期刊
NATURAL PRODUCT RESEARCH
卷 35, 期 23, 页码 5373-5377出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2020.1765347
关键词
Calophyllum brasiliense Cambess; Clusiaceae; coumarins; Trypanosoma cruzi; Leishmania infantum
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo
The MeOH extract from Calophyllum brasiliense stems exhibited activity against Trypanosoma cruzi and Leishmania infantum, leading to the isolation of two coumarins calanolides E1 and E2. Compound E2 demonstrated the best selectivity index among the two compounds, suggesting their potential as scaffolds for novel drug candidates for leishmaniasis and Chagas disease.
In the present work, the MeOH extract from stem barks of Calophyllum brasiliense Cambess. (Clusiaceae) displayed activity against amastigote forms of Trypanosoma cruzi and Leishmania infantum and was subjected to a bioactivity-guided fractionation to give two related coumarins - calanolides E1 (1) and E2 (2). Compounds 1 and 2 were actives to T. cruzi with EC50 values of 12.1 and 8.2 mu M, respectively. When tested against L. infantum, the EC50 values were 37.1 and 29.1 mu M, respectively. Compound 2, corresponding to anti isomer, showed the best selectivity index (SI) with values >24.4 to T. cruzi and >6.9 to L. infantum in comparison to the syn isomer 1. Furthermore, using an in silico multi-parametric prediction, both compounds did not contain any PAINS sub-structures. Therefore, these data suggest that coumarins 1 and 2 may contribute as scaffolds for the design of novel drug candidates for leishmaniasis and Chagas disease.
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