Department of Pharmacology, Institute of Post Graduate Medical Education and Research, 244 B, Acharya Jagadish Chandra Bose Road, Kolkata 700 020, West Bengal, India.
Int J Antimicrob Agents. 2010 Jul;36(1):43-9. doi: 10.1016/j.ijantimicag.2010.03.008. Epub 2010 Apr 18.
Visceral leishmaniasis (VL), caused by the protozoan Leishmania sp., affects 500000 people annually, with the Indian subcontinent contributing a significant proportion of these cases. Emerging refractoriness to conventional antimony therapy has emphasised the need for safer yet effective antileishmanial drugs. Artemisinin, a widely used antimalarial, demonstrated anti-promastigote activity and the 50% inhibitory concentration (IC(50)) ranged from 100 microM to 120 microM irrespective of Leishmania species studied. Leishmania donovani-infected macrophages demonstrated decreased production of nitrite as well as mRNA expression of inducible nitric oxide synthase, which was normalised by artemisinin, indicating that it exerted both a direct parasiticidal activity as well as inducing a host protective response. Furthermore, in a BALB/c model of VL, orally administered artemisinin (10mg/kg and 25mg/kg body weight) effectively reduced both splenic weight and parasite burden, which was accompanied by a restoration of Th1 cytokines (interferon-gamma and interleukin-2). Taken together, these findings have delineated the therapeutic potential of artemisinin in experimental VL.
内脏利什曼病（VL）由原生动物利什曼虫引起，每年影响 50 万人，其中印度次大陆是这些病例的主要来源。对传统锑剂治疗的耐药性不断增加，强调了需要更安全但有效的抗利什曼病药物。青蒿素是一种广泛使用的抗疟药物，表现出抗前鞭毛体活性，半数抑制浓度（IC（50））范围为 100 microM 至 120 microM，与研究的利什曼虫种类无关。感染利什曼原虫的巨噬细胞表现出亚硝酸盐产生减少以及诱导型一氧化氮合酶的 mRNA 表达降低，青蒿素可使这些降低恢复正常，表明其具有直接的杀寄生虫活性以及诱导宿主保护性反应。此外，在 VL 的 BALB/c 模型中，口服给予青蒿素（10mg/kg 和 25mg/kg 体重）可有效降低脾脏重量和寄生虫负担，同时恢复 Th1 细胞因子（干扰素-γ和白细胞介素-2）。综上所述，这些发现描绘了青蒿素在实验性 VL 中的治疗潜力。
