Departamento de Sanidad Animal, Facultad de Veterinaria, Universidad Complutense, 28040 Madrid, Spain.
Exp Parasitol. 2012 Dec;132(4):475-82. doi: 10.1016/j.exppara.2012.08.016. Epub 2012 Sep 17.
Anti-leishmanial activity of allicin (=diallyl thiosulphinate) has been tested in vitro against promastigotes and intracellular amastigotes of Leishmania donovani and Leishmania infantum. Macrophage infections have been carried out in vitro in the murine cell line J774 and ex vivo with peritoneal macrophages from BALB/c mice with a modified method to isolate metacyclic promastigotes. The compound has shown a significant in vitro effect on the multiplication of promastigotes of L. donovani and L. infantum in a time- and dose-dependent manner. It has been shown for the first time the inhibition of multiplication of intracellular amastigotes of Leishmania by allicin. Inhibitory concentrations of the compound were in the micromolar range (10-30 μM) for both Leishmania species. Antileishmanial effect of allicin apparently was not related to products of degradation of the molecule as assessed by mass spectrometry analysis. Inhibitory activity of allicin against promastigotes and intracellular amastigotes increased when the compound was added to the cultures every 24 h. Two administrations of 5 μM allicin inhibited by ca. 50% the proliferation of Leishmania amastigotes. Low toxicity for mammalian cells of this compound suggests the interest of exploring the value of allicin in combined therapy against leishmanial infections.
大蒜素(二烯丙基硫代亚磺酸酯)的抗利什曼原虫活性已在体外针对利什曼原虫和利什曼原虫的前鞭毛体和内阿米巴进行了测试。已经在体外的 J774 鼠细胞系和用改良的方法从 BALB/c 小鼠的腹腔巨噬细胞中进行了体内感染,以分离循环前鞭毛体。该化合物在体外时间和剂量依赖性方式下显著抑制了利什曼原虫的前鞭毛体的增殖。这是首次证明大蒜素抑制利什曼原虫内阿米巴的增殖。该化合物对两种利什曼原虫的抑制浓度均在微摩尔范围内(10-30 μM)。大蒜素对前鞭毛体和内阿米巴的抗利什曼原虫作用显然与通过质谱分析评估的分子降解产物无关。当每隔 24 小时将该化合物添加到培养物中时,大蒜素对前鞭毛体和内阿米巴的抑制活性增加。两次给予 5 μM 的大蒜素可抑制约 50%的利什曼原虫内阿米巴的增殖。该化合物对哺乳动物细胞的低毒性表明,探索大蒜素在联合治疗利什曼原虫感染中的价值很有意义。