Wabwoba Byrum W, Anjili Christopher O, Ngeiywa Moses M, Ngure Peter K, Kigondu Elizabeth M, Ingonga Johnstone, Makwali Judith
Mombasa Technical Training Institute, Department of Applied Sciences, Mombasa, Kenya.
J Vector Borne Dis. 2010 Sep;47(3):160-7.
BACKGROUND & OBJECTIVES: Several plant products have been tested and found to possess antileishmanial activity. The present study was undertaken to establish whether methanolic extract of Allium sativum Linn has antileishmanial activity in comparison to standard drugs.
Methanolic extract of A. sativum bulbs was screened for in vitro and in vivo antileishmanial activity against Leishmania major strain (NLB 145) and L. donovani strain (NLB 065). Pentostam and Amphotericin B were used as standard drugs. BALB/c mice and golden hamsters (Mesocricetus auratus) were used in in vivo studies on L. major and L. donovani respectively.
The extract exhibited very low cytotoxicity (IC50 >450 μg/ml) against Vero cells. The extract had significantly better (p <0.001) leishmanicidal activity against both species (IC50 34.22 μg/ml to L. major, 37.41 μg/ml to L. donovani) than Pentostam. However, the activity was significantly lower (p <0.001) than that of Amphotericin B against both the species. At a concentration of 250 μg/ml, the extract induced the production of 60 μM of nitric oxide, a ten-fold up-regulation in activated macrophages. The multiplication indices for L. major amastigotes treated in 100 μg/ml were significantly different (p <0.05). Treatment with the extract, daily for 28 days led to a significant reduction (p <0.05) in footpad swelling in BALB/c mice; similar activity noticed in the treatment with standard drugs. The Leishman-Donovan Units (LDU) for the extract treated animals were significantly higher (p <0.05) than those of standard drugs, but lower compared to the negative control.
INTERPRETATION & CONCLUSION: Since the mechanism of action for the methanolic extract is apparently immunomodulatory, garlic compounds could be purified and tried as complementary medicine in the management of leishmaniases.
多种植物产品已被测试并发现具有抗利什曼原虫活性。本研究旨在确定大蒜（Allium sativum Linn）甲醇提取物与标准药物相比是否具有抗利什曼原虫活性。
对大蒜鳞茎的甲醇提取物进行体外和体内抗利什曼原虫活性筛选，针对硕大利什曼原虫菌株（NLB 145）和杜氏利什曼原虫菌株（NLB 065）。喷他脒和两性霉素B用作标准药物。分别使用BALB/c小鼠和金黄仓鼠（Mesocricetus auratus）对硕大利什曼原虫和杜氏利什曼原虫进行体内研究。
该提取物对Vero细胞表现出极低的细胞毒性（IC50>450μg/ml）。该提取物对两种利什曼原虫的杀利什曼原虫活性（对硕大利什曼原虫的IC50为34.22μg/ml，对杜氏利什曼原虫的IC50为37.41μg/ml）明显优于喷他脒（p<0.001）。然而，与两性霉素B相比，其对两种利什曼原虫的活性明显较低（p<0.001）。在浓度为250μg/ml时，该提取物诱导产生60μM的一氧化氮，在活化巨噬细胞中上调了10倍。用100μg/ml处理的硕大利什曼原虫无鞭毛体的增殖指数有显著差异（p<0.05）。每天用该提取物处理28天导致BALB/c小鼠足垫肿胀显著减轻（p<0.05）；在使用标准药物治疗中也观察到类似活性。提取物处理动物的利什曼-多诺万单位（LDU）明显高于标准药物（p<0.05），但低于阴性对照。
由于甲醇提取物的作用机制明显是免疫调节，大蒜化合物可被纯化并尝试作为治疗利什曼病的辅助药物。
