JP3689099B1 - Lipase inhibitor, method for producing the same, and anti-obesity composition - Google Patents
Lipase inhibitor, method for producing the same, and anti-obesity composition Download PDFInfo
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- JP3689099B1 JP3689099B1 JP2004244503A JP2004244503A JP3689099B1 JP 3689099 B1 JP3689099 B1 JP 3689099B1 JP 2004244503 A JP2004244503 A JP 2004244503A JP 2004244503 A JP2004244503 A JP 2004244503A JP 3689099 B1 JP3689099 B1 JP 3689099B1
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Abstract
【課題】安全で効果が高く、日常的に継続摂取可能なリパーゼ阻害剤、その製造方法、及び抗肥満症用組成物を提供する。
【解決手段】 水溶性成分を除去したケール又はその乾燥物である前処理ケールの、低級アルコール抽出物を有効成分とするリパーゼ阻害剤。
ケール又はその乾燥物を水に浸漬し、水溶性成分と残渣とに分配する前処理工程と、
前記残渣を低級アルコールに浸漬し、有効成分を低級アルコールで抽出するアルコール抽出工程とを備えていることを特徴とするリパーゼ阻害剤の製造方法。
前記製造方法において、アルコール抽出工程が、エタノール濃度が60〜80容量%のエタノールにより加熱抽出する工程であることが好適である。
前記リパーゼ阻害剤を含む抗肥満症用組成物。
The present invention provides a lipase inhibitor that is safe, highly effective, and can be continuously taken on a daily basis, a method for producing the same, and a composition for anti-obesity.
A lipase inhibitor comprising as an active ingredient a lower alcohol extract of a pretreated kale which is a kale from which water-soluble components have been removed or a dried product thereof.
A pretreatment step of immersing kale or a dried product thereof in water and distributing it to water-soluble components and residues;
A method for producing a lipase inhibitor, comprising: an alcohol extraction step of immersing the residue in a lower alcohol and extracting an active ingredient with the lower alcohol.
In the production method, it is preferable that the alcohol extraction step is a step of performing heat extraction with ethanol having an ethanol concentration of 60 to 80% by volume.
An anti-obesity composition comprising the lipase inhibitor.
Description
本発明はリパーゼ阻害剤、その製造方法、及び抗肥満症用組成物、特にケール成分を含むリパーゼ阻害剤に関する。 The present invention relates to a lipase inhibitor, a method for producing the same, and an anti-obesity composition, particularly a lipase inhibitor containing a kale component.
経口摂取された脂質は、膵臓より分泌される消化酵素リパーゼにより加水分解され、体内へ吸収される。脂質はエネルギーが高く、近年摂取量が増加する傾向にあるため、これが肥満を引き起こす一因となっている。肥満は、高血圧、耐糖能異常、高脂血症等を合併しやすく、虚血性心疾患、脳卒中、糖尿病、動脈硬化症、脂肪肝、胆石症、腎臓障害等の発症要因であるとされている。 Lipids taken orally are hydrolyzed by digestive enzyme lipase secreted from the pancreas and absorbed into the body. Lipids are high in energy and tend to increase in recent years, which contributes to obesity. Obesity is likely to be associated with hypertension, impaired glucose tolerance, hyperlipidemia, etc., and is considered to be a cause of ischemic heart disease, stroke, diabetes, arteriosclerosis, fatty liver, cholelithiasis, kidney disorder, etc. .
そこで脂質の吸収を抑制するべく、リパーゼの活性阻害機能を有するリパーゼ阻害剤が種々開発されており、これまで各種植物抽出物、例えば各種香辛料の抽出物(特開2001−120237号公報)、ヤーコン抽出物(特開2001−299272号公報)、芍薬の花の抽出物(特開2002−53484号公報)、マテ葉抽出物(特開2004−161644号公報)等がリパーゼ阻害剤として開示されている。また特開平03−219872号公報では、ピーマン、かぼちゃ等の水抽出物が、リパーゼ阻害剤として有効であることも開示されている。
しかしながら、前記技術においては、効果が低かったり、有効摂取量が非常に多量であったり、あるいは原料が入手しにくく高価であったりして、日常的に継続摂取することは実質的に不可能であった。このように充分満足できるものは未だ開発されていなかった。
本発明は前記従来技術の課題に鑑みなされたものであり、その目的は、安全で効果が高く、日常的に継続摂取可能なリパーゼ阻害剤、その製造方法、及び抗肥満症用組成物を提供することにある。
However, in the above technique, the effect is low, the effective intake is very large, or the raw material is difficult to obtain and is expensive, and it is practically impossible to continuously ingest. there were. Such a satisfactory product has not been developed yet.
The present invention has been made in view of the above-mentioned problems of the prior art, and its object is to provide a lipase inhibitor that is safe, highly effective, and can be continuously taken on a daily basis, a method for producing the same, and a composition for anti-obesity. There is to do.
前記目的を達成するために本発明者等が検討を行った結果、アブラナ科植物のケールがリパーゼ阻害剤として働き、特に水溶性成分を除去したケールの低級アルコール抽出物が非常に有効であることを見出し、本発明を完成するに至った。
本発明の第一の主題は、水溶性成分を除去したケール又はその乾燥物である前処理ケールの、低級アルコール抽出物を有効成分とするリパーゼ阻害剤である。
As a result of studies conducted by the present inventors in order to achieve the above object, the cruciferous plant kale acts as a lipase inhibitor, and in particular, a lower alcohol extract of kale from which water-soluble components have been removed is very effective. As a result, the present invention has been completed.
The first subject of the present invention is a lipase inhibitor containing as an active ingredient a lower alcohol extract of a pretreated kale which is a kale from which water-soluble components have been removed or a dried product thereof.
本発明の第二の主題は、ケール又はその乾燥物を水に浸漬し、水溶性成分と残渣とに分配する前処理工程と、
前記残渣を低級アルコールに浸漬し、有効成分を低級アルコールで抽出するアルコール抽出工程とを備えていることを特徴とするリパーゼ阻害剤の製造方法である。
前記製造方法において、アルコール抽出工程が、エタノール濃度が60〜80容量%のエタノールにより加熱抽出する工程であることが好適である。
本発明の第三の主題は、前記リパーゼ阻害剤を含む抗肥満症用組成物である。
The second subject of the present invention is a pretreatment step in which kale or a dried product thereof is immersed in water and distributed into water-soluble components and residues;
An alcohol extraction step of immersing the residue in a lower alcohol and extracting an active ingredient with the lower alcohol, and a method for producing a lipase inhibitor.
In the production method, it is preferable that the alcohol extraction step is a step of performing heat extraction with ethanol having an ethanol concentration of 60 to 80% by volume.
The third subject of the present invention is an anti-obesity composition comprising the lipase inhibitor.
本発明によれば、水溶性成分を除去したケールを低級アルコールで抽出することにより、安全で効果が高く、日常的に継続摂取可能なリパーゼ阻害剤、その製造方法、及び抗肥満症用組成物を得ることができる。 According to the present invention, by extracting kale from which water-soluble components have been removed with a lower alcohol, a safe, highly effective lipase inhibitor that can be continuously ingested daily, a method for producing the same, and an anti-obesity composition Can be obtained.
本発明で使用されるケール(Brassica oleracea var.acephala)は、南ヨーロッパ原産の野菜であり、アブラナ科の植物でキャベツの原種といわれている。キッチンケール、マローケール、ブッシュケール、ツリーケール、コラード、緑葉カンラン等の種類がある。
ケールは、適宜、生葉を用いることも乾燥物を用いることもできる。
本発明のリパーゼ阻害剤は、水溶性成分を除去したケール又はその乾燥物である前処理ケールの、低級アルコール抽出物を有効成分とすることを特徴とする。
本発明のリパーゼ阻害剤の製造方法は、ケール又はその乾燥物を水に浸漬し、水溶性成分と残渣とに分配する前処理工程と、前記残渣を低級アルコールに浸漬し、有効成分を低級アルコールで抽出するアルコール抽出工程とを備えていることを特徴とする。
前処理工程に使用するの水の量は特に限定されないが、ケール乾燥物に対して、質量で1〜50倍、好ましくは10倍程度が好ましい。1倍未満では水溶性成分が十分に除去できないことがあり、50倍を超えると作業性に劣る。
Kale (Brassica oleracea var. Acephala) used in the present invention is a vegetable native to Southern Europe, and is said to be the original species of cabbage in the cruciferous plant. There are kitchen kale, mallow kale, bush kale, tree kale, collard, green leaf kanran and so on.
As the kale, fresh leaves or dried products can be used as appropriate.
The lipase inhibitor of the present invention is characterized in that a lower alcohol extract of a kale from which water-soluble components have been removed or a pre-treated kale that is a dried product thereof is used as an active ingredient.
The method for producing a lipase inhibitor of the present invention comprises a pretreatment step in which kale or a dried product thereof is immersed in water and distributed to a water-soluble component and a residue, the residue is immersed in a lower alcohol, and an active ingredient is a lower alcohol. And an alcohol extraction step of extracting at the step.
The amount of water used in the pretreatment step is not particularly limited, but is preferably about 1 to 50 times, preferably about 10 times, by mass with respect to the dried kale. If it is less than 1 time, water-soluble components may not be sufficiently removed, and if it exceeds 50 times, workability is inferior.
アルコール抽出工程にて用いられる低級アルコールとしては、例えば、エタノール、プロパノール、イソプロパノール、イソブチルアルコール、t-ブチルアルコール等が挙げられるが、エタノール、特にエタノール濃度が60〜80容量%のエタノールを用いることが好ましい。
有効成分を抽出する際の低級アルコールの量は特に限定されないが、原料のケール乾燥物に対して、質量で1〜50倍、好ましくは10倍程度が好ましい。1倍未満では有効成分が十分に抽出されない恐れがあり、50倍を超えると多量のアルコールを蒸発させる必要があり、作業性に劣る。
例えば、ケールの葉の乾燥粉末100gに水1Lを加え1時間加熱還流し、ろ過後その残渣を乾燥させ、80容量%エタノール1Lを加え、1時間加熱還流し、低級アルコール抽出液を得る。
Examples of the lower alcohol used in the alcohol extraction step include ethanol, propanol, isopropanol, isobutyl alcohol, t-butyl alcohol, and the like. Ethanol, particularly ethanol having an ethanol concentration of 60 to 80% by volume, is used. preferable.
The amount of the lower alcohol when extracting the active ingredient is not particularly limited, but is preferably about 1 to 50 times, preferably about 10 times, by mass with respect to the dried kale material. If it is less than 1 time, the active ingredient may not be sufficiently extracted. If it exceeds 50 times, it is necessary to evaporate a large amount of alcohol, resulting in poor workability.
For example, 1 L of water is added to 100 g of dry powder of kale and heated under reflux for 1 hour. After filtration, the residue is dried, 1 L of 80 vol% ethanol is added and heated under reflux for 1 hour to obtain a lower alcohol extract.
本発明のリパーゼ阻害剤は、優れたリパーゼの活性阻害作用を有し、且つ安全性が非常に高いため、日常的に摂取することにより、脂質の体内吸収を抑制して、肥満症やそれに伴う疾患を予防・改善することができる。 The lipase inhibitor of the present invention has an excellent lipase activity inhibitory action and is very safe. Therefore, by taking it on a daily basis, it suppresses the absorption of lipids in the body, and obesity and accompanying it. Diseases can be prevented and ameliorated.
本発明のリパーゼ阻害剤は、錠剤、カプセル剤、顆粒剤、散剤等の固形剤;溶液剤、懸濁剤、乳剤等の液剤;凍結乾燥製剤等の形態にし、摂取することができる。これらの製剤は常套手段により調製することができる。また必要に応じて、例えば、グルコース、乳糖、ショ糖、澱粉、マンニトール、デキストリン、脂肪酸グリセリド、ポリエチレングルコール、ヒドロキシエチルデンプン、エチレングリコール、ポリオキシエチレンソルビタン脂肪酸エステル、アミノ酸、ゼラチン、ビタミン類、アルブミン、水、生理食塩水、安定化剤、湿潤剤、乳化剤、結合剤等を添加することができる。
また、本発明のリパーゼ阻害剤は、種々の食品、例えば油脂類(サラダ油、バター、マーガリン、ラード)、調味料、クリーム類、乳製品、肉類、魚介類、食肉加工食品(ハム、ソーセージ等)、水産加工食品(かまぼこ、ちくわ等)、卵類、菓子類、飲料類、パン、健康食品、加工食品等に添加して、摂取することもできる。
The lipase inhibitor of the present invention can be ingested in the form of a solid agent such as a tablet, capsule, granule or powder; a liquid agent such as a solution, suspension or emulsion; a lyophilized preparation. These formulations can be prepared by conventional means. If necessary, for example, glucose, lactose, sucrose, starch, mannitol, dextrin, fatty acid glyceride, polyethylene glycol, hydroxyethyl starch, ethylene glycol, polyoxyethylene sorbitan fatty acid ester, amino acid, gelatin, vitamins, albumin Water, physiological saline, stabilizer, wetting agent, emulsifier, binder and the like can be added.
Further, the lipase inhibitor of the present invention can be used for various foods such as fats and oils (salad oil, butter, margarine, lard), seasonings, creams, dairy products, meats, seafood, processed meat foods (ham, sausage, etc.) It can also be ingested by adding it to processed fishery products (kamaboko, chikuwa, etc.), eggs, confectionery, beverages, bread, health foods, processed foods and the like.
本発明のリパーゼ阻害剤の有効投与量は、患者の年齢、体重、投与時間、形態等により、適宜選択・決定されるが、有効成分が凝縮されているため、少量で済み、無理なく継続的に摂取できる。また1日に数回に分けて摂取してもよく、特に食事の前後1時間以内に摂取することが好ましい。
なお、特開2004−43375号公報では、ケール又その抽出物が、NPY受容体あるいはMCH受容体に拮抗作用を有し、食欲の異常亢進を抑制することが報告されている。しかしながら、リパーゼ活性を阻害し、摂取された脂質の消化吸収を抑制する作用については記載されていない。さらに上記技術においては、水抽出により水溶性成分を除去することなく、直接エタノール抽出を行っているため、十分な肥満予防・治療効果を得るためには、投与量が多くなり、事実上継続摂取が不可能であった。
The effective dose of the lipase inhibitor of the present invention is appropriately selected and determined according to the patient's age, weight, administration time, form, etc. However, since the active ingredient is condensed, a small amount can be used and it can be continued without difficulty. Can be consumed. In addition, it may be taken in several times a day, and in particular, it is preferably taken within 1 hour before and after a meal.
JP-A-2004-43375 reports that kale or an extract thereof has an antagonistic action on the NPY receptor or MCH receptor and suppresses an abnormal increase in appetite. However, it does not describe the action of inhibiting lipase activity and suppressing digestive absorption of ingested lipids. Furthermore, in the above technique, since ethanol extraction is directly performed without removing water-soluble components by water extraction, in order to obtain a sufficient obesity prevention / treatment effect, the dose is increased, and it is practically a continuous intake. Was impossible.
さらに本発明のリパーゼ阻害剤は、脂質を含む飲食品や皮膚外用剤中に添加すれば、微生物が産生するリパーゼによる脂質の分解を抑制し、変敗臭等の脂質の劣化を抑制することができる。また本発明のリパーゼ阻害剤は、皮膚上において、皮膚常在菌が産生するリパーゼによる皮脂の分解を抑制し、体臭や皮膚疾患を抑制することができる。
以下、実施例を挙げて本発明をさらに詳しく説明する。本発明はこれらの実施例により限定されるものではない。配合量については特に断りのない限り質量%を示す。
Furthermore, if the lipase inhibitor of the present invention is added to a food or drink containing lipids or an external preparation for skin, it can suppress degradation of lipids by lipase produced by microorganisms, and can suppress deterioration of lipids such as deteriorated odor. it can. Moreover, the lipase inhibitor of this invention can suppress decomposition | disassembly of the sebum by the lipase which a skin resident bacteria produces on skin, and can suppress a body odor and a skin disease.
Hereinafter, the present invention will be described in more detail with reference to examples. The present invention is not limited to these examples. Unless otherwise specified, the blending amount indicates mass%.
初めに、下記予備試料1〜7を調製した(図1)。
予備試料1 ケールの葉を凍結乾燥させ粉砕したケール乾燥粉末(14g)。
予備試料2 ケール乾燥粉末14gを、水140mLで1時間加熱抽出(還流)した抽出液。
予備試料3 試験例2の抽出液のエタノール沈殿物を乾燥させたもの(0.7g)
予備試料4 ケール乾燥粉末14gを、水140mLで1時間加熱抽出(還流)し、その残渣を乾燥させたもの(6.6g)。
予備試料5 試験例4の乾燥残渣6.6gを、80容量%エタノール140mLで1時間加熱抽出(還流)し、その残渣を乾燥させたもの(5.8g)。
予備試料6 試験例4の乾燥残渣6.6gを、80容量%エタノール140mLで1時間加熱抽出(還流)した抽出液。
予備試料7 ケール乾燥粉末14gを、80容量%エタノール140mLで1時間加熱抽出(100℃)した抽出液。
First, the following
Preliminary Sample 6 An extract obtained by heating (refluxing) 6.6 g of the dry residue of Test Example 4 with 140 mL of 80% ethanol by volume for 1 hour.
<リパーゼ阻害試験>
上記試料を用いて、リパーゼ阻害試験を行なった。
(各試験例の試料の調製)
試験例1:予備試料1に水120mLを加えた。
試験例2:予備試料2をロータリーエバポレーターにかけ、水を適宜除去し120mLにした。
試験例3:予備試料3に水120mLを加えた。
試験例4:予備試料4に水120mLを加えた。
試験例5:予備試料5に水120mLを加えた。
試験例6:予備試料6をロータリーエバポレーターにかけエタノールを除去し、水120mLを加えた。
試験例7:予備試料7をロータリーエバポレーターにかけエタノールを除去し、水120mLを加えた。
(試験方法)
試験管に試料0.1mL、McIlvain緩衝液0.7mL、トリオレイン0.1mLを入れよく攪拌し、豚膵リパーゼ0.1mLを加え、37℃で1時間振とうした。
エタノール2mLを加え反応を停止後、発色試液を加え、550nmで吸光度を測定し、下記式より血清遊離脂肪酸濃度を求めた。
また下記のように阻害率を計算した(n=3)。
血清遊離脂肪酸濃度(mEq/L)=S/(Std−BI)
(S:検体の吸光度、Std:標準、BI:試薬盲検)
リパーゼ阻害率(%)={(ブランクの値−各試料の値)/ブランクの値}×100
<Lipase inhibition test>
A lipase inhibition test was performed using the above sample.
(Preparation of samples for each test example)
Test Example 1: 120 mL of water was added to the
Test Example 2:
Test Example 3 120 mL of water was added to the
Test Example 4 120 mL of water was added to the
Test Example 5: 120 mL of water was added to the
Test Example 6: Preliminary sample 6 was subjected to a rotary evaporator to remove ethanol, and 120 mL of water was added.
Test Example 7:
(Test method)
A sample tube (0.1 mL), McIlvain buffer solution (0.7 mL), and triolein (0.1 mL) were added and stirred well. Porcine pancreatic lipase (0.1 mL) was added, and the mixture was shaken at 37 ° C. for 1 hour.
After 2 mL of ethanol was added to stop the reaction, a coloring reagent was added, the absorbance was measured at 550 nm, and the serum free fatty acid concentration was determined from the following formula.
The inhibition rate was calculated as follows (n = 3).
Serum free fatty acid concentration (mEq / L) = S / (Std-BI)
(S: sample absorbance, Std: standard, BI: reagent blind)
Lipase inhibition rate (%) = {(blank value−each sample value) / blank value} × 100
結果を表1に示す。
(表1)
試 験 例
1 2 3 4 5 6 7
リパーゼ阻害率(%)
73.7 47.0 0 0 0 78.9 78.0
試験例6は、本発明のリパーゼ阻害剤に相当する。
試験例6は、試験例4の収量と試験例5の収量の差から計算すると、ケール固形分0.8gとなる。これは元のケール乾燥粉末の5.5質量%に相当する。
リパーゼ阻害率を比較すると、驚くべきことに試験例6は量が少ないにも関わらず、試験例1のケール乾燥粉末を上回る値であった。
また、試験例6と試験例7とを比較すると、直接エタノールで抽出した試験例7ではケール固形分が4.7gであるのに対し、水溶性成分除去後にエタノール抽出した試験例6ではケール固形分が0.8gであり、量は1/6程度であるにもかかわらず、同等のリパーゼ阻害効果が得られることが確認された。試験例7には水溶性成分が含まれるが、試験例6では水溶性成分は除去されている。このことから本発明のリパーゼ阻害剤による効果は、過剰な栄養素の吸収を抑制するとされている水溶性食物繊維に由来する効果ではないことがわかる。
このように、本発明のリパーゼ阻害剤は、水溶性食物繊維等の水溶性成分を除去したケールの低級アルコール抽出物であるにもかかわらず、高いリパーゼ阻害効果が発揮され、少量で優れたリパーゼ阻害効果を有することがわかった。
試験例2,6,7のIR分析結果をそれぞれ図2〜4に、試験例2,6,7のLC分析結果をそれぞれ図5〜7に示す。
The results are shown in Table 1.
(Table 1)
Test example
1 2 3 4 5 6 7
Lipase inhibition rate (%)
73.7 47.0 0 0 0 78.9 78.0
Test Example 6 corresponds to the lipase inhibitor of the present invention.
When calculated from the difference between the yield of Test Example 4 and the yield of Test Example 5, Test Example 6 has a kale solid content of 0.8 g. This corresponds to 5.5% by weight of the original kale dry powder.
Comparing the lipase inhibition rate, surprisingly, the value of Test Example 6 was higher than that of Test Example 1 despite the small amount.
Further, when Test Example 6 and Test Example 7 are compared, in Test Example 7 extracted directly with ethanol, the kale solid content is 4.7 g, whereas in Test Example 6 extracted with ethanol after removing water-soluble components, Kale solids are obtained. It was confirmed that the equivalent lipase inhibitory effect was obtained even though the amount was 0.8 g and the amount was about 1/6. Test Example 7 includes a water-soluble component, but in Test Example 6, the water-soluble component is removed. From this, it can be seen that the effect of the lipase inhibitor of the present invention is not an effect derived from water-soluble dietary fiber that is supposed to suppress absorption of excess nutrients.
As described above, the lipase inhibitor of the present invention exhibits a high lipase inhibitory effect even though it is a lower alcohol extract of kale from which water-soluble components such as water-soluble dietary fiber have been removed. It was found to have an inhibitory effect.
The IR analysis results of Test Examples 2, 6, and 7 are shown in FIGS. 2 to 4, respectively, and the LC analysis results of Test Examples 2, 6, and 7 are shown in FIGS.
ケール抽出物の濃度と、リパーゼ阻害活性との関係を調べた。
(試料の調製)
ケール乾燥粉末100gを水1Lで加熱抽出(還流)し、ろ過後得られた乾燥残渣を80容量%エタノール1Lで1時間加熱抽出(還流)し、該抽出物を80%エタノールで固形分濃度2.6、5.2、10.4、20.9(mg/mL)となるように調製し、これらの試料を用いて上記と同様にして、各濃度におけるリパーゼ阻害効果を検討した。結果を以下の表2に示す。
The relationship between the concentration of Kale extract and lipase inhibitory activity was examined.
(Sample preparation)
100 g of dry kale powder was heated and extracted (refluxed) with 1 L of water, and the dried residue obtained after filtration was heated (refluxed) with 1 L of 80 vol% ethanol for 1 hour, and the extract was washed with 80% ethanol to obtain a solid concentration of 2.6. , 5.2, 10.4, 20.9 (mg / mL), and using these samples, the lipase inhibitory effect at each concentration was examined in the same manner as described above. The results are shown in Table 2 below.
(表2)
濃度(mg/mL) 1.6 3.2 6.3 12.6
リパーゼ阻害活性(%) 37.8 50.5 88.8 92.0
濃度依存的にリパーゼ阻害効果が高くなることが確認された。
(Table 2)
Concentration (mg / mL) 1.6 3.2 6.3 12.6
Lipase inhibitory activity (%) 37.8 50.5 88.8 92.0
It was confirmed that the lipase inhibitory effect was increased in a concentration-dependent manner.
<ラット試験>
次に、上記各試料をラットに投与し、抗肥満症効果を試験した。
(1)試験ラットの飼育、及び試料の投与方法
予備飼育(6〜7週齢)
Zucker-fattyラットは生後4週齢頃より体重が急速に増加し、外観上も同腹の正常仔と区別が付くほどの肥満状態を呈し始め、加齢に従い正常個体との体重差は拡大する。このためZucker-fattyラットは肥満症のモデルとして有用である。
遺伝形式は常染色体性の単純劣性遺伝様式を取り、病因遺伝子をホモに持つ固体のみが肥満を呈し(Zucker-fattyラット)、ヘテロ接合体及び野生型は肥満を示さない(Zucker-leanラット)。
日本チャールスリバー(株)より購入した6週齢の雄性Zucker-fattyラット、及び雄性Zucker-leanラットを、室温22±1℃、湿度60±10%に調節された飼育室において、白色蛍光灯で1日12時間(7〜19時明期)の光調節を行い、飼料及び水道水を自由摂取させ1週間予備飼育した。
予備飼育後、各個体の体重測定を行い、Zucker-fattyラットを、体重の平均値がほぼ等しくなるように1群5頭のA〜H群に分類した。またZucker-leanラット2頭をI群とした。
<Rat test>
Next, each of the above samples was administered to rats to test the anti-obesity effect.
(1) Rearing of test rats and sample administration method Preliminary rearing (6-7 weeks old)
Zucker-fatty rats gain weight rapidly from around the age of 4 weeks of age, begin to appear in an obese state that can be distinguished from normal litters in appearance, and the weight difference from normal individuals increases with age. For this reason, Zucker-fatty rats are useful as models of obesity.
Inheritance is an autosomal simple recessive inheritance mode, only individuals with homologous pathogenic genes exhibit obesity (Zucker-fatty rats), heterozygotes and wild type do not exhibit obesity (Zucker-lean rats) .
Six-week-old male Zucker-fatty rats and male Zucker-lean rats purchased from Nippon Charles River Co., Ltd. were bred with white fluorescent light in a breeding room adjusted to
After the preliminary breeding, the weight of each individual was measured, and the Zucker-fatty rats were classified into groups A to H of 5 per group so that the average values of body weights were almost equal. Two Zucker-lean rats were classified as Group I.
試料投与方法(7〜17週齢)
下記の要領で、各群のラットに試料投与を行い、さらに10週間、17週齢まで飼育した。飼料と水道水を各群とも自由摂取させた。飼育室の環境は、温度22±1℃、湿度60±10%、白色蛍光灯で1日12時間の採光下(7〜19時明期)とした。
各試料はすべて経口投与とし、毎日午前10時より施行し、投与後は滅菌水を自由摂取させた。なお、どの群においても試料投与により、飼料摂取量は変化しなかった。
Sample administration method (7-17 weeks old)
Samples were administered to each group of rats in the following manner and further reared for 10 weeks to 17 weeks of age. Feed and tap water were freely given to each group. The environment of the breeding room was a temperature of 22 ± 1 ° C., a humidity of 60 ± 10%, and white fluorescent lighting for 12 hours a day (7-19 o'clock light period).
All samples were administered orally and were administered daily from 10:00 am. After administration, sterilized water was ingested freely. In any group, the feed intake did not change with sample administration.
Zucker-fattyラット
A群:1日に体重1kg当たり試験例1の試料を2mL投与する。
B群:1日に体重1kg当たり試験例2の試料を2mL投与する。
C群:1日に体重1kg当たり試験例3の試料を2mL投与する。
D群:1日に体重1kg当たり試験例4の試料を2mL投与する。
E群:1日に体重1kg当たり試験例5の試料を2mL投与する。
F群:1日に体重1kg当たり試験例6の試料を2mL投与する。
G群:無投与
Zucker-leanラット
H群:無投与
Zucker-fatty rat group A: 2 mL of the sample of Test Example 1 is administered per kg of body weight per day.
Group B: 2 mL of the sample of Test Example 2 is administered per kg of body weight per day.
Group C: 2 mL of the sample of Test Example 3 is administered per kg of body weight per day.
Group D: 2 mL of the sample of Test Example 4 is administered per kg of body weight per day.
Group E: 2 mL of the sample of Test Example 5 is administered per kg of body weight per day.
Group F: 2 mL of the sample of Test Example 6 is administered per kg of body weight per day.
Group G: No administration
Zucker-lean rat group H: No administration
(2)結果
体重変動
体重測定は週1回、試料投与前に行い、各群ラットの体重の平均値を求めた。結果を図8に示す。
図8より、Zucker-fattyラットはZucker-leanラットと比較して、体重の増加が激しかったが、Zucker-fattyラット無投与群(A群)と比較して、ケール投与群(B〜G群)では8週齢当たりから体重増加の抑制が見られた。特に、本発明のリパーゼ阻害剤を投与したF群では、体重増加の抑制効果が最も高かった。また体重増加は抑制されたが、Zucker-leanラットの値以下になることはなかった。
以上より、水溶性成分を除去したケールの低級アルコール抽出物を投与することにより、特に優れた抗肥満症効果が見られることがわかった。また体重は、正常ラットの値以下にまで異常に抑制されることはなく、服用が安全であることが確認された。
(2) Results Body weight fluctuation The body weight was measured once a week before sample administration, and the average value of the body weight of each group of rats was determined. The results are shown in FIG.
FIG. 8 shows that the Zucker-fatty rat showed a significant increase in body weight compared to the Zucker-lean rat, but compared with the Zucker-fatty rat non-administration group (Group A), the kale administration group (Groups B to G). ) Showed suppression of weight gain from around 8 weeks of age. In particular, in group F to which the lipase inhibitor of the present invention was administered, the effect of suppressing weight gain was the highest. Moreover, although weight gain was suppressed, it was not less than that of Zucker-lean rats.
From the above, it was found that a particularly excellent anti-obesity effect can be seen by administering a lower alcohol extract of kale from which water-soluble components have been removed. Moreover, the body weight was not abnormally suppressed to a value lower than that of normal rats, and it was confirmed that the administration was safe.
血液検査
実験最終日の前日に全ラットを絶食させ、翌日に深麻酔(ネンブタール,45mg/kg,i.p.)し、左心室から20G採血針で可能な限り採血を行った。
採取した血液を用いて、下記の項目において生化学的検査(自動化学分析装置:Auto Lab, Radio lmmuno Assay 法)を行い、平均値を求めた。
結果を図9に示す。
Blood test All rats were fasted the day before the last day of the experiment, and the next day, deep anesthesia (Nembutal, 45 mg / kg, ip) was taken, and blood was collected from the left ventricle as much as possible with a 20G blood collection needle.
Using the collected blood, biochemical tests (automatic chemical analyzer: Auto Lab, Radio lmmuno Assay method) were performed on the following items, and the average value was obtained.
The results are shown in FIG.
図9のG群とH群とを比較すると、Zucker-fattyラットはZucker-leanラットと比較して、脂質関連の数値が高いが、Zucker-fattyラット無投与群(A群)と比較して、ケール投与群(B〜G群)では改善が見られた。
特に本発明のリパーゼ阻害剤を投与したF群では、中性脂肪、βリポ蛋白、遊離コレステロール値等が他の群よりも大きく低下し、正常ラットのH群の値に近づいた。また、細胞膜の構成成分であるリン脂質等と比較し、多くが動脈硬化を促進するLDLコレステロールであるβリポ蛋白や、中性脂肪においては、低下の割合が大きかった。
これらのことから、本発明のリパーゼ阻害剤は、肥満症やそれに伴う疾患を抑制する効果が期待できる。
When comparing G group and H group in Fig. 9, Zucker-fatty rats have higher lipid-related values than Zucker-lean rats, but compared to Zucker-fatty rats untreated group (Group A). Improvement was seen in the kale administration group (B to G group).
In particular, in group F to which the lipase inhibitor of the present invention was administered, the values of neutral fat, β-lipoprotein, free cholesterol and the like were significantly lower than those in the other groups, approaching the values of group H of normal rats. In addition, compared with phospholipids and the like, which are constituents of cell membranes, β lipoprotein, which is LDL cholesterol that promotes arteriosclerosis, and neutral fat showed a large decrease rate.
From these facts, the lipase inhibitor of the present invention can be expected to have an effect of suppressing obesity and diseases associated therewith.
また、肝細胞障害や肝・胆道系疾患の診断に有用である総ビリルビン・直接ビリルビンの値についても、本発明のリパーゼ阻害剤を投与したF群では有意に低下し、正常ラットのH群の値に近づいた。
その他の値について、本発明のリパーゼ阻害剤を投与したことによる異常は全く見られなかった。
In addition, the values of total bilirubin and direct bilirubin useful for the diagnosis of hepatocellular injury and liver / biliary tract diseases are also significantly decreased in the F group administered with the lipase inhibitor of the present invention, and in the normal rat H group. Approached the value.
Regarding other values, no abnormality was observed due to administration of the lipase inhibitor of the present invention.
<ヒト臨床検査>
モニター3名に、本発明のリパーゼ阻害剤である前記試験例6の試料を1日1.6g(乾固物換算)、あるいは試験例7の試料を1日5.5g(乾固物換算)、毎日服用してもらい、服用前、服用2週間目、服用1ヶ月目にそれぞれ採血し、中性脂肪値を測定した。結果を表3に示す。
<Human clinical examination>
For 3 monitors, the sample of the above-mentioned Test Example 6 which is the lipase inhibitor of the present invention is 1.6 g per day (in terms of dry matter), or the sample of Test Example 7 is 5.5 g per day (in terms of dry matter) They were taken every day, and blood was collected before taking, at 2 weeks after taking, and at 1 month of taking, and the neutral fat level was measured. The results are shown in Table 3.
(表3)
服 用 後
年齢 性別 服用前 2週間 1ヶ月 服用試料
パネラー1: 30代 男性 288 151 90 試験例6:1.6g
パネラー2: 40代 男性 218 111 157 試験例6:1.6g
パネラー3: 30代 男性 149 133 135 試験例6:1.6g
パネラー3: 20代 女性 175 133 140 試験例7:5.5g (Table 3)
After taking
Age Gender Before taking 2
Paneler 1: 30s Male 288 151 90 Test Example 6: 1.6g
Paneler 2: 40s Male 218 111 157 Test Example 6: 1.6g
Paneler 3: 30s Male 149 133 135 Test Example 6: 1.6g
Paneler 3: 20s Female 175 133 140 Test Example 7: 5.5g
中性脂肪値の標準範囲は30〜149mg/dlとされている。服用前は3人が正常範囲を超えていたが、服用2週間目で早くも低下が見られ、服用1ヶ月目には全員が標準範囲内になった。また、驚くべきことに本発明のリパーゼ阻害剤である前記試験例6の試料は、1日1.6gしか服用しなかったのにも関わらず、試験例7の試料を1日5.5gと多量に服用したのと同様の効果が発揮された。
さらに、元々中性脂肪値が標準範囲内であったパネラー3においても、服用により中性脂肪値の低下が見られた。すなわち中性脂肪値が標準範囲内の人に対しても、標準範囲内において積極的に作用することが確認された。
よって、ヒト臨床検査においても、本発明のリパーゼ阻害剤は、少量で優れたリパーゼ阻害効果が発揮され、その効果は中性脂肪値が異常な人はもちろん、標準範囲内の人に対しても、正常範囲内において発揮されることが確認された。また服用によって、下痢、嘔吐、排尿異常等の副作用は一切起こらず、安全に服用できるものであった。
The standard range of neutral fat is 30-149 mg / dl. Three people were out of the normal range before taking, but a decrease was seen as early as the second week of taking, and all were within the standard range in the first month of taking. Surprisingly, the sample of Test Example 6 that is the lipase inhibitor of the present invention was only 1.6 g per day, but the sample of Test Example 7 was 5.5 g per day. The same effect as taking a large amount was demonstrated.
In addition,
Therefore, even in human clinical examinations, the lipase inhibitor of the present invention exerts an excellent lipase inhibitory effect in a small amount, and the effect is not only for people with an abnormal triglyceride level but also for people within the standard range. It was confirmed that it was exhibited within the normal range. In addition, side effects such as diarrhea, vomiting, and abnormal urination did not occur by taking, and it was safe to take.
<抽出温度条件とリパーゼ阻害効果>
次に、水溶性成分除去工程における水の温度、及びアルコール抽出工程における低級アルコールの温度と、リパーゼ阻害効果との関係を試験した。
(試料の調製)
試験例9−1(水加熱抽出→エタノール加熱抽出)
ケール乾燥粉末10gを、水100mLで1時間加熱抽出(還流)し、ろ過後得られた残渣を乾燥させ、80容量%エタノール100mLで1時間加熱抽出(還流)した。
試験例9−2(水冷蔵抽出→エタノール加熱抽出)
ケール乾燥粉末10gを、水100mLで48時間冷蔵抽出(5℃)し、ろ過後得られた残渣を乾燥させ、80容量%エタノール100mLで1時間加熱抽出(還流)した。
試験例9−3(水冷蔵抽出→エタノール冷蔵抽出)
ケール乾燥粉末10gを、水100mLで48時間冷蔵抽出(5℃)し、得られた残渣を乾燥させ、80容量%エタノール100mLで48時間冷蔵抽出(5℃)した。
試験例9−4(水加熱抽出→エタノール冷蔵抽出)
ケール乾燥粉末10gを、水100mLで1時間加熱抽出(還流)し、ろ過後得られた残渣を乾燥させ、80容量%エタノール100mLで48時間冷蔵抽出(5℃)した。
<Extraction temperature condition and lipase inhibitory effect>
Next, the relationship between the temperature of water in the water-soluble component removal step, the temperature of the lower alcohol in the alcohol extraction step, and the lipase inhibitory effect was tested.
(Sample preparation)
Test Example 9-1 (water heating extraction → ethanol heating extraction)
10 g of the dry kale powder was heated and extracted (refluxed) with 100 mL of water for 1 hour, the residue obtained after filtration was dried, and heated and extracted (refluxed) with 100 mL of 80 vol% ethanol for 1 hour.
Test Example 9-2 (water-cooled extraction → ethanol heated extraction)
10 g of dry kale powder was chilled and extracted (5 ° C.) for 48 hours with 100 mL of water, and the residue obtained after filtration was dried and heated (refluxed) with 100 mL of 80 vol% ethanol for 1 hour.
Test Example 9-3 (water refrigerated extraction → ethanol refrigerated extraction)
10 g of dry kale powder was chilled and extracted (5 ° C.) with 100 mL of water for 48 hours, and the resulting residue was dried and chilled and extracted (5 ° C.) with 100 mL of 80 vol% ethanol for 48 hours.
Test Example 9-4 (water heating extraction → ethanol refrigerated extraction)
10 g of dry kale powder was heated and extracted (refluxed) with 100 mL of water for 1 hour, and the residue obtained after filtration was dried and refrigerated and extracted (5 ° C.) for 48 hours with 100 mL of 80 vol% ethanol.
試験例9−1〜9−4で得られた抽出液を用いて、上述したリパーゼ阻害試験を行ない、リパーゼ阻害率が50%となる抽出液中の固形分の濃度(IC50)(mg/mL)を調べた。この値が少ないほど、一定量当たりのリパーゼ阻害効果が高いことを表す。
(表4)
試験例9−1 試験例9−2 試験例9−3 試験例9−4
IC50(mg/mL) 2.9 6.2 5.6 7.8
加熱によりリパーゼ阻害効果は低下せず、むしろ加熱抽出した方が効果の高い物が得られることがわかった。またエタノール抽出を冷蔵条件で行うと、得られる固形分が少なくなる。よってアルコール抽出は、加熱下で行うことが好ましい。
Using the extract obtained in Test Examples 9-1 to 9-4, the lipase inhibition test described above was performed, and the solid content concentration (IC50) (mg / mL) in the extract at which the lipase inhibition rate was 50%. ) Was investigated. The smaller this value, the higher the lipase inhibitory effect per certain amount.
(Table 4)
Test Example 9-1 Test Example 9-2 Test Example 9-3 Test Example 9-4
IC50 (mg / mL) 2.9 6.2 5.6 7.8
It was found that the lipase inhibitory effect was not reduced by heating, but rather a product with higher effect was obtained by heat extraction. Moreover, when ethanol extraction is performed on refrigeration conditions, the solid content obtained will decrease. Therefore, alcohol extraction is preferably performed under heating.
<抽出アルコール濃度とリパーゼ阻害効果>
次に、抽出アルコール濃度と、リパーゼ阻害効果との関係を試験した。
ケール乾燥粉末100gを水1Lで加熱抽出(還流)し、ろ過後得られた乾燥残渣を各エタノール濃度のエタノール溶液1Lで1時間加熱抽出(還流)し、ろ過後抽出液を得た。
得られた抽出液を用いて、上述したリパーゼ阻害試験を行ない、リパーゼ阻害率が50%となる抽出液中の固形分の濃度(IC50)(mg/mL)を調べた。この値が少ないほど、一定量当たりのリパーゼ阻害効果が高いことを表す
<Extracted alcohol concentration and lipase inhibitory effect>
Next, the relationship between the extracted alcohol concentration and the lipase inhibitory effect was tested.
100 g of dry kale powder was heated and extracted (refluxed) with 1 L of water, and the dried residue obtained after filtration was heated and extracted (refluxed) with 1 L of ethanol solution of each ethanol concentration for 1 hour to obtain an extract after filtration.
Using the obtained extract, the lipase inhibition test described above was performed, and the concentration of solid content (IC50) (mg / mL) in the extract at which the lipase inhibition rate was 50% was examined. The smaller this value, the higher the lipase inhibitory effect per fixed amount.
(表5)
エタノール濃度 IC50(mg/mL)
50容量% 11.5
60容量% 5.0
70容量% 5.0
80容量% 2.9
90容量% 7.6
99.5容量% 6.3
エタノール濃度が60〜80容量%の時、阻害効果の高いものが得られた。
よってエタノール濃度は60〜80容量%が好ましいことが確認された。
(Table 5)
Ethanol concentration IC50 (mg / mL)
50% by volume 11.5
60% by volume 5.0
70% by volume 5.0
80% by volume 2.9
90% by volume 7.6
99.5% by volume 6.3
When the ethanol concentration was 60 to 80% by volume, a high inhibitory effect was obtained.
Therefore, it was confirmed that the ethanol concentration is preferably 60 to 80% by volume.
<各種野菜のリパーゼ阻害効果>
各種野菜について、抽出液を用いて実施例1の試験例7と同様にして、リパーゼ阻害率を測定した。結果を表6に示す。
(表6)
野菜名 リパーゼ阻害率(%)
ケール(アブラナ科) 76.0
キャベツ(アブラナ科) 44.0
白菜(アブラナ科) 31.6
辛味大根(アブラナ科) 43.8
ナス(ナス科) 57.1
カボチャ(ウリ科) 2.9
<Lipase inhibitory effect of various vegetables>
About various vegetables, the lipase inhibition rate was measured like the test example 7 of Example 1 using the extract. The results are shown in Table 6.
(Table 6)
Vegetable name Lipase inhibition rate (%)
Kale (Brassicaceae) 76.0
Cabbage (Brassicaceae) 44.0
Chinese cabbage (Brassicaceae) 31.6
Spicy radish (Brassicaceae) 43.8
Eggplant (Solanum) 57.1
Pumpkin (Cucurbitaceae) 2.9
他の野菜では、どれもリパーゼ阻害活性が低かった。また同じアブラナ科の野菜でも、ケール以外はほとんど活性がなかった。このように本発明では、ケールの驚くべきリパーゼ阻害活性を見出したのである。 All other vegetables had low lipase inhibitory activity. Even the same cruciferous vegetables had little activity except for kale. Thus, in the present invention, Kale's surprising lipase inhibitory activity was found.
<散剤>
(処方)
(1)本発明のリパーゼ阻害剤(試験例7の抽出物) 2質量部
(2)乾燥コーンスターチ 38質量部
(3)微結晶セルロース 60質量部
(製法)(1)〜(3)を混合し、2gずつ分封し、散剤を得た。
<Powder>
(Prescription)
(1) Lipase inhibitor of the present invention (Extract of Test Example 7) 2 parts by mass (2) Dry corn starch 38 parts by mass (3)
<錠剤>
(処方)
(1)本発明のリパーゼ阻害剤(試験例7の抽出物) 15質量部
(2)乳糖 80質量部
(3)合成ケイ酸アルミニウム 4質量部
(4)ステアリン酸マグネシウム 1質量部
(製法)
上記の各成分を混合し、その混合物を打錠機で1錠300mgに打錠し、錠剤を得た。
<Tablets>
(Prescription)
(1) Lipase inhibitor of the present invention (extract of Test Example 7) 15 parts by mass (2) Lactose 80 parts by mass (3)
The above components were mixed, and the mixture was tableted into 300 mg tablets with a tableting machine to obtain tablets.
<液剤>
(処方)
(1)本発明のリパーゼ阻害剤(試験例7の抽出物) 110g
(2)エリスリトール 200g
(3)スクラロース 2g
(4)クエン酸 28g
(5)リンゴ酸 20g
(6)安息香酸ナトリウム 4g
(7)パラオキシ安息香酸ブチル 0.3g
(8)パラオキシ安息香酸エチル 0.7g
(9)香料 適量
(10)精製水 適量
(製法)
(2)〜(8)を精製水6Lに加熱溶解後、冷却し、50℃付近で(1)、(2)、(9)を加えて、更に精製水を加えて10Lとした。この液を100mLずつ容器に分注した。
<Liquid>
(Prescription)
(1) Lipase inhibitor of the present invention (Extract of Test Example 7) 110 g
(2) Erythritol 200g
(3) Sucralose 2g
(4) Citric acid 28g
(5) Malic acid 20g
(6) Sodium benzoate 4g
(7) Butyl paraoxybenzoate 0.3g
(8) 0.7 g of ethyl paraoxybenzoate
(9) Perfume appropriate amount (10) Purified water Appropriate amount (production method)
(2) to (8) were dissolved in 6 L of purified water by heating and then cooled, (1), (2) and (9) were added at around 50 ° C., and purified water was further added to make 10 L. 100 mL of this solution was dispensed into a container.
<マーガリン>
(処方)
(1)なたね油 81.2質量部
(2)水 10.0質量部
(3)食塩 1.5質量部
(4)脱脂粉乳 2.0質量部
(5)レシチン 0.3質量部
(6)本発明のリパーゼ阻害剤(試験例7の抽出物) 5.0質量部
(7)香料 適量
(8)着色料 適量
(製法)
常法により製造した。
<Margarine>
(Prescription)
(1) rapeseed oil 81.2 parts by mass
(2) Water 10.0 parts by mass (3) Sodium chloride 1.5 parts by mass (4) Nonfat dry milk 2.0 parts by mass (5) Lecithin 0.3 parts by mass (6) Lipase inhibitor of the present invention (Test Example 7) 5.0 parts by mass (7) perfume appropriate amount (8) colorant appropriate amount
(Manufacturing method)
Manufactured in a conventional manner.
<保湿クリーム>
(処方)
油相成分;
ホホバ油 3.0質量%
流動パラフィン 4.0質量%
POE(40)硬化ヒマシ油 2.0質量%
ミリスチン酸イソステアリン酸ジクリセライド 15.0質量%
メチルフェニルポリシロキサン 5.0質量%
香料 適量
水相成分;
ステアロイルメチルタウリンナトリウム 0.5質量%
グリセリン 20.0質量%
メチルパラベン 0.1質量%
本発明のリパーゼ阻害剤(試験例7の抽出物) 5.0質量%
精製水 残余
(製法)
上記水相成分を加熱混合して、70℃に保った。上記油相成分も同様に70℃で加熱溶解分散した。この油相部に上記の水相部を加え、乳化機にて乳化し、25℃まで冷却した。
<Moisturizing cream>
(Prescription)
Oil phase component;
Jojoba oil 3.0% by mass
Liquid paraffin 4.0% by mass
POE (40) hydrogenated castor oil 2.0% by mass
Myristic acid isostearic acid diglyceride 15.0% by mass
Methylphenylpolysiloxane 5.0% by mass
Perfume appropriate amount water phase component;
Stearoyl methyl taurine sodium 0.5% by mass
Glycerin 20.0% by mass
Methylparaben 0.1% by mass
Lipase inhibitor of the present invention (extract of Test Example 7) 5.0% by mass
Purified water residue (production method)
The aqueous phase component was heated and mixed and kept at 70 ° C. The oil phase component was similarly dissolved by heating at 70 ° C. The above aqueous phase was added to the oil phase, emulsified with an emulsifier, and cooled to 25 ° C.
Claims (4)
前記残渣を低級アルコールに浸漬し、有効成分を低級アルコールで抽出するアルコール抽出工程とを備えていることを特徴とするリパーゼ阻害剤の製造方法。 A pretreatment step of immersing kale or a dried product thereof in water and distributing it to water-soluble components and residues;
A method for producing a lipase inhibitor, comprising: an alcohol extraction step of immersing the residue in a lower alcohol and extracting an active ingredient with the lower alcohol.
An anti-obesity composition comprising the lipase inhibitor according to claim 1.
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