Potent antiprotozoal activity of a novel semi-synthetic berberine derivative

被引：37

作者：

Bahar, Mark ^{[1
]}

Deng, Ye ^{[1
]}

Zhu, Xiaohua ^{[1
]}

He, Shanshan ^{[1
]}

Pandharkar, Trupti ^{[1
]}

Drew, Mark E. ^{[1
,2
]}

Navarro-Vazquez, Armando ^{[3
]}

Anklin, Clemens ^{[5
]}

Gil, Roberto R. ^{[4
]}

Doskotch, Raymond W. ^{[1
]}

Werbovetz, Karl A. ^{[1
]}

Kinghorn, A. Douglas ^{[1
]}

机构：

[1] Ohio State Univ, Coll Pharm, Columbus, OH 43210 USA

[2] Ohio State Univ, Coll Med, Columbus, OH 43210 USA

[3] Univ Vigo, Dept Quim Organ, Vigo 36310, Spain

[4] Carnegie Mellon Univ, Dept Chem, Pittsburgh, PA 15213 USA

[5] Bruker BioSpin Corp, Billerica, MA 01821 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 09期

关键词：

Berberine; 5,6-Didehydro-8,8-diethyl-13-oxodihydroberberine chloride; African trypanosomiasis; Leishmaniasis; Malaria; Inhibitory activity; NEGLECTED TROPICAL DISEASES; LEISHMANIA-DONOVANI; ENANTIA-CHLORANTHA; PARTNERSHIPS; ELIMINATION; ALKALOIDS; FAILURE; BRUCEI; MODELS; DEATH;

D O I：

10.1016/j.bmcl.2011.01.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：2606 / 2610

页数：5

共 36 条

[1]

[Anonymous], NEGLECTED TROPICAL D

[2] NATURAL ABUNDANCE C-13-C-13 COUPLING OBSERVED VIA DOUBLE-QUANTUM COHERENCE [J].