Anti-cancer potential of sophoridine and its derivatives: Recent progress and future perspectives
Anti-cancer potential of sophoridine and its derivatives: Recent progress and future perspectives
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DOI：
10.1016/j.bioorg.2020.103863
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发表时间：
2020-06-01
影响因子：
5.1
通讯作者：
Martines, Marco Antonio Utrera
中科院分区：
文献类型：
--
作者：
Rashid, Haroon Ur;Rasool, Shagufta;Martines, Marco Antonio Utrera
癌症是第二大死亡原因，2018年全球约有960万人死于癌症。预计到2030年，全世界因癌症死亡的人数将达到1150万。由于癌症的致命性，全世界都在努力对抗它。植物成分如某些生物碱、皂苷、单宁、多酚和萜类化合物表现出抗癌作用。槐定碱是从药用植物苦豆子（Sophora alopecuroides L.）和Euchresta japonica Benth，苦豆子（Sophora alopecuroides Ait.）中国食品药品监督管理局（CFDA）于2005年批准槐定碱作为抗肿瘤药物。本文综述了槐定碱及其衍生物的抗肿瘤活性。槐定碱类似物的功效相对于其半最大抑制浓度（IC 50值）表示。对槐定碱类化合物的构效关系进行了研究。此外，还讨论了抗癌药物的当前市场及其预期增长。展望槐定碱类抗癌药物的发展前景，为开发具有更高预期疗效和最小毒性的新型槐定碱类抗癌药物提供了建议和线索。
Cancer is the second leading cause of mortality and has resulted in about 9.6 million deaths around the world in 2018. Cancer-caused deaths are expected to be 11.5 million by 2030 all over the world. Because of the fatal nature of cancer, substantial efforts are made all over the world to combat it. Phytoconstituents such as certain alkaloids, saponins, tannins, polyphenols, and terpenoids exhibit anticancer effects. Sophoridine is a tetracyclic quinolizidine alkaloid isolated from the stem and leaves of medicinal plants Sophora alopecuroides L., and Euchresta japonica Benth, and roots of Sophora alopecuroides Ait. Chinese Food and Drug Administration (CFDA) approved sophoridine as an antitumor agent in 2005. This review covers the antitumor activities of sophoridine and its derivatives. The efficacy of sophoridine analogs is expressed with respect to their half-maximal inhibitory concentration (IC50 values). Structure-activity relationship (SAR) study for most of the sophoridine derivatives has been explained. Moreover, the current market of anticancer drugs and its expected growth are discussed. Prospects provide suggestions and clues for novel sophoridine-based anticancer agents with enhanced expected efficacy and minimum toxicity.