Novel betulin derivatives inhibit IFN-γ and modulates COX-2 expression.

Autor: Gonçalves, Sayonara Maria Calado, Silva, Glória Najara, Pitta, Ivan da Rocha, Rêgo, Moacyr Jesus Barreto de Melo, Gnoato, Simone Cristina Baggio, Pitta, Maira Galdino da Rocha
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Zdroj: Natural Product Research; Jun2020, Vol. 34 Issue 12, p1702-1711, 10p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index