二烯丙基三硫醚对人畜致病性原生动物(锥虫、溶组织内阿米巴和鞭毛虫)体外抗寄生活性的研究。

Z R Lun, C Burri, M Menzinger, R Kaminsky
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摘要

大蒜(Allium sativum L.)及其主要成分之一大蒜素(allicin)长期以来一直被认为具有抗菌和抗真菌活性。二烯丙基三硫醚是大蒜素化学性质稳定的最终转化产物,于1981年在中国合成,用于治疗人体细菌、真菌和寄生虫感染。研究了二烯丙基三硫醚在几种重要原生动物寄生虫体内的体外活性。布氏锥虫、罗得西亚锥虫、冈比亚锥虫、伊瓦西锥虫、刚果锥虫和装备锥虫的IC50(抑制寄生虫代谢或生长50%的浓度)在0.8 ~ 5.5微克/ml。溶组织内阿米巴的IC50值为59微克/毫升,贾第鞭毛虫的IC50值为14微克/毫升。体外对两种成纤维细胞系(MASEF, Mastomys natalensis胚胎成纤维细胞和HEFL-12,人胚胎成纤维细胞)进行了细胞毒性评价。两种细胞系的最大耐受浓度均为25微克/毫升。结果表明,该化合物具有治疗多种人畜寄生虫病的潜力。
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Antiparasitic activity of diallyl trisulfide (Dasuansu) on human and animal pathogenic protozoa (Trypanosoma sp., Entamoeba histolytica and Giardia lamblia) in vitro.

Garlic (Allium sativum L.) and one of its major components, allicin, have been known to have antibacterial and antifungal activity for a long time. Diallyl trisulfide is a chemically stable final transformation product of allicin which was synthesized in 1981 in China and used for treatment of bacterial, fungal and parasitic infections in man. The activity of diallyl trisulfide was investigated in several important protozoan parasites in vitro. The IC50 (concentration which inhibits metabolism or growth of parasites by 50%) for Trypanosoma brucei brucei, T.b. rhodesiense, T.b. gambiense, T. evansi, T. congolense and T. equiperdum was in the range of 0.8-5.5 micrograms/ml. IC50 values were 59 micrograms/ml for Entamoeba histolytica and 14 micrograms/ml for Giardia lamblia. The cytotoxicity of the compound was evaluated on two fibroblast cell lines (MASEF, Mastomys natalensis embryo fibroblast and HEFL-12, human embryo fibroblast) in vitro. The maximum tolerated concentration for both cell lines was 25 micrograms/ml. The results indicate that the compound has potential to be used for treatment of several human and animal parasitic diseases.

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