JP2022007769A - Composition for inhibiting phosphodiesterase 5 activity or improving erectile function - Google Patents

Composition for inhibiting phosphodiesterase 5 activity or improving erectile function Download PDF

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JP2022007769A
JP2022007769A JP2020110894A JP2020110894A JP2022007769A JP 2022007769 A JP2022007769 A JP 2022007769A JP 2020110894 A JP2020110894 A JP 2020110894A JP 2020110894 A JP2020110894 A JP 2020110894A JP 2022007769 A JP2022007769 A JP 2022007769A
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雄気 伊藤
Yuki Ito
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    • AHUMAN NECESSITIES
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    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Abstract

To provide a new application of a processed product of a Phyllanthus plant.SOLUTION: The present invention discloses a composition for inhibiting phosphodiesterase 5 activity, a composition for improving the erectile function, and a composition for improving at least one selected from the group consisting of prostatic hyperplasia, the urination function, the urine storage function, and the male vigor, containing a processed product of a Phyllanthus plant as an active ingredient.SELECTED DRAWING: None

Description

本発明はコミカンソウ属植物の加工物の新たな用途に関する。 The present invention relates to new uses for processed products of plants of the genus Phyllanthus.

アムラは、別名をユカン(油柑、学名:Phyllanthus emblica)と称するコミカンソウ科コミカンソウ属の植物であり、エラオカルプシン(Elaeocarpusin)、ケブラグ酸(Chebulagicacid)、ゲラニイン(Geraniin)などのエラジタンニン類など、ポリフェノールが多く含まれることが知られている(特許文献1)。 Amla is a plant belonging to the genus Phyllanthaceae, also known as gooseberry (scientific name: Phyllanthus emblica), and is rich in polyphenols such as Elaeocarpusin, Chebulagicacid, and Geraniin. It is known to be included (Patent Document 1).

従来より、アムラには、血流改善作用、フィブリン形成阻害作用、及び血小板凝集抑制作用があり(特許文献2-4)、また肩こり改善効果、抗血栓効果、むくみ改善効果、エコノミークラス症候群の予防効果があることも知られている(特許文献5-8)。
アムラに含まれるエラジタンニンは、グルコースとエラグ酸とのエステルであり、加水分解されるとエラグ酸が生成する(非特許文献1)。エラグ酸には、高い抗酸化作用、抗ガン作用、レジスチン分泌抑制作用による肝脂肪症の改善効果があることが報告されている(非特許文献2-4)。
Conventionally, Amla has an effect of improving blood flow, an effect of inhibiting fibrin formation, and an effect of suppressing platelet aggregation (Patent Document 2-4), and also has an effect of improving stiff shoulders, an antithrombotic effect, an effect of improving swelling, and prevention of economy class syndrome. It is also known to be effective (Patent Document 5-8).
Elagitannin contained in Amla is an ester of glucose and ellagic acid, and when hydrolyzed, ellagic acid is produced (Non-Patent Document 1). It has been reported that ellagic acid has a high antioxidant effect, an anticancer effect, and an effect of improving hepatic steatosis due to a resistin secretion inhibitory effect (Non-Patent Document 2-4).

しかし、これらの先行文献には、いずれも、アムラやそれに含まれる成分にホスホジエステラーゼ活性を阻害する作用や、また勃起機能改善作用があることについての記載はない。 However, none of these prior literatures describe that amla and its components have an action of inhibiting phosphodiesterase activity or an action of improving erectile function.

特開2006-335736号公報Japanese Unexamined Patent Publication No. 2006-335736 特開2006-335708号公報Japanese Unexamined Patent Publication No. 2006-335708 特開2006-8529号公報Japanese Unexamined Patent Publication No. 2006-8259 特開2006-137701号公報Japanese Unexamined Patent Publication No. 2006-137071 特開2006-335721号公報Japanese Unexamined Patent Publication No. 2006-335721 特開2005-162684号公報Japanese Unexamined Patent Publication No. 2005-162648 特開2006-335711号公報Japanese Unexamined Patent Publication No. 2006-335711 特開2006-335710号公報Japanese Unexamined Patent Publication No. 2006-335710

Lei F., Xi ng DM., Xiang L., Zhao YN., Wang W (2003) Pharmakokinetic study of ellagic acid in rat after oral administration of pomegranate leaf extract. J Chromatogr B 796: 189-194.Lei F., Xi ng DM., Xiang L., Zhao YN., Wang W (2003) Pharmakokinetic study of ellagic acid in rat after oral administration of pomegranate leaf extract. J Chromatogr B 796: 189-194. Hassoun, E. A., Walter, A. C., Alshar if, N. Z., & Stohs, S. J. Modulation of TCDD induced fetotoxicity and oxidative stress in embryonic and placental tissues of C57BL/6J mice by vitamin E succinate and ellagic acid. Toxicology 124 1: 27 37.Hassoun, E. A., Walter, A. C., Alshar if, N. Z., & Stohs, S. J. Modulation of TCDD induced fetotoxicity and oxidative stress in embryonic and placental tissues of C57BL / 6J mice by vitamin E succinate and ellagic acid. Toxicology 124 1: 27 37. A. Nar ayanan, Bhagavathi & Geoffroy, Otto & C. Willingham, Mark & G. Re, Gian & W. Nixon, Daniel (1999) P53/p21 (WAF1/CIP1) expression and its possible role in G1 arrest and apoptosis in ellagic acid treated cancer cells. Cancer Letters 136:215 221.A. Nar ayanan, Bhagavathi & Geoffroy, Otto & C. Willingham, Mark & G. Re, Gian & W. Nixon, Daniel (1999) P53 / p21 (WAF1 / CIP1) expression and its possible role in G1 arrest and apoptosis in ellagic acid treated cancer cells. Cancer Letters 136: 215 221. Yoshimura Y., Nishii S., Zaima N., Moriyama T., Kaw amura Y. (2013) Ellagic acid improves hepatic steatosis and serum lipid composition through reduction of serum resistin levels and transcriptional activation of hepatic ppara in obese, diabetic KK Ay mice. Biochem Biophys Res Commun 434:486 491.Yoshimura Y., Nishii S., Zaima N., Moriyama T., Kaw amura Y. (2013) Ellagic acid improves hepatic steatosis and serum lipid composition through reduction of serum resistin levels and transcriptional activation of hepatic ppara in obese, diabetic KK Ay mice. Biochem Biophys Res Commun 434: 486 491. Prapapan T., Thomas R. H., Joseph A. B., Jarupa V., Khanit S., Wittaya P., Pattara S., Kornkanok I. (2013) Kaempferia Parviflora, a Plant Used in Traditional Medicine to Enhance Sexual Performance Contains Large Amounts of Low Affinity PDE5 Inhibitors. J Ethnopharmacol, 2011 Oct 11;137(3):1437-41.Prapapan T., Thomas RH, Joseph AB, Jarupa V., Khanit S., Wittaya P., Pattara S., Kornkanok I. (2013) Kaempferia Parviflora, a Plant Used in Traditional Medicine to Enhance Sexual Performance Contains Large Amounts of Low Affinity PDE5 Inhibitors. J Ethnopharmacol, 2011 Oct 11; 137 (3): 1437-41.

本発明はコミカンソウ属植物の加工物の新たな用途を提供することを課題とする。具体的には、本発明はコミカンソウ属植物の加工物を有効成分とするホスホジエステラーゼ5(以下、「PDE5」と称する)活性を阻害する組成物、または男性の勃起機能を改善する組成物を提供することを課題とする。さらに本発明は、前記植物加工物を有効成分とする前立腺肥大症状、排尿機能、畜尿機能、及び男性活力を改善する組成物を提供することを課題とする。 An object of the present invention is to provide a new use of a processed product of a plant belonging to the genus Phyllanthus. Specifically, the present invention provides a composition that inhibits the activity of phosphodiesterase 5 (hereinafter referred to as "PDE5") containing a processed product of a plant of the genus Phyllanthus as an active ingredient, or a composition that improves erectile function in men. That is the issue. Further, it is an object of the present invention to provide a composition containing the processed plant product as an active ingredient to improve benign prostatic hyperplasia, urination function, urination function, and male vitality.

本発明者らは、前記課題を解決すべく鋭意検討を重ねていたところ、コミカンソウ属植物の加工物、特にアムラの果実から抽出したエキスに、優れたPDE5活性阻害作用、勃起機能改善作用があること、言い換えれば男性の活力を改善し、また向上する作用があることを見出した。本件発明は、これらの知見に基づいて、さらに検討を重ねて完成したものであり、下記の実施態様を含むものである。 As a result of diligent studies to solve the above problems, the present inventors have found that processed products of Phyllanthus genus plants, particularly extracts extracted from Amla fruits, have excellent PDE5 activity inhibitory action and erectile function improving action. In other words, it has been found to have the effect of improving and improving the vitality of men. The present invention has been completed with further studies based on these findings, and includes the following embodiments.

1.コミカンソウ属植物の加工物を有効成分とするPDE5活性阻害用組成物。
2.コミカンソウ属植物の加工物を有効成分とする勃起機能改善用組成物。
3.コミカンソウ属植物の加工物を有効成分とする前立腺肥大症状、排尿機能、畜尿機能、及び男性活力からなる群より選択される少なくとも1つの改善用組成物。
4.前記コミカンソウ属植物がアムラである、項1~3のいずれか1項に記載する組成物。
5.前記組成物が、飲食物組成物、医薬組成物または飼料組成物である、項1~4のいずれか1項に記載する組成物。
1. 1. A composition for inhibiting PDE5 activity containing a processed product of a plant belonging to the genus Phyllanthus as an active ingredient.
2. 2. A composition for improving erectile function containing a processed product of a plant of the genus Phyllanthus as an active ingredient.
3. 3. At least one composition for improvement selected from the group consisting of benign prostatic hyperplasia symptoms, urinary function, livestock urinary function, and male vitality containing a processed product of a plant of the genus Phyllanthus as an active ingredient.
4. Item 6. The composition according to any one of Items 1 to 3, wherein the plant of the genus Phyllanthus is Amla.
5. Item 6. The composition according to any one of Items 1 to 4, wherein the composition is a food or drink composition, a pharmaceutical composition or a feed composition.

本発明の組成物によれば、PDE5の活性を阻害することができる。このため、本発明の組成物は血流低下に起因する症状、例えば陰茎勃起機能、下部尿路機能障害、前立腺肥大等といった状態の改善や向上を目的として、特に男性の健康や活力の維持増進を目的として使用することができる。 According to the composition of the present invention, the activity of PDE5 can be inhibited. Therefore, the composition of the present invention maintains and enhances the health and vitality of men, in particular, for the purpose of improving or improving conditions caused by decreased blood flow, such as penile erection function, lower urinary tract dysfunction, and benign prostatic hyperplasia. Can be used for the purpose.

実験例2において、アムラエキスの勃起誘発作用を、ウサギを用いて陰茎長の測定により評価した結果を示す。図中、「SNP」は、一酸化窒素(NO)供与体であるニトロプルシドナトリウムを意味する(以下の図も同じ)。(A)は、アムラエキスを継続的に経口投与した後、SNPの静脈内投与前(0 min)と投与後30分(30 min)における陰茎長(mm)の変化を示す。(B)は、4つの被験群についてSNP投与後30分の時点における陰茎長(mm)を、棒グラフにて比較した図である。In Experimental Example 2, the result of evaluating the erection-inducing effect of Amla extract by measuring the penis length using a rabbit is shown. In the figure, "SNP" means nitric oxide (NO) donor sodium nitroprusside (same for the following figures). (A) shows the change in penis length (mm) before intravenous administration of SNP (0 min) and 30 minutes (30 min) after intravenous administration of Amla extract after continuous oral administration. (B) is a figure comparing the penis length (mm) at the time point of 30 minutes after SNP administration for four test groups by a bar graph. 実験例2において、特に顕著な作用を示したSNP 1mg/kg+アムラエキス 500mg/kg投与群のウサギのSNP投与前(左図)、及びSNP投与30分後(右図)の陰茎部の撮影画像である。In Experimental Example 2, the images of the penis of rabbits in the SNP 1 mg / kg + Amla extract 500 mg / kg administration group, which showed particularly remarkable effects, before SNP administration (left figure) and 30 minutes after SNP administration (right figure). be. 実験例3において、シルデナフィル、クルミエキス、モズクエキス、及びアムラエキスの勃起誘発作用を、ウサギを用いて陰茎長の測定により評価した結果を示す。各試料を継続的に経口投与した後、SNPの静脈内投与前(0 min)と投与後30~120分(30~120 min)における各陰茎長(mm)の変化を示す。In Experimental Example 3, the results of evaluating the erection-inducing effects of sildenafil, walnut extract, mozuku extract, and amla extract by measuring the penis length using rabbits are shown. The changes in penis length (mm) between before intravenous administration of SNP (0 min) and 30 to 120 minutes (30 to 120 min) after continuous oral administration of each sample are shown.

本発明は、コミカンソウ(Phyllanthus)属植物の加工物を有効成分として含有するPDE5活性阻害用組成物を提供する。また、本発明は当該加工物を有効成分として含有する勃起機能改善用組成物を提供する。 The present invention provides a composition for inhibiting PDE5 activity, which comprises a processed product of a plant belonging to the genus Phyllanthus as an active ingredient. The present invention also provides a composition for improving erectile function containing the processed product as an active ingredient.

コミカンソウ属植物は、コミカンソウ科(Phyllanthaceae)に属する植物であり、なかでもアムラ(Phyllanthus emblica)は、前述するように、従来より血流改善作用、フィブリン形成阻害作用、及び血小板凝集抑制作用等の有用な薬理作用を有することが知られている植物である。 The leaves of the genus Phyllanthaceae are plants belonging to the family Phyllanthaceae, and among them, Amla (Phyllanthus emblica) has been conventionally useful for improving blood flow, inhibiting fibrin formation, suppressing platelet aggregation and the like, as described above. It is a plant known to have various pharmacological actions.

本発明の各種組成物は、当該コミカンソウ属植物の加工物を原料として調製することができる。原料として使用するコミカンソウ属植物の部位は、本発明の効果を奏することを限度として、特に限定されず、葉、茎、果実、花、芽、枝、幹、樹皮、根、花蕾、種子、種皮等の中から選択することができる。好ましくは果実、樹皮、根、葉であり、より好ましくは果実である。 The various compositions of the present invention can be prepared from the processed products of the leaves of the genus Phyllanthus as raw materials. The site of the plant of the genus Phyllanthus used as a raw material is not particularly limited as long as the effect of the present invention is exhibited, and leaves, stems, fruits, flowers, buds, branches, trunks, bark, roots, flower buds, seeds, seed coats. Etc. can be selected. Fruits, bark, roots and leaves are preferable, and fruits are more preferable.

本発明において、コミカンソウ属植物の加工物には、前記植物部位の粉砕物、搾汁、乾燥物、及び抽出物等が含まれる。 In the present invention, the processed products of Phyllanthus genus include crushed products, juices, dried products, extracts and the like of the plant parts.

粉砕物は、前記植物部位を粉砕したものであればよく、その調製方法やその粉砕状態は特に限定されない。例えばジェットミル等の本分野で公知の粉砕器により粉砕する方法を例示することができる。また、搾汁の調製も定法に従って行うことができる。 The crushed product may be any crushed product of the plant part, and the preparation method thereof and the crushed state thereof are not particularly limited. For example, a method of crushing with a crusher known in the art such as a jet mill can be exemplified. In addition, the juice can be prepared according to a conventional method.

乾燥物は、前記植物部位を乾燥させたものであればよく、その調製方法やその乾燥状態は特に限定されない。例えば、天日乾燥、遠赤外線照射、乾燥機(熱風乾燥、冷風乾燥、真空凍結乾燥等)等の従来公知の乾燥方法を例示することができる。乾燥物中の水分量としては、制限されないものの、好ましくは10重量%程度以下、より好ましくは8重量%程度以下を例示することができる。本発明において乾燥物の形態は問わず、植物部位そのものの乾燥物、乾燥物の粉砕物等のいずれでもよい。乾燥粉砕物は、前記粉砕物と同様の方法に従って乾燥物を粉砕することにより得ることができる。なお、前述する搾汁も、汁を搾取後、乾燥することで、搾汁乾燥物として調製することができる。 The dried product may be any product obtained by drying the plant part, and the preparation method thereof and the dried state thereof are not particularly limited. For example, conventionally known drying methods such as sun drying, far infrared irradiation, and a dryer (hot air drying, cold air drying, vacuum freezing drying, etc.) can be exemplified. Although the amount of water in the dried product is not limited, it can be preferably about 10% by weight or less, more preferably about 8% by weight or less. In the present invention, the form of the dried product is not limited, and any of the dried product of the plant part itself, the crushed product of the dried product, and the like may be used. The dried pulverized product can be obtained by pulverizing the dried product according to the same method as the pulverized product. The above-mentioned juice can also be prepared as a dried juice by squeezing the juice and then drying it.

抽出物は、前記植物部位から後述する溶媒を用いて成分を抽出したものであればよく、その調製方法(抽出方法及び抽出条件等)は特に限定されない。例えば、前記植物部位をそのまま、必要に応じて裁断、粉砕または乾燥等したのち、溶媒抽出によって抽出物を得ることができる。溶媒抽出の方法としては、本分野において公知の方法を採用すればよく、例えば水(温水、熱水を含む)抽出、アルコール抽出、超臨界抽出等の従来公知の抽出方法を利用することができる。 The extract may be any one obtained by extracting the components from the plant site using a solvent described later, and the preparation method (extraction method, extraction conditions, etc.) thereof is not particularly limited. For example, the plant part can be cut, crushed, dried or the like as it is, if necessary, and then extracted with a solvent to obtain an extract. As the solvent extraction method, a method known in the art may be adopted, and conventionally known extraction methods such as water (including hot water and hot water) extraction, alcohol extraction, supercritical extraction and the like can be used. ..

溶媒抽出を行う場合、溶媒としては例えば水;メタノール、エタノール、イソプロパノール等の低級アルコールや、プロピレングリコール、1,3-ブチレングリコール等の多価アルコール等のアルコール類(無水、含水の別を問わない);アセトン等のケトン類、ジエチルエーテル、ジオキサン、アセトニトリル、酢酸エチルエステル等のエステル類、キシレン、ベンゼン、クロロホルム等が挙げられる。溶媒として好ましくは水、低級アルコール、1,3-ブチレングリコール等であり、より好ましくは水、メタノール、エタノール、1,3-ブチレングリコールであり、更に好ましくは水、メタノール、含水エタノールである。これらの溶媒は1種単独で使用してもよく、2種以上を組み合わせて使用してもよい。 When solvent extraction is performed, the solvent may be, for example, water; lower alcohols such as methanol, ethanol and isopropanol, and alcohols such as polyhydric alcohols such as propylene glycol and 1,3-butylene glycol (whether anhydrous or water-containing). ); Ketones such as acetone, esters such as diethyl ether, dioxane, acetonitrile and ethyl acetate, xylene, benzene, chloroform and the like. The solvent is preferably water, a lower alcohol, 1,3-butylene glycol or the like, more preferably water, methanol, ethanol or 1,3-butylene glycol, and further preferably water, methanol or hydrous ethanol. These solvents may be used alone or in combination of two or more.

本発明において、このように溶媒抽出を経て得た抽出物を特に溶媒抽出物と称することができる。更に、本発明を制限するものではないが、例えば溶媒として水を用いた場合は水抽出物、アルコール類を用いた場合はアルコール抽出物、含水アルコールを用いた場合は含水アルコール抽出物等と称することができる。 In the present invention, the extract thus obtained through solvent extraction can be particularly referred to as a solvent extract. Further, although not limiting the present invention, for example, when water is used as a solvent, it is referred to as a water extract, when alcohols are used, it is referred to as an alcohol extract, and when a hydrous alcohol is used, it is referred to as a hydrous alcohol extract. be able to.

得られた抽出物は、そのままの状態で使用してもよく、乾燥させて粉末状や顆粒状等の固形の状態で使用してもよい。また、必要に応じて、得られた抽出物に精製、濃縮処理、高活性画分の分離処理等を施してもよい。本発明を制限するものではないが、精製処理としては、濾過、イオン交換樹脂や活性炭カラム等を用いた吸着、脱色といった処理が挙げられる。また、濃縮処理としては、エバポレーター等の常法を利用できる。また、高活性画分の分離処理としては、ゲル濾過、吸着処理、シリカゲルカラムクロマトグラフィー、HPLC(High performance liquid chromatography)等の公知の分離処理を利用できる。 The obtained extract may be used as it is, or may be dried and used in a solid state such as powder or granules. Further, if necessary, the obtained extract may be subjected to purification, concentration treatment, separation treatment of highly active fractions and the like. Although not limiting the present invention, examples of the purification treatment include treatments such as filtration, adsorption using an ion exchange resin, an activated carbon column, and decolorization. Further, as the concentration treatment, a conventional method such as an evaporator can be used. Further, as the separation treatment of the highly active fraction, known separation treatments such as gel filtration, adsorption treatment, silica gel column chromatography, and HPLC (High performance liquid chromatography) can be used.

また、例えば、前述のようにして得られた抽出物(更にはその乾燥物、精製処理物、濃縮処理物、高活性画分)を、凍結乾燥処理に供して粉末化する方法、必要に応じてデキストリン、コーンスターチ、アラビアゴム等の賦形剤を添加して、スプレードライ処理により粉末化する方法等の従来公知の方法に従って粉末化し、本発明で用いる抽出物としてもよい。また、該抽出物を、必要に応じてさらに水、エタノール等の可食性溶剤に溶解して用いてもよい。 Further, for example, a method for pulverizing the extract obtained as described above (further, its dried product, purified product, concentrated product, highly active fraction) by freeze-drying treatment, if necessary. The extract may be used in the present invention by adding excipients such as dextrin, cornstarch, and gum arabic and pulverizing according to a conventionally known method such as a method of pulverizing by spray-drying. Further, the extract may be further dissolved in an edible solvent such as water or ethanol, if necessary, and used.

本発明においてコミカンソウ属植物の加工物として好ましくは抽出物(その濃縮物及び/又は乾燥物等を含む)である。当該抽出物として、特に好ましくは、原料とするコミカンソウ属植物の使用部位を乾燥、破砕及び/または裁断し、好適な溶媒を使用して抽出、濾過して得られる抽出物、また、このようにして得られる抽出物を更に乾燥させることにより得られる抽出物である。本発明を制限するものではないが、当該抽出物は、例えば、原料となるコミカンソウ属植物の使用部位(好ましくは果実)、好ましくは当該使用部位の乾燥物、破砕物及び/または裁断物100gに対して1~50リットルの抽出溶媒を用いて、任意の温度(例えば15~90℃)で、必要に応じて攪拌しながら、任意の時間(例えば10分~24時間)、浸出抽出を行い、次いで濾過することにより得ることができる。 In the present invention, the processed product of a plant belonging to the genus Phyllanthus is preferably an extract (including a concentrate and / or a dried product thereof). The extract is particularly preferably an extract obtained by drying, crushing and / or cutting the site of use of the leafflower genus plant as a raw material, extracting and filtering using a suitable solvent, and in this way. It is an extract obtained by further drying the obtained extract. Although not limiting the present invention, the extract may be used, for example, in 100 g of a used site (preferably fruit) of a plant of the genus Phyllanthus as a raw material, preferably a dried product, a crushed product and / or a cut product of the used site. On the other hand, using 1 to 50 liters of extraction solvent, leach-extraction was performed at an arbitrary temperature (for example, 15 to 90 ° C.) for an arbitrary time (for example, 10 minutes to 24 hours) with stirring as needed. It can then be obtained by filtering.

本発明において使用するコミカンソウ属植物の加工物は市販品でもよく、市販品に対して更に乾燥等の処理を適宜施したものでもよい。 The processed product of the plant of the genus Phyllanthus used in the present invention may be a commercially available product, or may be a commercially available product that has been further subjected to a treatment such as drying.

本発明の組成物中の前記コミカンソウ属植物の加工物の含有量は、組成物中に当該加工物が含まれており、本発明の効果が得られる限り制限されない。例えば本組成物中、前記加工物が、乾燥物換算で0重量%より多く100重量%以下、好ましくは0.001~99重量%の範囲から選択することができる。 The content of the processed product of the plant of the genus Phyllanthus in the composition of the present invention is not limited as long as the processed product is contained in the composition and the effect of the present invention can be obtained. For example, in the present composition, the processed product can be selected from the range of more than 0% by weight and 100% by weight or less, preferably 0.001 to 99% by weight in terms of dry matter.

また、本発明の組成物において、前記コミカンソウ属植物の加工物の投与(摂取)量は、本発明の効果が奏される限り特に限定されず、対象者(対象動物)の体格、年齢、症状、適用形態、期待される効果の程度等に応じて適宜設定すればよい。なお、本組成物の対象者(対象動物)は、雄性の成人(成体)、ヒトの年齢でいうと18歳以上、好ましくは40歳以上の男性(雄)である。1日投与(摂取)量としては、制限されないものの、体重60kgの成人を基準として、植物加工物の乾燥重量換算として、好ましくは0.5~10000mg、より好ましくは5~4000mgが例示される。本発明の組成物は、1日あたり単回投与(摂取)であってもよく複数回投与(摂取)であってもよい。 Further, in the composition of the present invention, the dose (ingestion) of the processed product of the plant of the genus Phyllanthus is not particularly limited as long as the effect of the present invention is exhibited, and the physique, age and symptoms of the subject (target animal). , Appropriately set according to the application form, the degree of expected effect, and the like. The subject (target animal) of the present composition is a male adult (adult), a male (male) 18 years or older, preferably 40 years or older in terms of human age. The daily dose (intake) is not limited, but is preferably 0.5 to 10000 mg, more preferably 5 to 4000 mg in terms of dry weight of the processed plant product, based on an adult having a body weight of 60 kg. The composition of the present invention may be a single dose (ingestion) or a plurality of doses (ingestion) per day.

本発明の組成物は、経口投与または非経口投与の形態に調製することができるが、好ましくは経口投与形態を有する。その具体的な形態は特に制限されず、目的に応じて適宜設定すればよい。本発明の組成物の形態として、液剤、乳剤、懸濁剤、シロップ剤、エキス剤、酒精剤、エリキシル剤等の液状形態;散剤、顆粒剤、細粒剤、錠剤、丸剤、カプセル剤(ハードカプセル、ソフトカプセルを含む)、トローチ、チュアブル等の固形形態;その他、ゲル状、クリーム状、ペースト状、ムース状等の半固形状形態等の各種形態が例示される。 The composition of the present invention can be prepared in a form of oral administration or parenteral administration, but preferably has an oral administration form. The specific form is not particularly limited, and may be appropriately set according to the purpose. Liquid forms of the composition of the present invention include liquids, emulsions, suspensions, syrups, extracts, liquor, elixirs, etc .; powders, granules, fine granules, tablets, pills, capsules ( Solid forms such as hard capsules and soft capsules), troches, chewables, etc .; In addition, various forms such as gel-like, cream-like, paste-like, mousse-like semi-solid forms are exemplified.

例えば本発明の組成物が固形形態である場合、これは用時に水等と混合して使用してもよい。また、本発明の組成物は徐放性の剤形であってもよい。また、例えば錠剤は、必要に応じて、従来公知の剤皮を施した錠剤、例えば糖衣錠、ゼラチン被包錠、腸溶被錠、フィルムコーティング錠、あるいは二重錠、多層錠とすることができる。 For example, when the composition of the present invention is in a solid form, it may be mixed with water or the like at the time of use. Further, the composition of the present invention may be a sustained release dosage form. Further, for example, the tablet may be a conventionally known coated tablet, for example, a sugar-coated tablet, a gelatin-encapsulated tablet, an enteric-coated tablet, a film-coated tablet, a double tablet, or a multi-layer tablet, if necessary. ..

また、本発明の組成物の使用態様も制限されず、目的に応じて適宜設定すればよい。本発明の組成物の使用態様として、食品組成物(飲料を含む、保健機能食品(特定保健用食品、栄養機能食品、機能性表示食品、サプリメント等を含む)、病者用食品を含む)、医薬組成物、飼料組成物、また、食品組成物、医薬組成物、飼料等への添加剤等として使用することができる。 Further, the mode of use of the composition of the present invention is not limited, and may be appropriately set according to the intended purpose. As a mode of use of the composition of the present invention, food compositions (including beverages, health functional foods (including specified health foods, nutritional functional foods, foods with functional claims, supplements, etc.), foods for the sick, etc.), It can be used as a pharmaceutical composition, a feed composition, an additive to a food composition, a pharmaceutical composition, a feed, or the like.

本発明の組成物は、前述の各種形態、使用態様等における従来公知の通常の手順に従い製造すればよく、必要に応じて、食品の製造に許容されている成分、薬学的に許容される成分、可食性の成分といった任意の成分と混合等して製造すればよい。該任意の成分として、溶剤(水、メタノール、エタノール、イソプロパノール等の低級アルコール、プロピレングリコール、1,3-ブチレングリコール等の多価アルコール等のアルコール類(無水、含水の別を問わない)等)、賦形剤、崩壊剤、希釈剤、滑沢剤、香料、着色料、甘味料、矯味剤、懸濁剤、湿潤剤、乳化剤、可溶化剤、分散剤、緩衝剤、結合剤、浸透促進剤、安定剤、増量剤、防腐剤、増粘剤、pH調整剤、界面活性剤、コーティング剤、吸収促進剤、吸着剤、充填剤、酸化防止剤、清涼剤、皮膜形成剤、ゲル化剤、アミノ酸、ビタミン、酵素、各種栄養成分等が例示される。これらは1種単独で使用してもよく、2種以上を組み合わせて使用してもよい。 The composition of the present invention may be produced according to conventionally known conventional procedures in the above-mentioned various forms, usage modes, etc., and if necessary, components permitted for the production of foods, components pharmaceutically acceptable. , It may be manufactured by mixing with an arbitrary component such as an edible component. As the optional component, a solvent (water, lower alcohol such as methanol, ethanol, isopropanol, alcohols such as propylene glycol, polyhydric alcohol such as 1,3-butylene glycol (whether anhydrous or water-containing), etc.) and the like). , Excipients, disintegrants, diluents, lubricants, fragrances, colorants, sweeteners, flavoring agents, suspending agents, wetting agents, emulsifiers, solubilizers, dispersants, buffers, binders, penetration promoting Agents, stabilizers, bulking agents, preservatives, thickeners, pH regulators, surfactants, coating agents, absorption promoters, adsorbents, fillers, antioxidants, refreshing agents, film forming agents, gelling agents , Amino acids, vitamins, enzymes, various nutritional components and the like are exemplified. These may be used alone or in combination of two or more.

本発明において、本組成物の対象者(対象動物)は前述の通りであるが、対象動物としては、マウス、ラット、モルモット、ウサギ、イヌ、ネコ、サル、ブタ、牛、馬等の動物、好ましくはマウス、ラット、モルモット、ウサギ、イヌ、サル等の動物が例示される。 In the present invention, the subject (target animal) of the present composition is as described above, and the target animal includes animals such as mice, rats, guinea pigs, rabbits, dogs, cats, monkeys, pigs, cows, and horses. Animals such as mice, rats, guinea pigs, rabbits, dogs and monkeys are preferably exemplified.

本発明の組成物によれば、後述する実験例1に示すように、前記コミカンソウ属植物の加工物の作用に基づいてホスホジエステラーゼ5(PDE5)活性を阻害することができる。このことから、本発明は、前記植物の加工物を有効成分とするPDE5活性阻害用組成物を提供するものであり、また前記植物の加工物を調製する工程を含有するPDE5活性阻害用組成物の製造方法を提供するものである。また、本発明は、前記植物の加工物を用いることを特徴とするPDE5活性阻害方法を提供するものということもできる。さらに、本発明は、前記植物の加工物を、食品組成物、医薬組成物、または飼料組成物に配合することで、これらの組成物にPDE5活性阻害作用を付与する方法を提供するものということもできる。 According to the composition of the present invention, as shown in Experimental Example 1 described later, the phosphodiesterase 5 (PDE5) activity can be inhibited based on the action of the processed product of the plant of the genus Phyllanthus. From this, the present invention provides a composition for inhibiting PDE5 activity containing the processed product of the plant as an active ingredient, and also comprises a step of preparing the processed product of the plant. It provides a manufacturing method of. It can also be said that the present invention provides a method for inhibiting PDE5 activity, which is characterized by using the processed product of the plant. Furthermore, the present invention provides a method for imparting a PDE5 activity inhibitory effect to a food composition, a pharmaceutical composition, or a feed composition by blending the processed plant product with the food composition, the pharmaceutical composition, or the feed composition. You can also.

本発明の組成物によれば、後述する実験例2及び3に示すように、前記コミカンソウ属植物の加工物の作用に基づいて勃起を誘発し、また勃起の持続力を高めることができる。このことから、本発明は、前記植物の加工物を有効成分とする勃起機能改善用組成物を提供するものであり、また前記植物の加工物を調製する工程を含有する勃起機能改善用組成物の製造方法を提供するものである。また、本発明は、前記植物の加工物を用いることを特徴とする勃起機能改善方法(例えば、勃起誘発及び/または勃起の持続力向上方法)を提供するものということもできる。さらに、本発明は、前記植物の加工物を、食品組成物、医薬組成物、または飼料組成物に配合することで、これらの組成物に勃起機能改善作用(例えば勃起誘発作用及び/または勃起の持続力向上作用)を付与する方法を提供するものということもできる。このように、本発明の組成物は、精力減退、勃起力不全、または早漏等を改善して男性の活力を改善・向上するために好適に使用することができる。 According to the composition of the present invention, as shown in Experimental Examples 2 and 3 described later, it is possible to induce an erection based on the action of the processed product of the leafflower genus plant and to enhance the sustainability of the erection. From this, the present invention provides a composition for improving erectile function containing the processed product of the plant as an active ingredient, and the composition for improving erectile function including a step of preparing the processed product of the plant. It provides a manufacturing method of. It can also be said that the present invention provides a method for improving erection function (for example, a method for inducing erection and / or improving sustainability of erection), which is characterized by using the processed product of the plant. Further, according to the present invention, by blending the processed plant product into a food composition, a pharmaceutical composition, or a feed composition, an erection function improving action (for example, an erection-inducing action and / or an erection) is added to these compositions. It can also be said to provide a method of imparting a sustainability improving effect). As described above, the composition of the present invention can be suitably used for improving and improving the vitality of men by improving energy loss, erectile dysfunction, premature ejaculation and the like.

なお、PDE5は主にcGMPの分解に関与する酵素である。cGMPは、細胞内セカンドメッセンジャーとして作用し、平滑筋を弛緩させ、血流を増加させる。このため、PDE5の活性を阻害することで、平滑筋が弛緩し、血流が増加する。この作用を利用した薬剤として、今日、PDE5阻害薬が知られており、代表的なものとしてシルデナフィルクエン酸塩を有効成分とする医薬品等が知られている。PDE5阻害薬は、前述する作用に基づいて局所血流を増加させることにより、陰茎勃起能力の低下、膀胱や前立腺の機能低下、肺高血圧症といった症状の改善を目的として利用されている。このため、本発明の組成物も、PDE5阻害作用により平滑筋が弛緩し、これにより陰茎海綿体への血流を増加させることで陰茎勃起機能の改善を図ることができるものと考えられる。同様に、PDE5阻害作用により、泌尿器系への血流を増加させることで下部尿路障害の改善(例えば排尿機能や蓄尿機能の改善)を図ることができ、前立腺や尿道の血流を増加させることで前立腺肥大の緩和を図ることができると考えられる。さらに、PDE5阻害作用により、肺組織への血流を増加させることで肺動脈圧の低下を図ることができる。 PDE5 is an enzyme mainly involved in the degradation of cGMP. cGMP acts as an intracellular second messenger, relaxing smooth muscle and increasing blood flow. Therefore, by inhibiting the activity of PDE5, smooth muscle relaxes and blood flow increases. As a drug utilizing this action, a PDE5 inhibitor is known today, and a typical drug such as a drug containing sildenafil citrate as an active ingredient is known. PDE5 inhibitors have been used for the purpose of improving symptoms such as decreased penile erection ability, decreased bladder and prostate function, and pulmonary hypertension by increasing local blood flow based on the above-mentioned effects. Therefore, it is considered that the composition of the present invention can also improve the penile erectile function by relaxing the smooth muscle due to the PDE5 inhibitory action and thereby increasing the blood flow to the corpus cavernosum penis. Similarly, the PDE5 inhibitory effect can improve lower urinary tract disorders (for example, improvement of urinary function and urinary storage function) by increasing blood flow to the urinary system, and increase blood flow in the prostate and urethra. It is thought that this can alleviate the enlargement of the prostate. Furthermore, due to the PDE5 inhibitory action, it is possible to reduce the pulmonary arterial pressure by increasing the blood flow to the lung tissue.

このことから、本発明の組成物はまた、男性機能が気になる対象者(男性の活力を改善し向上させたい対象者)、排尿機能が気になる対象者等に好ましく適用することができる。このように、本発明の組成物は、PDE5活性阻害用組成物、陰茎勃起機能(不全)改善用組成物、下部尿路機能改善用組成物、前立腺肥大改善用組成物、肺高血圧症改善用組成物(特に肺動脈性肺高血圧症)等としても、好適に使用することができる。 From this, the composition of the present invention can also be preferably applied to a subject who is concerned about male function (a subject who wants to improve and improve male vitality), a subject who is concerned about urination function, and the like. .. As described above, the composition of the present invention is a composition for inhibiting PDE5 activity, a composition for improving penile erection function (deficiency), a composition for improving lower urinary tract function, a composition for improving benign prostatic hyperplasia, and a composition for improving pulmonary hypertension. It can also be suitably used as a composition (particularly pulmonary arterial hypertension) and the like.

以上、本明細書において、「含む」及び「含有する」の用語には、「からなる」及び「から実質的になる」という意味が含まれる。 As described above, in the present specification, the terms "contains" and "contains" include the meanings of "consisting of" and "substantially consisting of".

以下、本発明の構成及び効果について、その理解を助けるために、実験例を用いて本発明を説明する。但し、本発明はこれらの実験例によって何ら制限を受けるものではない。以下の実験は、特に言及しない限り、室温(25±5℃)、及び大気圧条件下で実施した。なお、特に言及しない限り、以下に記載する「%」は「質量%」、「部」は「質量部」を意味する。 Hereinafter, the present invention will be described with reference to experimental examples in order to help understanding the structure and effects of the present invention. However, the present invention is not limited by these experimental examples. The following experiments were performed under room temperature (25 ± 5 ° C.) and atmospheric pressure conditions, unless otherwise noted. Unless otherwise specified, "%" described below means "% by mass" and "part" means "part by mass".

試験に使用した被験試料は、下記の通りである。なお、シルデナフィルクエン酸塩は、PDE5阻害作用を有し、勃起不全治療剤の有効成分として使用されている化合物であり、下記の試験ではpositive controlとして使用した。
(1)シルデナフィル:シルデナフィルクエン酸塩
(2)アムラエキス:果実から皮と種を取り除いて濃縮し、乾燥粉末化したエキス
(3)黒ショウガエキス:根茎を含水エタノールで抽出、乾燥粉末化したエキス
(4)ヒハツエキス:果実を熱水で抽出し、乾燥粉末化したエキス
(5)黒コショウエキス:乾燥黒コショウを、含水エタノールで抽出し、乾燥粉末化したエキス
(6)クルミエキス:種皮を含水エタノールで抽出し、乾燥粉末化したエキス
(7)モズクエキス:オキナワモズクをクエン酸で抽出し、中和後に濃縮させ、乾燥粉末化したエキス。
The test samples used in the test are as follows. Sildenafil citrate is a compound that has a PDE5 inhibitory effect and is used as an active ingredient of a therapeutic agent for erectile dysfunction, and was used as a positive control in the following tests.
(1) Syldenafil: Syldenafil citrate (2) Amla extract: Extract obtained by removing the skin and seeds from the fruit, concentrating and drying and powdering (3) Black ginger extract: Extract of rhizome with hydrous ethanol and dried and powdered ( 4) Hihatsu extract: Extract of fruits extracted with hot water and dried and powdered (5) Black pepper extract: Extract of dried black pepper extracted with hydrous ethanol and powdered (6) Walnut extract: Seed coat with hydrous ethanol Extract and dry powdered extract (7) Mozuku extract: An extract of Okinawa mozuku extracted with citric acid, neutralized, concentrated and dried and powdered.

実験例1 PDE5阻害作用の評価(in vitro)
(1)実験方法
PDE5Aアッセイキット(ビーピーエス バイオサイエンス社/BPS Bioscience Inc.製)を用いて、下記の工程に従って、各被験試料のPDE5阻害率を測定し、PDE5阻害作用を評価した。
(a)希釈調製したFAM-Cyclic-3’,5’-GMPを、25μLずつ各ウェル(Test、Blank、Substrate control、Positive control)に添加した。
(b)「Blank」のウェルに25μLずつPDEバッファーを添加し、次いで、各被験試料溶液(10%DMSOで300μg/mLになるように調製したもの)(「Test」[被験試料(2)~(5)]のウェル及び「Positive control」[被験試料(1)]のウェル)、または溶媒(10%DMSO)(「Blank」及び「Substrate control」のウェル)を、該当する各ウェルに5μL添加した。
(c)次いで、「Blank」と「Substrate control」のウェルに20μLずつPDEアッセイバッファーを添加した。希釈調製したPDE5Aを「Test」と「Positive control」のウェルに20μLずつ添加した(200 pg/反応ウェル)。
(d)25℃で1時間反応させた。反応は、希釈調製したBinding agentを100μLずつ各ウェルに添加し、25℃で30分間強く振とうしながら行った。
(e)反応後、プレートリーダーで各ウェルの蛍光偏光を測定した(Excitation:475-495 nm、Emission:518-538 nm)。
(f)「Blank」のウェルの測定値(Blank値)を、各ウェル(「Test」、「Substrate control」、「Positive control」のウェル)の測定値から減じ、蛍光偏光値を算出した。「Substrate control」の蛍光偏光値との比率から、各被験試料(Test:被験試料(2)~(5)、Positive control:被験試料(1))のPDE5阻害率%を算出した。
Experimental Example 1 Evaluation of PDE5 inhibitory effect (in vitro)
(1) Experimental method
Using the PDE5A assay kit (manufactured by BPS Bioscience Inc.), the PDE5 inhibition rate of each test sample was measured according to the following steps, and the PDE5 inhibitory effect was evaluated.
(A) 25 μL of diluted FAM-Cyclic-3', 5'-GMP was added to each well (Test, Blank, Substrate control, Positive control).
(B) Add 25 μL of PDE buffer to each well of “Blank”, and then each test sample solution (prepared to 300 μg / mL with 10% DMSO) (“Test” [test sample (2) to). (5)] wells and "Positive control" [test sample (1)] wells) or solvent (10% DMSO) ("Blank" and "Substrate control" wells) were added to each applicable well in an amount of 5 μL. did.
(C) Next, 20 μL of PDE assay buffer was added to each of the “Blank” and “Substrate control” wells. 20 μL of diluted PDE5A was added to the “Test” and “Positive control” wells (200 pg / reaction well).
(D) The reaction was carried out at 25 ° C. for 1 hour. The reaction was carried out by adding 100 μL of the diluted Binder to each well and shaking vigorously at 25 ° C. for 30 minutes.
(E) After the reaction, the fluorescence polarization of each well was measured with a plate reader (Excitation: 475-495 nm, Emission: 518-538 nm).
(F) The measured value (Blank value) of the well of "Blank" was subtracted from the measured value of each well (well of "Test", "Substrate control", "Positive control") to calculate the fluorescence polarization value. The PDE5 inhibition rate% of each test sample (Test: test sample (2) to (5), Positive control: test sample (1)) was calculated from the ratio with the fluorescence polarization value of "Substrate control".

(2)実験結果
結果を表1に示す。

Figure 2022007769000001
(2) Experimental results The results are shown in Table 1.
Figure 2022007769000001

表1に示すように、Positive controlであるシルデナフィル(100nM)のPDE5阻害率は89.6%であった。この系におけるアムラエキス(実施例1)のPDE5阻害率は 59.2%であった。これに対して、黒ショウガエキス(比較例1)の阻害率は40.8%、ヒハツエキス(比較例2)の阻害率は8.2%、黒コショウエキス(比較例3)の阻害率は0.3%であった。比較例の中でも黒ショウガエキスはホスホジエステラーゼ活性阻害作用を示すことで知られる5,7-ジメトキシフラボンを含有する植物であるが(非特許文献5)、本実験によって、そのPDE5阻害作用よりもアムラエキスによる阻害作用の方が顕著に高いことが確認された。
このように、コミカンソウ属植物であるアムラのエキスには、シルデナフィルには劣るものの、強いPDE5阻害作用があることが確認された。
As shown in Table 1, the PDE5 inhibition rate of sildenafil (100 nM), which is a positive control, was 89.6%. The PDE5 inhibition rate of Amla extract (Example 1) in this system was 59.2%. On the other hand, the inhibition rate of black ginger extract (Comparative Example 1) was 40.8%, the inhibition rate of Hihatsu extract (Comparative Example 2) was 8.2%, and the inhibition rate of black pepper extract (Comparative Example 3) was 0.3%. .. Among the comparative examples, black ginger extract is a plant containing 5,7-dimethoxyflavone, which is known to exhibit an inhibitory effect on phosphodiesterase activity (Non-Patent Document 5). It was confirmed that the inhibitory effect was significantly higher.
Thus, it was confirmed that the extract of Amla, a plant of the genus Phyllanthus, has a strong PDE5 inhibitory effect, although it is inferior to sildenafil.

実験例2 勃起誘発作用の評価(その1)
(1)実験方法
ウサギ(ニュージーランドホワイト)を、コントロール群(SNP[1mg/kg]のみ投与群:2匹)と、被験試料投与群(SNP[1mg/kg]+アムラエキス[50mg/kg/日]投与群、SNP[1mg/kg]+アムラエキス[150mg/kg/日]投与群、SNP[1mg/kg]+アムラエキス[500mg/kg/日]投与群:各群4匹)の合計4群に分けた。被験試料投与群には、アムラエキスを7日間連続経口投与した後、NO供与体であるSNP(ニトロプルシドナトリウム)を単回、静脈内投与した。アムラエキス最終投与日(7日目)はSNP投与60分前にアムラエキスを経口摂取させ、SNP投与前、及びSNP投与30分後に、陰茎部を撮影するとともに、陰茎露出部の長さを測定した。コントロール群も同日にSNP投与前及びSNP投与30分後に、陰茎部を撮影し、また陰茎露出部の長さを測定した。陰茎露出部の長さ(mm)はノギスによって測定し、NO供与体による勃起誘発作用に対するアムラエキスの作用を評価した。
Experimental Example 2 Evaluation of erection-inducing action (Part 1)
(1) Experimental method Rabbit (New Zealand White) was administered to the control group (SNP [1 mg / kg] only administration group: 2 animals) and the test sample administration group (SNP [1 mg / kg] + Amla extract [50 mg / kg / day]]. Divided into a total of 4 groups: SNP [1 mg / kg] + Amla extract [150 mg / kg / day] administration group, SNP [1 mg / kg] + Amla extract [500 mg / kg / day] administration group: 4 animals in each group) rice field. In the test sample administration group, Amla extract was orally administered continuously for 7 days, and then SNP (sodium nitroprusside), which is a NO donor, was intravenously administered once. On the final day of administration of Amla extract (7th day), Amla extract was orally ingested 60 minutes before SNP administration, and the penis was photographed before SNP administration and 30 minutes after SNP administration, and the length of the exposed penis was measured. In the control group, the penis was photographed before SNP administration and 30 minutes after SNP administration on the same day, and the length of the exposed penis was measured. The length (mm) of the exposed penis was measured by caliper to evaluate the effect of Amla extract on the erection-inducing effect of NO donors.

(2)実験結果
陰茎露出部の長さを測定した結果を図1に示す。図1に示すように、アムラエキスは用量依存的に陰茎勃起の誘発作用を示した。被験試料投与群のうち、特に顕著な作用を示したSNP[1mg/kg]+アムラエキス[500mg/kg/日]投与群のSNP投与前(左側)、及び(右側)SNP投与30分後の陰茎部の撮影画像を図2に示す。
(2) Experimental results Figure 1 shows the results of measuring the length of the exposed penis. As shown in FIG. 1, Amla extract showed a dose-dependent effect of inducing penile erection. Penis before (left) and (right) SNP administration in the SNP [1 mg / kg] + Amla extract [500 mg / kg / day] administration group, which showed particularly remarkable effects among the test sample administration groups. The photographed image of the part is shown in FIG.

実験例3 勃起誘発作用の評価(その2)
(1)実験方法
実験例2と同様の試験を、各群3匹のウサギを用いて、経口投与する被験試料としてアムラエキスに代えて、シルデナフィル[50mg/kg/日](比較例4)、クルミエキス[500mg/kg/日](比較例5)、モズクエキス[500mg/kg/日](比較例6)を用いて実施した。また、経口投与するとしてアムラエキス[500mg/kg/日](実施例1)についても同様に実験を行った。但し、アムラエキス最終投与日(7日目)のSNP投与前、及びSNP投与から30分後、60分後、90分後及び120分後の5ポイントで陰茎露出部の長さを測定した。最終投与日は、アムラエキスをSNP投与60分前に経口摂取させた。
Experimental Example 3 Evaluation of erection-inducing action (Part 2)
(1) Experimental method Sildenafil [50 mg / kg / day] (Comparative Example 4) and walnuts were used in the same test as in Experimental Example 2 in place of Amla extract as a test sample to be orally administered using 3 rabbits in each group. It was carried out using an extract [500 mg / kg / day] (Comparative Example 5) and a mozuku extract [500 mg / kg / day] (Comparative Example 6). In addition, an experiment was also conducted on Amla extract [500 mg / kg / day] (Example 1) for oral administration. However, the length of the exposed penis was measured at 5 points before SNP administration on the final administration day (7th day) of Amla extract, and 30 minutes, 60 minutes, 90 minutes, and 120 minutes after SNP administration. On the final administration day, Amla extract was orally ingested 60 minutes before SNP administration.

(2)実験結果
結果を図3に示す。図3に示すように、比較例5(SNP[1mg/kg]+クルミエキス[500mg/kg/日]投与)及び比較例6(SNP[1mg/kg]+モズクエキス[500mg/kg/日]投与)はいずれもコントロール群(SNP[1mg/kg]のみ投与)よりも陰茎勃起の誘発作用は低かった。比較例4(SNP[1mg/kg]+シルデナフィル[50mg/kg/日]投与)はSNP投与から60分までは陰茎勃起の誘発作用が持続したが、その後著しく低下した。一方、実施例1(SNP[1mg/kg]+アムラエキス[500mg/kg/日]投与)は、SNP投与から90分まで陰茎勃起の誘発作用が持続し、陰茎勃起が長く持続することが確認された。以上よりアムラエキスはポリフェノールを含有する他の植物エキスと比較して、高い勃起機能を増強する作用があることが示された。
(2) Experimental results The results are shown in FIG. As shown in FIG. 3, Comparative Example 5 (SNP [1 mg / kg] + walnut extract [500 mg / kg / day] administration) and Comparative Example 6 (SNP [1 mg / kg] + mozuku extract [500 mg / kg / day]] In all cases, the effect of inducing penile erection was lower than that in the control group (administering only SNP [1 mg / kg]). In Comparative Example 4 (SNP [1 mg / kg] + sildenafil [50 mg / kg / day] administration), the penile erection-inducing effect was sustained from SNP administration to 60 minutes, but was significantly reduced thereafter. On the other hand, in Example 1 (SNP [1 mg / kg] + Amla extract [500 mg / kg / day] administration), it was confirmed that the penile erection-inducing action was sustained from SNP administration to 90 minutes, and the penile erection was sustained for a long time. rice field. From the above, it was shown that Amla extract has an effect of enhancing high erectile function as compared with other plant extracts containing polyphenols.

Claims (5)

コミカンソウ属植物の加工物を有効成分とするホスホジエステラーゼ5活性阻害用組成物。 A composition for inhibiting the activity of phosphodiesterase 5 containing a processed product of a plant belonging to the genus Phyllanthus as an active ingredient. コミカンソウ属植物の加工物を有効成分とする勃起機能改善用組成物。 A composition for improving erectile function containing a processed product of a plant of the genus Phyllanthus as an active ingredient. コミカンソウ属植物の加工物を有効成分とする前立腺肥大症状、排尿機能、畜尿機能、及び男性活力からなる群より選択される少なくとも1つの改善用組成物。 At least one composition for improvement selected from the group consisting of benign prostatic hyperplasia symptoms, urinary function, livestock urinary function, and male vitality containing a processed product of a plant of the genus Phyllanthus as an active ingredient. 前記コミカンソウ属植物がアムラである、請求項1~3のいずれか1項に記載する組成物。 The composition according to any one of claims 1 to 3, wherein the plant of the genus Phyllanthus is Amla. 前記組成物が、飲食物組成物、医薬組成物または飼料組成物である、請求項1~4のいずれか1項に記載する組成物。 The composition according to any one of claims 1 to 4, wherein the composition is a food or drink composition, a pharmaceutical composition or a feed composition.
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