Calanolides E1 and E2, two related coumarins from Calophyllum brasiliense Cambess. (Clusiaceae), displayed in  vitro activity against amastigote forms of Trypanosoma cruzi and Leishmania infantum.

Calanolides E1 and E2, two related coumarins from Calophyllum brasiliense Cambess. (Clusiaceae), displayed in vitro activity against amastigote forms of Trypanosoma cruzi and Leishmania infantum. Nat Prod Res. 2020 May 22;:1-5 Authors: Silva LG, Gomes KS, Costa-Silva TA, Romanelli MM, Tempone AG, Sartorelli P, Lago JHG Abstract 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 μM, respectively. When tested against L. infantum, the EC50 values were 37.1 and 29.1 μM, 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. PMID: 32441133 [PubMed - as supplied by publisher]
Source: Natural Product Research - Category: Biochemistry Authors: Tags: Nat Prod Res Source Type: research