RESUMO
Three anthraquinones, Cdc25B phosphatase inhibitors, were isolated from the methanolic extract of the roots of Polygonum multiflorum Thunb. (Polygonaceae). Anthraquinones, physcion (1), emodin (2), and questin (3), inhibited the enzymatic activity of Cdc25B phosphatase with IC(50) values of 62.5, 30, and 34 microg mL(-1), respectively. Emodin (2) and questin (3) strongly inhibited the growth of human colon cancer cells, SW620 with GI(50) values of 6.1 and 0.9 microg mL(-1), respectively. Commercially available anthraquinones, chrysophanol (4), and rhein (5) also inhibited Cdc25B phosphatase with IC(50) values of 10.7 and 22.1 microg mL(-1), respectively.
Assuntos
Proteínas de Ciclo Celular/antagonistas & inibidores , Emodina/análogos & derivados , Emodina/farmacologia , Inibidores Enzimáticos/isolamento & purificação , Raízes de Plantas/química , Polygonum/química , Fosfatases cdc25/antagonistas & inibidores , Linhagem Celular Tumoral , Neoplasias do Colo , Emodina/química , Emodina/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Humanos , Estrutura MolecularRESUMO
Two cyclic diarylheptanoids, garugamblin-3 (1) and acerogenin L (2), isolated from the MeOH extract of the fruits of Alnus japonica Steud., inhibited human low-density lipoprotein (LDL) oxidation in the thiobarbituric acid-reactive substance assay with IC(50) values of 2.9 and 1.7 microM, respectively, and they also inhibited cell-mediated LDL oxidation more than 5 times more strongly than that of a well-known antioxidant, probucol, at a concentration of 10 microM. Compound (1) had no effect on the anti-atherogenesis in low-density lipoprotein receptor-deficient mice.
Assuntos
Heptanos/farmacologia , Lipoproteínas LDL/efeitos dos fármacos , Alnus/química , Animais , Humanos , Lipoproteínas LDL/metabolismo , Camundongos , Oxirredução , Substâncias Reativas com Ácido TiobarbitúricoRESUMO
Two cyclic diarylheptanoids, garugamblin-3 (1) and acerogenin L (2), isolated from the MeOH extract of the fruits of Alnus japonica Steud., inhibited human low-density lipoprotein (LDL) oxidation in the thiobarbituric acid-reactive substance assay with IC50 values of 2.9 and 1.7 microM, respectively, and they also inhibited cell-mediated LDL oxidation more than five times more strongly than that of a well-known antioxidant, probucol, at a concentration of 10 microM. 1 had no effect on the anti-atherogenesis in low-density lipoprotein receptor- deficient mice.
