摘要
倍半萜内酯由于其强大的生物活性从而引起了大家很大的兴趣,包括在体内研究癌细胞的细胞毒性和抗肿瘤疗效。在这些化合物中,青蒿琥酯,dimethylaminoparthenolide,L12ADT肽前体药物,以及一些毒胡萝卜素的衍生物是目前癌症临床或临床前试验评价的标准。基于几种抗肿瘤的倍半萜内酯结构,一些类似物显示出更大的效果,从而已被分离作为天然产品,部分合成的产品和一些潜在的抗癌药物已被广泛研究。本文重点综述青蒿素,小白菊内酯,毒胡萝卜素,和他们的天然的或合成的类似物中显示出潜在的抗癌活性的部分。这提供了倍半萜内酯作为潜在的抗癌药物的发展进展,包括它们的结构特征、合成改造和抗肿瘤的潜力,其作用及构效关系的机制也正在被讨论中。我们希望这将刺激倍半萜内酯及其衍生物作为新的抗癌药物的发展,对进一步的研究是有帮助的。
关键词: 青蒿素;二聚体青蒿素;dimethylaminoparthenolide;小白菊内酯二聚体;潜在的抗癌药物;倍半萜内酯;胡萝卜素内酯。
Current Medicinal Chemistry
Title:Development of Anticancer Agents from Plant-Derived Sesquiterpene Lactones
Volume: 23 Issue: 23
Author(s): Yulin Ren, Jianhua Yu, A. Douglas Kinghorn
Affiliation:
关键词: 青蒿素;二聚体青蒿素;dimethylaminoparthenolide;小白菊内酯二聚体;潜在的抗癌药物;倍半萜内酯;胡萝卜素内酯。
摘要: Sesquiterpene lactones are of considerable interest due to their potent bioactivities, including cancer cell cytotoxicity and antineoplastic efficacy in in vivo studies. Among these compounds, artesunate, dimethylaminoparthenolide, and L12ADT peptide prodrug, a derivative of thapsigargin, are being evaluated in the current cancer clinical or preclinical trials. Based on the structures of several antitumor sesquiterpene lactones, a number of analogues showing greater potency have been either isolated as natural products or partially synthesized, and some potential anticancer agents that have emerged from this group of lead compounds have been investigated extensively. The present review focuses on artemisinin, parthenolide, thapsigargin, and their naturally occurring or synthetic analogues showing potential anticancer activity. This provides an overview of the advances in the development of these types of sesquiterpene lactones as potential anticancer agents, including their structural characterization, synthesis and synthetic modification, and antitumor potential, with the mechanism of action and structure-activity relationships also discussed. It is hoped that this will be helpful in stimulating the further interest in developing sesquiterpene lactones and their derivatives as new anticancer agents.
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Cite this article as:
Yulin Ren, Jianhua Yu, A. Douglas Kinghorn , Development of Anticancer Agents from Plant-Derived Sesquiterpene Lactones, Current Medicinal Chemistry 2016; 23 (23) . https://dx.doi.org/10.2174/0929867323666160510123255
DOI https://dx.doi.org/10.2174/0929867323666160510123255 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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