Study of novel anti-leishmanial drug

我利用利什曼原虫的前鞭毛体对有机化合物和天然产物中的68种化合物进行了新药发现研究。其中2个菌株的EC50值分别为42 nM和27 nM。相比之下，两性霉素B作为阳性对照，对主要致病菌的EC50值为63 nM，选择性毒性是其哺乳动物细胞的46倍。对其构效关系的研究还有待进一步深入。建立了HSP90的作用机理分析和复杂关系，发现HSP90抑制剂及其类似物具有较强的抗利什曼效应，包括小分子(EC50值；30-40 nM)对大鼠前鞭毛体的抑制作用。

I performed to new drug discovery research for 68 compounds from organic compounds and natural product using promastigotes of Leishmania major. The EC50values among 2 of them for L. majorwere 42 nM and 27 nM. In contrast, Amphotericin B as a positive control was show 63 nM of EC50value for L. majorand selective toxicity of 46-fold compare tomammalian cells of it. The structure-activity relationship study will be need more. I established the mechanism analysis of HSP90 and complex relationship in L. major and also we found the high anti-leishmanial effect for HSP90 inhibitor and it’s analogs include small molecules (EC50values; 30-40 nM) against L. major promastigotes.