RESUMO
Nineteen isosteviol derivatives were designed and synthesized by C-16, C-19 and D-ring modifications of isosteviol. These compounds were screened for their cytotoxic activities against Hela and A549 cells in vitro. Among them, the inhibitory effect of compounds 3b and 16 on Hela cells was comparable to that of the positive control gefitinib, and the compounds 3b (IC50=7.84 ± 0.84 µM) and 7a (IC50=6.89 ± 0.33 µM) exhibited significant cytotoxicity superior to gefitinib (IC50=11.02 ± 3.27 µM) against A549 cells.
Assuntos
Diterpenos do Tipo Caurano , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Diterpenos do Tipo Caurano/farmacologia , Diterpenos do Tipo Caurano/síntese química , Diterpenos do Tipo Caurano/química , Estrutura Molecular , Células HeLa , Antineoplásicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Células A549 , Gefitinibe/farmacologia , Relação Estrutura-Atividade , Proliferação de Células/efeitos dos fármacos , Quinazolinas/farmacologia , Quinazolinas/química , Quinazolinas/síntese químicaRESUMO
Two new stilbene glucosides, trans-3,5-dihydroxy-4-methoxystilbene 3-O-ß-D-glucopyranoside (1), cis-3,5-dihydroxy-4-methoxystilbene 3-O-ß-D-glucopyranoside (2), one new benzoic acid derivative, cis-4-hydroxy-3-hydroxymethyl-2-butenyl benzoate 4-O-ß-D-glucopyranoside (3), and four known compounds (4 - 7) were isolated from Tournefortia sibirica L. The structures of these compounds were elucidated on the basis of spectral data. Anti-inflammatory effects of compounds (1 - 7) were evaluated in terms of inhibition on production of NO, TNF-α and IL-6 in LPS-induced RAW 264.7 cells. Compounds 1, 2 and 5 - 7 could inhibit the levels of NO, TNF-α and IL-6 in LPS-induced RAW264.7 cells with IC50 values ranging from 40.96 to 88.76 µM.
