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Active components of Ligustrum lucidum inhibiting hepatitis C virus replicase activity / 药学学报
Acta Pharmaceutica Sinica ; (12): 1390-1396, 2013.
Artigo em Chinês | WPRIM | ID: wpr-259464
ABSTRACT
Based on previous report that the Chinese herb Ligustrum lucidum (LL) extract directly inhibited hepatitis C virus (HCV) replicase (NS5B) activity, the active components of LL extract to inhibit HCV NS5B activity and their inhibition mode were investigated in this study. LL extract was separated using ethyl acetate and thin layer chromatography (TLC). The inhibitory activity of separated fractions on HCV NS5B was analyzed by the inhibitory assay of NS5B activity. The results showed that only fractions 1 and 2 inhibited NS5B activity, and fraction 2 possessed higher inhibitory activity than fraction 1. HPLC analysis combined with inhibitory assays indicated that ursolic acid and oleanolic acid are the active components within fractions 1 and 2 to inhibit NS5B activity, separately. Moreover, oleanolic acid possessed higher inhibitory activity than ursolic acid. Further inhibition mode analysis found that both oleanolic acid and ursolic acid suppressed NS5B activity as noncompetitive inhibitors. The Ki values of ursolic acid and oleanolic acid were about 4.7 microg x mL(-1) (10 micromol x kg(-1)) and 2.5 microg x mL(-1) (5.5 micromol x kg(-1)), respectively. Taken together, these results demonstrated that oleanolic acid and ursolic acid suppressed NS5B activity as noncompetitive inhibitors, implying that the two natural products have potential value for HCV therapy.
Assuntos
Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Ácido Oleanólico / Antivirais / Farmacologia / Plantas Medicinais / Triterpenos / Medicamentos de Ervas Chinesas / Química / Cromatografia Líquida de Alta Pressão / Proteínas não Estruturais Virais / Ligustrum Limite: Humanos Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2013 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Ácido Oleanólico / Antivirais / Farmacologia / Plantas Medicinais / Triterpenos / Medicamentos de Ervas Chinesas / Química / Cromatografia Líquida de Alta Pressão / Proteínas não Estruturais Virais / Ligustrum Limite: Humanos Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2013 Tipo de documento: Artigo