| Autor: |
Gonçalves SMC; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil., Silva GN; Organic Synthesis Laboratory of Phytochemistry, Federal University of Rio Grande do Sul, Porto Alegre, Brazil., Pitta IDR; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil., Rêgo MJBM; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil., Gnoato SCB; Organic Synthesis Laboratory of Phytochemistry, Federal University of Rio Grande do Sul, Porto Alegre, Brazil., Pitta MGDR; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil. |
| 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 . |
