《生命科学》 2015, 27(8): 1005-1019

植物次生代谢产物及其衍生物的抗肿瘤成药研究进展

王红晓1，闵军霞1， 2*

（1 浙江大学医学院第一附属医院， 杭州 310003；2 浙江大学转化医学研究院， 杭州 310058）

摘　要：摘　要：面对严重威胁健康的肿瘤，人类从未间断过抗肿瘤药物的研发。纵观历史，从非选择性的化疗药物，到特异性阻断驱动致癌基因的靶向药物，直到今天以患者为中心的个体化肿瘤治疗，抗癌药物迅猛发展，成为提高肿瘤患者生存率的重要治疗手段。然而，由于大多数抗癌药物存在难以克服的短期耐药及毒副作用等问题，严重影响临床治疗效果。近年，筛选植物来源的天然提取物及其次生代谢产物的抗癌作用，倍受关注并取得令人瞩目的进展，包括临床广泛应用的紫杉醇、长春新碱、依托泊苷及喜树碱等。总结植物的抗肿瘤活性成分、筛选方法、潜在作用机制及临床应用等国内外研究现状，旨在为植物来源的抗肿瘤药物的深入研发提供参考。

Advances in discovering anticancer agents from plant secondary metabolites    and their derivatives

WANG Hong-Xiao1， MIN Jun-Xia1，2*

(1 The First Affiliated Hospital， School of Medicine， Zhejiang University， Hangzhou 310003， China; 2 Institute of Translational Medicine， School of Medicine， Zhejiang University， Hangzhou 310058， China)

Abstract: Abstract: Cancer is a big threat to human beings. From historical perspective， it goes through two paradigm shifts in anticancer drug discovery. The first is from “non-selective chemotherapeutics” to highly selective “molecular targeted cancer therapeutics”， and the second is from “disease centered” drug discovery phase to the “patient-centered” personalized cancer therapeutics. Although much progress has been made， there are still limited effective options for most cancer patients. Recently， a great attention has been paid to screening effective components from plant extracts， including the most widely used chemotherapy agents such as paclitaxel， vincristine， etoposide， and irinotecan. In this review article， we summarize the current progress of the antitumor activity of plant extracts， the proposed potential molecular mechanisms， clinical application， and screening methods. In addition， this review explores and discusses potential strategies to facilitate discovery of effective anticancer agents from plant secondary metabolites and the derivatives.