JP2005289984A - Hyperlipidemia ameliorating agent comprising patrinia scabiosaefolia - Google Patents
Hyperlipidemia ameliorating agent comprising patrinia scabiosaefolia Download PDFInfo
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Abstract
Description
本発明は、長期間服用しても安全な高脂血症の予防又は改善剤に関し、医薬品、医薬部外品又は食品の分野に属する。 The present invention relates to a preventive or ameliorating agent for hyperlipidemia that is safe even if taken for a long period of time, and belongs to the fields of pharmaceuticals, quasi drugs, and foods.
近年、食習慣、運動習慣、休養、喫煙、飲酒など生活習慣病がその発症・進行に影響を及ぼすとされている生活習慣病が注目されている。特に、先進諸国においては、食習慣・運動習慣との関連が大きいとされる高脂血症、肥満、II型糖尿病のようなインスリン非依存型の疾患、高血圧などが急増することにより、国民の健康維持に支障をきたし、その結果、国民医療費の高騰を引き起こすなど、深刻な社会問題となっている。 In recent years, lifestyle-related diseases such as eating habits, exercise habits, rest, smoking, drinking, etc., which are said to affect the onset and progression of such diseases, have attracted attention. In developed countries, in particular, the rise of hyperlipidemia, obesity, non-insulin-dependent diseases such as type II diabetes, hypertension, etc. It has become a serious social problem that has hindered the maintenance of health and, as a result, has caused soaring national medical expenses.
高脂血症は血液中の脂質が増加する病態であって、その診断には、一般的な指標として血清コレステロール及びトリグリセライドが用いられている。また、高脂血症は血清のトリグリセライドが増加する高トリグリセライド血症とコレステロールが増加する高コレステロール血症に分類される。 Hyperlipidemia is a condition in which lipids in the blood increase, and serum cholesterol and triglycerides are used as a general index for the diagnosis. Hyperlipidemia is classified into hypertriglyceridemia in which serum triglyceride increases and hypercholesterolemia in which cholesterol increases.
トリグリセライドは動物が活動するためのエネルギー源として重要であり、食物から吸収あるいは体内で合成される。過剰なトリグリセライドは内臓周辺や皮下に脂肪として蓄積され、肥満を誘発し、II型糖尿病や高血圧症を促進させる可能性がある。また、動脈硬化との関連からも、高トリグリセライド血症との関係が指摘されている。 Triglycerides are important as an energy source for animal activity and are absorbed from food or synthesized in the body. Excess triglyceride accumulates as fat around the viscera and subcutaneously, induces obesity, and may promote type II diabetes and hypertension. Moreover, the relationship with hypertriglyceridemia is pointed out also from the relationship with arteriosclerosis.
コレステロールは生体内で細胞膜の構成成分やある種のホルモンの原材料として利用されている。血清コレステロールの増加がすべて生体に悪影響を及ぼすわけではないが、現代人には食生活の変化により必要以上の増加傾向が観られる。コレステロールは体内でリポ蛋白と結合した形で存在する。このリポ蛋白は比重の違いにより、カイロミクロン、ＶＬＤＬ、ＬＤＬ、ＨＤＬに分類される。高コレステロール血症で特に問題とされるのはＬＤＬの増加であり、ＬＤＬコレステロールの増加は動脈硬化や循環器疾患などを惹起するといわれている。 Cholesterol is used in vivo as a constituent of cell membranes and as a raw material for certain hormones. Although an increase in serum cholesterol does not all have an adverse effect on the living body, modern people tend to increase more than necessary due to changes in dietary habits. Cholesterol is present in a form bound to lipoproteins in the body. This lipoprotein is classified into chylomicron, VLDL, LDL, and HDL depending on the specific gravity. It is said that an increase in LDL is particularly problematic in hypercholesterolemia, and an increase in LDL cholesterol is said to cause arteriosclerosis and cardiovascular disease.
近年、生活習慣の中でも特に注目されている食習慣、運動習慣、すなわち、過食や運動不足を考慮すると、高脂血症の中でも血清トリグリセライド濃度すなわち血清の中性脂肪を調節する薬剤の開発が特に望まれている（以上、非特許文献１及び２参照）。
ハイショウソウ（敗醤草）はオミナエシ科のオトコエシ（Patrinia villosa）、オミナエシ（Patrinia scabiosaefolia）、アブラナ科のグンバイナズナ（Thlaspi arvense）の地上部又は全草を乾燥したものである。オミナエシ科のオトコエシ（Patrinia villosa）、オミナエシ（Patrinia scabiosaefolia）は眼病の薬として鎮痛、消炎等の作用を期待して用いられているが、アブラナ科のグンバイナズナ（Thlaspi arvense）の薬効については知られていない。また、ハイショウソウの中でも、オミナエシ科のオトコエシ及びオミナエシは、古来、食用に供されてきた植物でもある（以上、非特許文献３及び４参照）。
Considering dietary habits and exercise habits that have attracted particular attention in recent lifestyles, that is, overeating and lack of exercise, the development of drugs that regulate serum triglyceride levels, that is, serum triglycerides, is particularly important among hyperlipidemias. It is desired (see Non-Patent Documents 1 and 2 above).
Hishosou (defeated soy grass) is a product obtained by drying the above-ground parts or whole grasses of the family Opatidae (Patrinia villosa), Ominaeshi (Patrinia scabiosaefolia) and the Brassica family Thlaspi arvense. Otriae (Patrinia villosa) and Ominae (Patrinia scabiosaefolia) have been used as anti-ophthalmic drugs for analgesia and anti-inflammation, but the efficacy of the Brassicaceae Thlaspi arvense is known. Not. In addition, among the high-capacity Shrimp, Otochosushi and Ominae of the Ominae family are also plants that have been used for food since ancient times (see Non-Patent Documents 3 and 4 above).
本発明の目的は、長期間継続的に服用しても安全かつ効果的に高脂血症を予防又は改善できる薬剤を提供することである。 The objective of this invention is providing the chemical | medical agent which can prevent or improve hyperlipidemia safely and effectively, even if it takes continuously for a long period of time.
本発明者らは、上記課題を解決するために鋭意検討を行った結果、ハイショウソウの抽出物に高脂血症動物の血清トリグリセライド濃度及び血清遊離脂肪酸濃度の上昇を抑制する作用があることを見いだした。すなわち、ハイショウソウ抽出物の投与によって高脂血症を予防し、改善しうることを見いだした。 As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that the extract of Hibisou has an action of suppressing an increase in serum triglyceride concentration and serum free fatty acid concentration in hyperlipidemic animals. I found. That is, it has been found that administration of a high-shower extract can prevent and improve hyperlipidemia.
また、上記知見を得るために使用したob/obマウスには食欲調節と密接に関連するレプチンが欠損しており、過食による肥満・高血糖を発現することが知られている。そこで、ハイショウソウ抽出物の投与は、過食に起因する高脂血症に特に有効であると考えられる。 The ob / ob mice used to obtain the above findings are deficient in leptin, which is closely related to appetite regulation, and is known to develop obesity and hyperglycemia due to overeating. Therefore, it is considered that administration of the high-shower extract is particularly effective for hyperlipidemia caused by overeating.
かかる知見に基づく本発明の態様は次の（１）〜（４）である。
（１）ハイショウソウを含有することを特徴とする高脂血症の予防又は改善剤。
（２）ハイショウソウを含有することを特徴とする高グリセライド血症の予防又は改善剤。
（３）ハイショウソウを含有することを特徴とする高遊離脂肪酸血症の予防又は改善剤。
（４）ハイショウソウがオミナエシ科のオトコエシ又はオミナエシである前記予防又は改善剤。
Aspects of the present invention based on such findings are the following (1) to (4).
(1) A prophylactic or ameliorating agent for hyperlipidemia, characterized by containing Hishoso.
(2) A prophylactic or ameliorating agent for hyperglycerideemia, characterized by containing Hishoso.
(3) A preventive or ameliorating agent for hyperfree fatty acidemia, characterized by containing Hisho-so.
(4) The preventive or ameliorating agent as described above, wherein Hisho-sou is Otomeshi or Ominae.
本発明により、安全性が高く、長期間の服用に適した高脂血症の予防又は改善剤を提供することが可能となった。 The present invention makes it possible to provide an agent for preventing or improving hyperlipidemia that is highly safe and suitable for long-term use.
ハイショウソウとしてはオトコエシ、オミナエシ、グンバイナズナのいずれを用いることもできるが、高脂血症の予防又は改善の目的ではオミナエシ科に属するオトコエシ及びオミナエシが好ましく、オトコエシが特に好ましい。 As the high show, any one of Otokoeshi, Ominaeshi, and Gumbinazuna can be used, but for the purpose of prevention or improvement of hyperlipidemia, Otokoeshi and Ominaeshi belonging to the Ominae family are preferable, and Otokoeshi is particularly preferable.
ハイショウソウの有効投与量は、年齢、性別などを考慮して適宜増減できるが、通常成人で１日当たり原生薬換算量として１００mg〜５０gの範囲で用いることができ、好ましくは、５００mg〜３０gである。 The effective dose of Hisho-sou can be appropriately increased or decreased in consideration of age, sex, etc., but can be generally used in the range of 100 mg to 50 g as an active ingredient equivalent per day for an adult, preferably 500 mg to 30 g. is there.
ハイショウソウは粉末の他、エキスを使用することができる。ここでいうエキスとは、生薬抽出物、濃縮エキス、乾燥エキスなどいずれの形態も含む。エキスは抽出溶媒として水、アルコール（メタノール、エタノール、プロパノール、イソプロパノール、ブタノールなど）、酢酸エチル、アセトン、ヘキサン、それらの混液などを用いて通常の方法で製造することができる。 In addition to powder, high extract can use an extract. The extract here includes any form such as a herbal extract, a concentrated extract, and a dry extract. The extract can be produced by an ordinary method using water, alcohol (methanol, ethanol, propanol, isopropanol, butanol, etc.), ethyl acetate, acetone, hexane, a mixed solution thereof or the like as an extraction solvent.
ハイショウソウの中でも、特にオミナエシ科に属するオトコエシ及びオミナエシは、江戸時代に編纂された食糧書である『救荒食糧かてもの』にも収載され、長期間に渡り食用に供されてきたことから、その安全性に問題がないことが確認されている。そのため、連続投与や連続摂取も可能である。 Among the high show, especially Otokoeshi and Ominae, which belong to the Ominae family, are listed in the food book edited by the Edo period, and have been used for food for a long time. It has been confirmed that there is no problem with its safety. Therefore, continuous administration and continuous intake are possible.
ハイショウソウは、高脂血症、高グリセライド血症、高遊離脂肪酸血症の予防又は改善に使用できる。高遊離酸脂肪血症とは、血清中の遊離脂肪酸の濃度が上昇することにより惹起される病態で、具体的には、動脈硬化症やインスリン抵抗性を惹起するといわれている。 Hishosou can be used to prevent or ameliorate hyperlipidemia, hyperglycerideemia, and high free fatty acidemia. High free acid lipolipidemia is a pathological condition caused by an increase in the concentration of free fatty acid in serum, and specifically, it is said to cause arteriosclerosis and insulin resistance.
本発明の効果を損なわない質的及び量的範囲で、ビタミン、キサンチン誘導体、生薬、天然物、賦形剤、ｐＨ調節剤、清涼化剤、懸濁化剤、消泡剤、粘稠剤、溶解補助剤、崩壊剤、結合剤、滑沢剤、抗酸化剤、コーティング剤、着色剤、矯味矯臭剤、界面活性剤、可塑剤、香料などを混合して常法により、液剤、錠剤、顆粒剤、散剤、カプセル剤、ドライシロップ剤、チュアブル錠、経粘膜剤などの経口又は非経口製剤とすることができる。 Vitamin, xanthine derivatives, crude drugs, natural products, excipients, pH adjusters, cooling agents, suspending agents, antifoaming agents, viscous agents, within the qualitative and quantitative ranges that do not impair the effects of the present invention Solubilizers, disintegrants, binders, lubricants, antioxidants, coating agents, colorants, flavoring agents, surfactants, plasticizers, fragrances, etc. are mixed in a conventional manner to prepare liquids, tablets, granules Oral or parenteral preparations such as preparations, powders, capsules, dry syrups, chewable tablets, and transmucosal agents.
以下に実施例及び試験例を挙げ、本発明をさらに具体的に説明する。 Hereinafter, the present invention will be described more specifically with reference to examples and test examples.
実施例１
オトコエシを細切後、１０倍量の５０％エタノールを加え、約８０℃で加熱抽出し、濾過後減圧下でエタノールを留去し、さらに、濃縮を行うことにより、エキスを得た。
Example 1
After chopping the mango shrimp, 10 times the amount of 50% ethanol was added, extracted by heating at about 80 ° C., filtered and the ethanol was distilled off under reduced pressure, and further concentrated to obtain an extract.
実施例２
オミナエシを細切後、１０倍量の５０％エタノールを加え、約８０℃で加熱抽出し、濾過後減圧下でエタノールを留去し、さらに、濃縮を行うことにより、エキスを得た。
Example 2
After mincing the minced shrimp, 10 times the amount of 50% ethanol was added, extracted by heating at about 80 ° C., filtered and the ethanol was distilled off under reduced pressure, followed by concentration to obtain an extract.
実施例３
グンバイナズナを細切後、１０倍量の５０％エタノールを加え、約８０℃で加熱抽出し、濾過後減圧下でエタノールを留去し、さらに、濃縮を行うことにより、エキスを得た。
Example 3
After cutting the gum binas, 10 times the amount of 50% ethanol was added, and the mixture was extracted by heating at about 80 ° C. After filtration, the ethanol was distilled off under reduced pressure, and further concentrated to obtain an extract.
試験例１
実験にはob/ob系雄性マウス［6週齢、チャールスリバー（株）］を用いた。実験に使用するまで約１週間の予備飼育を行った後、実施例１で製造したハイショウソウエキスを投与する群及び対照群の２群に分けた。ハイショウソウエキスは300 mg/kg（乾燥エキスとして）の用量で１日１回、16−17時の間に経口投与した。8週間飼育した後、採血し、血清を分離した。なお，正常群にはC57BL/6Jマウスを用い、ob/obマウスの対照群と同様の処置を施した。
Test example 1
Ob / ob male mice [6 weeks old, Charles River Co., Ltd.] were used in the experiment. After preliminary breeding for about one week until use in the experiment, it was divided into two groups: a group to which the high-brush extract produced in Example 1 was administered and a control group. Hisho-so extract was orally administered at a dose of 300 mg / kg (as a dry extract) once a day between 16-17. After raising for 8 weeks, blood was collected and serum was separated. In the normal group, C57BL / 6J mice were used, and the same treatment as in the ob / ob mouse control group was performed.
得られた血清中のトリグリセライド（ＴＧと略記）及び遊離脂肪酸（ＮＥＦＡと略記）濃度は和光純薬工業製の各測定キット（トリグリセライドＧ−テストワコー、ＮＥＦＡ Ｃ−テストワコー）を用いて定量した。 Triglyceride (abbreviated as TG) and free fatty acid (abbreviated as NEFA) concentrations in the obtained serum were quantified using each measurement kit (Triglyceride G-Test Wako, NEFA C-Test Wako) manufactured by Wako Pure Chemical Industries.
表１、図１及び２に示したごとく、ob/obマウスの血清TG濃度及び血清NEFA濃度は正常マウスに比較して有意に増加し、高脂血症状態が観察された。ob/obマウスにハイショウソウエキスを３００ｍｇ／ｋｇ（乾燥エキス重量として）の用量で、１日１回８週間経口投与すると血清脂質の上昇が有意に抑制され、高脂血症の改善作用が認められた。 As shown in Table 1 and FIGS. 1 and 2, the serum TG concentration and serum NEFA concentration of ob / ob mice were significantly increased compared to normal mice, and a hyperlipidemic state was observed. When administered orally to ob / ob mice at a dose of 300 mg / kg (as a dry extract weight) once a day for 8 weeks, the increase in serum lipids is significantly suppressed, and hyperlipidemia is improved. Admitted.
以上の結果から、ハイショウソウを配合することにより、高脂血症に対して予防又は改善作用を有することが明らかになった。 From the above results, it has been clarified that, by blending Hishoso, it has a preventive or ameliorating action against hyperlipidemia.
これまでの検討により、ハイショウソウは、血清中のトリグリセライド濃度や遊離脂肪酸濃度を低下させるだけでなく、高くならないようにする作用も有しており、高脂血症の治療剤としてはもちろん予防剤としても有用である。 As a result of studies so far, Hisho-so has the effect of not only lowering the triglyceride concentration and free fatty acid concentration in serum, but also preventing it from becoming high, and of course it is a preventive agent for the treatment of hyperlipidemia. It is also useful as an agent.
また、レプチンが欠損したob/obマウスによってその作用が確認されていることから、過食に起因する高脂血症の予防及び治療に特に有効であると考えられ、ハイショウソウを含有した医薬品、医薬部外品、食品を継続的に投与・摂取することによって、健常人であれば食べ過ぎても高脂血症になりにくい状態を維持でき、すでに高脂血症に罹患している人では食物摂取量を極端に制限することなく高脂血症の治療ができるというメリットがある。 In addition, since its action has been confirmed by ob / ob mice lacking leptin, it is considered to be particularly effective in the prevention and treatment of hyperlipidemia caused by overeating, By continually administering and taking quasi-drugs and foods, a healthy person can maintain a state that is unlikely to become hyperlipidemic even if they eat too much. There is an advantage that hyperlipidemia can be treated without extremely restricting food intake.
よって、高脂血症の予防及び改善に有効で、長期間服用しても安全な医薬品、医薬部外品及び食品の開発への応用が期待される。例えば、ハイショウソウエキスをお茶に配合し、中性脂肪が高く、高脂血症が懸念される人のための健康食品の提供などが考えられる。 Therefore, it is effective for the prevention and improvement of hyperlipidemia, and is expected to be applied to the development of pharmaceuticals, quasi-drugs and foods that are safe for long-term use. For example, it can be considered to provide a health food for a person who is high in triglyceride and is concerned about hyperlipidemia by blending a high-shower extract into tea.
Claims (4)
The prophylactic or ameliorating agent according to any one of claims 1 to 3, wherein the high-capacity is Otoeshi or Ominae in the family Ominae.
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| JP2005058269A JP2005289984A (en) | 2004-03-10 | 2005-03-03 | Hyperlipidemia ameliorating agent comprising patrinia scabiosaefolia |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101007088B1 (en) * | 2005-12-30 | 2011-01-10 | (주)아모레퍼시픽 | Composition for promoting oxidation of fatty acid comprising extract of crude drugs and native plants |
| CN103636862A (en) * | 2013-11-30 | 2014-03-19 | 黄山市百倍岭食品有限责任公司 | Patrima villosa tea and preparation method thereof |
| CN111574362A (en) * | 2020-06-22 | 2020-08-25 | 沈阳市第七人民医院 | Fatty acid compound |
-
2005
- 2005-03-03 JP JP2005058269A patent/JP2005289984A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101007088B1 (en) * | 2005-12-30 | 2011-01-10 | (주)아모레퍼시픽 | Composition for promoting oxidation of fatty acid comprising extract of crude drugs and native plants |
| CN103636862A (en) * | 2013-11-30 | 2014-03-19 | 黄山市百倍岭食品有限责任公司 | Patrima villosa tea and preparation method thereof |
| CN111574362A (en) * | 2020-06-22 | 2020-08-25 | 沈阳市第七人民医院 | Fatty acid compound |
| CN111574362B (en) * | 2020-06-22 | 2022-09-16 | 沈阳市第七人民医院 | Fatty acid compound |
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