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天然β-咔啉生物碱的体外抗疟活性研究进展。

Review on in-vitro anti-malarial activity of natural β-carboline alkaloids.

机构信息

Department of Pharmacy, Birla Institute of Technology & Science, Pilani-333031, Rajasthan, India.

出版信息

Mini Rev Med Chem. 2013 Oct;13(12):1778-91. doi: 10.2174/1389557511313120008.

DOI:10.2174/1389557511313120008
PMID:24059727
Abstract

Malaria is one of the major health problems in developing countries. It kills 1-2 million people every year and also it affects financial status of many countries. Developed resistance to aminoquinoline (chloroquine), quinoline methanols (Quinine, Mefloquine) created troubles in malarial chemotherapy and signs of appearance of resistance to artemisinin based combination therapy (ACT) created emergency to develop novel antimalarial agents with high efficacy before spreading of resistance to ACT. From the ages natural products played an important role in antimalarial therapy, identification of natural products, semisynthetic and synthetic analogs with potent antiplasmodium activity is one of the best methods to develop novel antimalarial agents. In this review, we are presenting the antimalarial activity of natural β-carboline alkaloids and special interest on manzamine alkaloids and their structure activity relationship.

摘要

疟疾是发展中国家的主要卫生问题之一。它每年导致 100 万人至 200 万人死亡,也影响到许多国家的财政状况。对氨基喹啉(氯喹)、喹啉甲醇(奎宁、甲氟喹)的耐药性发展给疟疾化疗带来了麻烦,青蒿素为基础的联合疗法(ACT)出现耐药迹象也给开发高效新型抗疟药物带来了紧急需求,以防止 ACT 耐药性的扩散。自古以来,天然产物在抗疟治疗中发挥了重要作用,鉴定具有高效抗疟活性的天然产物、半合成和合成类似物是开发新型抗疟药物的最佳方法之一。在这篇综述中,我们介绍了天然β-咔啉生物碱的抗疟活性,特别关注马尼嗪生物碱及其结构-活性关系。

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