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

一种尼泊尔传统药物“Bayubidanga”，即Embelia ribes（桃科的一个科）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，我们的工作是澄清哪些成分对这种活性负责。用乙醚萃取得到已知的有效成分——栓塞素，而热水萃取得到另一种有效成分——没食子酸，说明栓塞素与热水接触后分解成不同的化合物。对犬鞭虫的体外活性分别为0.01 mg/ml和0.5 ~ 1 mg/ml。分别是毛线虫。澄清了栓塞素在沸水和甲醇（有机溶剂）中分解的特点，前者处理得到“二聚体”，后者处理得到o -甲基衍生物。用小鼠感染墨氏杆菌，检测了栓塞素及其衍生物的体内抗滴虫活性。结果发现，在感染前经醋酸氢化可的松预处理的BALB/c小鼠中，只有栓塞酸钾有效（治愈率为70-100%）。活性与已知的抗trichuris药物甲苯达唑相当。另一方面，在经丁乳酸泼尼松龙预处理的感染小鼠（BALB/c和ICR）中，甲苯达唑和保酸钾均无效，说明感染方式对药物疗效的影响很大。与这些药物相反，伊维菌素对本研究中测试的所有小鼠都持续有效。

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.