C‑methylated Flavanones with Antitrypanosomal Activity Isolated of Geopropolis from Melipona mondury

从蜜蜂蜂(Melipona mondury)蜂胶中分离得到的具有抗锥虫活性的C-甲基化黄烷酮

阅读:1

Abstract

Geopropolis is a natural antibiotic produced by stingless bees, supplemented with earth and clay. Bee products are a promising source of natural bioactive compounds with potential for the development of new drugs for neglected tropical diseases, such as Chagas disease. This study analyzed extracts of Melipona mondury geopropolis from the Bosque da Barra da Tijuca (RJ, Brazil) and evaluated their activity against Trypanosoma cruzi. The extracts were obtained using commercial grain alcohol 96° GL and fractionated with hexane and dichloromethane. The antichagasic activity was determined, with IC(50) values ranging from 4.54 to 53.02 μg/mL. Phytochemical investigation of the dichloromethane fraction resulted in the isolation of two C-methylated flavanones, (2S)-strobopinin and (2S)-cryptostrobin, which were identified for the first time in Brazilian geopropolis. These compounds showed IC(50) values of 21.21 μM and 21.55 μM, respectively, with distinct cytotoxities: 33.80 μM for strobopinin and 99.79 μM for cryptostrobin. Molecular modeling studies were conducted to propose a mechanism of action on a candidate enzyme target, glyceraldehyde-3-phosphate dehydrogenase, and possible reasons for the selectivity differences caused by C-methylation. The results highlight M. mondury geopropolis as a promising natural source of antiparasitic agents, supporting its potential for drug development.

特别声明

1、本页面内容包含部分的内容是基于公开信息的合理引用;引用内容仅为补充信息,不代表本站立场。

2、若认为本页面引用内容涉及侵权,请及时与本站联系,我们将第一时间处理。

3、其他媒体/个人如需使用本页面原创内容,需注明“来源:[生知库]”并获得授权;使用引用内容的,需自行联系原作者获得许可。

4、投稿及合作请联系:info@biocloudy.com。