Potent antiprotozoal activity of a novel semi-synthetic berberine derivative
Potent antiprotozoal activity of a novel semi-synthetic berberine derivative
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DOI：
10.1016/j.bmcl.2011.01.101
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发表时间：
2011-05-01
影响因子：
2.7
通讯作者：
Kinghorn, A. Douglas
中科院分区：
文献类型：
--
作者：
Bahar, Mark;Deng, Ye;Kinghorn, A. Douglas
非洲昏睡病和利什曼病等疾病的治疗往往依赖于相对昂贵或有毒的药物，对目前化疗药物的耐药性是治疗这些疾病和疟疾的一个问题。在这项研究中，一种新的半合成小檗碱类似物，5，6-二氯-8，8-二乙基-13-氧代二氢小檗碱氯化物（1），显示出纳摩尔水平的抗利什曼病、疟疾和锥虫病体外模型的效力，以及在体内内脏利什曼病模型中的活性。由于合成的起始原料，小檗碱半硫酸盐，是廉价的，8，8-二烷基取代的小檗碱类似物可能会导致一类新的负担得起的抗原动物化合物。(C)2011年由Elsevier Ltd.出版
Treatment of diseases such as African sleeping sickness and leishmaniasis often depends on relatively expensive or toxic drugs, and resistance to current chemotherapeutics is an issue in treating these diseases and malaria. In this study, a new semi-synthetic berberine analogue, 5,6-didehydro-8, 8-diethyl-13-oxodihydroberberine chloride (1), showed nanomolar level potency against in vitro models of leishmaniasis, malaria, and trypanosomiasis as well as activity in an in vivo visceral leishmaniasis model. Since the synthetic starting material, berberine hemisulfate, is inexpensive, 8,8-dialkyl-substituted analogues of berberine may lead to a new class of affordable antiprotozoal compounds. (C) 2011 Published by Elsevier Ltd.