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精选天然产物作为抗癌治疗药物的疗效。

Efficacy of selected natural products as therapeutic agents against cancer.

作者信息

Banerjee Sanjeev, Wang Zhiwei, Mohammad Mussop, Sarkar Fazlul H, Mohammad Ramzi M

机构信息

Department of Pathology, School of Medicine, Wayne State University, Detroit, Michigan 48201, USA.

出版信息

J Nat Prod. 2008 Mar;71(3):492-6. doi: 10.1021/np0705716. Epub 2008 Feb 27.

Abstract

With emerging sophistication in the exploration of ocean environment, a number of marine bioactive products have been identified with promising anticancer activity. Many of these are in active phase I or phase II clinical trials or have been terminated because of adverse side effects, mainly hematological in nature. Nonetheless, the information derived has aided enormously in providing leads for laboratory synthesis with modifications in the parent structure affecting compound solubility, absorption, and toxicity, resulting in less severe toxicity while achieving maximum efficacy in smaller doses. We describe herein, a few of the compounds obtained from marine and terrestrial sources [bryostatin 1 ( 1), dolastatin 10 ( 2), auristatin PE ( 3), and combretastatin A4 ( 4)] that have been extensively investigated in our laboratory and continue to be investigated for their sensitization effects with other cytotoxic agents in several different site-specific tumors employing murine models or human subjects.

摘要

随着海洋环境探索技术的日益成熟,已鉴定出许多具有潜在抗癌活性的海洋生物活性产品。其中许多正处于I期或II期临床试验的活跃阶段,或者由于主要是血液学性质的不良副作用而被终止。尽管如此,所获得的信息极大地有助于为实验室合成提供线索,对母体结构进行修饰以影响化合物的溶解度、吸收和毒性,从而在小剂量下实现最大疗效的同时降低毒性。我们在此描述了一些从海洋和陆地来源获得的化合物[苔藓抑素1(1)、多拉司他汀10(2)、奥瑞他汀PE(3)和康普瑞他汀A4(4)],这些化合物在我们实验室中已得到广泛研究,并继续在使用小鼠模型或人类受试者的几种不同部位特异性肿瘤中研究它们与其他细胞毒性药物的致敏作用。

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