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Studies on Anti-Trichuris Constituents of Embelia ribes, A Nepali Traditional Medicine

尼泊尔传统药物余甘子抗鞭毛虫成分的研究

基本信息

批准号：
04670226
负责人：
TSUDA Yoshisuke
金额：
$ 1.28万
依托单位：
Kanazawa University
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (C)
财政年份：
1992
资助国家：
日本
起止时间：
1992 至 1993
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-04670226/
关键词：
Embelia ribes Anti-Trichuris activity Trichuris muris Embelin Gallic acid Potassium embelate Dimer BALB c mice 殺鞭虫作用 embelin gallic acid

项目摘要

A nepali traditional medicine "Bayubidanga", fruits of Embelia ribes (a family of Myrsinaceae), has been known to be effective to tapeworms. Since the medicine is reported to be also effective to whipworms and Ascaris, our work was undertaken to clarify what constituent(s) is responsible to this activity.Extraction of E.ribes with ether gave known constituent, embelin, as an active principle, while extraction with hot water resulted in another active principle, gallic acid, suggesting that embelin was decomposed into different compound(s) on contact with hot water. In vitro activities of these principles were 0.01 mg/ml and 0.5-1 mg/ml to dog whipworm. Trichuris vulpis, respectively.The features of decomposition of embelin in boiling water and in methanol (organic solvant) were clarified that the former treatment yielded a "dimer" and the leatter treatment gae O-methyl derivative.In vivo anti-Trichuris activity of embelin and its derivatives was examined using mice infected with T.muris. It was found that, among E.ribes decoction, embelin, and its derivatives, onlyh potassium embelate was effective (70-100%) cure rate), when applied to BALB/c mice pretreated with hydrocortisone acetate before infection. The activity was comparable to the known anti-Trichuris drug, mebendazole. On the other hand, neither potassiumembelate nor mebendazole was effective, when applied to infected mice (both BALB/c and ICR) pretreated with predonisolone butylacetate, suggesting that infection method largely influences on the result of eficacy of medicine. Contrary to these medicines, ivermectin was constantly effective to all mice tested in this investigation.

尼泊尔传统药物“Bayubidanga”是紫金牛科（Myrsinaceae）酸藤子（Embelia ribes）的果实，已知对绦虫有效。由于该药物据报道对鞭虫和蛔虫也有效，我们的工作是为了澄清哪些成分负责这种活性。用乙醚提取E.ribes得到已知成分Embelin作为活性成分，而用热水提取得到另一种活性成分，没食子酸，这表明Embelin在接触热水时分解成不同的化合物。这些成分对狗鞭虫的体外活性分别为0.01mg/ml和0.5-1 mg/ml。Embelin在沸水和甲醇（有机溶剂）中的分解特点是前者生成二聚体，后者生成O-甲基衍生物。结果表明，在茶藨子水煎剂、恩贝林及其衍生物中，只有恩贝酸钾对感染前用醋酸氢化可的松预处理的BALB/c小鼠有效（治愈率70-100%）。活性与已知的抗鞭虫药物甲苯咪唑相当。另一方面，用醋酸泼尼松龙预处理的感染小鼠（BALB/c和ICR小鼠），用恩贝酸钾和甲苯咪唑均无效，提示感染方法对药物疗效有很大影响。与这些药物相反，伊维菌素对本研究中测试的所有小鼠持续有效。