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是什么使得倍半萜内酯进入癌症临床试验?

What made sesquiterpene lactones reach cancer clinical trials?

机构信息

Biology Department, American University of Beirut, Beirut, Lebanon.

出版信息

Drug Discov Today. 2010 Aug;15(15-16):668-78. doi: 10.1016/j.drudis.2010.06.002. Epub 2010 Jun 9.

Abstract

Sesquiterpene lactones (SLs) are plant-derived compounds often used in traditional medicine against inflammation and cancer. This review focuses on the chemical and biological properties of SLs that lead to enhanced anticancer and anti-inflammatory effects. The chemical properties comprise alkylating center reactivity, lipophilicity, and molecular geometry and electronic features. SLs in clinical trials are artemisinin, thapsigargin and parthenolide and many of their synthetic derivatives. These drugs are selective toward tumor and cancer stem cells by targeting specific signaling pathways, which make them lead compounds in cancer clinical trials.

摘要

倍半萜内酯(SLs)是植物衍生的化合物,常用于传统医学治疗炎症和癌症。本综述重点介绍了导致增强抗癌和抗炎作用的 SLs 的化学和生物学特性。化学特性包括烷基化中心反应性、亲脂性、分子几何形状和电子特征。临床试验中的 SLs 包括青蒿素、他普西醇和紫铆因及其许多合成衍生物。这些药物通过靶向特定信号通路对肿瘤和癌症干细胞具有选择性,使它们成为癌症临床试验中的先导化合物。

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