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Nat Prod Res ; 34(12): 1702-1711, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30580627

RESUMO

Betulin (BE) is a pentacyclic triterpenes, obtained from natural sources and with several biological activities described, such as anti-tumoral and anti-inflammatory activities. The BE esterification at hydroxyl group (C-3 and C-28) resulted in five new ester derivatives with different numbers of carbons or halogens (chlorine and fluorine). Among these BE derivatives, two (2a e 2c) were able to significantly decrease IFN-g (*p = 0.0391; **p = 0.0156) and 2c modulated the expression of COX-2 better than Dexamethasone (DEXA). Regarding to cytotoxic assay, the best results were obtained for BE without modifications, with emphasis on tumoral cell lines Raji and MCF-7. The derivatives 2a and 2c showed immunomodulation activity (for the cytokines IFN-g). The presence of chorine in BE seems to be important for the ability of modulate COX-2 expression, since the ester chloride derivative 2c at 100 µM is more powerful inhibitor of COX-2 than DEXA.


Assuntos
Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Ciclo-Oxigenase 2/metabolismo , Interferon gama/antagonistas & inibidores , Fragmentos de Peptídeos/antagonistas & inibidores , Triterpenos/farmacologia , Linhagem Celular Tumoral , Ciclo-Oxigenase 2/efeitos dos fármacos , Citocinas/metabolismo , Ésteres/farmacologia , Halogenação , Humanos , Células MCF-7 , Relação Estrutura-Atividade , Triterpenos/química
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