组蛋白去乙酰化酶与组蛋白乙酰转移酶及其抑制剂抗血吸虫作用研究进展

Histone deacetylase and histone acetyltransferase inhibitors as antischisto-somal agents:a review

血吸虫病是一种被忽视的人兽共患寄生虫病。目前,吡喹酮是治疗血吸虫病的首选药物,也是治疗日本血吸虫病的唯一有效药物。自20世纪70年代问世以来,吡喹酮已在大规模血吸虫病化疗中应用了40余年,长期大规模使用导致部分地区血吸虫对其产生了抗性,因此迫切需要研发新型抗血吸虫药物作为候选替代药物。近期研究表明,组蛋白去乙酰化酶和组蛋白乙酰转移酶在血吸虫的生长发育以及繁殖等阶段中均起关键作用,被认为是治疗血吸虫病的潜在药物靶点。本文总结了组蛋白去乙酰化酶抑制剂与组蛋白乙酰转移酶抑制剂在抗血吸虫药物研究中的最新进展,以期为抗血吸虫新药的研发提供参考。

Schistosomiasis is a neglected zoonotic parasitic disease.Currently,praziquantel is the drug of choice for the treatment of schistosomiasis,and is the only effective chemical for treatment of schistosomiasis japonica.Since its introduction in the 1970s,praziquantel has been used for large-scale chemotherapy of schistosomiasis for over 40 years.However,there have been reports pertaining to the resistance to praziquantel in schistosomes.Therefore,development of novel antischistosomal agents as alternatives of praziquantel,is of great need.Histone deacetylases and histone acetyltransferases have been recently reported to play critical roles in the growth,development and reproduction of schistosomes,and are considered as potential drug targets for the treatment of schistosomiasis.This review summarizes the latest advances of histone deacetylase and histone acetyltransferase inhibitors in the research on antischistosomal drugs,so as to provide insights into research and development of novelantischistosomal agents.