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来自树木的抗癌生物碱:向药物的转化

Anticancer Alkaloids from Trees: Development into Drugs.

作者信息

Isah Tasiu

机构信息

Department of Botany, Cellular Differentiation and Molecular Genetics Section, Hamdard University, New Delhi, India.

出版信息

Pharmacogn Rev. 2016 Jul-Dec;10(20):90-99. doi: 10.4103/0973-7847.194047.

DOI:10.4103/0973-7847.194047
PMID:28082790
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5214563/
Abstract

Trees have made an enormous phytochemical contribution in anticancer drugs' development more than any other life form. The contributions include alkaloids that are biosynthesized in various ways and yield. Lead alkaloids isolated from the trees are taxol and camptothecins that currently have annual sales in billion dollars. Other important alkaloids isolated from these life forms include rohitukine, harringtonine, acronycine, thalicarpine, usambarensine, ellipticine, and matrines. Studies on their mechanism of action and target on the DNA and protein of cancerous cells aided the development of potent hemisynthesized congeners. The molecules and their congeners passed/are passing a long period of historical development before approved as antineoplastic drugs for cancer chemotherapy. Some of them did not find the application as anticancer drugs due to ineffectiveness in clinical trials; others are generating research interest in the antineoplastic activity at the present and have reached clinical trial stages. Potentials in antineoplastic molecules from trees are high and are hoped to be commensurate with cancer types afflicting human society in the future.

摘要

在抗癌药物的研发中,树木所做出的植物化学贡献比其他任何生命形式都要大。这些贡献包括以各种方式生物合成的生物碱及其产量。从树木中分离出的主要生物碱是紫杉醇和喜树碱,它们目前的年销售额达数十亿美元。从这些生命形式中分离出的其他重要生物碱包括洛石碱、高三尖杉酯碱、山油柑碱、紫堇碱、乌桑巴拉新碱、玫瑰树碱和苦参碱。对它们作用机制以及对癌细胞DNA和蛋白质靶点的研究,推动了高效半合成类似物的开发。这些分子及其类似物在被批准用于癌症化疗的抗肿瘤药物之前,经历了漫长的历史发展过程。其中一些由于在临床试验中无效而未能作为抗癌药物得到应用;其他一些目前正在引发人们对其抗肿瘤活性的研究兴趣,并已进入临床试验阶段。来自树木的抗肿瘤分子潜力巨大,有望在未来与困扰人类社会的各类癌症相匹配。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a854/5214563/9f5340ac3f53/PRev-10-90-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a854/5214563/d62a6678a9b4/PRev-10-90-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a854/5214563/9f5340ac3f53/PRev-10-90-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a854/5214563/d62a6678a9b4/PRev-10-90-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a854/5214563/9f5340ac3f53/PRev-10-90-g003.jpg

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