to Item 3-4, wherein the subjective symptom is stiff shoulder, nape, back or lower back.
Item 3-13. Item 3. The ophthalmic composition according to Item 3-5, for the prevention and / or treatment of eye diseases.
Item 3-14. Item 2. Ophthalmology according to Item 3-5, wherein the eye disease is selected from the group consisting of eyestrain, cataract, age-related yellow spot degeneration, uveitis, presbyopia, myopia, dry eye, pterygium and inflammatory eye disease. Composition for.
Item 3-15. Item 3. The ophthalmic composition according to Item 3-6, wherein the corneal disorder is a corneal epithelial cell disorder.
The invention in which items 3-1 to 3-15 are appropriately selected and combined is also within the scope of the present invention.
項3−16.ルテイン又はその塩を含有する眼科用組成物であって、紫外線により誘発される視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための該組成物の使用。
項3−17.紫外線により誘発される視機能低下及びそれに伴う自覚症状を予防及び/又は改善する方法であって、ルテイン又はその塩の有効量を投与することを含む方法。
項3−18.ルテイン又はその塩を含有する眼科用組成物であって、紫外線により誘発される眼疾患の予防及び/又は治療のための該組成物の使用。
項3−19.紫外線により誘発される眼疾患を予防及び/又は改善する方法であって、ルテイン又はその塩の有効量を投与することを含む方法。
なお、項3−1〜3−19を適宜選択して、組み合わせた発明も本発明の範囲である。
Item 3-16. Use of an ophthalmic composition containing lutein or a salt thereof for the prevention and / or amelioration of ultraviolet-induced visual dysfunction and associated subjective symptoms.
Item 3-17. A method for preventing and / or ameliorating UV-induced visual dysfunction and associated subjective symptoms, which comprises administering an effective amount of lutein or a salt thereof.
Item 3-18. Use of an ophthalmic composition containing lutein or a salt thereof for the prevention and / or treatment of UV-induced eye diseases.
Item 3-19. A method of preventing and / or ameliorating UV-induced eye disease, which comprises administering an effective amount of lutein or a salt thereof.
The invention in which items 3-1 to 3-19 are appropriately selected and combined is also within the scope of the present invention.
本発明は、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物を提供する。また、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物の眼科用途、特に、視機能低下等の予防及び/又は改善並びに眼疾患等の予防及び/又は治療用途を提供する。 The present invention provides a composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa. Further, the present invention provides ophthalmic uses of a composition containing xanthophyll or a salt thereof and a processed product of a Trapa plant, in particular, prevention and / or improvement of visual function deterioration and prevention and / or therapeutic use of eye diseases and the like.
キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物は、紫外線照射により誘発される角膜上皮細胞死を効果的に抑制することから、紫外線に起因する(紫外線によるDNA損傷に起因)視機能低下(眼の疲労、眼の老化等)およびそれに伴う自覚症状(肩、首筋、背中、腰等のこり)の予防及び/又は改善並びに眼疾患(眼精疲労、白内障、加齢黄斑変性、炎症性眼疾患、翼状片等)の予防又は治療、に有用であることが期待される。
同時に、紫外線に起因する生体細胞死を効果的に抑制することから、皮膚がんの誘発、肌のシミの生成、各組織の老化の加速等をも予防、改善及び/又は治療に有用であることも期待される。
A composition containing xanthophile or a salt thereof and a processed product of the genus Hishi effectively suppresses corneal epithelial cell death induced by ultraviolet irradiation, and thus is caused by ultraviolet rays (due to DNA damage caused by ultraviolet rays). Prevention and / or improvement of functional deterioration (eye fatigue, eye aging, etc.) and associated subjective symptoms (stiffness of shoulders, neck muscles, back, hips, etc.) and eye diseases (eye strain, cataracts, age-related pterygium degeneration, inflammation, etc.) It is expected to be useful for the prevention or treatment of sexual eye diseases, pterygium, etc.).
At the same time, since it effectively suppresses the death of living cells caused by ultraviolet rays, it is also useful for prevention, improvement and / or treatment of induction of skin cancer, formation of skin stains, acceleration of aging of each tissue, and the like. It is also expected.
また、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物は、水晶体の白濁を効果的に抑制することから、水晶体の混濁(白濁)、すなわち、水晶体の変性に起因する視機能低下(眼の疲労、眼の老化、眼のピント調節機能の低下等)およびそれに伴う自覚症状(肩、首筋、背中、腰等のこり)の予防及び/又は改善並びに眼疾患(眼精疲労、白内障、老視等)の予防又は治療に有用であることが期待される。特に水晶体の変性は、眼のピント調節機能に大きく影響を与えるので、ピント調節機能に関する疾患である老視、近視等の予防、改善及び/又は治療に特に有効であることが期待される。 In addition, since the composition containing xanthophile or a salt thereof and a processed product of the genus Hishi effectively suppresses the white turbidity of the crystalline lens, the opacity of the crystalline lens (white turbidity), that is, the deterioration of visual function due to the degeneration of the crystalline lens. Prevention and / or improvement of (eye fatigue, presbyopia, deterioration of eye focus adjustment function, etc.) and associated subjective symptoms (stiffness of shoulders, neck muscles, back, hips, etc.) and eye diseases (eye fatigue, cataracts, etc.) It is expected to be useful for the prevention or treatment of presbyopia, etc.). In particular, degeneration of the crystalline lens greatly affects the focus adjustment function of the eye, and is therefore expected to be particularly effective in the prevention, improvement and / or treatment of presbyopia, myopia and the like, which are diseases related to the focus adjustment function.
さらに、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物は、網膜の損傷を効果的に抑制または改善することから、網脈絡膜の損傷を伴う視機能低下(眼の疲労、眼の老化等)およびそれに伴う自覚症状(肩、首筋、背中、腰等のこり)の予防及び/又は改善並びに眼疾患(眼精疲労、加齢黄斑変性、糖尿病網膜症、網膜色素変性症、中心性漿液性脈絡網膜症、緑内障、ブドウ膜炎等の網脈絡膜疾患)の予防又は治療に有効であることが期待される。 Furthermore, compositions containing xanthophile or salts thereof and processed products of the genus Hishi effectively suppress or ameliorate damage to the retinopathy, and thus impair visual function (eye strain, eye fatigue) accompanied by damage to the retinochoroid. Prevention and / or improvement of (aging, etc.) and associated subjective symptoms (stiffness of shoulders, neck muscles, back, hips, etc.) and eye diseases (eye strain, age-related macular degeneration, diabetic retinopathy, retinitis pigmentosa, central serous chorioret) It is expected to be effective in the prevention or treatment of retinitis chorioretopathy, glaucoma, uveitis and other retinous choroidal diseases).
本発明は、ヒシ属植物の加工物を含有する眼科用組成物を提供する。また、ヒシ属植物の加工物を眼科用途、特に、視機能低下等の予防及び/又は改善並びに眼疾患等の予防及び/又は治療用途を提供する。 The present invention provides an ophthalmic composition containing a processed product of the genus Trapa. Further, the processed product of the genus Trapa is provided for ophthalmic use, particularly for prevention and / or improvement of visual function deterioration and prevention and / or treatment of eye diseases and the like.
ヒシ属植物の加工物を含有する組成物は、紫外線照射により誘発される角膜上皮細胞死を効果的に抑制することから、紫外線に起因する視機能低下(眼の疲労、眼の老化等)およびそれに伴う自覚症状(肩、首筋、背中、腰等のこり)の予防及び/又は改善並びに眼疾患(眼精疲労、白内障、加齢黄斑変性、炎症性眼疾患、翼状片等)の予防又は治療、に有用であることが期待される。 Compositions containing processed products of the genus Hishi effectively suppress corneal epithelial cell death induced by UV irradiation, resulting in decreased visual function (eye strain, eye aging, etc.) and eye aging caused by UV light. Prevention and / or improvement of subjective symptoms (stiffness of shoulders, neck muscles, back, hips, etc.) and prevention or treatment of eye diseases (eye strain, cataracts, age-related yellow spot degeneration, inflammatory eye diseases, pterygium, etc.) It is expected to be useful for.
また、ヒシ属植物の加工物を含有する組成物は、水晶体の白濁を効果的に抑制することから、水晶体の混濁(白濁)、すなわち、水晶体の変性に起因する視機能低下(眼の疲労、眼の老化、眼のピント調節機能の低下等)およびそれに伴う自覚症状(肩、首筋、背中、腰等のこり)の予防及び/又は改善並びに眼疾患(眼精疲労、白内障、老視等)の予防又は治療に有用であることが期待される。特に水晶体の変性は、眼のピント調節機能に大きく影響を与えるので、ピント調節機能に関する疾患である老視、近視等の予防、改善及び/又は治療に特に有効であることが期待される。 In addition, since the composition containing the processed product of the genus Hishi effectively suppresses the white turbidity of the crystalline lens, the opacity of the crystalline lens (white turbidity), that is, the deterioration of visual function due to the degeneration of the crystalline lens (eye fatigue, Prevention and / or improvement of eye aging, deterioration of eye focus adjustment function, etc.) and associated subjective symptoms (stiffness of shoulder, neck muscle, back, waist, etc.) and eye diseases (eye fatigue, cataract, presbyopia, etc.) It is expected to be useful for prevention or treatment. In particular, degeneration of the crystalline lens greatly affects the focus adjustment function of the eye, and is therefore expected to be particularly effective in the prevention, improvement and / or treatment of presbyopia, myopia and the like, which are diseases related to the focus adjustment function.
さらに、ヒシ属植物の加工物を含有する組成物は、網膜の損傷を効果的に抑制または改善することから、網脈絡膜の損傷を伴う視機能低下(眼の疲労、眼の老化等)およびそれに伴う自覚症状(肩、首筋、背中、腰等のこり)の予防及び/又は改善並びに眼疾患(眼精疲労、加齢黄斑変性、糖尿病網膜症、網膜色素変性症、中心性漿液性脈絡網膜症、緑内障、ブドウ膜炎等の網脈絡膜疾患)の予防又は治療に有効であることが期待される。 In addition, compositions containing processed products of the genus Hishi effectively suppress or ameliorate retinal damage, resulting in visual deterioration (eye strain, eye aging, etc.) associated with glaucoma damage and the like. Prevention and / or improvement of accompanying subjective symptoms (stiffness of shoulders, neck muscles, back, hips, etc.) and eye diseases (eye strain, age-related macular degeneration, diabetic retinopathy, retinitis pigmentosa, central serous chorioretinopathy, It is expected to be effective in the prevention or treatment of glaucoma, retinopathy such as uveitis).
本発明は、ルテイン又はその塩を含有する角膜上皮細胞死抑制剤を提供する。特に、紫外線により誘発される角膜上皮細胞死抑制剤を提供する。 The present invention provides a corneal epithelial cell death inhibitor containing lutein or a salt thereof. In particular, it provides an agent for suppressing corneal epithelial cell death induced by ultraviolet rays.
以下に、本発明について詳細に説明する。 Hereinafter, the present invention will be described in detail.
本発明の一態様は、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物である。 One aspect of the present invention is a composition containing xanthophyll or a salt thereof and a processed product of a Trapa plant.
本発明において、キサントフィルは、特に限定されない。キサントフィルの具体例として、ルテイン、アスタキサンチン、ゼアキサンチン、メソゼアキサンチン、β−クリプトキサンチン、ツナキサンチン、サルモキサンチン、パラシロキサンチン、ビオラキサンチン、アンテラキサンチン、ククルビタキサンチン、ディアトキサンチン、アロキサンチン、ペクテノール、ペクテノロン、マクトラキサンチン、カプサンチン、カプサンチノール、フコキサンチン、フコキサンチノール、ペリジニン、ハロシンチアキサンチン、アマロウシアキサンチン、カンタキサンチン、エキネノン、ロドキサンチン、ビキシン、ノルビキシン等が挙げられる。好ましくは、ルテイン、アスタキサンチン、β−クリプトキサンチン、ゼアキサンチン、メソゼアキサンチン、カンタキサンチン、カプサンチン又はフコキサンチンが挙げられ、特に好ましくは、ルテイン、アスタキサンチン、ゼアキサンチン又はメソゼアキサンチンが挙げられる。また、前記キサントフィルは、植物、動物、微生物等の天然物由来のもの(例えば、マリーゴールド、ホウレンソウ、ケール等の植物、動物脂肪、卵黄、黄体、甲殻類の殻、甲殻類の殻を餌とするマダイの体表、サケ科魚類の筋肉の赤色部分、目の網膜、黄斑等から得られるもの)であってもよく、化学的に合成されたもの(一般的な合成方法で製造されたもの)であってもよい。さらに、天然物由来のものは、その原料の種類、産地、製造方法等により、特に限定されない。 In the present invention, xanthophyll is not particularly limited. Specific examples of xanthophylls include lutein, astaxanthin, zeaxanthin, mesozeaxanthin, β-cryptoxanthin, tunaxanthin, salmoxanthin, parasiloxanetin, violaxanthin, anteraxanthin, kukurubitaxanthin, diatoxanthin, alloxanthin, pectenol, pectenolone. , Mactraxanthin, Capsantin, Capsantinol, Fucoxanthin, Fucoxanthinol, Peridinin, Halosinthiaxanthin, Amarousiaxanthin, Canthaxanthin, Equinenone, Rodoxanthin, Bixin, Norbicin and the like. Preferred examples include lutein, astaxanthin, β-cryptoxanthin, zeaxanthin, mesozeaxanthin, canthaxanthin, capsanthin or fucoxanthin, and particularly preferably lutein, astaxanthin, zeaxanthin or mesozeaxanthin. The xanthophyll is derived from natural substances such as plants, animals, and microorganisms (for example, plants such as marigold, spinach, and kale, animal fat, egg yolk, macula, crustacean shell, and crustacean shell as food. It may be obtained from the body surface of a crustacean, the red part of the muscle of a crustacean, the retina of the eye, the macula, etc.), or it may be chemically synthesized (manufactured by a general synthetic method). ) May be. Further, those derived from natural products are not particularly limited depending on the type of raw material, the place of production, the manufacturing method and the like.
本発明において、ルテインは、(3R,3’R,6’R)−β,ε−カロテン−3,3’−ジオール:
本発明において、アスタキサンチンは、(3S,3’S)−3,3’−ジヒドロキシ−β,β−カロテン−4,4’−ジオン:
本発明において、β−クリプトキサンチンは、(3R)−β,β−カロテン−3−オール:
本発明において、ゼアキサンチンは、(3R,3’R)−β,β−カロテン−3,3’−ジオール:
本発明において、メソゼアキサンチンは、(3R,3’S)−β,β−カロテン−3,3’−ジオール:
本発明において、カンタキサンチンは、β,β−カロテン−4,4’−ジオン:
本発明において、カプサンチンは、(3R,3’S)−3,3’−ジヒドロキシ−β,κ−カロテン−6’−オン:
本発明において、フコキサンチンは、(3S,3′S,5R,5′R,6S,6′R)‐3′‐アセトキシ‐6′,7′‐ジデヒドロ‐5,6‐エポキシ‐5,5′,6,6′,7,8‐ヘキサヒドロ‐3,5′‐ジヒドロキシ‐8‐オキソ‐β,β‐カロテン:
本発明において、キサントフィルは、特に記載がない限り、キサントフィル及び/又はそのエステル体を含む。更に、キサントフィルのエステルは、モノエステル体及び/又はジエステル体を含む。 In the present invention, xanthophylls include xanthophylls and / or esters thereof, unless otherwise specified. In addition, xanthophyll esters include monoesters and / or diesters.
本発明において、キサントフィルのモノエステル体として、例えば、低級若しくは高級飽和脂肪酸又は低級若しくは高級不飽和脂肪酸によりエステル化されたエステル類をあげることができる。前記低級若しくは高級飽和脂肪酸又は低級若しくは高級不飽和脂肪酸の具体例として、例えば、酢酸、ラウリン酸、ミリスチン酸、カプリル酸、ペンタデカン酸、パルミチン酸、パルミトオレイン酸、へブタデカン酸、エライジン酸、リシノール酸、ベトロセリン酸、バクセン酸、エレオステアリン酸、プニシン酸、リカン酸、パリナリン酸、ガドール酸、5−エイコセン酸、5−ドコセン酸、セトール酸、エルシン酸、5,13−ドコサジエン酸、セラコール酸、デセン酸、ドデセン酸、オレイン酸、ステアリン酸、エイコサオペンタエン酸、ドコサヘキサエン酸、リノール酸、リノレン酸、アラキドン酸等が挙げられる。 In the present invention, examples of the monoester of xanthophile include esters esterified with lower or higher saturated fatty acids or lower or higher unsaturated fatty acids. Specific examples of the lower or higher saturated fatty acids or lower or higher unsaturated fatty acids include acetic acid, lauric acid, myristic acid, capric acid, pentadecanoic acid, palmitic acid, palmitooleic acid, hebutadecanoic acid, ellaidic acid and ricinol. Acids, betroceric acid, baccenoic acid, eleostearic acid, punicinic acid, licanoic acid, parinaric acid, gadoric acid, 5-eicosenoic acid, 5-dococenoic acid, cetolic acid, erucic acid, 5,13-docosadienoic acid, ceracolic acid , Decenoic acid, dodecenoic acid, oleic acid, stearic acid, eikosaopentaenoic acid, docosahexaenoic acid, linoleic acid, linolenic acid, arachidonic acid and the like.
本発明において、更なる、キサントフィルのモノエステル体として、例えば、グリシン、アラニン等のアミノ酸;酢酸、クエン酸等の一価又は多価カルボン酸;リン酸、硫酸等の無機酸;グルコシド等の糖;グリセロ糖脂肪酸、スフィンゴ糖脂肪酸等の糖脂肪酸;グリセロ脂肪酸等の脂肪酸;グリセロリン酸等によりエステル化されたモノエステル体が挙げられる。なお、前記モノエステル体として塩が想定されうる場合は前記モノエステル体の塩も含む。ここで、脂肪酸の誘導体としては、前記脂肪酸のリン脂質型、アルコール型、エーテル型、ショ糖エステル型、ポリグリセリンエステル型等が挙げられる。 In the present invention, as further monoesters of xanthophile, for example, fatty acids such as glycine and alanine; monovalent or polyvalent carboxylic acids such as acetic acid and citric acid; inorganic acids such as phosphoric acid and sulfuric acid; sugars such as glucoside. Examples thereof include sugar fatty acids such as glycerosaccharide fatty acids and spingosaccharide fatty acids; fatty acids such as glycero fatty acids; and monoesters esterified with glycerophosphate and the like. When a salt can be assumed as the monoester, the salt of the monoester is also included. Here, examples of the fatty acid derivative include a phospholipid type, an alcohol type, an ether type, a sucrose ester type, and a polyglycerin ester type of the fatty acid.
本発明において、キサントフィルのジエステル体として、例えば、前記低級飽和脂肪酸、高級飽和脂肪酸、低級不飽和脂肪酸、高級不飽和脂肪酸、アミノ酸、一価又は多価カルボン酸、無機酸、糖、糖脂肪酸、脂肪酸及びグリセロリン酸からなる群から選択される同一又は異種の酸によりエステル化されたジエステル体が挙げられる。なお、前記ジエステル体として塩が想定されうる場合は前記ジエステル体の塩も含む。ここで、グリセロリン酸のジエステルとしては、グリセロリン酸の飽和脂肪酸エステル類又は高級不飽和脂肪酸、不飽和脂肪酸又は飽和脂肪酸から選択される脂肪酸類を含有するグリセロリン酸エステル類等が挙げられる。 In the present invention, the diester form of xanthophile includes, for example, the lower saturated fatty acid, higher saturated fatty acid, lower unsaturated fatty acid, higher unsaturated fatty acid, amino acid, monovalent or polyvalent carboxylic acid, inorganic acid, sugar, sugar fatty acid, fatty acid. And diesters esterified with the same or different acids selected from the group consisting of glycerophosphate. When a salt can be assumed as the diester, the salt of the diester is also included. Here, examples of the diester of glycerophosphate include saturated fatty acid esters of glycerophosphate or glycerophosphates containing fatty acids selected from higher unsaturated fatty acids, unsaturated fatty acids and saturated fatty acids.
本発明において、キサントフィルの塩は、生理学的又は医薬的に許容される塩であれば特に限定されない。例えば、塩酸、臭化水素酸、ヨウ化水素酸、硝酸、硫酸、リン酸等の無機酸との塩;酢酸、フマル酸、マレイン酸、コハク酸、クエン酸、酒石酸、アジピン酸、グルコン酸、グルコヘプト酸、グルクロン酸、テレフタル酸、メタンスルホン酸、乳酸、馬尿酸、1,2−エタンジスルホン酸、イセチオン酸、ラクトビオン酸、オレイン酸、パモ酸、ポリガラクツロン酸、ステアリン酸、タンニン酸、トリフルオロメタンスルホン酸、ベンゼンスルホン酸、p−トルエンスルホン酸、硫酸ラウリルエステル、硫酸メチル、ナフタレンスルホン酸、スルホサリチル酸等の有機酸との塩;臭化メチル、ヨウ化メチル等との四級アンモニウム塩;臭素イオン、塩素イオン、ヨウ素イオン等のハロゲンイオンとの塩;リチウム、ナトリウム、カリウム等のアルカリ金属との塩;カルシウム、マグネシウム等のアルカリ土類金属との塩;鉄、亜鉛等との金属塩;アンモニアとの塩;トリエチレンジアミン、2−アミノエタノール、2,2−イミノビス(エタノール)、1−デオキシ−1−(メチルアミノ)−2−D−ソルビトール、2−アミノ−2−(ヒドロキシメチル)−1,3−プロパンジオール、プロカイン、N,N−ビス(フェニルメチル)−1,2−エタンジアミン等の有機アミンとの塩等が挙げられる。 In the present invention, the salt of xanthophyll is not particularly limited as long as it is a physiologically or pharmaceutically acceptable salt. For example, salts with inorganic acids such as hydrochloric acid, hydrobromic acid, hydroiodic acid, nitrate, sulfuric acid, phosphoric acid; acetic acid, fumaric acid, maleic acid, succinic acid, citric acid, tartrate acid, adipic acid, gluconic acid, Glucoheptoic acid, glucuronic acid, terephthalic acid, methanesulfonic acid, lactic acid, horseuric acid, 1,2-ethanedisulfonic acid, isetionic acid, lactobionic acid, oleic acid, pamoic acid, polygalacturonic acid, stearic acid, tannic acid, trifluoromethane Salts with organic acids such as sulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, lauryl ester sulfate, methyl sulfate, naphthalenesulfonic acid, sulfosalicylic acid; quaternary ammonium salt with methyl bromide, methyl iodide, etc .; bromine Salts with halogen ions such as ions, chlorine ions and iodine ions; Salts with alkali metals such as lithium, sodium and potassium; Salts with alkaline earth metals such as calcium and magnesium; Metal salts with iron, zinc and the like; Salt with ammonia; triethylenediamine, 2-aminoethanol, 2,2-iminobis (ethanol), 1-deoxy-1- (methylamino) -2-D-sorbitol, 2-amino-2- (hydroxymethyl)- Examples thereof include salts with organic amines such as 1,3-propanediol, procaine, N, N-bis (phenylmethyl) -1,2-ethanediamine and the like.
本発明において、キサントフィル又はその塩は、本発明の組成物の総量に対して、その下限は0.1重量%、好ましくは0.5重量%、より好ましくは1重量%、更に好ましくは1.5重量%であり、特に好ましくは2重量%である。また、その上限は90重量%、好ましくは80重量%、より好ましくは70重量%、更に好ましくは60重量%、特に好ましくは50重量%である。さらに、それらの上限と下限は適宜組み合わせて使用することができる。より具体的には、例えば、0.1〜90重量%、好ましくは0.5〜80重量%、より好ましくは0.1〜70重量%、更に好ましくは1.5〜60重量%、特に好ましくは2〜50重量%で使用することができる。 In the present invention, the lower limit of xanthophyll or a salt thereof is 0.1% by weight, preferably 0.5% by weight, more preferably 1% by weight, still more preferably 1. It is 5% by weight, particularly preferably 2% by weight. The upper limit thereof is 90% by weight, preferably 80% by weight, more preferably 70% by weight, still more preferably 60% by weight, and particularly preferably 50% by weight. Further, the upper limit and the lower limit thereof can be used in combination as appropriate. More specifically, for example, 0.1 to 90% by weight, preferably 0.5 to 80% by weight, more preferably 0.1 to 70% by weight, still more preferably 1.5 to 60% by weight, particularly preferably. Can be used in 2 to 50% by weight.
本発明において、ヒシ属(Trapa)植物は、特に限定されない。ヒシ属(Trapa)植物の具体例として、ツノナシビシ(Trapa acornis Nakano)、ヒメビシ(Trapa incisa Sieb. et Zuc.)、ヒシ(Trapa japonica Flerov)、トウビシ(Trapa bispinosa Roxb.)、トラパ・ナタンス(Trapa natans L.)、オニビシ(Trapa natans L.var.japonica Nakai)等が挙げられ、好ましくは、ヒシ(Trapa japonica Flerov)、トウビシ(Trapa bispinosa Roxb.)、オニビシ(Trapa natans L.var.japonica Nakai)が挙げられ、特に好ましくは、トウビシ(Trapa bispinosa Roxb.)が挙げられる。 In the present invention, the Trapa plant is not particularly limited. Specific examples of the water chestnut genus (Trapa) plants, Tsunonashibishi (Trapa acornis Nakano), Himebishi (Trapa incisa Sieb. Et Zuc.), Water chestnut (Trapa japonica Flerov), Toubishi (Trapa bispinosa Roxb.), Torapa-Natansu (Trapa natans L.), Onibishi (Trapa natans L. var. Japanica Nakai) and the like, preferably Hishi (Trapa japonica Flelov), Tobishi (Trapa bispinosa Roxb.), Onibishi (Tr). In particular, trapa trapa (Trapa bispinosa Roxb.) Can be mentioned.
本発明において、ヒシ属植物の加工物は、前記ヒシ属植物の全体又は各部位から調製・製造できる。各部位としては、例えば、花、花穂、果皮、果実、果肉、茎、葉、枝、枝葉、幹、樹皮、根茎、根皮、根、種子、虫えい、心材、地上部、又は地下部が挙げられ、特に果皮が好ましい。また、ヒシ属植物の加工物の調製・製造方法は、特に限定されず、例えば、通常用いられる方法により調製・製造することができる。 In the present invention, a processed product of a Trapa plant can be prepared and produced from the whole or each part of the Trapa plant. Examples of each part include flowers, spikes, pericarp, fruits, flesh, stems, leaves, branches, branches and leaves, trunks, bark, rhizomes, root bark, roots, seeds, insects, heartwood, above-ground parts, or underground parts. The peel is particularly preferable. The method for preparing and producing a processed product of the genus Trapa is not particularly limited, and for example, it can be prepared and produced by a commonly used method.
本発明において、ヒシ属植物の加工物の総重量に対するポリフェノールの含量の下限は、0.1重量%、好ましくは5重量%、特に好ましくは10重量%である。また、その上限は80重量%、好ましくは70重量%、特に好ましくは60重量%である。さらに、それらの上限と下限は適宜組み合わせて使用することができる。より具体的には、ヒシ属植物の加工物の総重量に対するポリフェノールの含量は、0.1〜80重量%、好ましくは5〜70重量%、特に好ましくは10〜60重量%である。また、ポリフェノール含量は、例えば、FOLIN−CIOCALTEU法等により測定することができる。 In the present invention, the lower limit of the content of polyphenols based on the total weight of the processed products of Trapa plants is 0.1% by weight, preferably 5% by weight, and particularly preferably 10% by weight. The upper limit is 80% by weight, preferably 70% by weight, and particularly preferably 60% by weight. Further, the upper limit and the lower limit thereof can be used in combination as appropriate. More specifically, the content of polyphenols based on the total weight of the processed products of the genus Trapa is 0.1 to 80% by weight, preferably 5 to 70% by weight, and particularly preferably 10 to 60% by weight. Moreover, the polyphenol content can be measured by, for example, the FOLIN-CIOCALTEU method or the like.
本発明において、ヒシ属植物の加工物は、例えば、前記ヒシ属植物の粉砕物、抽出物及それら乾燥物である。ヒシ属植物の粉砕物、抽出物及びそれら乾燥物は、例えば、ヒシ属植物の根、茎、葉、花蕾、花、樹皮、果実(種子)、果皮等の各部位をそのまま又は適当な大きさに切断、粉砕、搾汁、溶媒抽出等により、また、場合によりそれらを乾燥させることで調製・製造できる。さらに、1種類以上のヒシ属植物の各部位を混合して調製・製造することもできる。 In the present invention, the processed product of the Trapa plant is, for example, a pulverized product, an extract of the Trapa plant, and a dried product thereof. The crushed products, extracts and dried products of Trapa plants have, for example, roots, stems, leaves, flower buds, flowers, bark, fruits (seed), fruit skins, etc. of the Trapa plants as they are or of appropriate size. It can be prepared and manufactured by cutting, crushing, squeezing, extracting a solvent, etc., and in some cases, drying them. Further, it is also possible to prepare and produce by mixing each part of one or more kinds of Trapa plants.
本発明において、ヒシ属植物の抽出物の調製・製造には、抽出溶媒として、例えば、水、有機溶媒又はそれらの混合溶媒を使用できる。有機溶媒としては、例えば、メタノール、エタノール等の低級アルコール、クロロホルム、酢酸エチル、n−ヘキサン等が挙げられ、好ましくは、メタノール、エタノールが挙げられる。また、これらの有機溶媒の二種以上混合して使用することもできる。 In the present invention, for the preparation and production of the extract of the genus Trapa, for example, water, an organic solvent or a mixed solvent thereof can be used as the extraction solvent. Examples of the organic solvent include lower alcohols such as methanol and ethanol, chloroform, ethyl acetate, n-hexane and the like, and preferred examples include methanol and ethanol. In addition, two or more of these organic solvents can be mixed and used.
本発明において、抽出溶媒の使用量は、ヒシ属植物の種類や部位、抽出溶媒の種類等により適宜選択できる。ヒシ属植物と抽出溶媒との重量比は、例えば、1:2〜1:30、好ましくは、1:3〜1:20、特に好ましくは、1:5〜1:10である。また、抽出時間は、例えば、数分〜30日、好ましくは1時間〜15日である。抽出温度は、例えば、5〜100℃である。抽出方法は特に制限されず、例えば、バッチ抽出、カラム抽出を用いた連続抽出等、任意の方法を適用することができる。 In the present invention, the amount of the extraction solvent used can be appropriately selected depending on the type and site of the Trapa plant, the type of the extraction solvent, and the like. The weight ratio of the Trapa plant to the extraction solvent is, for example, 1: 2 to 1:30, preferably 1: 3 to 1:20, and particularly preferably 1: 5 to 1:10. The extraction time is, for example, several minutes to 30 days, preferably 1 hour to 15 days. The extraction temperature is, for example, 5 to 100 ° C. The extraction method is not particularly limited, and any method such as batch extraction and continuous extraction using column extraction can be applied.
本発明において、得られるヒシ属植物の抽出物は、そのままの状態で用いることができる。また、必要に応じて、更に精製処理を加えることもできる。この精製処理は、通常の方法により行えばよく、例えば、ヒシ属植物の抽出物を常法によりろ過することで精製することができる。その後、得られたろ液を減圧濃縮、凍結乾燥等して、本発明に関するヒシ属植物の抽出物とすることもできる。 In the present invention, the obtained extract of the genus Trapa can be used as it is. Further, if necessary, further purification treatment can be added. This purification treatment may be carried out by a usual method, and for example, it can be purified by filtering an extract of a Trapa plant by a conventional method. Then, the obtained filtrate can be concentrated under reduced pressure, freeze-dried, or the like to obtain an extract of the Trapa plant according to the present invention.
本発明において、ヒシ属植物の加工物として、例えば、ヒシ属植物の果皮の抽出物又はその乾燥物を使用することができる。ヒシ属植物の果皮の抽出物又はその乾燥物は、例えば、ヒシ属植物の果皮を水やメタノール、エタノール等の低級アルコールで抽出し、ろ過、濃縮し、場合により賦形剤等を加えて、乾燥することにより、調製・製造することができる。 In the present invention, as a processed product of the Trapa plant, for example, an extract of the pericarp of the Trapa plant or a dried product thereof can be used. The extract of the fruit skin of the Trapa genus plant or a dried product thereof is obtained by, for example, extracting the fruit skin of the Trapa genus plant with water or a lower alcohol such as methanol or ethanol, filtering and concentrating it, and optionally adding an excipient or the like. It can be prepared and manufactured by drying.
本発明において、ヒシ属植物の加工物として、特に好ましいものは、トウビシの加工物であるヒシエキスである。 In the present invention, a particularly preferable processed product of the genus Trapa is a trapa extract, which is a processed product of Trapa.
本発明において、ヒシ属植物の果皮の抽出物の総重量に対するポリフェノールの含量の下限は、0.1重量%、好ましくは1重量%、より好ましくは5重量%、更に好ましくは10重量%、特に20重量%である。また、その上限は90重量%、好ましくは80重量%、より好ましくは70重量%、更に好ましくは65重量%、特に好ましくは60重量%である。さらに、それらの上限と下限は適宜組み合わせて使用することができる。より具体的には、ヒシ属植物の果皮の抽出物の総重量に対するポリフェノールの含量は、0.1〜90重量%、好ましくは1〜80重量%、より好ましくは5〜70重量%、更に好ましくは10〜65重量%、特に好ましくは20〜60重量%である。 In the present invention, the lower limit of the content of polyphenols based on the total weight of the extract of the peel of a plant of the genus Trapa is 0.1% by weight, preferably 1% by weight, more preferably 5% by weight, still more preferably 10% by weight, particularly. 20% by weight. The upper limit is 90% by weight, preferably 80% by weight, more preferably 70% by weight, still more preferably 65% by weight, and particularly preferably 60% by weight. Further, the upper limit and the lower limit thereof can be used in combination as appropriate. More specifically, the content of polyphenols based on the total weight of the extract of the peel of a plant of the genus Trapa is 0.1 to 90% by weight, preferably 1 to 80% by weight, more preferably 5 to 70% by weight, still more preferably. Is 10 to 65% by weight, particularly preferably 20 to 60% by weight.
本発明において、ヒシ属植物の加工物に加える賦形剤は、例えば、デキストリン、シクロデキストリン、乳糖、結晶セルロース、二酸化ケイ素、環状オリゴ糖等が挙げられ、好ましくは、シクロデキストリン、環状オリゴ糖が挙げられ、特に好ましくはシクロデキストリンが挙げられる。 In the present invention, examples of excipients added to the processed products of Trapa plants include dextrin, cyclodextrin, lactose, crystalline cellulose, silicon dioxide, cyclic oligosaccharides and the like, and cyclodextrin and cyclic oligosaccharides are preferable. Included, with particular preference being cyclodextrin.
本発明において、ヒシ属植物の加工物は、本発明の組成物の総量に対して、その下限は0.1重量%、好ましくは1重量%、より好ましくは10重量%、更に好ましくは25重量%、特に60重量%であり、その上限は99重量%、好ましくは95重量%、より好ましくは90重量%、更に好ましくは85重量%、特に好ましくは80重量%である。さらに、それらの上限と下限は適宜組み合わせて使用することもできる。
より具体的には、0.1〜99重量%、好ましくは1〜95重量%、より好ましくは10〜90重量%、更に好ましくは25〜85重量%、特に好ましくは60〜80重量%で使用することができる。
In the present invention, the lower limit of the processed product of the genus Hishi is 0.1% by weight, preferably 1% by weight, more preferably 10% by weight, still more preferably 25% by weight, based on the total amount of the composition of the present invention. %, Especially 60% by weight, and the upper limit thereof is 99% by weight, preferably 95% by weight, more preferably 90% by weight, still more preferably 85% by weight, and particularly preferably 80% by weight. Further, the upper limit and the lower limit thereof can be used in combination as appropriate.
More specifically, it is used in an amount of 0.1 to 99% by weight, preferably 1 to 95% by weight, more preferably 10 to 90% by weight, still more preferably 25 to 85% by weight, and particularly preferably 60 to 80% by weight. can do.
本発明において、更に、キサントフィル及び/又はヒシ属植物の加工物に加えて、その他の有効成分(例えば、補助的な効果を有する物質)を添加することができる。例えば、ビタミンA類;カロテノイド類(キサントフィル除く);ビタミンB類;ビタミンC類;ビタミンD類、ビタミンE類;トコトリエノール類;グルタチオン及びこれらの誘導体並びにこれらの塩;カテキン、アントシアニン、タンニン、ルチン、イソフラボン、クロロゲン酸、エラグ酸、クルクミン、クマリン等のポリフェノール類;リノール酸、α−又はγ−リノレン酸、アラキドン酸、エイコサペンタエン酸、イワシ酸、ドコサヘキサエン酸及びその誘導体並びにそれらの塩;コラーゲン、エラスチン、フィブロネクチン、ケラチンから選ばれるタンパク質及びそれらの誘導体並びに加水分解物;グリコール酸、乳酸、リンゴ酸、クエン酸、サリチル酸等のα−ヒドロキシ酸及びそれらの誘導体並びにそれらの塩;血清除蛋白、脾臓、胎盤、鶏冠、ローヤルゼリー、酵母、乳酸菌、ビフィズス菌、霊芝、ニンジン、センブリ、ローズマリー、オウバク、ニンニク、ヒノキチオール、セファランチン、アロエ、サルビア、アルニカ、カミツレ、シラカバ、オトギリソウ、ユーカリ、ムクロジ、センプクカ、ケイケットウ、サンペンズ、ソウハクヒ、トウキ、イブキトラノオ、クララ、サンザシ、シラユリ、ホップ、ノイバラ、ヨクイニン、ドクダミ、海藻、納豆、レモングラス、ハイビスカス、イチョウ葉エキス、ホスファチジルセリン等の天然物並びにそれらの抽出物;アデノシン三リン酸、アデノシン二リン酸、アデノシン一リン酸等のアデニル酸誘導体;鉄、バナジウム、モリブデン、マンガン、銅、カリウム、マグネシウム、カルシウム、亜鉛、セレン、ヨウ素等のミネラル類;マンニトール、キシリトール、グルコサミン等の単糖類;ヒアルロン酸、コンドロイチン硫酸、デルマタン硫酸、ヘパラン硫酸、ヘパリン、ケラタン硫酸、グリコーゲン、キチン、キトサン等の多糖類;デオキシリボ核酸、リボ核酸等の核酸類;その他のグリチルリチン酸、グアニン、ムチン、ユビキノン、α−リポ酸、オクタコサノール、アリシン、アリイン等、並びにそれらの混合物からなる群から1種又は2種以上選択することができる。好ましくはビタミンA類;カロテノイド類(キサントフィル除く);ビタミンB類;ビタミンC類;ビタミンD類、ビタミンE類;トコトリエノール類;グルタチオン及びこれらの誘導体並びにこれらの塩;カテキン、アントシアニン、エラグ酸等のポリフェノール類;リノール酸、α−又はγ−リノレン酸、アラキドン酸、エイコサペンタエン酸、イワシ酸、ドコサヘキサエン酸及びその誘導体並びにそれらの塩;コラーゲン、エラスチン、フィブロネクチン、ケラチンから選ばれるタンパク質及びそれらの誘導体並びに加水分解物;銅、亜鉛等のミネラル類;ムチン、ユビキノン、α−リポ酸等、並びにそれらの混合物からなる群から1種又は2種以上選択することができる。更に好ましくは、ビタミンA類;カロテノイド類(キサントフィル除く);ビタミンC類;ビタミンE類;トコトリエノール類;グルタチオン及びこれらの誘導体並びにこれらの塩;カテキン、アントシアニン、エラグ酸等のポリフェノール類;エイコサペンタエン酸、ドコサヘキサエン酸及びその誘導体並びにそれらの塩;銅、亜鉛等のミネラル類;ムチン、ユビキノン、α−リポ酸等、並びにそれらの混合物からなる群から1種又は2種以上選択することができる。 In the present invention, other active ingredients (for example, substances having an auxiliary effect) can be further added in addition to xanthophylls and / or processed products of Trapa plants. For example, vitamin A; carotenoids (excluding xanthophile); vitamin B; vitamin C; vitamin D, vitamin E; tocotrienol; glutathione and its derivatives and salts thereof; catechin, anthocyanin, tannin, rutin, Polyphenols such as isoflavone, chlorogenic acid, ellagic acid, curcumin, coumarin; linoleic acid, α- or γ-linolenic acid, arachidonic acid, eicosapentaenoic acid, sardine acid, docosahexaenoic acid and its derivatives and salts thereof; collagen, elastin , Fibronectin, proteins selected from keratin and their derivatives and hydrolyzates; α-hydroxy acids such as glycolic acid, lactic acid, malic acid, citric acid, salicylic acid and their derivatives and their salts; serum deproteinized, spleen, Placenta, chicken crown, royal jelly, yeast, lactic acid bacteria, bifidus, reishi, carrot, senburi, rosemary, aubergine, garlic, hinokithiol, cepharanthin, aloe, salvia, arnica, chamomile, white birch, otogirisou, eucalyptus, mukuroji , Sanpens, Souhakuhi, Touki, Ibukitranoo, Clara, Sanzashi, Shirayuri, Hop, Neubara, Yokuinin, Dokudami, Seaweed, Natto, Lemongrass, Hibiscus, Ginkgo biloba extract, Phosphatidylserine and other natural products and their extracts; Adenylic acid derivatives such as triphosphate, adenosine diphosphate, adenosine monophosphate; minerals such as iron, vanadium, molybdenum, manganese, copper, potassium, magnesium, calcium, zinc, selenium, iodine; mannitol, xylitol, glucosamine Monosaccharides such as: Hyaluronic acid, chondroitin sulfate, dermatan sulfate, heparan sulfate, heparin, keratane sulfate, glycogen, chitin, chitosan and other polysaccharides; deoxyribonucleic acid, ribonucleic acid and other nucleic acids; other glycyrrhizinic acid, guanine, mutin , Ubiquinone, α-lipoic acid, octacosanol, alicin, aliine, etc., and a mixture thereof can be selected from one or more. Preferably, vitamin A; carotenoids (excluding xanthophylls); vitamin B; vitamin C; vitamin D, vitamin E; tocotrienol; glutathione and derivatives thereof and salts thereof; catechin, anthocyanin, ellagic acid and the like. Polyphenols; linoleic acid, α- or γ-linolenic acid, arachidonic acid, eikosapentaenoic acid, sardine acid, docosahexaenoic acid and salts thereof; proteins selected from collagen, elastin, fibronectin, keratin and derivatives thereof, and Hydrolyzate; minerals such as copper and zinc; one or more can be selected from the group consisting of mutin, ubiquinone, α-lipoic acid and the like, and mixtures thereof. More preferably, vitamin A; carotenoids (excluding xanthophylls); vitamin C; vitamin E; tocotrienols; glutathione and derivatives thereof and salts thereof; polyphenols such as catechin, anthocyanin, ellagic acid; , Docosahexaenoic acid and its derivatives and salts thereof; minerals such as copper and zinc; one or more can be selected from the group consisting of mutin, ubiquinone, α-lipoic acid and the like, and mixtures thereof.
本発明において、前記のその他の有効成分は、組成物の総量に対して、その下限は0.1重量%、好ましくは1重量%、より好ましくは5重量%、更に好ましくは10重量%、特に20重量%であり、その上限は99重量%、好ましくは90重量%、より好ましくは80重量%、更に好ましくは70重量%、特に好ましくは60重量%である。また、それらの上限と下限は適宜組み合わせて使用することもできる。
より具体的には、例えば0.1〜99重量%、好ましくは1〜90重量%、より好ましくは5〜80重量%、更に好ましくは10〜80重量%、特に好ましくは20〜70重量%で配合され、一種以上組み合わせて用いることができる。
In the present invention, the lower limit of the other active ingredient is 0.1% by weight, preferably 1% by weight, more preferably 5% by weight, still more preferably 10% by weight, based on the total amount of the composition. It is 20% by weight, and the upper limit thereof is 99% by weight, preferably 90% by weight, more preferably 80% by weight, still more preferably 70% by weight, and particularly preferably 60% by weight. Further, the upper limit and the lower limit thereof can be used in combination as appropriate.
More specifically, for example, 0.1 to 99% by weight, preferably 1 to 90% by weight, more preferably 5 to 80% by weight, still more preferably 10 to 80% by weight, and particularly preferably 20 to 70% by weight. It is compounded and can be used in combination of one or more.
本発明において、本発明の組成物は、飲食品、機能性表示食品、特定保健食品、医薬部外品、医薬品(ヒト以外の哺乳類用医薬品を含む)等に使用可能な有効成分や添加剤を適宜配合することができ、また、当該品目で通常使用される製剤化方法により、適宜製剤化することができる。 In the present invention, the composition of the present invention contains active ingredients and additives that can be used for foods and drinks, foods with functional claims, specified health foods, quasi-drugs, pharmaceuticals (including pharmaceuticals for mammals other than humans) and the like. It can be appropriately blended, and can be appropriately formulated by the formulation method usually used for the product.
本発明において、症状の改善・予防が許可されている飲食品とは、国や公共団体が許可・指定している医薬品的な効能を有する食品であり、例えば、機能性表示食品、特定保健食品等の保健機能食品、特別用途食品等である。なお、状況や時代、各国の制度により名称や規程が変化するが、本質的に同じであるものは本発明に含まれる。 In the present invention, foods and drinks for which improvement / prevention of symptoms is permitted are foods having medicinal effects permitted / designated by the national government or public organizations, and are, for example, foods with functional claims and foods with specified health claims. Such as health functional foods, special purpose foods, etc. Although the names and regulations change depending on the situation, the times, and the systems of each country, those that are essentially the same are included in the present invention.
本発明において、本発明の組成物の配合量は、特に制限されず、適用の目的(対象疾患や症状の種類等)、適用対象(ヒト、ヒト以外の動物(好ましくは哺乳類であり、特に好ましくは犬、猫等のペット))、適用対象部位、適用対象の性別や年齢、飲食品、機能性表示食品、特定保健食品、医薬部外品、又は医薬品の形態、これらの投与又は摂取方法や回数、嗜好等に応じて適宜設定される。 In the present invention, the blending amount of the composition of the present invention is not particularly limited, and the purpose of application (type of target disease or symptom, etc.) and the target of application (human beings, animals other than humans (preferably mammals, particularly preferable). (Pets such as dogs and cats)), applicable parts, applicable gender and age, foods and drinks, foods with functional claims, specified health foods, quasi-drugs, or forms of pharmaceuticals, their administration or ingestion methods, etc. It is appropriately set according to the number of times, taste, and the like.
本発明において、本発明の組成物の飲食品、機能性表示食品、特定保健食品、医薬部外品、又は医薬品への配合量は、特に制限されないが、本発明の組成物の成人1日当たりの適用量は、その下限は0.1mg、好ましくは1mg、より好ましくは10mg、更に好ましくは30mg、特に好ましくは50mgであり、その上限は2000mg、好ましくは1500mg、より好ましくは1000mg、更に好ましくは500mg、特に好ましくは300mgである。また、それらの上限と下限は適宜組み合わせて使用することもできる。
より具体的には、例えば、0.1〜2000mgであり、好ましくは1〜1500mg、より好ましくは10〜1000mg、更に好ましくは30〜500mg、特に好ましくは50〜300mgである。
In the present invention, the amount of the composition of the present invention to be added to foods and drinks, foods with functional claims, specified health foods, quasi-drugs, or pharmaceuticals is not particularly limited, but the composition of the present invention per adult per day. The lower limit of the applied amount is 0.1 mg, preferably 1 mg, more preferably 10 mg, further preferably 30 mg, particularly preferably 50 mg, and the upper limit thereof is 2000 mg, preferably 1500 mg, more preferably 1000 mg, still more preferably 500 mg. , Particularly preferably 300 mg. Further, the upper limit and the lower limit thereof can be used in combination as appropriate.
More specifically, for example, it is 0.1 to 2000 mg, preferably 1 to 1500 mg, more preferably 10 to 1000 mg, still more preferably 30 to 500 mg, and particularly preferably 50 to 300 mg.
本発明において、本発明の組成物を使用する場合には、キサントフィル又はその塩の成人1日当たりの適用量は、その下限は0.1mg、好ましくは0.5mg、より好ましくは1mg、更に好ましくは3mg、特に好ましくは5mgであり、その上限は500mg、好ましくは250mg、より好ましくは100mg、更に好ましくは75mg、特に好ましくは50mgである。また、それらの上限と下限は適宜組み合わせて使用することもできる。
より具体的には、例えば0.1〜500mg、好ましくは0.5〜250mg、より好ましくは1〜100mg、更に好ましくは3〜75mg、特に好ましくは5〜50mgである。
In the present invention, when the composition of the present invention is used, the lower limit of the amount of xanthophyll or a salt thereof applied per day for an adult is 0.1 mg, preferably 0.5 mg, more preferably 1 mg, still more preferably. It is 3 mg, particularly preferably 5 mg, the upper limit of which is 500 mg, preferably 250 mg, more preferably 100 mg, still more preferably 75 mg, and particularly preferably 50 mg. Further, the upper limit and the lower limit thereof can be used in combination as appropriate.
More specifically, for example, it is 0.1 to 500 mg, preferably 0.5 to 250 mg, more preferably 1 to 100 mg, still more preferably 3 to 75 mg, and particularly preferably 5 to 50 mg.
本発明において、本発明の組成物を使用する場合には、ヒシ属植物の加工物の成人1日当たりの適用量は、その下限は0.1mg、好ましくは1mg、より好ましくは10mg、更に好ましくは25mg、特に好ましくは50mgであり、その上限は2000mg、好ましくは1500mg、より好ましくは1000mg、更に好ましくは500mg、特に好ましくは300mgである。また、それらの上限と下限は適宜組み合わせて使用することもできる。
より具体的には、例えば0.1〜2000mg、好ましくは1〜1500mg、より好ましくは10〜1000mg、更に好ましくは25〜500mg、特に好ましくは50〜300mgである。
In the present invention, when the composition of the present invention is used, the lower limit of the applied amount of the processed product of the genus Trapa per adult is 0.1 mg, preferably 1 mg, more preferably 10 mg, still more preferably. It is 25 mg, particularly preferably 50 mg, the upper limit of which is 2000 mg, preferably 1500 mg, more preferably 1000 mg, still more preferably 500 mg, and particularly preferably 300 mg. Further, the upper limit and the lower limit thereof can be used in combination as appropriate.
More specifically, for example, it is 0.1 to 2000 mg, preferably 1 to 1500 mg, more preferably 10 to 1000 mg, still more preferably 25 to 500 mg, and particularly preferably 50 to 300 mg.
本発明の一態様は、キサントフィル又はその塩及びヒシ属植物の加工物を含有する、経口用又は非経口用の組成物である。本発明の組成物は、経口用組成物及び非経口用組成物として使用することができる。 One aspect of the present invention is an oral or parenteral composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa. The composition of the present invention can be used as an oral composition and a parenteral composition.
本発明の一態様は、キサントフィル又はその塩及びヒシ属植物の加工物を含有する、飲食品又は医薬用の組成物である。本発明の組成物は、飲食品及び医薬として使用することができる。 One aspect of the present invention is a food or drink or pharmaceutical composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa. The composition of the present invention can be used as a food or drink and a medicine.
本発明の一態様は、キサントフィル又はその塩及びヒシ属植物の加工物を含有する、サプリメント用の組成物である。本発明の組成物は、サプリメントとして使用することができる。 One aspect of the present invention is a composition for supplements containing xanthophyll or a salt thereof and a processed product of the genus Trapa. The composition of the present invention can be used as a supplement.
本発明の一態様は、キサントフィル又はその塩及びヒシ属植物の加工物を含有する、眼科用の組成物である。 One aspect of the present invention is an ophthalmic composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa.
本発明において、本発明の組成物は、キサントフィル及び/又はヒシ属植物の加工物に加えて、その他の成分、例えば、賦形剤、増粘剤、乳化剤(例えば、蜜蝋、グリセリン脂肪酸エステル)等を混合して、所望の形態に調製することができる。本発明の組成物の形態については、特に制限はなく、例えば、ソフトカプセル、ハードカプセル、液剤、ゼリー、グミ、錠剤、散剤、ゲル状剤等のサプリメント等の形態が挙げられる。 In the present invention, in addition to xanthophile and / or processed products of Trapa plants, the compositions of the present invention include other components such as excipients, thickeners, emulsifiers (eg, beeswax, glycerin fatty acid ester) and the like. Can be mixed to prepare the desired form. The form of the composition of the present invention is not particularly limited, and examples thereof include supplements such as soft capsules, hard capsules, liquids, jellies, gummies, tablets, powders, and gels.
本発明において、本発明の飲食品用の組成物として調製する場合、キサントフィル及び/又はヒシ属植物の加工物に加えて、その他の成分、例えば、甘味料、着色料、保存料、増粘剤、安定剤、ゲル化剤、糊剤、酸化防止剤、発色剤、漂白剤、防かび剤(防ばい剤)、イーストフード、ガムベース、香料、酸味料、調味料、乳化剤、pH調整剤、かんすい、膨脹剤、栄養強化剤、その他飲食品素材等を混合等して、所望の形態に調製することができる。例えば、その形態については、特に制限されるものではなく、ゲル状剤、顆粒、細粒、カプセル、ソフトカプセル、錠剤、粉末、液剤、半固形剤等のサプリメントタイプの食品;炭酸飲料、清涼飲料、乳飲料、アルコール飲料、果汁飲料、茶類、栄養飲料等の飲料;粉末ジュース、粉末スープ等の粉末飲料;ガム、タブレット、キャンディー、クッキー、グミ、せんべい、ビスケット、ゼリー等の菓子類;パン、麺類、シリアル、ジャム、調味料等の形態とすることができる。これらの形態は、例えば、視機能低下の予防及び/又は改善のための飲食品として使用することができ、例えば、一般の飲食品の他、栄養補助食品、機能性表示食品、特定保健用食品、病者用食品等のニュートラシューティカルとしても使用することもできる。 In the present invention, when prepared as a composition for foods and drinks of the present invention, in addition to xanthophile and / or processed products of the genus Hishi, other ingredients such as sweeteners, colorants, preservatives and thickeners , Stabilizers, gelling agents, glues, antioxidants, color formers, bleaching agents, fungicides (antibacterial agents), yeast foods, gum bases, fragrances, acidulants, seasonings, emulsifiers, pH adjusters, kansui , A swelling agent, a nutrient enhancer, and other food and drink materials can be mixed to prepare a desired form. For example, the form thereof is not particularly limited, and supplement-type foods such as gels, granules, fine granules, capsules, soft capsules, tablets, powders, liquids, and semi-solids; carbonated drinks, soft drinks, etc. Beverages such as dairy drinks, alcoholic drinks, fruit juice drinks, teas and nutritional drinks; powdered drinks such as powdered juices and powdered soups; sweets such as gums, tablets, candies, cookies, gummies, senbei, biscuits and jellies; bread, It can be in the form of noodles, cereals, jams, seasonings, etc. These forms can be used, for example, as foods and drinks for preventing and / or improving visual function deterioration. For example, in addition to general foods and drinks, dietary supplements, foods with functional claims, foods for specified health use, etc. It can also be used as a nutritive for foods for the sick.
本発明において、本発明の医薬用の組成物(医薬品、医薬部外品等)として調製する場合、キサントフィル及び/又はヒシ属植物の加工物に加えて、必要に応じて他の薬効成分、薬学的に許容される担体や添加剤等を配合することができる。例えば、薬学的に許容される担体及び添加剤として、結合剤、崩壊剤、滑沢剤、湿潤化剤、緩衝剤、保存剤、香料等を混合等して、所望の形態に調製することができる。
例えば、その形態については、特に制限されるものではなく、注射剤、外用剤、吸入剤、座剤、フィルム剤、トローチ剤、液剤、散剤、錠剤、顆粒剤、カプセル剤、シロップ剤、点眼剤、洗眼剤、点鼻剤等の形態とすることができる。これらの形態の中でも、経口投与に適した形態(即ち、内服用医薬品)が好ましく、例えば、トローチ剤、液剤、散剤、錠剤、顆粒剤、カプセル剤、ソフトカプセル剤、シロップ剤等が特に好ましい。これらの形態は、例えば、視機能低下の予防及び/又は治療のための医薬品として使用することができる。
In the present invention, when prepared as a pharmaceutical composition (pharmaceutical product, quasi-drug, etc.) of the present invention, in addition to xanthophyll and / or processed products of Trapa plants, other medicinal ingredients and pharmaceuticals as necessary. It is possible to blend a carrier, an additive, etc. that are generally acceptable. For example, as a pharmaceutically acceptable carrier and additive, a binder, a disintegrant, a lubricant, a wetting agent, a buffer, a preservative, a fragrance and the like can be mixed to prepare a desired form. it can.
For example, the form thereof is not particularly limited, and injections, external preparations, inhalants, suppositories, films, troches, liquids, powders, tablets, granules, capsules, syrups, eye drops. , Eye drops, nasal drops, etc. Among these forms, a form suitable for oral administration (that is, an oral drug) is preferable, and for example, a troche agent, a liquid agent, a powder, a tablet, a granule, a capsule, a soft capsule, a syrup, or the like is particularly preferable. These forms can be used, for example, as pharmaceuticals for the prevention and / or treatment of visual impairment.
本発明の一態様は、視機能低下及びそれに伴う自覚症状の予防及び/又は改善のための、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物である。本発明の組成物は、視機能低下の予防及び/又は改善のために使用することができる。 One aspect of the present invention is a composition containing xanthophyll or a salt thereof and a processed product of a Trapa plant for prevention and / or improvement of visual function deterioration and associated subjective symptoms. The composition of the present invention can be used for prevention and / or improvement of visual deterioration.
本発明において、「視機能低下」とは、文字や画像等の視覚情報、すなわち対象の形態、色、明暗、運動等の視覚情報を知覚する能力が衰えることを意味し、例えば、眼の疲労、眼の老化、又は眼のピント調節機能の低下(毛様体筋の収縮、弛緩等により水晶体の厚みを変化させ網膜にピント調節する機能が衰えること);老視、老人性白内障等の加齢による視力の低下;疲れ目、白内障、糖尿病網膜症等の疾患に伴う視力の低下を含む。また、「視機能低下の予防及び/又は改善」とは、前記の視機能低下の予防又は抑止、治療又は改善を意味し、そして視機能の維持を含む。視機能低下は、例えば、加齢、紫外線、血行不良、乾燥、及び/又は活性酸素により誘発される。さらに、「それに伴う自覚症状」とは、視機能低下による自覚症状であれば、特に制限されるものではないが、例えば、肩、首筋、背中又は腰のこり、が挙げられる。 In the present invention, "decreased visual function" means that the ability to perceive visual information such as characters and images, that is, visual information such as morphology, color, lightness and darkness, and movement of an object is diminished. For example, eye fatigue. , Eye aging, or decreased eye focus adjustment function (decrease in the ability to adjust the focus on the retina by changing the thickness of the crystalline body due to contraction and relaxation of hairy muscles); Addition of senile vision, senile cataract, etc. Age-related loss of vision; includes loss of vision associated with diseases such as tired eyes, cataracts, and diabetic retinopathy. In addition, "prevention and / or improvement of visual function deterioration" means prevention or suppression, treatment or improvement of the above-mentioned visual function deterioration, and includes maintenance of visual function. Visual decline is induced, for example, by aging, UV light, poor circulation, dryness, and / or reactive oxygen species. Further, the "subsequent subjective symptom" is not particularly limited as long as it is a subjective symptom due to a decrease in visual function, and examples thereof include shoulder, nape, back or waist stiffness.
本発明において、本発明の組成物に係る商品、商品の包装、商品に係る情報、又は商品に係る広告(例えば、取引書類、取扱い説明書、添付文書、通信販売のカタログやインターネットサイト等)には、「視機能低下の予防(若しくは抑止)及び/又は改善(若しくは治療)」と表示することができ、また、「視機能低下の予防及び/又は改善」は、例えば、紫外線により誘発される眼障害の抑制、加齢等によって減少する目の黄斑部の色素量を上昇させる、ブルーライト等の光の刺激からの保護、(低下した)コントラスト感度の改善、目の調子を整える、目の疲労感を和らげる、(VDT作業等による)眼の疲労感を軽減する、網膜中心部の色素量を増やす、(日常生活で受ける)光の刺激から目を保護、目の健康を維持、(正常な目の)ピント調節機能を維持、目の疲労感の緩和、目の乾きの緩和、ピント調節機能の低下を緩和、視覚機能を維持、目の黄斑部の健康を維持、ピント調節機能をサポート、コントラスト感度(色の濃さの判別力)をサポート、見る力の維持、手元のピント調節機能を助ける、目の使用による肩・首筋への負担を和らげる等と表示をすることもでき、更にそれらに類似する表示をすることもできる。 In the present invention, for a product related to the composition of the present invention, packaging of the product, information related to the product, or an advertisement related to the product (for example, transaction documents, instruction manuals, attachments, mail-order catalogs, Internet sites, etc.) Can be labeled as "prevention (or suppression) and / or improvement (or treatment) of visual deterioration", and "prevention and / or improvement of visual deterioration" is induced by, for example, ultraviolet rays. Suppression of eye damage, increase of pigment amount in the yellow spot of the eye, which decreases with aging, protection from light stimuli such as blue light, improvement of (decreased) contrast sensitivity, tone of the eye, eye Relieves fatigue, reduces eye fatigue (due to VDT work, etc.), increases the amount of pigment in the central part of the retina, protects the eyes from light stimuli (received in daily life), maintains eye health, (normal) Maintains focus adjustment function, relieves eye fatigue, relieves dry eyes, relieves deterioration of focus adjustment function, maintains visual function, maintains health of yellow spots of eyes, supports focus adjustment function , Supports contrast sensitivity (distinguishing power of color depth), maintains viewing power, helps focus adjustment function at hand, relieves the burden on the shoulders and neck muscles due to the use of eyes, etc. It is also possible to display similar to them.
本発明の一態様は、眼疾患の予防及び/又は治療のための、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物である。本発明の組成物は、眼疾患の予防及び/又は治療のために使用することができる。 One aspect of the present invention is a composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa for the prevention and / or treatment of eye diseases. The compositions of the present invention can be used for the prevention and / or treatment of eye diseases.
本発明において、眼疾患は、加齢、紫外線、血行不良、乾燥、活性酸素及び/又は炎症により誘発される疾患であり、具体的には、眼精疲労、白内障、加齢黄斑変性、糖尿病網膜症、網膜色素変性症、中心性漿液性脈絡網膜症、緑内障、ブドウ膜炎、老視、近視、ドライアイ、翼状片、炎症性眼疾患等が挙げられ、好ましくは、眼精疲労、白内障、加齢黄斑変性、糖尿病網膜症、老視、近視、ドライアイであり、特に好ましくは、老視である。 In the present invention, the eye disease is a disease induced by aging, ultraviolet rays, poor circulation, dryness, active oxygen and / or inflammation, and specifically, presbyopia, cataract, age-related luteal degeneration, diabetic retinopathy. Diseases, retinal pigment degeneration, central serous chorioretinopathy, glaucoma, diabetic retinopathy, presbyopia, myopia, dry eyes, winglets, inflammatory eye diseases, etc., preferably eye fatigue, cataracts, etc. Age-related cataracts, diabetic retinopathy, presbyopia, myopia, dry eyes, with presbyopia being particularly preferred.
本発明において、角膜障害とは、角膜上皮細胞死及びそれに起因する眼疾患(ドライアイ、炎症性眼疾患等)であれば特に制限はない。好ましくは、紫外線により誘発される角膜障害であり、紫外線により誘発される角膜上皮細胞死及びそれに起因する眼疾患である。 In the present invention, the corneal disorder is not particularly limited as long as it is corneal epithelial cell death and eye diseases caused by it (dry eye, inflammatory eye disease, etc.). Preferably, it is UV-induced corneal damage, UV-induced corneal epithelial cell death and the resulting eye disease.
本発明において、水晶体変性とは、水晶体に存在するタンパク質が変性した状態であり、その原因については特に制限はない。好ましくは、水晶体が混濁(白濁)、硬化、着色(黄色化)又は形状変化した状態であり、特に好ましくは、水晶体が混濁(白濁)又は硬化した状態である。 In the present invention, lens degeneration is a state in which a protein existing in the lens is denatured, and the cause thereof is not particularly limited. Preferably, the crystalline lens is turbid (white turbid), hardened, colored (yellowed) or changed in shape, and particularly preferably, the crystalline lens is turbid (white turbid) or hardened.
本発明において、眼調節機能とは、視機能を調節する機能であれば特に制限はない。好ましくは、ピント調節機能であり、特に好ましくは、水晶体におけるピント調節機能である。 In the present invention, the eye accommodation function is not particularly limited as long as it is a function of adjusting the visual function. It is preferably a focus adjustment function, and particularly preferably a focus adjustment function in the crystalline lens.
本発明において、網脈絡膜障害とは、網膜の損傷およびその損傷に起因する眼疾患であり、好ましくは、網膜の損傷およびその損傷に起因するブドウ膜疾患(網膜、脈絡膜、強膜等の疾患)である。 In the present invention, the retinal choroidal disorder is an eye disease caused by damage to the retina and the damage thereof, and preferably a damage to the retina and a uveal disease caused by the damage (a disease of the retina, choroid, sclera, etc.). Is.
本発明において、「キサントフィル又はその塩とヒシ属植物の加工物とを組み合わせることを特徴とする」とは、キサントフィル又はその塩とヒシ属植物の加工物を各単剤として併用してもよく、各成分の配合剤として使用してもよいことを意味する。より好ましくは、配合剤としての使用である。 In the present invention, "characterized by combining xanthophyll or a salt thereof with a processed product of a Trapa plant" may mean that xanthophyll or a salt thereof and a processed product of a Trapa plant may be used in combination as each single agent. It means that it may be used as a combination drug of each component. More preferably, it is used as a compounding agent.
本発明において、「予防」とは、各症状や疾患の発症及び/又は進行の予防を意味する。 In the present invention, "prevention" means prevention of the onset and / or progression of each symptom or disease.
本発明において「治療」とは、各症状や疾患の治療を意味する。 In the present invention, "treatment" means treatment of each symptom or disease.
本発明において「改善」とは、各症状や疾患の改善を意味する。 In the present invention, "improvement" means improvement of each symptom or disease.
本発明において、「〜を含有する」は、「実質的に〜のみを含有する」、「〜のみを含有する」、「〜を有効成分として含有する」、「実質的に〜のみを有効成分として含有する」、「〜のみを有効成分として含有する」と読み替えたものも本発明の範囲である。 In the present invention, "contains ~" means "substantially contains only ~", "contains only ~", "contains ~ as an active ingredient", and "substantially contains only ~ as an active ingredient". It is also within the scope of the present invention to read "contains as" and "contains only ... as an active ingredient".
本発明の別の一態様は、ヒシ属植物の加工物を含有する眼科用組成物、およびその用途である。尚、当該態様の各定義については、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物の各定義を準用できる。 Another aspect of the present invention is an ophthalmic composition containing a processed product of a Trapa plant, and its use. For each definition of the embodiment, each definition of the composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa can be applied mutatis mutandis.
本発明の別の一態様は、ルテイン又はその塩を含有する角膜上皮細胞死抑制剤及びルテイン又はその塩を含有する眼科用組成物の新規用途である。尚、当該態様の各定義については、キサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物の各定義を準用できる。 Another aspect of the present invention is a novel use of a corneal epithelial cell death inhibitor containing lutein or a salt thereof and an ophthalmic composition containing lutein or a salt thereof. For each definition of the embodiment, each definition of the composition containing xanthophyll or a salt thereof and a processed product of the genus Trapa can be applied mutatis mutandis.
以下に、薬理試験例を示すが、これらの例示は本発明をよりよく理解するためのものであり、本発明の範囲を限定するものではない。 Examples of pharmacological tests are shown below, but these examples are for better understanding of the present invention and do not limit the scope of the present invention.
[薬理試験1]
紫外線(UV−B)照射前に角膜上皮細胞を本発明の組成物で処置した場合に、紫外線照射による生細胞数の低下が抑制されるか否かを評価した。
[Pharmacology test 1]
When the corneal epithelial cells were treated with the composition of the present invention before irradiation with ultraviolet rays (UV-B), it was evaluated whether or not the decrease in the number of living cells due to irradiation with ultraviolet rays was suppressed.
(試験方法)
SV40不死化ヒト角膜上皮細胞(HCE−T:理化学研究所、バイオリソースセンター、Cell No.:RCB2280)を96ウェルプレートに播種(1×104個/ウェル)し、SHEM培地(15%Fetal Bovine Serum、5μg/mL Insulin、10ng/mL Human Epidermal Growth Factor、40μg/mL Gentamicin含有DMEM/F−12培地)で1日培養した。
翌日、前記SHEM培地を除去して、PBS(Phosphate Buffered Saline、リン酸緩衝生理食塩水)でSV40不死化ヒト角膜上皮細胞を洗浄した。
0.01%(w/v)ヒシエキスを含有するPBS、100μMルテインを含有するPBS、0.01%(w/v)ヒシエキス及び100μMルテインを含有するPBS、又は被験物質を含有しないPBS(コントロール)に交換した。
その後、角膜上皮細胞に120mJ/cm2UV−B(照射強度:約1mW/cm2、照射時間:約120秒)を照射した。
各群の培地をDMEM/F−12培地に交換してから、37℃で翌日まで培養した後、CellTiter96(登録商標) Aqueous One Solution Cell Proliferation Assay(Promega社製、カタログ番号:G3580)を用いて生細胞数を測定し、下記式1に従って、細胞生存率を算出した。
なお、本試験で使用したヒシエキス及びルテインは、それぞれ林兼産業株式会社及びChromaDex社から購入した。
(Test method)
SV40 immortalized human corneal epithelial cells (HCE-T: Institute of Physical and Chemical Research, Bioresource Center, Cell No .: RCB2280) were seeded in 96-well plates (1 × 10 4 cells / well), and SHEM medium (15% Fetal Bovine Serum) was used. 5 μg / mL Insulin, 10 ng / mL Human Epidermal Growth Factor, 40 μg / mL Genamicin-containing DMEM / F-12 medium) was cultured for 1 day.
The next day, the SHEM medium was removed, and SV40 immortalized human corneal epithelial cells were washed with PBS (Phosphate Buffered Saline).
PBS containing 0.01% (w / v) Hishi extract, PBS containing 100 μM lutein, PBS containing 0.01% (w / v) Hishi extract and 100 μM lutein, or PBS containing no test substance (control) Exchanged for.
Then, the corneal epithelial cells were irradiated with 120 mJ / cm 2 UV-B (irradiation intensity: about 1 mW / cm 2 , irradiation time: about 120 seconds).
After exchanging the medium of each group with DMEM / F-12 medium, culturing at 37 ° C. until the next day, using CellTiter96 (registered trademark) Aqueous One Solution Cell Proliferation Assay (manufactured by Promega, Catalog No .: G3580). The number of viable cells was measured, and the cell viability was calculated according to the following
The Hishi extract and lutein used in this test were purchased from Hayashikane Sangyo Co., Ltd. and ChromaDex Co., Ltd., respectively.
[式1]
細胞生存率(%)=(各群の生細胞数/UV−B非照射群の生細胞数)×100
[Equation 1]
Cell viability (%) = (number of viable cells in each group / number of viable cells in UV-B non-irradiated group) × 100
(結果)
試験結果を図1に示す。なお、図1中、値は平均値±標準誤差を示す(N=3)。
(result)
The test results are shown in FIG. In FIG. 1, the values indicate the average value ± standard error (N = 3).
(考察)
図1から明らかなように、UV−B照射前に角膜上皮細胞をヒシエキス単独、ルテイン単独又はヒシエキス+ルテインで処置した場合のいずれもが、コントロールに対して、細胞生存率が向上した。すなわち、ヒシ属植物の加工物を単独で、キサントフィルを単独で及びヒシ属植物の加工物とキサントフィルを組み合わせて処置した場合のいずれにおいても、紫外線照射により誘発される角膜上皮細胞死を効果的に抑制できることが示された。特に、ヒシ属植物の加工物及びキサントフィルを組み合わせて使用した場合、両者は相乗的又は補完的に作用して、紫外線照射により誘発される角膜上皮細胞死を効果的に抑制できることが示された。
(Discussion)
As is clear from FIG. 1, when the corneal epithelial cells were treated with Hishi extract alone, Lutein alone, or Hishi extract + lutein before UV-B irradiation, the cell viability was improved with respect to the control. That is, effective treatment of corneal epithelial cell death induced by UV irradiation, regardless of whether the processed product of Trapa is treated alone, xanthophyll is treated alone, or the processed product of Trapa is treated with xanthophyll in combination. It was shown that it can be suppressed. In particular, when a processed product of Trapa and xanthophyll were used in combination, it was shown that both act synergistically or complementarily to effectively suppress corneal epithelial cell death induced by ultraviolet irradiation.
[薬理試験2]
糖尿病モデルラットを本発明の組成物で処置した場合に、水晶体の白濁(混濁)、及び網膜の損傷が改善されるか否かを評価した。
[Pharmacology test 2]
It was evaluated whether or not the white turbidity (opacity) of the crystalline lens and the damage to the retina were improved when the diabetic model rat was treated with the composition of the present invention.
1.試験動物(使用動物)
Wistar系雄性ラット(7週齢、日本チャールス・リバー株式会社 日野飼育センター)を株式会社イナリサーチ試験研究センター飼育室に搬入した。6日間の馴化を含めた検疫を行った後、実験に供した。
試験期間中は、温度23±2℃,湿度55±15%,明暗サイクル12時間(明期:午前7時〜、暗期:午後7時〜)に管理された同実験室で飼育した。固形飼料(CRF−1,オリエンタル酵母工業株式会社,千葉)及び飲水はそれぞれ自由に摂取させた。
1. 1. Test animal (use animal)
A Wistar male rat (7 weeks old, Japan Charles River Co., Ltd. Hino Breeding Center) was brought into the breeding room of Ina Research Research Center Co., Ltd. After quarantine including acclimation for 6 days, it was used for the experiment.
During the test period, the animals were bred in the same laboratory controlled at a temperature of 23 ± 2 ° C., a humidity of 55 ± 15%, and a light-dark cycle of 12 hours (light period: 7:00 am-, dark period: 7:00 pm-). Solid feed (CRF-1, Oriental Yeast Co., Ltd., Chiba) and drinking water were allowed to be freely ingested.
2.糖尿病モデルラットの作製
ラットにストレプトゾトシン(STZ)を生理食塩液で45mg/mLに調製し、1回目として1mL/kgを単回尾静脈内投与し、7日後にSTZを生理食塩液で25mg/mLに調製し、2回目として1mL/kgを単回尾静脈内投与し、1型糖尿病を誘導した。対照群には生理食塩液を同量投与した(正常群)。2回目のSTZ投与後6日目の飽食時血糖値が250mg/dL以上(糖尿病群:DM)のものをその後の実験に使用した。
2. Preparation of Diabetes Model Rats Streptozotocin (STZ) was prepared in rats at 45 mg / mL with physiological saline, 1 mL / kg was administered once intravenously in the tail vein for the first time, and STZ was 25 mg / mL with physiological saline 7 days later. As a second dose, 1 mL / kg was administered intravenously to the tail vein to induce
3.実験プロトコール
上述のDMラットを2回目のSTZ投与後6日目に以下の4群に血糖値が均等になるように割り付けた。
正常群:注射用水2mL/kg/日(n=8)
コントロール群:DM+注射用水2mL/kg/日(n=8)
ヒシエキス群:DM+ヒシエキス66%含有物2mg/kg/日(n=8)
ルテイン群:DM+ルテイン20%含有物2mg/kg/日(n=8)
ヒシエキス+ルテイン群:DM+ヒシエキス66%含有物2mg/kg/日+ルテイン20%含有物2mg/kg/日(n=8)
割り付けた翌日より被験物投与を開始し、69日間経時的変化について観察した。ヒシエキスは注射用水で1mg/mLの濃度に希釈して2mL/kg/日、ルテインはサフラワー油で1mg/mLの濃度に希釈して2mL/kg/日をポリプロピレン製注射筒及びラット用経口ゾンデを用いて1日1回強制経口投与した。
水晶体の白濁(混濁)は投与開始日から70日目に採材して白濁(混濁)状態を評価した。網膜電図の測定は被験物投与開始2日前及び投与開始日から43日目の計2回測定した。
なお、本試験で用いたヒシエキス及びルテインは、それぞれ林兼産業株式会社及びKatra Phytochem [India] Private Limitedから購入した。
3. 3. Experimental Protocol The DM rats described above were assigned to the following 4 groups on the 6th day after the second STZ administration so that the blood glucose levels were even.
Normal group: Water for injection 2 mL / kg / day (n = 8)
Control group: DM + water for injection 2 mL / kg / day (n = 8)
Hishi extract group: DM + 66% Hishi extract content 2 mg / kg / day (n = 8)
Lutein group: DM +
Hishi extract + lutein group: DM + 66% lutein content 2 mg / kg / day +
The subject administration was started the day after the allocation, and the change over time was observed for 69 days. Hishi extract is diluted with water for injection to a concentration of 1 mg / mL and 2 mL / kg / day, and lutein is diluted with safflower oil to a concentration of 1 mg / mL and 2 mL / kg / day is diluted with a polypropylene injection tube and an oral sonde for rats. Was administered orally once daily.
The cloudiness (turbidity) of the crystalline lens was evaluated on the 70th day from the start date of administration to evaluate the cloudiness (turbidity) state. The electroretinogram was measured 2 days before the start of administration of the subject and 43 days after the start of administration, a total of 2 times.
The Hishi extract and lutein used in this test were purchased from Hayashikane Sangyo Co., Ltd. and Katra Phytochem [India] Private Limited, respectively.
4.水晶体の白濁(混濁)に対する効果
ヒシエキス、ルテイン及びヒシエキス+ルテインの水晶体の白濁(混濁)抑制作用の有無を、糖尿病モデルラットを用いて検討した。
Wistar系ラット(雄、8週齢)にストレプトゾトシンを1回目(45mg/kg,i.v.)、7日後に2回目(25mg/kg,i.v.)を投与して1型糖尿病を誘発させた。ヒシエキス群はヒシエキス66%含有物(2mg/kg)、ルテイン群はルテイン20%含有物(2mg/kg)、ヒシエキス+ルテイン群はヒシエキス66%含有物(2mg/kg)とルテイン20%含有物(2mg/kg)を1日1回経口投与した。
水晶体は69日間の投与期間終了後、70日目に水晶体を採材して完全白濁(混濁)した水晶体の数の割合(完全白濁の発生率)評価した。
なお、本試験で使用したヒシエキス及びルテインは、それぞれ林兼産業株式会社及びKatra Phytochem [India] Private Limitedから購入した。
4. Effect on lens white turbidity (turbidity) The presence or absence of the lens cloudiness (turbidity) inhibitory effect of Hishi extract, lutein and Hishi extract + lutein was examined using diabetic model rats.
Streptozotocin (45 mg / kg, iv) was administered to Wistar rats (male, 8 weeks old) for the first time (45 mg / kg, iv), and 7 days later, the second dose (25 mg / kg, iv) was administered to induce
The crystalline lens was collected on the 70th day after the end of the administration period of 69 days, and the ratio of the number of completely cloudy (opaque) crystalline lenses (incidence rate of complete cloudiness) was evaluated.
The Hishi extract and lutein used in this test were purchased from Hayashikane Sangyo Co., Ltd. and Katra Phytochem [India] Private Limited, respectively.
[式2]
完全白濁率(%)=(各群で完全白濁した眼数/各群の全眼数)×100
[Equation 2]
Complete cloudiness rate (%) = (number of eyes completely clouded in each group / total number of eyes in each group) x 100
(結果)
試験結果を図2に示す。
(result)
The test results are shown in FIG.
(考察)
図2から明らかなように、ヒシエキス単独、ルテイン単独、ヒシエキス+ルテインを投与した場合のいずれもが、コントロールと比較して、水晶体の白濁(混濁)を抑制した。すなわち、ヒシ属植物の加工物を単独で、キサントフィルを単独で及びヒシ属植物の加工物とキサントフィルを組み合わせて使用した場合のいずれにおいても、水晶体の白濁(混濁)を抑制することが示された。
(Discussion)
As is clear from FIG. 2, all of the administration of Hishi extract alone, lutein alone, and Hishi extract + lutein suppressed the cloudiness (opacity) of the crystalline lens as compared with the control. That is, it was shown that the white turbidity (turbidity) of the crystalline lens was suppressed in both the case where the processed product of the genus Trapa was used alone, the xanthophyll was used alone, and the processed product of the genus Trapa and the xanthophyll were used in combination. ..
5.網膜の損傷に対する効果
ヒシエキス、ルテイン及びヒシエキス+ルテインの網膜の損傷の抑制作用の有無を、糖尿病モデルラットを用いて検討した。
Wistar系ラット(雄、8週齢)にストレプトゾトシンを1回目(45mg/kg,i.v.)、7日後に2回目(25mg/kg,i.v.)を投与して1型糖尿病を誘発させた。ヒシエキス群はヒシエキス66%含有物(2mg/kg)、ルテイン群はルテイン20%含有物(2mg/kg)、ヒシエキス+ルテイン群はヒシエキス66%含有物(2mg/kg)とルテイン20%含有物(2mg/kg)を1日1回経口投与した。
データ収集・解析システムPowerLab(PowerLabシステム)を用いて、被験物投与開始2日前及び投与開始日から43日目の網膜電図(a波およびb波)を測定し、評価した。
なお、本試験で使用したヒシエキス及びルテインは、それぞれ林兼産業株式会社及びKatra Phytochem [India] Private Limitedから購入した。
ここで、網膜電図とは、網膜に光を照射した時に記録される電位変化であり、網膜機能を電気生理学的に評価する場合に使用する。
この網膜電図の基本形は、光照射による最初に生じる負の電位変動(a波)、次に、鋭く立ち上がった後に急降下する大きな正の電位変動(b波)に、分類され、a波振幅は視細胞由来の過分極相を、b波振幅はミュラー細胞由来の脱分極層を示し網膜機能の状態を把握するのに用いられる。すなわち、種々の疾患等により、網膜に何らかの障害が出れば、網膜電図上の各波の振幅が低下する。
5. Effect on retinal damage The presence or absence of the inhibitory effect of Hishi extract, lutein and Hishi extract + lutein on retinal damage was examined using diabetic model rats.
Streptozotocin (45 mg / kg, iv) was administered to Wistar rats (male, 8 weeks old) for the first time (45 mg / kg, iv), and 7 days later, the second dose (25 mg / kg, iv) was administered to induce
Using the data collection / analysis system PowerLab (PowerLab system), electroretinograms (waves a and b) were measured and evaluated 2 days before the start of administration of the subject and 43 days after the start of administration.
The Hishi extract and lutein used in this test were purchased from Hayashikane Sangyo Co., Ltd. and Katra Phytochem [India] Private Limited, respectively.
Here, the electroretinogram is a potential change recorded when the retina is irradiated with light, and is used when evaluating retinal function electrophysiologically.
The basic form of this electroretinogram is classified into the first negative potential fluctuation (a wave) caused by light irradiation, and then the large positive potential fluctuation (b wave) that rises sharply and then drops sharply. The hyperpolarized phase derived from photoreceptor cells and the b-wave amplitude indicate the depolarized layer derived from Muller cells and are used to grasp the state of retinal function. That is, if any damage occurs to the retina due to various diseases or the like, the amplitude of each wave on the electroretinogram decreases.
[式3]
振幅の変化率(%)=(各群の43日目の電位変動幅/投与開始2日前の電位変動幅)×100
[Equation 3]
Amplitude change rate (%) = (potential fluctuation range on the 43rd day of each group / potential fluctuation range 2 days before the start of administration) × 100
(結果)
試験結果を図3に示す。
(result)
The test results are shown in FIG.
(考察)
図3から明らかなように、ヒシエキス単独、ルテイン単独及びヒシエキス+ルテインを投与した場合のいずれもが、コントロールと比較して、a波およびb波の振幅の低下を抑制または改善した。すなわち、ヒシ属植物の加工物を単独で、キサントフィルを単独で及びヒシ属植物の加工物とキサントフィルを組み合わせて使用した場合のいずれにおいても、網膜の損傷を抑制または改善する可能性が示された。
[製剤例]
以下に、製剤例を示すが、これらの例示は本発明をよりよく理解するためのものであり、本発明の範囲を限定するものではなく、また、本発明はこれらの製剤例にのみ限定されるものではない。
(Discussion)
As is clear from FIG. 3, when Hishi extract alone, lutein alone, and Hishi extract + lutein were administered, the decrease in the amplitude of the a wave and the b wave was suppressed or improved as compared with the control. That is, it was shown that there is a possibility of suppressing or ameliorating retinal damage when the processed product of Trapa is used alone, xanthophyll is used alone, or the processed product of Trapa and xanthophyll are used in combination. ..
[Formulation example]
Examples of the preparations are shown below, but these examples are for better understanding of the present invention and do not limit the scope of the present invention, and the present invention is limited only to these examples of preparations. It's not something.
製剤例中の各成分の配合量はソフトカプセルとした場合の1カプセル当たりの含有量である。 The blending amount of each component in the pharmaceutical product example is the content per capsule in the case of soft capsules.
製剤例1
ヒシエキス 33mg
グリセリン脂肪酸エステル 適量
Pharmaceutical example 1
Hishi extract 33mg
Glycerin fatty acid ester suitable amount
製剤例2
ルテイン 7.5mg
ヒシエキス 33mg
グリセリン脂肪酸エステル 適量
Pharmaceutical example 2
Lutein 7.5mg
Hishi extract 33mg
Glycerin fatty acid ester suitable amount
製剤例3
ルテイン 7.5mg
ヒシエキス 33mg
ビタミンE 75mg
グリセリン脂肪酸エステル 適量
Pharmaceutical example 3
Lutein 7.5mg
Hishi extract 33mg
Glycerin fatty acid ester suitable amount
製剤例4
ルテイン 7.5mg
ヒシエキス 33mg
ドコサヘキサエン酸 100mg
グリセリン脂肪酸エステル 適量
Pharmaceutical example 4
Lutein 7.5mg
Hishi extract 33mg
Docosahexaenoic acid 100 mg
Glycerin fatty acid ester suitable amount
製剤例5
ヒシエキス 33mg
ドコサヘキサエン酸 100mg
グリセリン脂肪酸エステル 適量
Pharmaceutical example 5
Hishi extract 33mg
Docosahexaenoic acid 100 mg
Glycerin fatty acid ester suitable amount
製剤例6
ルテイン 7.5mg
ドコサヘキサエン酸 100mg
グリセリン脂肪酸エステル 適量
Pharmaceutical example 6
Lutein 7.5mg
Docosahexaenoic acid 100 mg
Glycerin fatty acid ester suitable amount
製剤例1〜6において、ルテイン、ヒシエキス、他の配合成分の種類や配合量を適宜調整することで所望の製剤を処方することができる。 In Formulation Examples 1 to 6, a desired formulation can be formulated by appropriately adjusting the type and amount of lutein, hissi extract, and other compounding components.
本発明のキサントフィル又はその塩及びヒシ属植物の加工物を含有する組成物は、視機能低下の予防及び/又は改善のために使用できる。 The composition containing xanthophyll of the present invention or a salt thereof and a processed product of the genus Trapa can be used for prevention and / or improvement of deterioration of visual function.
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