汉防己碱药理作用及抗埃博拉病毒活性研究进展

Abstract

埃博拉病毒是世界上最具威胁的病原体之一，2013年9月13日始于西非几内亚的埃博拉病(Ebola virus diseases, EVD)，是记载以来最严重的一次爆发。目前缺乏有效的治疗药物，研究发现埃博拉病毒通过胞内钙双孔通道(TPCs)释放基因组来完成病毒复制，汉防己甲素通过阻断胞内钙双孔通道(TPCs)来阻止埃博拉病毒基因组的释放从而阻止了病毒的复制。本文综述汉防己甲素(Tet)的抗埃博拉病毒的药理作用和作用机制及其它方面的药理活性；汉防己碱(Tet)肌松药中的苄基异奎琳的结构改造合成。同时展望了目前几种待进一步研究的钙离子拮抗剂包括钙双孔通道(TPCs)阻断剂如维拉帕米等应用于抗埃博拉病毒药物的可能性，为进一步推进汉肌松类药物深入研究提供重要参考。 The Ebola virus is one of the world’s most threatening pathogens. Ebola virus disease (EVD) which began in 13 September 2013 in Guinea, West Africa was the worst breakout since its first outbreak. Up till now we lack effective drugs. Some studies have found the Ebola virus completed virus rep-lication by endosomal calcium channels called two-pore channels (TPCs) release genome, and by blocking endosomal calcium channels TPCs, tetrandrine (Tet) prevented the release of the Ebola virus genome in order to stop the replication of the virus. Pharmacological effect and mechanism of action and other pharmacological activities of Tet in anti-Ebola virus in this review were sum-marized in detail; Tet as muscle loose medicine of the structure of benzylisonicotinamide was transformed and synthesized. At the same time, the prospects of several pending further study of calcium antagonists including blocking calcium TPCs such as verapamil applied for the possibility of anti-Ebola virus drugs were discussed, which provided important references for promoting the in-depth study of those muscle relaxant drugs.