Antileishmanial activity of HIV protease inhibitors

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• 作者：Savoia ; Dianella ; Allice ; Tiziano ; Tovo ; Pier-Angelo
• 关键词：Leishmania major ; Leishmania infantum ; Protease inhibitors ; Proteasomes
• 刊名：International Journal of Antimicrobial Agents
• 出版年：2005
• 出版时间：July, 2005
• 年：2005
• 卷：26
• 期：1
• 页码：92-94
• 全文大小：61.5 K

文摘

The proteasomes of some protozoa are possible targets for chemotherapy. Leishmaniasis is a major health problem in human immunodeficiency virus (HIV) co-infected subjects. Two HIV protease inhibitors (PI), indinavir and saquinavir, have been shown to block proteasome functions; we therefore investigated their effects on the growth of two Leishmania spp. (Leishmania major and Leishmania infantum). After 24 h of treatment, both drugs exhibited a dose-dependent antileishmanial activity, with 50 % lethal dose (LD₅₀) values of, respectively, 8.3 μM and 7 μM on L. major; minor activity was observed on L. infantum. These results add new in vitro insights into the wide-spectrum efficacy of PI and suggest studying their action on amastigote forms of leishmania within macrophages in order to validate their potential contribution against opportunistic infections in treated seropositive patients.