JP2009102419A - Blood cholesterol-reducing agent - Google Patents

Blood cholesterol-reducing agent Download PDF

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JP2009102419A
JP2009102419A JP2009023958A JP2009023958A JP2009102419A JP 2009102419 A JP2009102419 A JP 2009102419A JP 2009023958 A JP2009023958 A JP 2009023958A JP 2009023958 A JP2009023958 A JP 2009023958A JP 2009102419 A JP2009102419 A JP 2009102419A
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extract
water
reducing agent
blood cholesterol
mass
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Akihiro Yamashita
明宏 山下
Takashi Takashita
崇 高下
Takeo Ishihara
健夫 石原
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BHN Co Ltd
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BHN Co Ltd
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Abstract

<P>PROBLEM TO BE SOLVED: To provide a blood cholesterol-reducing agent capable of suppressing increase of blood lipid concentration by ingestion of dietary fat and reducing the level of blood fat amount and using a material derived from a natural product, and a composition capable of industrially effectively utilizing the agent. <P>SOLUTION: The blood cholesterol-reducing agent comprises an extract of root and/or rhizome of Astilbe thunbergii which is a plant belonging to the genus Astilbe, more preferably, a water-containing ethanol extract (having 10-50 mass% water-containing ratio) of the root and/or the rhizome or an ethyl acetate-soluble fraction of water-containing acetone extract (having 10-30 mass% water-containing ratio) of the root and/or the rhizome, and an extract of root and/or rhizome of Platycodon grandiflorum, more preferably, a hot water extract of the root and/or the rhizome of Platycodon grandiflorum or ethanol or water-containing ethanol (having 5 mass% water-containing ratio)-soluble fraction of the hot water extract. A food composition or a pharmaceutical composition is obtained by formulating the blood cholesterol-reducing agent therein. <P>COPYRIGHT: (C)2009,JPO&INPIT

Description

本発明は、チダケサシ属に属する植物であるアカショウマの抽出物とキキョウの抽出物とを有効成分としてなる血中コレステロール低減剤及びこれを配合してなる食用組成物又は医薬用組成物に関する。   The present invention relates to a blood cholesterol-reducing agent comprising as an active ingredient an extract of red pepper that is a plant belonging to the genus Pleurotus and an extract of Kyoji, and an edible composition or a pharmaceutical composition comprising the same.

近年、欧米型の食事形態や過食による摂取エネルギーの増加と運動不足による消費エネルギーの減少との格差が増大し、体脂肪の過剰蓄積をともなう肥満体形が増えており、高脂血症等の循環器系疾患をはじめとする各種生活習慣病の増加原因となっている。一般的に、高脂血症は血清中の脂質すなわちコレステロール、トリグリセリド、リン脂質、遊離脂肪酸等のうち1種以上の脂質成分が異常に増加してさまざまな障害をまねく疾病であり、その主なものとして高コレステロール血症と高トリグリセリド血症がある。高脂血症状態が慢性化すると動脈硬化症、脂肪肝、脳卒中、狭心症等を惹起し、また、糖尿病、腎臓障害等の疾患を合併症として起こしやすくなるといわれている。   In recent years, there has been an increase in the disparity between Western-style dietary forms and increased energy intake due to overeating and reduced energy consumption due to lack of exercise, increasing obesity with excessive body fat accumulation, and circulation such as hyperlipidemia It is an increasing cause of various lifestyle-related diseases including systemic diseases. In general, hyperlipidemia is a disease in which one or more lipid components among lipids in serum, ie, cholesterol, triglycerides, phospholipids, free fatty acids, etc. increase abnormally and cause various disorders. There are hypercholesterolemia and hypertriglyceridemia. It is said that when the hyperlipidemia state becomes chronic, arteriosclerosis, fatty liver, stroke, angina pectoris, etc. are caused, and diseases such as diabetes and kidney disorders are likely to occur as complications.

高脂血症を防止するために、医療分野における治療や予防はもとより、食品に含まれる成分を利用して血中脂質の異常な増加を抑制する試みがこれまでに数多くなされてきた。すなわち、血中コレステロールの濃度を低下させる薬剤としてブラバスタチンをはじめとする種々の化学合成物質が治療に利用されており、高トリグリセリド血症に対してはデキストラン硫酸ナトリウム、ニコチン酸トコフェロール、パンテチン、ステリン誘導体等の薬剤が治療に用いられている。また、血中コレステロールやトリグリセリドの濃度を低減させる作用のある食品成分としては、米やトウモロコシ等の胚芽に多く含まれるγ−オリザノール(非特許文献1)、大豆、トウモロコシ、ゴマ等のフィトステロール(非特許文献2)、大豆油やコーン油等の植物油脂に含まれるトリテルペンアルコール(非特許文献3)等が知られている。   In order to prevent hyperlipidemia, many attempts have been made to suppress abnormal increases in blood lipids using ingredients contained in foods as well as treatment and prevention in the medical field. In other words, various chemical synthetic substances such as bravastatin are used in the treatment as drugs to lower the blood cholesterol level. For hypertriglyceridemia, sodium dextran sulfate, tocopherol nicotinate, pantethine, and sterin Drugs such as derivatives are used for treatment. In addition, food ingredients having an action of reducing blood cholesterol and triglyceride concentrations include γ-oryzanol (Non-patent Document 1), which is contained in a large amount of germs such as rice and corn, phytosterols such as soybean, corn and sesame (non- Patent Document 2), triterpene alcohol (Non-Patent Document 3) and the like contained in vegetable oils such as soybean oil and corn oil are known.

なお、本発明に係るアカショウマ等のチゲタサシ属に属する植物の根と根茎には、デンプンやタンニンのほかにベルゲニン、アスチルビン、アスチルビン酸等のフラボノイド類が含まれていることが知られており、これらの成分が前述の薬理作用を示すといわれている(非特許文献4)。   In addition, it is known that the roots and rhizomes of plants belonging to the genus Tigetasas such as red pepper according to the present invention contain flavonoids such as bergenin, astilbine, astilbic acid in addition to starch and tannin, these Is said to exhibit the above-mentioned pharmacological action (Non-Patent Document 4).

また、キキョウ(Platycodon grandiflorum A.DECANDOLLE)はわが国を含む東アジアに自生する多年生草であり、キキョウ科に属する。その根や根茎はプラティコディン(platycodin)A、C、Dやポリガラシン(polygalacin)D等のサポニン類を含み、古来より鎮咳、去痰、消炎、排膿等の効能を有する生薬・漢方薬として用いられている。また、キキョウのエキスを利用する例として、プロテアーゼ阻害剤として歯周病の予防や治療のための組成物(特許文献1)、温浴効果を期待する入浴剤(特許文献2)、養毛・育毛料(特許文献3)、アトピー性皮膚炎の予防・治療剤(特許文献4)、抗チロシナーゼ活性をもつ化粧料(特許文献5)等が提案されている。   Oyster (Platycodon grandiflorum A. DECANDOLLE) is a perennial grass that grows naturally in East Asia including Japan and belongs to the family Oleaceae. Its roots and rhizomes contain saponins such as platycodin A, C, D and polygalacin D, and have been used as herbal medicines and herbal medicines with antitussive, expectorant, antiphlogistic, drainage, etc. since ancient times. ing. In addition, as an example of using an extract of Kyoukyo, a composition for preventing or treating periodontal disease as a protease inhibitor (Patent Document 1), a bathing agent expected to have a warm bath effect (Patent Document 2), hair nourishing / hair growth (Patent Document 3), preventive and therapeutic agents for atopic dermatitis (Patent Document 4), cosmetics having anti-tyrosinase activity (Patent Document 5) and the like have been proposed.

特開平6−25000号公報JP-A-6-25000 特開平6−206814号公報JP-A-6-206814 特開平8−73324号公報JP-A-8-73324 特開平11−199500号公報JP 11-199500 A 特開2000−198712号公報JP 2000-198712 A

「基礎と臨床」、第17巻、No.4、第123頁−第140頁、1983年“Basics and Clinical”, Vol. 4, pp. 123-140, 1983 The Lipid、第5巻、No.1、第101頁−第105頁、1994年The Lipid, Vol. 1, pp. 101-105, 1994 「動脈硬化」、第13巻、No.2、第273頁−第278頁、1985年“Arteriosclerosis”, Vol. 2, pp. 273-278, 1985 Shimada,Hら、Yakugaku Zasshi、第72巻、第578頁−第588頁、1952年Shimada, H et al., Yakugaku Zashi, 72, 578-588, 1952

しかしながら、前記薬剤は優れた効果を有するものの副作用があり、医師の指導のもとに用法用量を守らなければならない制限があった。また、食品から分離した前記成分は実際的には効果が低かったり、実用的ではない摂取条件下での実験結果に基づくものであったり、あるいは通常の食事形態において多量に摂取しなければならず、いずれも十分に満足できる効果を発揮し得るものではなかった。かかる現状に鑑み、本発明では、血中脂質濃度の異常な増加を防止したり、高脂血症の予防や治療に有効利用し得る天然物由来の血中コレステロール低減剤を開発、提供し、これを産業上有用に活用できる態様の組成物として提供することを課題とした。なお、本明細書では、血中のコレステロールやトリグリセリド等の前記血中脂質のうち少なくとも1成分の濃度を低減させることを血中脂質改善ということがある。   However, although the drug has an excellent effect, it has side effects, and there is a restriction that the dosage must be observed under the guidance of a doctor. In addition, the ingredients separated from the food are practically ineffective, are based on experimental results under impractical intake conditions, or must be consumed in large amounts in normal dietary forms. Neither of them was able to exert a sufficiently satisfactory effect. In view of the present situation, the present invention develops and provides a natural product-derived blood cholesterol reducing agent that can prevent abnormal increase in blood lipid concentration or can be effectively used for the prevention and treatment of hyperlipidemia, It was made into the subject to provide as a composition of the aspect which can utilize this industrially usefully. In the present specification, reducing the concentration of at least one of the blood lipids such as cholesterol and triglycerides in blood is sometimes referred to as blood lipid improvement.

本発明者らは、前記課題を解決するために、多数の植物原料及びそのエキス類と脂質代謝との関連性について鋭意検討を行った結果、アカショウマをはじめとするチダケサシ属に属する植物とキキョウが本発明の所望の効果を顕著に奏することを見出し、本発明を完成するに至った。   In order to solve the above problems, the present inventors have conducted extensive studies on the relationship between a large number of plant raw materials and their extracts and lipid metabolism. The inventors have found that the desired effects of the present invention are remarkably exhibited, and have completed the present invention.

すなわち、本発明によれば、チダケサシ属に属する植物であるアカショウマの抽出物及びキキョウの抽出物を含有してなることを特徴とする血中コレステロール低減剤が提供される。また、これを配合してなる食用組成物又は医薬用組成物が提供される。   That is, according to the present invention, there is provided a blood cholesterol reducing agent characterized by comprising an extract of red pepper that is a plant belonging to the genus Pleurotus and an extract of Kyoma. Moreover, the edible composition or pharmaceutical composition which mix | blends this is provided.

ここで、チダケサシ属に属する植物はユキノシタ科のチダケサシ(Astilbe)属の植物であり、本発明では、アカショウマを用い、その根及び/又は根茎の抽出物(以下、エキスということがある)又は精製物を使用することを特徴とする。アカショウマの抽出物は、含水率が10〜50質量%の含水エタノールを用いて抽出したものであることが望ましく、さらには含水率が10〜30質量%の含水アセトンを用いた抽出物の酢酸エチル可溶画分であることがより望ましい。   Here, the plant belonging to the genus Pleurotus is a plant belonging to the genus Astilbe belonging to the family of the family Uchinosida, and in the present invention, a red pepper is used and its root and / or rhizome extract (hereinafter sometimes referred to as extract) or purified. It is characterized by using a thing. It is desirable that the red pepper extract is extracted with water-containing ethanol having a water content of 10 to 50% by mass, and further, ethyl acetate of the extract using water-containing acetone having a water content of 10 to 30% by mass. More preferably, it is a soluble fraction.

また、キキョウはキキョウ科に属し、その根及び/又は根茎の抽出物又は精製物を使用することを特徴とする。キキョウの抽出物は、熱水抽出物であることが望ましく、さらには該熱水抽出物をエタノール若しくは含水率が5質量%の含水エタノールで抽出した可溶画分であることがより望ましい。   In addition, Kyokyo belongs to the family Kleopteraceae and is characterized by using an extract or purified product of its roots and / or rhizomes. The extract of Kyoko is preferably a hot water extract, and more preferably a soluble fraction obtained by extracting the hot water extract with ethanol or water-containing ethanol having a water content of 5% by mass.

本発明の食用組成物と医薬用組成物は前記血中コレステロール低減剤を配合してなることを特徴とするものである。   The edible composition and the pharmaceutical composition of the present invention are characterized by comprising the blood cholesterol reducing agent.

本発明によれば、アカショウマの抽出物とキキョウの抽出物とを含有してなる血中コレステロール低減剤が提供される。この血中コレステロール低減剤を経口摂取することにより、とりわけ脂肪含有量の多い高脂肪食を長期間摂取する場合に、アカショウマ抽出物を単独で摂取するときの血中コレステロール濃度の低減効果をキキョウ抽出物が補助的に増強促進させ得る効果を奏する。また、アカショウマの生理活性成分として知られているベルゲニンやアスチルビンそのものと比較しても優れた血中コレステロール低減効果を発現する。本発明の血中コレステロール低減剤は、また、血中トリグリセリド濃度の低減効果を併せもつものである。本発明では、さらに、前記血中コレステロール低減剤を配合してなる食用組成物又は医薬用組成物が提供され、これは血中コレステロール含量の低減のみならず高脂血症やこれから惹起される前記各種疾病の予防及び治療、減体重や肥満防止、ダイエット等の為に有効利用され得る。   ADVANTAGE OF THE INVENTION According to this invention, the blood cholesterol reducing agent containing the extract of a red pepper and an extract of Kyoko is provided. By taking this blood cholesterol reducing agent orally, especially when taking a high-fat diet with a high fat content for a long period of time, the effect of reducing blood cholesterol concentration when taking Akashoma extract alone is extracted with Kyōki. There is an effect that the object can be supplementarily promoted. In addition, it exhibits an excellent blood cholesterol reducing effect even compared to bergenin or astilbine itself, which is known as a physiologically active component of red pepper. The blood cholesterol reducing agent of the present invention also has an effect of reducing blood triglyceride concentration. In the present invention, there is further provided an edible composition or a pharmaceutical composition comprising the blood cholesterol-reducing agent, which is not only reduced in the blood cholesterol content but also caused by hyperlipidemia and the above. It can be effectively used for prevention and treatment of various diseases, weight loss and obesity prevention, dieting and the like.

以下に本発明を詳細に説明する。まず、本発明の血中コレステロール低減剤は、チダケサシ属に属する植物であるアカショウマの抽出物とキキョウの抽出物とを含有してなることを特徴とするものである。チダケサシ(Astilbe)属に属する植物はユキノシタ科に分類され、この例は後述するように種々あるが、代表例としてアカショウマ(学名:Astilbe thunbergii(SIEB.et ZUCC.)MIQ.等)を挙げることができる。アカショウマは日本の山地にも自生する多年草で、その根茎を赤升麻とよび、古来より下熱や解毒等の目的で升麻(キンポウゲ科のサラシナショウマ:Cimicifuga simplex WORMSKJORD等)の代用品として利用されてきた。本発明では赤升麻あるいは紅升麻と称せられるものも包含する。   The present invention is described in detail below. First, the blood cholesterol-reducing agent of the present invention is characterized by containing an extract of red ginger which is a plant belonging to the genus Pleurotus and an extract of Kyoka. Plants belonging to the genus Astilbe are classified into the family Uchinosidae, and there are various examples, as will be described later. As a representative example, Akashima (scientific name: Astilbe thunbergii (SIEB. Et ZUCC.) MIQ. Etc.) can be mentioned. it can. A red ginger is a perennial that grows naturally in the mountains of Japan, and its rhizome is called red hemp, and has been used as a substitute for urtices (such as Cimifuga simplex WORMSKJORD) for the purpose of lower fever and detoxification since ancient times. It has been. In the present invention, what is referred to as red hemp or red hemp is also included.

チゲタサシ属に属する植物の例としてAstilbe chinensis、A.austrosinensis、A.thunbergii、A.thunbergii(SIEB.et ZUCC.)Miq.:アカショウマ、A.thunbergii(SIEB.et ZUCC.)MIQ.var.congesta BOISS.(=A.odontophylla MIQ.):トリアシショウマ、A.polyandra、A.grandis、A.rivularis、A.japonica(MORR.et DECNE.)A.GRAY:アワモリショウマ、A.microphylla KNOLL:チダケサシ、A.myriantha等を挙げることができる。本発明においてはアカショウマを用いる。   As an example of a plant belonging to the genus Tigetasashi, Astilbe chinensis, A. austrosinensis, A.M. thunbergii, A.M. thunbergii (SIEB. et ZUCC.) Miq. : Akashouma, A. thunbergii (SIEB. et ZUCC.) MIQ. var. congesta BOISS. (= A. Odontophylla MIQ.): Triashoma, A. polyandra, A.M. grandis, A.M. rivularis, A.M. japonica (MORR.et DECNE.) A. GRAY: Awamorisho, A. microphylla KNOLL: S. pylori, A. myriantha and the like. In the present invention, red pepper is used.

アカショウマの態様は、その根及び/又は根茎を適宜に乾燥、細断あるいは粉砕等の加工処理を施したものを用いる。アカショウマの抽出物は、前記の根及び/又は根茎を溶媒で抽出処理した抽出液、該抽出液から溶媒を除いた抽出物、該抽出物にシリカゲル、ケイ酸マグネシウム、イオン交換樹脂、活性アルミナ、セルロース、活性炭等の吸着剤を用いたカラムクロマトグラフィーや溶剤分別等の精製処理を施した精製物のいずれでもよい。食品用途に使用する場合は、アカショウマの根及び/又は根茎を乾燥し適宜に粉砕した粉末や該乾燥物の細断片を水や親水性有機溶媒で抽出した抽出物とするのが利便性や製造コストの点から望ましい。また、医薬品用途に利用する場合は、前記の抽出液、抽出物あるいは高純度の精製物が望ましい。   As the aspect of red pepper, the root and / or rhizome is appropriately subjected to processing such as drying, chopping or grinding. The extract of red pepper is an extract obtained by extracting the root and / or rhizome with a solvent, an extract obtained by removing the solvent from the extract, silica gel, magnesium silicate, ion exchange resin, activated alumina in the extract, Any of purified products subjected to purification treatment such as column chromatography using an adsorbent such as cellulose and activated carbon and solvent fractionation may be used. For use in food applications, it is convenient and easy to produce powder obtained by drying and appropriately milling roots and / or rhizomes of red pepper and extracting the fine fragments of the dried product with water or a hydrophilic organic solvent. Desirable in terms of cost. Moreover, when using for a pharmaceutical use, the said extract, an extract, or a highly purified product is desirable.

親水性有機溶媒としてメタノール、エタノール、プロパノール、イソプロパノール等の低級一価アルコール類、プロピレングリコール、1,3−ブタンジオール、グリセリン等の多価アルコール類、アセトン、メチルエチルケトン、エーテル、石油エーテル、酢酸エチル及びこれらの含水物や混合物を例示することができる。本発明の所望の効果を奏するための抽出物を効率的に得るには、エタノール、アセトン、酢酸エチル及びこれらの含水物を抽出用溶媒とすることが好ましい。含水物の水分含量は、例えば、エタノールの場合では1〜99質量%、より好ましくは10〜50質量%であり、アセトンの場合には1〜50質量%、より好ましくは10〜30質量%であり、酢酸エチルの場合は80〜99質量%、より好ましくは85〜95質量%である。これらの範囲を外れると本発明の所望の効果が減少し又は抽出物の収量が低下する。   As hydrophilic organic solvents, lower monohydric alcohols such as methanol, ethanol, propanol and isopropanol, polyhydric alcohols such as propylene glycol, 1,3-butanediol and glycerin, acetone, methyl ethyl ketone, ether, petroleum ether, ethyl acetate and These hydrates and mixtures can be exemplified. In order to efficiently obtain an extract for producing the desired effect of the present invention, it is preferable to use ethanol, acetone, ethyl acetate and a hydrated product thereof as an extraction solvent. The water content of the hydrated product is, for example, 1 to 99% by mass in the case of ethanol, more preferably 10 to 50% by mass, and 1 to 50% by mass in the case of acetone, more preferably 10 to 30% by mass. Yes, in the case of ethyl acetate, it is 80-99 mass%, More preferably, it is 85-95 mass%. Outside these ranges, the desired effect of the present invention is reduced or the yield of the extract is reduced.

本発明に係る抽出物を簡便かつ効率的に得るには、前記の含水エタノール又は含水アセトンで抽出し、該抽出物をさらに酢酸エチルで分別してその可溶画分を採取するのがよい。抽出処理は該処理原料に対して1〜100質量倍程度の前記抽出用溶媒を加え、常圧もしくは加圧下、常温又は加熱状態で、適宜に攪拌して10分〜数日間抽出処理する。不溶物を濾過又は遠心分離して除き本発明に係る抽出液を得ることができ、さらに該抽出液から減圧蒸留、噴霧乾燥、凍結乾燥等の公知の手段で溶媒を除去することによって本発明に係る抽出物を得ることができる。   In order to easily and efficiently obtain the extract according to the present invention, it is preferable to extract with the above-mentioned water-containing ethanol or water-containing acetone, and further extract the extract with ethyl acetate to collect the soluble fraction. In the extraction treatment, the extraction solvent is added in an amount of about 1 to 100 mass times with respect to the treatment raw material, and the mixture is subjected to extraction treatment at normal temperature or under pressure at room temperature or in a heated state for 10 minutes to several days. The insoluble matter can be removed by filtration or centrifugation to obtain the extract according to the present invention, and the solvent can be removed from the extract by known means such as vacuum distillation, spray drying, freeze drying, etc. Such an extract can be obtained.

一方、キキョウの形態は、その根及び/又は根茎に適宜に乾燥、細断あるいは粉砕等の加工処理を施したものを用い、キキョウの抽出物は、これらに溶媒を加えて抽出処理して抽出液とし、該抽出液から溶媒を除いて抽出物となし、さらには該抽出物にシリカゲル、ケイ酸マグネシウム、イオン交換樹脂、活性アルミナ、セルロース、活性炭等の吸着剤を充填したカラムクロマトグラフィーや溶剤分別等の精製処理を施した精製物となすことができ、これらのいずれでもよい。食品用途に利用する場合は、キキョウの根及び/又は根茎を乾燥し適宜に粉砕した粉末や該乾燥物の細断物を水や親水性有機溶媒を用いて抽出した抽出物となすのが簡便かつ利便であり、医薬品用途に使用する場合は、前記の抽出液、抽出物あるいは精製物が望ましい。   On the other hand, as for the form of Kyoukyo, the roots and / or rhizomes are appropriately dried, shredded, or crushed, and the Kyoko extract is extracted by adding a solvent to these extracts. Column chromatography or solvent in which the solvent is removed from the extract to obtain an extract, and the extract is further filled with an adsorbent such as silica gel, magnesium silicate, ion exchange resin, activated alumina, cellulose, activated carbon, etc. It can be set as the refined | purified material which gave refinement | purification processes, such as fractionation, and any of these may be sufficient. When used for food applications, it is easy to dry powdered roots and / or rhizomes and appropriately pulverize the powder or shreds of the dried product with water or a hydrophilic organic solvent. In addition, the extract, extract or purified product described above is desirable for use in pharmaceutical applications.

この抽出処理に用いる親水性有機溶媒としてメタノール、エタノール、プロパノール、イソプロパノール等の低級一価アルコール類、プロピレングリコール、1,3−ブタンジオール、グリセリン等の多価アルコール類、アセトン、メチルエチルケトン、エーテル、石油エーテル、酢酸エチル及びこれらの混合物を例示できる。本発明の所望の効果を奏する抽出物を効率的に得るための抽出溶媒としては水、エタノール、アセトン又はこれらの含水溶媒を用いるのが好ましく、さらには水又は水分含有率が50質量%以上の含水エタノールがより好ましい。50質量%未満では抽出物の収量や所望の活性が低下する。抽出物の好適な態様の例は水で抽出した抽出物をさらにエタノールで分別して得られる可溶画分である。   As the hydrophilic organic solvent used in this extraction treatment, lower monohydric alcohols such as methanol, ethanol, propanol and isopropanol, polyhydric alcohols such as propylene glycol, 1,3-butanediol and glycerin, acetone, methyl ethyl ketone, ether, petroleum Examples include ether, ethyl acetate, and mixtures thereof. As an extraction solvent for efficiently obtaining an extract exhibiting the desired effect of the present invention, it is preferable to use water, ethanol, acetone or a water-containing solvent thereof, and further, water or water content is 50% by mass or more. Hydrous ethanol is more preferred. If it is less than 50% by mass, the yield and desired activity of the extract are lowered. An example of a suitable embodiment of the extract is a soluble fraction obtained by further fractionating an extract extracted with water with ethanol.

抽出処理は次のように行えばよい。すなわち、前記形態の原料に対して等質量ないしは約100質量倍の前記抽出用溶媒を加え、常圧もしくは加圧の下、常温又は加熱状態で、必要に応じて攪拌しながら10分〜数日間抽出処理し、不溶物を遠心分離又は濾過して除去すれば本発明に係る抽出液を得ることができ、さらに該抽出液から減圧蒸留、凍結乾燥、噴霧乾燥等の手段で溶媒を除去することにより本発明に係る抽出物を得ることができる。   The extraction process may be performed as follows. That is, the extraction solvent is added in an equal mass or about 100 mass times with respect to the raw material in the above form, and at normal temperature or under pressure, at room temperature or in a heated state for 10 minutes to several days with stirring as necessary. When the extraction treatment is performed and the insoluble matter is removed by centrifugation or filtration, the extract according to the present invention can be obtained, and the solvent is further removed from the extract by means such as vacuum distillation, freeze drying, spray drying and the like. Thus, the extract according to the present invention can be obtained.

本発明の血中コレステロール低減剤の望ましい態様は、前述のようにして得られるチダケサシ属に属する植物であるアカショウマの根及び/又は根茎の抽出物あるいは精製物と、キキョウの根及び/又は根茎の抽出物あるいは精製物とを必須原料として含有せしめてなるものである。より望ましい態様はアカショウマ由来のものを必須の主要原料とし、これにキキョウ由来のものを併用して含むものであり、最も望ましくは主たる原料としてアカショウマの根茎の抽出物又は精製物を用い、これにキキョウの根茎の抽出物又は精製物を含有せしめてなるものである。これら二種類の植物由来の原料を併用すると、本発明の目的である血中コレステロール濃度の改善効果が相乗的に発現する。この血中コレステロール低減剤における両原料の配合比率は、所望の効果を奏するための使用目的と用途、製造コスト等により適宜に変動させることができ、アカショウマ由来原料/キキョウ由来原料(質量比)は、より好ましくは両原料が等量になるまでの比率であり、最も好ましくは90/10〜60/40である。   Desirable embodiments of the blood cholesterol-reducing agent of the present invention include an extract or purified product of the root and / or rhizome of red ginger which is a plant belonging to the genus Pleurotus obtained as described above, and the root and / or rhizome of kikyo. An extract or purified product is contained as an essential raw material. A more desirable embodiment is that the one derived from red pepper is used as an essential main raw material, and the one derived from Kyoka is used in combination with this, and most preferably, an extract or purified product of red pepper is used as the main raw material. It contains an extract or a purified product of rhizomes. When these two kinds of plant-derived materials are used in combination, the effect of improving the blood cholesterol concentration, which is the object of the present invention, is synergistically expressed. The mixing ratio of both raw materials in this blood cholesterol reducing agent can be appropriately varied depending on the purpose and application for producing the desired effect, production cost, etc. More preferably, it is a ratio until both raw materials become equal amounts, and most preferably 90/10 to 60/40.

本発明の血中コレステロール低減剤では、本発明の趣旨に反しないかぎり種々の原料や成分を併用して配合することができる。例えば、通常の食品や医薬品に使用される賦形剤、防湿剤、防腐剤、強化剤、増粘剤、乳化剤、酸化防止剤、甘味料、酸味料、調味料、着色料、香料等がある。また、血中のコレステロール、トリグリセリド、中性脂肪等の血中脂質を低減させる作用をもつ公知の素材を併用することは本発明の望ましい態様のひとつである。この公知素材としては前記の植物ステロール、γ−オリザノール、トリテルペンアルコール、これらのエステル類のほか次のような具体例を挙げることができるが、本発明はこれらに限定されるものではない。   In the blood cholesterol reducing agent of the present invention, various raw materials and components can be used in combination as long as not departing from the spirit of the present invention. For example, there are excipients, moisture-proofing agents, preservatives, toughening agents, thickeners, emulsifiers, antioxidants, sweeteners, acidulants, seasonings, colorants, fragrances and the like used in ordinary foods and pharmaceuticals. . Moreover, it is one of the desirable aspects of this invention to use together the well-known raw material which has the effect | action which reduces blood lipids, such as blood cholesterol, a triglyceride, and a neutral fat. In addition to the above-mentioned plant sterol, γ-oryzanol, triterpene alcohol, and esters thereof, the following specific examples can be given as examples of this known material, but the present invention is not limited thereto.

ガルシニア・カンボジア果皮エキス、ヒドロキシクエン酸及びその塩、ブドウ種子エキス、リンゴ、茶、カカオ豆等のポリフェノール、カテキン類(カテキン、エピカテキン、エピガロカテキンガレート等)、グアバ葉エキス、ギムネマ・シルベスタ葉エキス、イチョウ葉エキス、蕎麦種子エキス、ナツメ葉抽出物、桑葉エキス、スイカズラ抽出物、ニガウリ抽出物、ユーカリ葉エキス、プロシアニジン、フラボノイド類(ケンフェロール、ルテオリン、イソクエルシトリン等及びこれらの配糖体)、リパーゼ阻害剤、クロロフィリン、タウリン、田七人参エキス、杜仲エキス、乳清蛋白質、柑橘類成分(ヘスペレチン、ナリンゲニン、リモノイド、これらの配糖体等)、ゴマ由来リグナン及びこの配糖体、α−及びβ−アミラーゼ阻害剤、L−カルニチン及びこれを含む畜肉ペプチド、緑藻類や褐藻類の多糖類(アルギン酸、アミロペクチン、カラギーナン、寒天等)、植物性ガム(グアーガム、ローカストビーンガム、トラガントガム、タマリンドガム等)、キシログルカン、オリゴガラクチュロン酸、プロリン、スレオニン、n=3〜4のペプチド類、蛋白加水分解物、二重結合を2〜6個有するポリエン脂肪酸(リノール酸、α−リノレン酸、γ−リノレン酸、イコサペント酸、ドコサヘキサエン酸等)及びそのエステルや塩、大豆や卵黄由来のグリセロリン脂質(ホスファチジルコリン、ホスファチジルエタノールアミン、ホスファチジルセリン、ホスファチジルイノシトール、ホスファチジン酸等)及びこれらのリゾ体、ボラージ油、月見草油、唐辛子末及びそのエキス、ニンニク抽出エキス、スベリヒユ、緑茶やプーアール茶葉粉末及びそのエキス、杜仲末及びそのエキス、ウーロン茶葉粉末及びそのエキス、食物繊維(サイリウム種皮、ポリデキストロース、グルコマンナン、ペクチン等)、アカメガシワ抽出物、キチン、キトサン、キサンチン誘導体、シトラス・アウランチウム抽出エキス等がある。   Garcinia cambodia skin extract, hydroxycitric acid and its salts, grape seed extract, polyphenols such as apple, tea, cacao beans, catechins (catechin, epicatechin, epigallocatechin gallate, etc.), guava leaf extract, gymnema silvesta leaf Extract, Ginkgo biloba extract, buckwheat seed extract, jujube leaf extract, mulberry leaf extract, honeysuckle extract, bitter gourd extract, eucalyptus leaf extract, procyanidins, flavonoids (kaempferol, luteolin, isoquercitrin, etc. and their glycosides Body), lipase inhibitor, chlorophyllin, taurine, ginseng extract, Tochu extract, whey protein, citrus components (eg hesperetin, naringenin, limonoids, glycosides thereof), sesame-derived lignans and glycosides thereof, α -And β-amylase inhibitors, L -Carnitine and meat peptides containing it, polysaccharides of green algae and brown algae (alginic acid, amylopectin, carrageenan, agar, etc.), vegetable gums (guar gum, locust bean gum, tragacanth gum, tamarind gum, etc.), xyloglucan, oligogalactu Ronic acid, proline, threonine, peptides with n = 3-4, protein hydrolyzate, polyene fatty acid having 2-6 double bonds (linoleic acid, α-linolenic acid, γ-linolenic acid, icosapentanoic acid, docosahexaene Acid) and esters and salts thereof, glycerophospholipids derived from soybeans and egg yolk (phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidic acid, etc.) and their lyso forms, borage oil, evening primrose oil, pepper powder and extracts thereof , Garlic extract, green lily, green tea and pu-erh tea leaf powder and extract thereof, tsuchu naka powder and extract thereof, oolong tea leaf powder and extract thereof, dietary fiber (such as psyllium seed coat, polydextrose, glucomannan, pectin, etc.), akamegasiwa extract, chitin, Chitosan, xanthine derivatives, citrus aurantium extract, etc.

前述のように、本発明によれば、血中コレステロール濃度を低減させ、これらの異常な増加を抑制して血中脂質の代謝を改善する作用を有する、アカショウマ抽出物とキキョウ抽出物とを含む、望ましくはアカショウマ抽出物を主原料として含有してなる血中コレステロール低減剤が提供される。かかる血中コレステロール低減剤はそのまま本発明の所望の目的のために使用しても差し支えないが、本発明ではこれを配合してなる組成物も提供される。該組成物の態様としては飲食物、食品添加物、家畜用飼料、ペットフード等の種々のものがあるが、食用組成物又は医薬用組成物が好適である。   As described above, according to the present invention, the present invention includes a red pepper extract and a kyoukyo extract, which have the action of reducing blood cholesterol levels and suppressing these abnormal increases to improve blood lipid metabolism. Preferably, a blood cholesterol reducing agent comprising a red pepper extract as a main raw material is provided. Such a blood cholesterol reducing agent may be used as it is for the desired purpose of the present invention, but the present invention also provides a composition comprising this. Examples of the composition include various foods, food additives, livestock feeds, pet foods and the like, and edible compositions or pharmaceutical compositions are preferred.

本発明の食用組成物は、前述の血中コレステロール低減剤、すなわち、アカショウマ及びキキョウであって、これらの形態が根及び/又は根茎の抽出物あるいは精製物であるものを必須原料として含有してなる前記血中コレステロール低減剤を配合してなることを特徴とする。   The edible composition of the present invention contains, as an essential ingredient, the aforementioned blood cholesterol-reducing agent, that is, red pepper and kyoto, whose form is a root and / or rhizome extract or purified product. The blood cholesterol-reducing agent is blended.

この食用組成物の態様としては、前記の抽出物若しくは精製物をそのまま又は前記血中コレステロール低減剤を液状、ゲル状、粉末状あるいは固形状の食品、例えば、果実飲料、清涼飲料、茶、スープ、ゼリー、ヨーグルト、プリン、ケーキミックス、ふりかけ、味噌、醤油、ドレッシング、マヨネーズ、焼肉のたれ等の調味料、麺類、ハムやソーセージ等の畜肉魚肉加工食品、ジャム、牛乳、クリーム、バターやチーズ等の粉末状、固形状又は液状の乳製品、マーガリン、パン、ケーキ、クッキー等に添加した形態となすことができる。   As an aspect of this edible composition, the extract or purified product is used as it is or the blood cholesterol reducing agent is used as a liquid, gel, powder or solid food, for example, fruit drink, soft drink, tea, soup , Jelly, yogurt, pudding, cake mix, sprinkle, miso, soy sauce, dressing, mayonnaise, grilled meat sauce, noodles, processed meat and meat such as ham and sausage, jam, milk, cream, butter and cheese, etc. The powder, solid or liquid dairy product, margarine, bread, cake, cookie and the like can be added.

また、必要に応じてデキストリン、乳糖、澱粉又はその加工素材、セルロース末等の賦形剤、ビタミン、ミネラル、動植物や魚介類の油脂、たん白質、糖質、色素、香料、その他の前記食用添加剤等と共に粉末、顆粒、ペレット、錠剤等に加工したり、ゼラチン等で被覆してカプセルに成形したり、あるいはドリンク類にして、栄養補助食品や健康食品として利用できる。このとき、前記の血中脂質改善作用を有する公知の食用素材を併用した組成物は好適である。なお、本発明の食用組成物は極めて多種類の形態にわたり、前記の例示に限定されるものではないが、脂質代謝改善の点から油脂類や糖質を多量に含む食品類に添加した形態、前記の栄養補助食品や健康食品の形態が望ましい。   If necessary, dextrin, lactose, starch or processed materials thereof, excipients such as cellulose powder, vitamins, minerals, fats and oils of animals and plants and seafood, proteins, sugars, pigments, flavors, and other edible additives It can be processed into powders, granules, pellets, tablets, etc. together with agents, etc., coated with gelatin or the like to form capsules, or used as a drink or as a dietary supplement or health food. At this time, the composition which used together the well-known edible material which has the said blood lipid improvement effect is suitable. In addition, the edible composition of the present invention is not limited to the above exemplification over a wide variety of forms, but is added to foods containing a large amount of oils and carbohydrates from the viewpoint of lipid metabolism improvement, The above-mentioned dietary supplements and health foods are desirable.

前記の食品類や食用組成物における本発明の血中コレステロール低減剤の配合量は、当該食品や食用組成物の種類、形態、利用目的や本血中コレステロール低減剤の種類、形態等により一律に規定し難いが、一般の加工食品類に添加する場合では、例えば、本発明の血中コレステロール低減剤がアカショウマの根茎を含水率50質量%の含水エタノールで抽出した抽出物:キキョウの根茎を水で抽出した抽出物=50:50(質量比)のものであれば、概ね0.01〜50質量%であり、より好ましくは0.1〜30質量%である。この範囲を外れて少ないと経口摂取による本発明の所望効果が小さく、逆に多すぎると食品の種類によっては風味を損ねたり、当該食品を調製することが不可能になる場合がある。なお、本発明の血中コレステロール低減剤はそのまま食用に供しても差し支えない。   The amount of the blood cholesterol reducing agent of the present invention in the foods and edible compositions is uniformly according to the type and form of the food and edible composition, the purpose of use and the type and form of the blood cholesterol reducing agent. Although it is difficult to specify, when added to general processed foods, for example, an extract obtained by extracting the rhizome of red pepper with water-containing ethanol having a water content of 50% by mass with the blood cholesterol reducing agent of the present invention: water If the extract is 50:50 (mass ratio), it is generally 0.01 to 50% by mass, more preferably 0.1 to 30% by mass. If it is less than this range, the desired effect of the present invention by ingestion is small. Conversely, if it is too much, depending on the type of food, the flavor may be impaired or it may be impossible to prepare the food. The blood cholesterol reducing agent of the present invention may be used for food as it is.

本発明の医薬用組成物は、前記の血中コレステロール低減剤に本発明の趣旨に反しない公知の賦形剤や添加剤を必要に応じて加え、常法により加工して錠剤、カプセル剤、顆粒剤、散剤、注射剤等の製剤となしたものである。経口あるいは経腸投与、血管投与又は皮内投与して、高脂血症及びこれにともなう各種疾病の予防又は治療のために適用する。本発明の血中コレステロール低減剤の配合量はその形態や前記医薬用製剤の種類、形態、用法及び用量等により一律に設定し難いが、概ね0.01〜50質量%である。経口投与する場合の摂取量は特に限定されるものではないが、例えば、本血中コレステロール低減剤がアカショウマの根茎を含水率20質量%の含水アセトンで抽出した抽出物をさらに酢酸エチルで分別した可溶画分:キキョウの根茎を水抽出した抽出物=75:25(質量比)であるものをベースとして、成人(体重50kg)1日あたり0.01〜20g、より好ましくは0.1〜10gである。この範囲を外れて少ないと所望の効果が低下し、逆に多すぎても更なる効果は期待できない。   The pharmaceutical composition of the present invention is prepared by adding known excipients and additives that do not violate the spirit of the present invention to the blood cholesterol reducing agent as necessary, and processing by conventional methods to produce tablets, capsules, It is a preparation such as a granule, powder, or injection. It is applied for the prevention or treatment of hyperlipidemia and various diseases associated therewith by oral or enteral administration, vascular administration or intradermal administration. The compounding amount of the blood cholesterol reducing agent of the present invention is generally 0.01 to 50% by mass, although it is difficult to set uniformly depending on the form and the type, form, usage and dosage of the pharmaceutical preparation. The amount of intake in the case of oral administration is not particularly limited. For example, an extract obtained by extracting the rhizome of red blood with a water-containing acetone having a water content of 20% by mass as a cholesterol-reducing agent in blood is further fractionated with ethyl acetate. Soluble fraction: Extract obtained by water extraction of Rhizome rhizome = 75:25 (mass ratio), based on adult (weight 50 kg), 0.01-20 g per day, more preferably 0.1 10 g. If it is less than this range, the desired effect is lowered, and if it is too much, no further effect can be expected.

参考製造例1
アカショウマ(Astilbe thunbergii(SIEB.et ZUCC.)MIQ.)の乾燥根茎を約5mm角以下のサイズに破砕し、これをさらに粉砕機で処理して200タイラーメッシュをパスした微粉末(試料A−1)を調製した。
Reference production example 1
A dried rhizome of Astilbe thumbergii (SIEB. Et ZUCC.) MIQ. Was crushed to a size of about 5 mm square or less, and this was further processed by a pulverizer to give a fine powder that passed 200 Tyler mesh (Sample A-1 ) Was prepared.

製造例1
参考製造例1で得たアカショウマの根茎の破砕片1kgをステンレス製抽出釜に仕込み、含水率40質量%の含水エタノール10Lを加え、時々かき混ぜながら60℃で6時間抽出処理した。ついで、残渣を濾別して抽出液を得、該抽出液から減圧下に溶媒を留去して赤褐色の抽出物(試料A−2)75gを得た。
Production Example 1
1 kg of red stalk rhizome fragments obtained in Reference Production Example 1 was placed in a stainless steel extraction kettle, 10 L of hydrous ethanol having a water content of 40% by mass was added, and the mixture was extracted at 60 ° C. for 6 hours with occasional stirring. Subsequently, the residue was separated by filtration to obtain an extract, and the solvent was distilled off from the extract under reduced pressure to obtain 75 g of a reddish brown extract (sample A-2).

製造例2
参考製造例1で得たアカショウマの根茎の微粉末1kgをステンレス製抽出釜に仕込み、含水率20質量%の含水アセトン5Lを加えて還流下で3時間抽出処理した後、濾過して抽出液と残渣に分けた。該残渣に再び前記含水アセトン5Lを添加して同様に処理して抽出液を得た。両抽出液をあわせて減圧下に溶媒を留去して赤褐色の抽出物(試料A−3)68gを調製した。
Production Example 2
A 1 kg fine powder of rhizome of red pepper obtained in Reference Production Example 1 was placed in a stainless steel extraction kettle, and 5 L of water-containing acetone having a water content of 20% by mass was added and subjected to extraction treatment under reflux for 3 hours. Divided into residues. The residue was again added with 5 L of water-containing acetone and treated in the same manner to obtain an extract. Both extracts were combined and the solvent was distilled off under reduced pressure to prepare 68 g of a reddish brown extract (Sample A-3).

製造例3
製造例2で得たアカショウマの根茎の抽出物(試料A−3)45gを蒸留水1Lに懸濁させ、該懸濁液を酢酸エチル200mLずつで5回に分けて溶剤分別処理に供し、溶媒を減圧留去して酢酸エチル可溶画分(試料A−4)29g及び不溶画分(試料A−5)15gの各精製物を調製した。
Production Example 3
45 g of red rhizome extract (Sample A-3) obtained in Production Example 2 was suspended in 1 L of distilled water, and the suspension was divided into 5 portions of 200 mL of ethyl acetate and subjected to solvent fractionation treatment. Was distilled off under reduced pressure to prepare each purified product of 29 g of ethyl acetate soluble fraction (sample A-4) and 15 g of insoluble fraction (sample A-5).

参考製造例2
トリアシショウマ(Astilbe odontophylla MIQ.)の根茎を日干しにして乾燥後、この破砕片1kgを製造例1と同様に処理して赤茶色の抽出物(試料A−6)85gを得た。
Reference production example 2
After drying the rhizomes of tricholoma (Astilbe odontophylla MIQ.) By sun-drying, 1 kg of the crushed pieces were treated in the same manner as in Production Example 1 to obtain 85 g of a reddish brown extract (sample A-6).

参考製造例3
キキョウ(Platycodon grandiflorum A.DC.)の根を含む根茎の天日乾燥物を約5mm角以下のサイズに破砕し、これをさらに粉砕処理して200タイラーメッシュ通過の微粉末(試料P−1)を調製した。
Reference production example 3
The dried sun-dried rhizomes containing roots of Pyocodon grandiflorum A.DC. were crushed to a size of about 5 mm square or less and further pulverized to give fine powder passing through 200 Tyler mesh (sample P-1) Was prepared.

製造例4
参考製造例3で得たキキョウの根を含む根茎の破砕片1kgをステンレス製抽出釜に仕込み、蒸留水20Lを加えて還流下で5時間抽出処理した後、残渣を濾別して抽出液を得、該抽出液の水分を蒸発させて褐色の抽出物(試料P−2)310gを得た。
Production Example 4
After charging 1 kg of rhizome fragment containing the roots of Kyocera obtained in Reference Production Example 3 into a stainless steel extraction kettle, adding 20 L of distilled water and extracting under reflux for 5 hours, the residue was filtered to obtain an extract, The water in the extract was evaporated to obtain 310 g of a brown extract (sample P-2).

製造例5
製造例4で得たキキョウの根を含む根茎の抽出物(試料P−2)150gに含水率5質量%の含水エタノール1Lを加え、室温にて時々かき混ぜながら抽出処理して可溶分と不溶分とに分け、溶媒を減圧留去してエタノール可溶画分(試料P−3)110g及び不溶画分(試料P−4)35gの各精製物を調製した。
Production Example 5
1 L of hydrous ethanol having a water content of 5% by mass was added to 150 g of a rhizome extract (Sample P-2) containing the roots of Kyocera obtained in Production Example 4, and the extract was treated with occasional stirring at room temperature to dissolve and dissolve insoluble matter. The solvent was distilled off under reduced pressure to prepare each purified product of 110 g of ethanol-soluble fraction (sample P-3) and 35 g of insoluble fraction (sample P-4).

試験例
本発明に係るアカショウマ及びキキョウの各種加工処理物について、以下に述べる方法を用いて血中脂質濃度に及ぼす影響を調べた。
(A)参考試験例:脂肪負荷による血中脂質の上昇に及ぼす影響
ウィスター系雄性ラット(日本クレア(株)から購入、体重:370±5g)を一晩絶食させ、対照群及び試験物質投与群(1群7匹)に分け、対照群ではコーン油6mL、コール酸80mg、コレステロールオレアート2g及び蒸留水6mLを超音波処理して得た脂質エマルジョン2mL(蒸留水1mL含有)を、また、試験物質投与群では試験物質を含む前記脂質エマルジョン2mL(試験物質の最終投与量が1g/kgラット体重となるように調製した試験物質の溶液1mL含有)をそれぞれ非麻酔下で経口投与した。脂質エマルジョンを投与してから経時的に非麻酔下でラット尾静脈から採血し、直ちに血漿を分離し、市販のテスト用キット(和光純薬工業(株)製、トリグリセライド−E−テストキット)を用いて血漿中の中性脂肪含量を測定した。
Test Example The effects of various processed products of red pepper and red pepper according to the present invention on blood lipid concentration were examined using the method described below.
(A) Reference test example: Effect of fat load on blood lipid elevation Wistar male rats (purchased from Nippon Claire Co., Ltd., body weight: 370 ± 5 g) were fasted overnight, control group and test substance administration group In the control group, 2 mL of lipid emulsion (containing 1 mL of distilled water) obtained by sonication of 6 mL of corn oil, 80 mg of cholic acid, 2 g of cholesterol oleate and 6 mL of distilled water was also tested. In the substance administration group, 2 mL of the lipid emulsion containing the test substance (containing 1 mL of the test substance solution prepared so that the final dose of the test substance was 1 g / kg rat body weight) was orally administered under non-anaesthesia. Blood was collected from the rat tail vein under non-anaesthesia over time after the lipid emulsion was administered, and plasma was immediately separated, and a commercially available test kit (manufactured by Wako Pure Chemical Industries, Ltd., triglyceride-E-test kit) was used. Used to measure the neutral fat content in plasma.

なお、試験物質として本発明の試料A−2、A−3、A−4及び試料P−2、P−3と参考の試料A−1、A−5、A−6及び試料P−1、P−4のほか、公知の素材すなわちグアバ葉エキス(ビーエイチエヌ(株)製)、ガルシニア カンボジア抽出物(日本新薬(株)製)、ギムネマ シルベスタ葉エキス(ビーエイチエヌ(株)製)、γ−オリザノール(オリザ油化(株)製)、キトサン(甲陽ケミカル(株)製)、大豆由来のβ−シトステロール(シグマ社製、試薬)、ベルゲニン(アルドリッチ ケミカル社製、試薬)、アスチルビン(非特許文献4に記載の方法で採取)を単独又は組み合わせて用いた。試験物質の投与量はラット体重(1kg)あたり1gである。この結果を表1に示した。表1において、複数の試験物質を併用した場合はそれらの質量基準の混合比率を( )内に記載した。また、血中トリグリセリド含量は平均値±標準偏差で示した。   As test substances, Samples A-2, A-3, A-4 and Samples P-2, P-3 of the present invention and Reference Samples A-1, A-5, A-6 and Sample P-1, In addition to P-4, known materials such as guava leaf extract (manufactured by BN Co., Ltd.), Garcinia Cambodian extract (manufactured by Nippon Shinyaku Co., Ltd.), Gymnema sylvesta leaf extract (manufactured by BN Co., Ltd.), γ-oryzanol ( Oriza Oil Chemical Co., Ltd.), chitosan (manufactured by Koyo Chemical Co., Ltd.), soybean-derived β-sitosterol (manufactured by Sigma Co., reagent), bergenin (manufactured by Aldrich Chemical Co., reagent), astilbine (non-patent document 4) Collected by the described method) was used alone or in combination. The dose of test substance is 1 g per rat body weight (1 kg). The results are shown in Table 1. In Table 1, when a plurality of test substances are used in combination, the mixing ratio based on their mass is shown in parentheses. The blood triglyceride content is shown as an average value ± standard deviation.

表1のデータから、アカショウマ及びキキョウ由来の試験物質(乾燥粉末、その抽出物及び精製物)を含む脂質エマルジョンを投与した場合は、脂質エマルジョンのみ投与による一過性の血中トリグリセリド(中性脂肪)量の経時的上昇を顕著に抑制することが明らかになった。また、アカショウマ、トリアシショウマ、キキョウの根や根茎から抽出したエキス類及びその精製物では血中トリグリセリド量のレベルを低下させる作用も認められた。さらに、これらを併用したり、血中脂質改善作用を有する公知の素材との併用によっても同様もしくはより一層顕著な効果が認められた。   From the data in Table 1, when a lipid emulsion containing a test substance (dry powder, extract thereof and purified product) derived from red pepper and Kyocera was administered, transient blood triglycerides (neutral fat by administration of the lipid emulsion alone) ) It was found that the increase in the amount over time was significantly suppressed. In addition, extracts extracted from the roots and rhizomes of red pepper, triaciforma and kikyo and purified products thereof were also found to reduce blood triglyceride levels. Furthermore, the same or even more remarkable effects were observed when these were used in combination or with a known material having a blood lipid improving action.

Figure 2009102419
Figure 2009102419

(B)試験例:高脂肪食摂取による血中脂質量の変化に及ぼす影響
3週齢のICR系雌性マウス(日本クレア(株)から購入)を23℃、12時間の明暗サイクル下で、飼料(日本クレア(株)製、CE−2)を与えて1週間予備飼育した。4週齢の健康なマウス(体重:19.5〜20.4g)を平均体重がほぼ均等になるように普通食群(飼料:CE−2、n=11)、高脂肪食群(n=11)、(高脂肪食+試験物質1%)群(n=11)及び(高脂肪食+試験物質3%)群(n=11)に分け、12週間、前記各実験食と水を自由摂取させた。この後、マウスをエーテルで麻酔して腹部下大静脈より採血し、直ちに血漿を分離した。血漿中のトリグリセリド(中性脂肪)量及び総コレステロール量はテスト用キット(和光純薬工業(株)製、トリグリセライド−E−テストキット及び総コレステロール−E−テストキット)を用いて常法により測定した。この結果を表2に示す。
(B) Test example: Effect on changes in blood lipid level due to intake of high-fat diet A 3-week-old ICR female mouse (purchased from CLEA Japan, Inc.) was fed under a light-dark cycle of 23 ° C for 12 hours. (CE-2 manufactured by Japan Claire Co., Ltd.) was given and pre-bred for 1 week. Four week old healthy mice (weight: 19.5 to 20.4 g) were fed to a normal diet group (feed: CE-2, n = 11) and a high fat diet group (n = 11) Divided into (high fat diet + test substance 1%) group (n = 11) and (high fat diet + test substance 3%) group (n = 11), and freed each experimental diet and water for 12 weeks Ingested. Thereafter, the mouse was anesthetized with ether, blood was collected from the inferior vena cava, and plasma was immediately separated. The amount of triglyceride (neutral fat) and total cholesterol in plasma is measured by a conventional method using test kits (manufactured by Wako Pure Chemical Industries, Ltd., triglyceride-E-test kit and total cholesterol-E-test kit). did. The results are shown in Table 2.

なお、前記高脂肪食の組成は、牛脂:40部(質量基準。以下同様)、α−コーン澱粉:10部、グラニュー糖:9部、ビタミン混合物:1部、ミネラル混合物:4部、カゼイン:36部(グラニュー糖を除きオリエンタル酵母工業(株)製)であり、試験物質を添加した実験食では試験物質の添加質量をカゼイン質量の一部で置き換えた。   The composition of the high-fat diet is: beef tallow: 40 parts (mass basis; the same applies hereinafter), α-corn starch: 10 parts, granulated sugar: 9 parts, vitamin mixture: 1 part, mineral mixture: 4 parts, casein: It was 36 parts (excluding granulated sugar, manufactured by Oriental Yeast Co., Ltd.). In the experimental food to which the test substance was added, the added mass of the test substance was replaced with a part of the casein mass.

表2のデータから、高脂肪食投与群では普通食投与群に比べて血中脂質量が上昇するが、アカショウマやトリアシショウマ等のチダケサシ属に属する植物、またキキョウの抽出物やその精製物を所定量添加した高脂肪食を投与した群では、血中トリグリセリド量及び血中コレステロール量が普通食投与群なみ又はそれ以下に低下することが認められた。また、血中脂質改善作用のある公知の素材を単独で投与しても所望効果は小さいが、本発明の前記加工処理物(抽出物や精製物)との組み合わせによって顕著な効果が奏せられることが明らかになった。   From the data in Table 2, the lipid level in the high fat diet group is higher than that in the normal diet group. However, plants belonging to the genus Pichia, such as red pepper and triashoma, as well as extracts of Kyary and purified products thereof. In the group administered with a high-fat diet to which a predetermined amount was added, the blood triglyceride level and blood cholesterol level were found to be lower than or below that of the normal diet group. In addition, even if a known material having blood lipid improving action is administered alone, the desired effect is small, but a remarkable effect can be obtained by combining with the processed product (extract or purified product) of the present invention. It became clear.

Figure 2009102419
Figure 2009102419

試作例1
試料A−2及び試料P−3の混合物(1:1、質量比)からなる本発明の血中コレステロール低減剤120mgにガルシニア・カンボジア果皮エキス30mg、ミツロウ45mg及びボラージ油55mgを加え、約45℃で十分に混合して均質な状態にし、これをカプセル充填機に供して一粒あたり内容量が250mgのゼラチン被覆カプセル製剤を試作した。本カプセル製剤をボランティア(成人男女)15名に1日あたり1粒、2週間摂取のモニター試験に供したところ、13名に血中トリグリセリド量の低下、12名に血中総コレステロール量の低下が認められた。この製剤は経口摂取が可能な血中脂質改善用の食用組成物又は医薬用組成物として利用できる。
Prototype example 1
30 mg of Garcinia camphor skin extract, 45 mg of beeswax peel and 55 mg of borage oil were added to 120 mg of the blood cholesterol reducing agent of the present invention consisting of a mixture of sample A-2 and sample P-3 (1: 1, mass ratio), and about 45 ° C. Were mixed thoroughly to obtain a homogeneous state, and this was subjected to a capsule filling machine to prepare a gelatin-coated capsule preparation having an inner volume of 250 mg per grain. When 15 capsules (adult males and females) of this capsule preparation were given a monitor test of 1 capsule per day for 2 weeks, 13 patients had decreased blood triglyceride levels and 12 patients had decreased total blood cholesterol levels. Admitted. This preparation can be used as an edible composition for improving blood lipids or a pharmaceutical composition that can be taken orally.

参考試作例1
試料A−2:ウーロン茶葉粉末=3:2(質量比)の混合物5.0kgを化工澱粉(松谷化学(株)製、商品名:パインフロー)3.5kg、第三リン酸カルシウム0.3kg、ビタミンB0.3kg、ビタミンB0.2kg、ビタミンB0.2kg及びビタミンC0.5kgとともに配合機に仕込み10分間攪拌混合した。該混合物を直打式打錠機に供給して直径7mm、高さ4mm、質量150mgのタブレットを作成した後、コーティング機でシェラック薄膜をコーティングして錠剤形状の食品を試作した。
Reference prototype 1
Sample A-2: Oolong tea leaf powder = 5.0 kg of a mixture of 3: 2 (mass ratio), modified starch (Matsuya Chemical Co., Ltd., trade name: Pine Flow) 3.5 kg, tribasic calcium phosphate 0.3 kg, vitamins B 1 0.3 kg, Vitamin B 2 0.2 kg, Vitamin B 6 0.2 kg and Vitamin C 0.5 kg were charged into the blender and stirred and mixed for 10 minutes. The mixture was supplied to a direct compression tableting machine to prepare a tablet having a diameter of 7 mm, a height of 4 mm, and a mass of 150 mg, and then a shellac thin film was coated on the coating machine to produce a tablet-shaped food.

参考試作例2
家庭用ホイッパーにバター110g、ショートニング110g、上白糖90g及び牛乳100mLを入れ、攪拌しながら鶏卵1個を加えて十分に混合した後、薄力粉190g、ベーキングパウダー2gとともに試料A−1及び試料P−2の混合物(3:1、質量比)10gを添加して十分に捏ねあわせた。これを30分間ねかせた後、金型で50個に分割し、オーブンで焼いてバタークッキーを試作した。
Reference prototype 2
Put 110g of butter, 110g of shortening, 90g of white sugar and 100ml of milk into a home whipper, add 1 egg with stirring and mix well, then sample A-1 and sample P-2 together with 190g of weak flour and 2g of baking powder 10 g of the mixture (3: 1, mass ratio) was added and kneaded sufficiently. This was allowed to stand for 30 minutes, then divided into 50 pieces with a mold and baked in an oven to produce a butter cookie.

試作例2
市販の野菜ジュース1Lに、試料A−2:試料P−3:葡萄種子エキス(インターヘルス社製、商品名:アクティビン)=1:2:1(質量比)からなる本発明の血中コレステロール低減剤5gを加えて混合し、中性脂肪やコレステロールが気になるひとのための血中脂質改善用野菜ジュースを試作した。これは元の野菜ジュースと比較して何ら遜色のないものであった。
Prototype example 2
Blood cholesterol of the present invention comprising 1 L of commercially available vegetable juice, sample A-2: sample P-3: camellia seed extract (trade name: activin, manufactured by Interhealth) = 1: 2: 1 (mass ratio) 5 g of a reducing agent was added and mixed to produce a vegetable juice for improving blood lipid for those who are concerned about neutral fat and cholesterol. This was no inferior to the original vegetable juice.

本発明の血中コレステロール低減剤は、これを摂取することにより、高脂肪食の摂取による血中コレステロール濃度の増加を低下させ、血中脂質の低減のみならず高脂血症やこれから惹起される各種疾病の予防及び治療、減体重や肥満防止、ダイエット等の為に有効利用され得る。   The blood cholesterol reducing agent of the present invention reduces the increase in blood cholesterol level due to ingestion of a high fat diet by ingesting it, and is caused not only by reduction of blood lipid but also hyperlipidemia and the like. It can be effectively used for prevention and treatment of various diseases, weight loss and obesity prevention, dieting and the like.

Claims (5)

チダケサシ属に属する植物であるアカショウマの抽出物及びキキョウの抽出物を含有してなる血中コレステロール低減剤。   A blood cholesterol-reducing agent comprising an extract of red ginger which is a plant belonging to the genus Pleurotus genus and an extract of Kyoka. 血中コレステロールの低減が高脂肪食の摂取におけるものである請求項1に記載の血中コレステロール低減剤。   The blood cholesterol reducing agent according to claim 1, wherein the blood cholesterol is reduced by intake of a high fat diet. アカショウマの抽出物が、アカショウマの根及び/又は根茎の含水エタノール(含水率10〜50質量%)抽出物、又は、含水アセトン(含水率10〜30質量%)抽出物の酢酸エチル可溶画分である請求項1又は請求項2に記載の血中コレステロール低減剤。   The extract of red pepper is a water-soluble ethanol (water content 10-50% by mass) extract of red pepper and / or rhizome, or an ethyl acetate-soluble fraction of water-containing acetone (water content 10-30% by mass) extract. The blood cholesterol-reducing agent according to claim 1 or 2. キキョウの抽出物が、キキョウの根及び/又は根茎の熱水抽出物又は該熱水抽出物のエタノール可溶画分若しくは含水エタノール(含水率5質量%)可溶画分である請求項1又は請求項2に記載の血中コレステロール低減剤。   The extract of Kyoukyo is a hot water extract of roots and / or rhizomes of Kyoukyo, or an ethanol-soluble fraction or a water-containing ethanol (water content 5 mass%) soluble fraction of the hot water extract. The blood cholesterol reducing agent according to claim 2. 請求項1〜4のいずれか1項に記載の血中コレステロール低減剤を配合してなる食用組成物又は医薬用組成物。   The edible composition or pharmaceutical composition formed by mix | blending the blood cholesterol reducing agent of any one of Claims 1-4.
JP2009023958A 2009-02-04 2009-02-04 Blood cholesterol-reducing agent Pending JP2009102419A (en)

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Cited By (1)

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Publication number Priority date Publication date Assignee Title
CN114532428A (en) * 2020-11-18 2022-05-27 焦新年 Nine-steaming and nine-sun-drying sophora fruit tea and preparation method thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07274832A (en) * 1994-04-15 1995-10-24 Maruzen Pharmaceut Co Ltd Food and drink, material and production thereof
JPH11180869A (en) * 1997-12-16 1999-07-06 Maruzen Seiyaku Kk Blood lipid improving agent, cyclic amp phosphodiesterase inhibitor, drink and food, and skin preparation for external use
JP2002255839A (en) * 2001-03-02 2002-09-11 Bhn Kk Antiobestic drug

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07274832A (en) * 1994-04-15 1995-10-24 Maruzen Pharmaceut Co Ltd Food and drink, material and production thereof
JPH11180869A (en) * 1997-12-16 1999-07-06 Maruzen Seiyaku Kk Blood lipid improving agent, cyclic amp phosphodiesterase inhibitor, drink and food, and skin preparation for external use
JP2002255839A (en) * 2001-03-02 2002-09-11 Bhn Kk Antiobestic drug

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114532428A (en) * 2020-11-18 2022-05-27 焦新年 Nine-steaming and nine-sun-drying sophora fruit tea and preparation method thereof

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