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曼泽明生物碱:分离、细胞毒性、抗疟活性及构效关系研究。

Manzamine alkaloids: isolation, cytotoxicity, antimalarial activity and SAR studies.

机构信息

Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India.

Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra 835215, India.

出版信息

Drug Discov Today. 2014 Nov;19(11):1781-1791. doi: 10.1016/j.drudis.2014.06.010. Epub 2014 Jun 20.

Abstract

The infectious disease Malaria is caused by different species of the genus Plasmodium. Resistance to quinoline antimalarial drugs and decreased susceptibility to artemisinin-based combination therapy have increased the need for novel antimalarial agents. Historically, natural products have been used for the treatment of infectious diseases. Identification of natural products and their semi-synthetic derivatives with potent antimalarial activity is an important method for developing novel antimalarial agents. Manzamine alkaloids are a unique group of β-carboline alkaloids isolated from various species of marine sponge displaying potent antimalarial activity against drug-sensitive and -resistant strains of Plasmodium. In this review, we demonstrate antimalarial potency, cytotoxicity and antimalarial SAR of manzamine alkaloids.

摘要

疟疾病由不同种属的疟原虫引起。奎宁类抗疟药物耐药性的增加以及对青蒿素为基础的联合疗法敏感性降低,增加了对新型抗疟药物的需求。从历史上看,天然产物一直被用于治疗传染病。鉴定具有强效抗疟活性的天然产物及其半合成衍生物是开发新型抗疟药物的重要方法。马钱胺生物碱是一类独特的β-咔啉生物碱,从各种海洋海绵中分离得到,对敏感和耐药的疟原虫菌株均具有很强的抗疟活性。在这篇综述中,我们展示了马钱胺生物碱的抗疟活性、细胞毒性和抗疟构效关系。

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