JPS62145015A - Anti-inflammatory agent - Google Patents
Anti-inflammatory agentInfo
- Publication number
- JPS62145015A JPS62145015A JP28731485A JP28731485A JPS62145015A JP S62145015 A JPS62145015 A JP S62145015A JP 28731485 A JP28731485 A JP 28731485A JP 28731485 A JP28731485 A JP 28731485A JP S62145015 A JPS62145015 A JP S62145015A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- inflammatory agent
- sialic acid
- edema
- injection
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Saccharide Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明は新規な抗炎症剤、さらに詳しくはシアル酸、と
くにＮ−アセチルノイラミン酸を有効成分とする抗炎症
剤に関する。DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to a novel anti-inflammatory agent, and more particularly to an anti-inflammatory agent containing sialic acid, particularly N-acetylneuraminic acid, as an active ingredient.
技術的背景と先行技術
哺乳動物の胎盤抽出物、プラセンタエキスには種々の薬
理活性成分が含まれ、そのために医薬品、化粧品などに
配合されている。このプラセンタエキスには、動物の種
類によっても多少変動があるが、多くのアミノ酸類、ビ
タミン類、無機成分、アルカリホスファターゼ、デオキ
シリボ核酸、中性Ｃｔｔケトステロイドなどが含まれて
いることが知られている。Technical background and prior art Mammalian placenta extracts contain various pharmacologically active ingredients, and are therefore incorporated into pharmaceuticals, cosmetics, and the like. This placenta extract is known to contain many amino acids, vitamins, inorganic components, alkaline phosphatase, deoxyribonucleic acid, neutral Ctt ketosteroids, etc., although it varies depending on the type of animal. There is.
発明の目的
本発明者らは、永年、プラセンタエキス、とくにウシの
プラセンタエキスの薬理活性、有効成分などについて研
究を重ね、今回、そのプラセンタエキスはシアル酸がＮ
−アセチルノイラミン酸の形で含まれていることを発見
し、このシアル酸に注目し、その薬理活性について種々
検討した。その結果、シアル酸にすぐれた抗炎症作用が
あることを知り本発明を完成した。Purpose of the Invention The present inventors have spent many years researching the pharmacological activity and active ingredients of placenta extract, especially bovine placenta extract, and have now discovered that the placenta extract contains sialic acid and N.
-We discovered that it is contained in the form of acetylneuraminic acid, focused on this sialic acid, and conducted various studies on its pharmacological activities. As a result, they discovered that sialic acid has an excellent anti-inflammatory effect and completed the present invention.
すなわち、本発明はシアル酸、ことにＮ−アセチルノイ
ラミン酸を有効成分とする抗炎症剤を提供するものであ
る。That is, the present invention provides an anti-inflammatory agent containing sialic acid, particularly N-acetylneuraminic acid, as an active ingredient.
発明の構成および効菓
本発明の抗炎症剤における有効成分であるシアル酸は本
発明者らによりグラセンタエキス中に含まれることが見
い出されたが、このシアル酸とはノイラミン酸のアシル
誘導体の一群を意味し、多くの動物多糖類の重要成分で
あることが知られており、その主な一種であるＮ−アセ
チルノイラミン酸は試薬などとしてずてに市販に供され
ている。Structure of the Invention and Effects Sialic acid, which is an active ingredient in the anti-inflammatory agent of the present invention, was found to be contained in Gracenta extract, but this sialic acid is an acyl derivative of neuraminic acid. It is known to be an important component of many animal polysaccharides, and one of its main types, N-acetylneuraminic acid, is commercially available as a reagent.
本発明にはいずれのシアル酸ら含むが、とくにＮ−アセ
デルノイラミン酸が好ましい活性成分として用いられる
。Although the present invention includes any sialic acid, N-acedelneuraminic acid is particularly preferably used as an active ingredient.
本発明者らの実験によれば、シアル酸（Ｎ−アセチルノ
イラミン酸）は下記のような薬理学的および生化学的作
用を示す。According to experiments conducted by the present inventors, sialic acid (N-acetylneuraminic acid) exhibits the following pharmacological and biochemical actions.
（＋）抗炎症作用
市販のＮ−アセチルノイラミン酸を用い、ラットにおけ
るカラゲニン誘発浮腫に対する抑制作用を実験した。な
お、対象薬物としてアスピリンを用いた。(+) Anti-inflammatory effect Commercially available N-acetylneuraminic acid was used to test its inhibitory effect on carrageenan-induced edema in rats. Note that aspirin was used as the target drug.
（ｉ）実験１
方法・
ウィスター系雄ラット（体重１３０〜１６２９．１群７
匹）を室内（温度２３±１℃、湿度５５±５％）に保ち
、１週間固型飼料（ＣＥ−２、日本クリア社製）および
飲料水を与えて飼育した。これにＮ−アセチルノイラミ
ン酸（Ｓ Ｅ Ａ）３０．１００．３００．５００よた
はｌ Ｏ００ｗ９／に９のグツド緩衝液（ｐＨ６，４）
［Ｇｏｏｄ Ｎ、ｌｌ、バイオケミストリイ（１１ｉ
ｏｃｈｃｍｉｓＬｒｙ）、 ５．４６７〜４７ Ｇ（
１９６６）］の溶液を皮下注射した。ついで、１％カラ
ゲニン生理食塩水溶液０ 、１ ｍ（ｌを動物の右後肢
の足’１Ｊｊｆへ注射してカラゲニン浮腫を誘発させた
。注射後３０分〜２４時間に亙って浮腫を観察した。(i) Experiment 1 Method - Wistar male rats (body weight 130-1629.1 Group 7
The mice were kept indoors (temperature: 23±1° C., humidity: 55±5%) and raised for one week with solid feed (CE-2, manufactured by Nippon Clear Co., Ltd.) and drinking water. Add N-acetylneuraminic acid (SEA) 30.100.300.500 liters to this and 000w9/9 gud buffer (pH 6,4).
[Good N,ll, Biochemistry (11i
ochcmisLry), 5.467-47 G(
(1966)] was injected subcutaneously. Next, 0.1 ml of 1% carrageenan saline solution was injected into the right hind paw of the animal to induce carrageenan edema. Edema was observed for 30 minutes to 24 hours after the injection.
結果：
得られた浮腫率を添付の第１図に示す。また、その浮腫
率よりＮ−アセチルノイラミン酸（ＳＩＡ）の浮腫抑制
率を算出すると下記第１表に示すとおりである。Results: The edema rates obtained are shown in the attached Figure 1. Furthermore, the edema suppression rate of N-acetylneuraminic acid (SIA) was calculated from the edema rate as shown in Table 1 below.
第 １ 表 （抑制率％）（１
１）実験２
シアル酸とアスピリンとの効果を比較するために、前記
実験ｌと同様にして、ラットにＮ−アセデルノイラミン
酸（Ｓ Ｉ Ａ）３００．ｏ／＆ｙおよび対照としてア
スピリン１ｏ ｏ ｍｇ／ｋｇのグツド緩衝液（ｐＨ６
、４）の溶液を皮下注射したのち、カラゲニンによる浮
腫誘発を行なった。Table 1 (Suppression rate %) (1
1) Experiment 2 In order to compare the effects of sialic acid and aspirin, rats were given 300. o/&y and as a control aspirin 1 o o mg/kg in Gud buffer (pH 6
, 4) was injected subcutaneously, and edema was induced with carrageenan.
その浮腫率を第２図に示す。まｌこ、その浮腫率より浮
腫抑制率を算出すると下記第２表に示すとおりである。The edema rate is shown in Figure 2. The edema suppression rate was calculated from the edema rate as shown in Table 2 below.
第 ２ 表 （抑制率％）上記結果
から明らかなように、Ｎ−アセチルノイラミン酸３００
ｍ９／ｋｆｔ以上でかなりの浮腫抑制率を示し、また
アスピリンに比べて作用持続性を示した。Table 2 (Inhibition rate %) As is clear from the above results, N-acetylneuraminic acid 300
It showed a considerable edema suppression rate at m9/kft or higher, and also showed a longer duration of action than aspirin.
２、急性毒性
ｄｄＹ系雄マウス（体重２２〜ａｏｙ、１群１０匹）に
Ｎ−アセデルノイラミン酸１００．３００．１０００お
よび５０００巧／に９のグツド緩衝液（ｐｌ−１６，４
）の溶液を皮下注射し、！週間一般症状を観察し、また
投与後２４時間、アーウィン（Ｉ ｒｗｉｎ）の変法［
ザイコファルマコロジア（Ｐ ｓｙｃｈｏｐｈａｒｍａ
−ｃｏｌｏｇｉａ）、 １，３． ２ ２ ２〜２
５ ７（＋ ９ ６ ８）コ（こ準じて行動症状を
観察した。その結果、死亡例はの影響ら認めら机なかっ
ｆこ。これより、Ｎ−アセデルノイラミン酸の急性毒性
、Ｌ Ｄ ｓ ｏは５００’ｍｇ／ｋｇ以」二であり、
毒性はきわめて低く安全であることがわかる。2. Acutely toxic ddY male mice (body weight 22~aoy, 10 mice per group) were injected with N-acedelneuraminic acid 100.300.1000 and 5000 μg/9 gud buffer (pl-16,4
) solution was injected subcutaneously, and! Observe general symptoms for a week and also for 24 hours after administration using a modified Irwin method [
P sychopharmacology
-cologia), 1,3. 2 2 2~2
5 7 (+ 9 6 8) (Accordingly, behavioral symptoms were observed. As a result, there were no cases of death due to the effects of Dso is 500'mg/kg or more,
It is found that toxicity is extremely low and safe.
本発明の抗炎症剤は、経口投与、注射、外用のいずれの
投与形態でら用いられ、一般的な医薬製剤、例えば錠剤
、乳剤、溶液剤、懸副剤、乳剤、顆粒剤、カプセル剤、
坐剤、注射剤、軟膏剤などの種々の剤形が採用される。The anti-inflammatory agent of the present invention can be used in any form of administration, including oral administration, injection, and external administration, and can be used in common pharmaceutical preparations, such as tablets, emulsions, solutions, suspensions, emulsions, granules, capsules,
Various dosage forms such as suppositories, injections, and ointments are employed.
これらの製剤は通常使用される充填剤、増ｍ剤、結合剤
、付湿剤、崩壊剤、滑沢剤などの賦形剤、希釈剤を用い
て常法により製造される。なお本発明の抗炎症剤には他
の公知の抗炎症活性薬物を適宜配合してもよい。These preparations are manufactured by conventional methods using commonly used excipients and diluents such as fillers, thickeners, binders, wetting agents, disintegrants, and lubricants. Note that the anti-inflammatory agent of the present invention may be appropriately blended with other known anti-inflammatory active drugs.
本発明の抗炎症剤における活性成分のシアル酸の用量は
、小者の年令、体重、さらに症状の程度などによっても
多少変動するが、通常、ヒトの大人において、Ｉ Ｏ〜
２０００ｍｇ／ｋｇ／日、好ましくはＩ ００−１００
０ｍｇ／ｋｇ／日の投与量にて用いられる。The dose of sialic acid, which is the active ingredient in the anti-inflammatory agent of the present invention, varies somewhat depending on the age and weight of the child, as well as the severity of symptoms, but usually, in an adult human, I O ~
2000mg/kg/day, preferably I 00-100
It is used at a dosage of 0 mg/kg/day.
つぎに実施例により本発明の抗炎症剤をさらに具体的に
説明−６るか本発明はこれらに限定されな０゜
実施例１
錠剤
成分 用量
Ｎ−アセチルノイラミン酸 １００ｍｇアスピ
リン １００ｍｇ乳糖
２０（１１１９″乾燥デンプン
２００１１ｇステアリン酸マグ
ネシウム ５０１９常法により１錠中に」−
記組成を有する錠剤を調製する。Next, the anti-inflammatory agent of the present invention will be explained in more detail with reference to Examples.
20 (1119″Dry starch 20011g Magnesium stearate 5019 in 1 tablet by conventional method”)
A tablet having the following composition is prepared.
実施例２
注射剤
成分 用量
Ｎ−アセチルノイラミン酸 １００１１ｇグツ
ド緩衝液 計１０００１１ｆ２常法に
より上記組成からなる注射剤を調製する。Example 2 Injection Components Dosage N-acetylneuraminic acid 10011g Gud buffer Total 100011f2 An injection having the above composition is prepared by a conventional method.
実施例３
軟膏剤（０／Ｗ型）
麻り一分□ 用量
流動パラフィン ９．００重量％ステア
リン酸 ４．００ 〃セタノール
３．００ 〃モノステアリン酸ボ
キオキシ
エヂレンソルビタン（２０ＥＯ）０．５０ 〃ノリコ
ン樹脂 ０．５０ 〃Ｎ−アセデル
ノイラミン酸 ３．００ 〃プロピレングリコール
１８．００”パラオキシ安息谷酸メヂル ０
．２０ 〃アヤコールＬＣ−ワックス ３．００
〃精製水 ５８．５０ 〃常
法により上記組成からなる軟膏剤を調製する。Example 3 Ointment (0/W type) Asari Ichibu□ Dose Liquid paraffin 9.00% by weight Stearic acid 4.00 Setanol
3.00 Boxoxyethylene sorbitan monostearate (20EO) 0.50 Noricon resin 0.50 N-acedelneuraminic acid 3.00 Propylene glycol 18.00” Medyl paraoxybenzoate 0
．． 20 Ayacol LC-Wax 3.00
Purified water 58.50 An ointment having the above composition is prepared by a conventional method.
第１図はカラゲニン誘発浮腫に対するＮ−アセデルノイ
ラミン酸の浮腫抑制活性（抗炎症活性）を示すグラフ、
第２図は、Ｎ−アセデルノイラミン酸および対照のアス
ピリンの抗カラゲニン誘発浮腫活性を示すグラフである
。
シー−１コントラージFigure 1 is a graph showing the edema-suppressing activity (anti-inflammatory activity) of N-acedelneuraminic acid against carrageenan-induced edema;
FIG. 2 is a graph showing the anti-carrageenan-induced edema activity of N-acedelneuraminic acid and control aspirin. C-1 Contrage
Claims (2)
する抗炎症剤。(1) An anti-inflammatory agent characterized by containing sialic acid as an active ingredient.
第１項記載の抗炎症剤。(2) The anti-inflammatory agent according to item 1 above, wherein the sialic acid is N-acetylneuraminic acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP28731485A JPS62145015A (en) | 1985-12-19 | 1985-12-19 | Anti-inflammatory agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP28731485A JPS62145015A (en) | 1985-12-19 | 1985-12-19 | Anti-inflammatory agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS62145015A true JPS62145015A (en) | 1987-06-29 |
Family
ID=17715760
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP28731485A Pending JPS62145015A (en) | 1985-12-19 | 1985-12-19 | Anti-inflammatory agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS62145015A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01163125A (en) * | 1987-12-21 | 1989-06-27 | Shiseido Co Ltd | Anti-inflammatory drug |
| WO2008096775A1 (en) | 2007-02-08 | 2008-08-14 | Nippon Zoki Pharmaceutical Co., Ltd. | Therapeutic agent for pain disease |
| US7781408B2 (en) | 2003-04-02 | 2010-08-24 | Mti Meta Tech Inc. | Formulations for mediating inflammation and for reducing blood cholesterol |
| US7851451B2 (en) | 2004-03-12 | 2010-12-14 | Mti Meta Tech Inc. | Formulations for mediating inflammatory bowel disorders |
| US8536140B2 (en) | 2004-03-12 | 2013-09-17 | Mti Meta Tech Inc. | Methods for treating inflammatory bowel disease |
| CN104586642A (en) * | 2015-02-06 | 2015-05-06 | 武汉中科光谷绿色生物技术有限公司 | Applications of N-acetvlneuraminic acid monomer, N-acetvlneuraminic acid hydrate or N-acetvlneuraminic acid salt in personal care supplies |
-
1985
- 1985-12-19 JP JP28731485A patent/JPS62145015A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| AGENTS AND ACTIONS=1978 * |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01163125A (en) * | 1987-12-21 | 1989-06-27 | Shiseido Co Ltd | Anti-inflammatory drug |
| JP2684179B2 (en) * | 1987-12-21 | 1997-12-03 | 雪印乳業株式会社 | Anti-inflammatory agent |
| US7781408B2 (en) | 2003-04-02 | 2010-08-24 | Mti Meta Tech Inc. | Formulations for mediating inflammation and for reducing blood cholesterol |
| US7851451B2 (en) | 2004-03-12 | 2010-12-14 | Mti Meta Tech Inc. | Formulations for mediating inflammatory bowel disorders |
| US8536140B2 (en) | 2004-03-12 | 2013-09-17 | Mti Meta Tech Inc. | Methods for treating inflammatory bowel disease |
| WO2008096775A1 (en) | 2007-02-08 | 2008-08-14 | Nippon Zoki Pharmaceutical Co., Ltd. | Therapeutic agent for pain disease |
| US8492350B2 (en) | 2007-02-08 | 2013-07-23 | Nippon Zoki Pharmaceutical Co., Ltd. | Therapeutic agent for pain disease |
| CN104586642A (en) * | 2015-02-06 | 2015-05-06 | 武汉中科光谷绿色生物技术有限公司 | Applications of N-acetvlneuraminic acid monomer, N-acetvlneuraminic acid hydrate or N-acetvlneuraminic acid salt in personal care supplies |
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