JP2008214211A - Cathartic - Google Patents
Cathartic Download PDFInfo
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- JP2008214211A JP2008214211A JP2007051059A JP2007051059A JP2008214211A JP 2008214211 A JP2008214211 A JP 2008214211A JP 2007051059 A JP2007051059 A JP 2007051059A JP 2007051059 A JP2007051059 A JP 2007051059A JP 2008214211 A JP2008214211 A JP 2008214211A
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Abstract
Description
本発明は、腸内で便秘改善作用を発揮する瀉下剤に関する。 The present invention relates to a laxative that exhibits an effect of improving constipation in the intestine.
本発明に係る瀉下剤では、Rheum 属から抽出されたアントラキノン類を有効成分として含有するが、Rheum 属がアントラキノン類を含有すること、およびアントラキノン類に便秘改善作用(瀉下作用)があることなどは、例えば、特許文献1、2などに記載されており公知である。
The laxative according to the present invention contains anthraquinones extracted from the genus Rheum as an active ingredient, but the genus Rheum contains anthraquinones, and that anthraquinones have an effect of improving constipation (the axillary action) For example, it is described in
特許文献1には、大腸刺激性下剤として、Rheum 属植物である大黄が挙げられている。また、瀉下成分として、大黄から抽出したアントラキノン系瀉下剤が挙げられている。
特許文献2は、大黄を含有する漢方処方の生薬末混合物及び/又はエキス粉末を含む下剤に関するものであり、アントラキノン系の瀉下剤の具体例として、大黄を有効成分とする生薬系下剤が挙げられている。
一般的に大黄は根茎類生薬として知られている。つまり、この種のRheum 属では、その地下部、すなわち根茎部分のみが、生薬成分として利用されている。 Daio is generally known as a rhizome herbal medicine. That is, in this kind of Rheum genus, only the underground part, that is, the rhizome part, is used as a herbal medicine component.
大黄の根茎は汎用生薬の一つであるにも拘らず、その95%以上が外国に依存する状況にある。この種の植物資源に関しては、資源ナショナリズムに代表される権利の問題もあり、他国への持ち出しが徐々に難しくなっている。このため、国内での栽培化の要請が近年急速に高まっている。 Despite the fact that Daiki's rhizome is one of the general-purpose herbal medicines, more than 95% of them are dependent on foreign countries. With regard to this kind of plant resources, there is a problem of rights represented by resource nationalism, and it is gradually becoming difficult to bring them out to other countries. For this reason, the demand for domestic cultivation has increased rapidly in recent years.
国内における大黄の栽培例としては、東京大学の柴田承二教授による、R.tanguticumの栽培が最初である。現在、北海道で栽培されている信州大黄は、先のR.tanguticumの原種を材料にして、1953年以降、R.palmatumとR.coreanumとの交配を繰り返して、10数年の時間を費やして発見されたものである。その他、富山医薬大薬用植物園による立山弥陀ヶ原や、利賀村糸田島における栽培報告もあるが、生産栽培のレベルには達していない。 The first example of cultivation of Daihuang in Japan is the cultivation of R. tanguticum by Professor Shoji Shibata of the University of Tokyo. Shinshu Daihuang currently cultivated in Hokkaido, using the former R. tanguticum seeds as material, repeated mating of R. palmumatum and R. coreanum since 1953 and spent more than 10 years It has been discovered. In addition, although there are reports of cultivation in Toyama Pharmaceutical University Medicinal Botanical Garden in Tateyama Yayogahara and Toga Village Itodajima, they have not reached the level of production cultivation.
このように、一口に栽培化といっても、生産栽培に至るまでには、栽培的種の選抜、育種、栽培適地の選択、育種法の検討など、多くの検討と時間を要するものであり、簡単では無い。また、外国における大黄の大部分が野生品に由来している事実や、先の資源ナショナリズムの台頭に鑑みても、今後の外国からの供給量の増加は到底期待できない。 In this way, even if it is said to be domesticated, it takes a lot of time and research to reach production cultivation, such as selection of cultivated species, breeding, selection of suitable land for cultivation, and examination of breeding methods. It ’s not easy. In addition, in view of the fact that most of the great yellows in foreign countries are derived from wild products and the emergence of the previous resource nationalism, we cannot expect any future increase in supply from overseas.
本発明は、以上のような問題点を解決するためになされたものであり、Rheum 属に由来する瀉下剤に係る有効成分の安定供給を図るとともに、植物資源であるRheum 属の有効活用を図り、結果として、Rheum 属の保護に貢献し得る、新規な瀉下剤を提供することを目的とする。 The present invention has been made to solve the above-described problems, and aims to stably supply an active ingredient related to a laxative derived from the genus Rheum and to effectively use the genus Rheum as a plant resource. As a result, the present invention aims to provide a novel laxative that can contribute to the protection of the genus Rheum.
本発明者等は、従前においては、Rheum 属の地下部、すなわち根茎部分のみが生薬成分として利用に供されていること、および地上部についての薬用については、何らの検討もなされておらず、多くの場合、地上部は廃棄処分となっていることに着目して鋭意研究を重ねた結果、本発明を完成するに至った。 In the past, the inventors of the present invention have not made any investigation on the underground part of the genus Rheum, that is, only the rhizome part is used as a herbal medicine component and the medicinal use of the above-ground part, In many cases, the present invention has been completed as a result of intensive studies focusing on the fact that the above-ground part is disposed of.
すなわち本発明は、Rheum 属の地上部から抽出されたアントラキノン類を有効成分とすることを特徴とする瀉下剤である。 That is, the present invention is a laxative characterized by containing anthraquinones extracted from the above-ground part of the genus Rheum as an active ingredient.
本発明におけるRheum の具体例としては、例えば、R.undulatum 、R.officinale、R.palmatum、R.tanguticumなどを挙げることができる。 Specific examples of Rheum in the present invention include R.undulatum, R.officinale, R.palmatum, R.tanguticum and the like.
本発明におけるアントラキノン類とは、以下の化学式で示される一般式を有するものである。
アントラキノン類の具体例としては、emodin、Aloe-emodin 、Chrysophanol、Aloe-emodin-1-O-β-D-glucopyranoside、Chrysophanol-1-O- β-D-glucopyranoside、Chrysophanol-8-O- β-D-glucopyranoside、Chrysophanol-8-O- β-D-(G-galloyl)-glucopyranosideなどを挙げることができる。 Specific examples of anthraquinones include emodin, Aloe-emodin, Chrysophanol, Aloe-emodin-1-O-β-D-glucopyranoside, Chrysophanol-1-O-β-D-glucopyranoside, Chrysophanol-8-O-β- And D-glucopyranoside and Chrysophanol-8-O-β-D- (G-galloyl) -glucopyranoside.
これらアントラキノン類のうち、尤も有効な成分は、下記の化学式3で示されるエモジン(emodin)であると考える。
本発明においては、従来より生薬成分として認められているRheum 属の地下部である根茎部に替えて、地上部からアントラキノン類を抽出し、これを瀉下剤の有効成分とした。かかるRheum 属の地上部は、生薬成分についての研究が殆どなされておらず、多くは廃棄処分されている。したがって、本発明のように、Rheum 属の地上部からアントラキノン類を抽出し、これを瀉下剤の有効成分として利用すれば、一本のRheum 属の地下部から地上部までの全体を、無駄なく有効利用することができるので、一本のRheum 属から、より多くの有効成分を抽出することが可能となる。
このことは、外国からの輸入量の増加が望み難く、しかも国内栽培が困難な状況にあるRheum 属に由来するアントラキノン類の安定供給に貢献できることを意味し、結果として、植物資源の保護に貢献できる。
In the present invention, anthraquinones were extracted from the aerial part instead of the rhizome part, which is the underground part of the Rheum genus which has been conventionally recognized as a herbal medicine component, and this was used as an active ingredient of a laxative. In the above-ground part of the genus Rheum, little research has been conducted on herbal ingredients, and many have been disposed of. Therefore, as in the present invention, if anthraquinones are extracted from the above-ground part of the genus Rheum and used as an active ingredient of the laxative, the whole from the underground part to the above-ground part of the genus Rheum can be used without waste. Since it can be used effectively, more active ingredients can be extracted from one Rheum genus.
This means that it is possible to contribute to the stable supply of anthraquinones derived from the genus Rheum, which is difficult to increase in imports from abroad and difficult to grow domestically. it can.
アントラキノン類には種々の誘導体があるが、本発明では、エモジンが瀉下剤の有効成分であると考える。かかるエモジンの瀉下作用を裏付ける文献としては、例えば、「Effect of emodin on small intestinal peristalsis of mice and relevant mechanism :World journal of Gastroenterlogy:2005年11月20日発行」を挙げることができる。 There are various derivatives of anthraquinones, but in the present invention, emodin is considered to be an active ingredient of a laxative. As a document supporting such a majesty action of emodin, for example, “Effect of emodin on small intestinal peristalsis of mice and relevant mechanism: World journal of Gastroenterlogy: published on November 20, 2005” can be cited.
以下、実験例を挙げて本発明を詳細に説明する。
乾燥した和大黄(Rheum undulatum )の葉柄5gを粉砕し、80%メタノール50mlにて室温下で一晩抽出した。ろ過した後、残渣に再び80%メタノール50mlを加え、ortexミキサーで1分間混合した。得られた混合液をろ過した。ろ液を合わせて減圧濃縮し抽出エキスとした。
抽出エキスを80%メタノールで10mlまでメスアップし、0.45μmフィルターでろ過して、HPLC分析用試料液とした。
Hereinafter, the present invention will be described in detail with reference to experimental examples.
5 g of dried Rheum undulatum petiole was ground and extracted with 50 ml of 80% methanol overnight at room temperature. After filtration, 50 ml of 80% methanol was added to the residue again and mixed for 1 minute with an ortex mixer. The resulting mixture was filtered. The filtrates were combined and concentrated under reduced pressure to obtain an extract.
The extract was made up to 10 ml with 80% methanol and filtered through a 0.45 μm filter to obtain a sample solution for HPLC analysis.
図1にHPLCの分析結果を示す。分析条件は以下のごとくである。
Column:Capcellpack C18AG-120A(5μm,4.6mm i.d.×250mm,Shiseido)
Solvent :MeCN/H2 O(0.1% formic acid)gradient of 15% MeCN to 25% MeCN in 15 min to 70% MeCN in another 35 min, then to 100% MeCN in 10 min.
Flow rate :0.9ml/min.
Column temp :40℃
Detector:Shimadzu photodiode array SPDM-6A system(Shimadzu),UV:275nm.
FIG. 1 shows the results of HPLC analysis. The analysis conditions are as follows.
Column: Capcellpack C18AG-120A (5μm, 4.6mm id x 250mm, Shiseido)
Solvent: MeCN / H 2 O (0.1% formic acid) gradient of 15% MeCN to 25% MeCN in 15 min to 70% MeCN in another 35 min, then to 100% MeCN in 10 min.
Flow rate: 0.9ml / min.
Column temp: 40 ℃
Detector: Shimadzu photodiode array SPDM-6A system (Shimadzu), UV: 275nm.
図1のHPLCパターン分析結果より、Rheum undulatum には、瀉下剤の有効成分となり得る、エモジンが含まれていることが分かる。具体的には、図1のピーク1はcinnamic acid (ケイ皮酸)を、ピーク2はemodin(エモジン)を示しており、ピーク2のピーク位置より、Rheum undulatum にはエモジンが含まれることを確認することができた。かかるエモジンが瀉下作用を有することは、先に挙げた「Effect of emodin on small intestinal peristalsis of mice and relevant mechanism :World journal of Gastroenterlogy:2005年11月20日発行」等より明らかである。
From the HPLC pattern analysis results of FIG. 1, it can be seen that Rheum undulatum contains emodin, which can be an active ingredient of a laxative. Specifically,
Claims (2)
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JP2007051059A JP2008214211A (en) | 2007-03-01 | 2007-03-01 | Cathartic |
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Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012035122A1 (en) * | 2010-09-17 | 2012-03-22 | Dundalk Institute Of Technology | Anthraquinone compounds and their uses |
EP2439200A1 (en) * | 2010-09-17 | 2012-04-11 | Dundalk Institute of Technology | Anthraquinone compounds and their uses |
CN103127251A (en) * | 2012-03-14 | 2013-06-05 | 成都中医药大学 | Overground part extract of rheum officinale, extraction and purification method and use thereof |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH04154728A (en) * | 1990-10-16 | 1992-05-27 | Keijiyun Go | Cathartic |
JPH05345724A (en) * | 1992-04-03 | 1993-12-27 | Haabaru Seiyaku Kk | Production of oral medicine solution containing sennoside compounds as active ingredient |
JPH08310960A (en) * | 1995-05-22 | 1996-11-26 | Biofuerumin Seiyaku Kk | Mixed cathartic |
JPH10117761A (en) * | 1996-10-25 | 1998-05-12 | Shinshu Hoon:Kk | Alcoholic beverage and its production |
JP2004083436A (en) * | 2002-08-23 | 2004-03-18 | Minofuaagen Seiyaku:Kk | Astrocyte activation inhibitor and prophylactic or therapeutic agent for organ fibrosis |
JP2005179316A (en) * | 2003-12-24 | 2005-07-07 | Kanebo Ltd | Composition with constipation ameliorating action |
WO2005099733A1 (en) * | 2004-03-31 | 2005-10-27 | Kobayashi Pharmaceutical Co., Ltd. | Vegetable antibacterial composition |
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2007
- 2007-03-01 JP JP2007051059A patent/JP2008214211A/en active Pending
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH04154728A (en) * | 1990-10-16 | 1992-05-27 | Keijiyun Go | Cathartic |
JPH05345724A (en) * | 1992-04-03 | 1993-12-27 | Haabaru Seiyaku Kk | Production of oral medicine solution containing sennoside compounds as active ingredient |
JPH08310960A (en) * | 1995-05-22 | 1996-11-26 | Biofuerumin Seiyaku Kk | Mixed cathartic |
JPH10117761A (en) * | 1996-10-25 | 1998-05-12 | Shinshu Hoon:Kk | Alcoholic beverage and its production |
JP2004083436A (en) * | 2002-08-23 | 2004-03-18 | Minofuaagen Seiyaku:Kk | Astrocyte activation inhibitor and prophylactic or therapeutic agent for organ fibrosis |
JP2005179316A (en) * | 2003-12-24 | 2005-07-07 | Kanebo Ltd | Composition with constipation ameliorating action |
WO2005099733A1 (en) * | 2004-03-31 | 2005-10-27 | Kobayashi Pharmaceutical Co., Ltd. | Vegetable antibacterial composition |
Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012035122A1 (en) * | 2010-09-17 | 2012-03-22 | Dundalk Institute Of Technology | Anthraquinone compounds and their uses |
EP2439200A1 (en) * | 2010-09-17 | 2012-04-11 | Dundalk Institute of Technology | Anthraquinone compounds and their uses |
US9877940B2 (en) | 2010-09-17 | 2018-01-30 | Dundalk Institute Of Technology | Anthraquinone compounds and their uses |
CN103127251A (en) * | 2012-03-14 | 2013-06-05 | 成都中医药大学 | Overground part extract of rheum officinale, extraction and purification method and use thereof |
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