Abstract Title:

Calanolides E1 and E2, two related coumarins fromCambess. (Clusiaceae), displayedactivity against amastigote forms ofand.

Abstract Source:

Nat Prod Res. 2021 Dec ;35(23):5373-5377. Epub 2020 May 22. PMID: 32441133

Abstract Author(s):

Luciana Grus Silva, Kaio S Gomes, Thais A Costa-Silva, Maiara M Romanelli, Andre G Tempone, Patricia Sartorelli, João Henrique G Lago

Article Affiliation:

Luciana Grus Silva


In the present work, the MeOH extract from stem barks ofCambess. (Clusiaceae) displayed activity against amastigote forms ofandand was subjected to a bioactivity-guided fractionation to give two related coumarins - calanolides E1 () and E2 (). Compoundsandwere actives towith ECvalues of 12.1 and 8.2 μM, respectively. When tested againstthe ECvalues were 37.1 and 29.1 μM, respectively. Compound, corresponding toisomer, showed the best selectivity index (SI) with values>24.4 toand>6.9 toin comparison to theisomer. Furthermore, using anmulti-parametric prediction, both compounds did not contain any PAINS sub-structures. Therefore, these data suggest that coumarinsandmay contribute as scaffolds for the design of novel drug candidates for leishmaniasis and Chagas disease.

Study Type : In Vitro Study

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