In vitro and in vivo antimalarial evaluation of semi-synthetic derivatives of gomphostenin |
| |
Authors: | Manisha Sathe MP Kaushik |
| |
Institution: | Discovery Center, Process Technology Development Division, Defence R&D Establishment, Jhansi Road, Gwalior 474 002, MP, India |
| |
Abstract: | A novel series of semi-synthetic gomphostenin derivatives (1–9) were prepared utilizing C-14 hydroxyl group for the first time and studied for their antimalarial properties. In vitro antiplasmodial activity was evaluated against both the chloroquine sensitive and resistant strains of Plasmodium falciparum. Most of the compounds exhibited superior or comparable antiplasmodial activity compared to parent compound, that is, gomphostenin (GN). Based upon in vitro antiplasmodial activity, compounds with IC50 values less than 10 μM were selected for in vivo antiplasmodial evaluation against Plasmodium berghei infection in mice model. GN derivatives 3 and 5 were found to have curative activity with moderate chemosuppression of 65% and 69%, respectively, at the dose level of 150 mg/kg/day. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|