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Potent antiprotozoal activity of a novel semi-synthetic berberine derivative |
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| Authors: | Bahar Mark Deng Ye Zhu Xiaohua He Shanshan Pandharkar Trupti Drew Mark E Navarro-Vázquez Armando Anklin Clemens Gil Roberto R Doskotch Raymond W Werbovetz Karl A Kinghorn A Douglas |
| Affiliation: | a College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA b College of Medicine, The Ohio State University, Columbus, Ohio 43210, USA c Departamento de Química Orgánica, Universidade de Vigo, Vigo 36310, Spain d Department of Chemistry, Carnegie Mellon University, Pittsburgh, PA 15213, USA e Bruker BioSpin Corp., 15 Fortune Dr., Billerica, MA 01821, USA |
| Abstract: | 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. |
| Keywords: | Berberine 5,6-Didehydro-8,8-diethyl-13-oxodihydroberberine chloride African trypanosomiasis Leishmaniasis Malaria Inhibitory activity |
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