α-Glucosidase Inhibitors from Salvia circinata. Flores-Bocanegra, L., González-Andrade, M., Bye, R., Linares, E., & Mata, R. Journal of Natural Products, 2017. abstract bibtex © 2017 The American Chemical Society and American Society of Pharmacognosy. A dried infusion prepared from the aerial parts of Salvia circinata did not provoke acute toxicity in mice (LD 50 > 5 g/kg). This infusion showed poor hypoglycemic and antihyperglycemic effects (100-570 mg/kg) when tested in normal and hyperglycemic mice using acute and oral glucose tolerance tests, respectively. However, this infusion possessed antihyperglycemic action in vivo during an oral sucrose tolerance test (31.6-316 mg/kg), suggesting the presence of α-glucosidase inhibitors in S. circinata. Fractionation of a nonpolar extract of the aerial parts of the plant yielded a new biflavone (1) and four new neoclerodane diterpenoid glucosides (2-5) along with the known compounds amarisolide (6), pedalitin (7), apigenin-7-O-β-d-glucoside (8), and the flavone 2-(3,4-dimethoxyphenyl)-5,6-dihydroxy-7-methoxy-4H-chromen-4-one (9). Compounds 1 and 6-9 were active against mammalian α-glucosidases; 6 and 7 were also active against a recombinant α-glucosidase from Ruminococcus obeum and reduced significantly the postprandial peak during an oral sucrose tolerance test in healthy mice, consistent with their α-glucosidase inhibitory activity. Molecular docking and dynamic studies revealed that compounds 6 and 7 might bind to α-glucosidases at the catalytic center of the enzyme.
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title = {α-Glucosidase Inhibitors from Salvia circinata},
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year = {2017},
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abstract = {© 2017 The American Chemical Society and American Society of Pharmacognosy. A dried infusion prepared from the aerial parts of Salvia circinata did not provoke acute toxicity in mice (LD 50 > 5 g/kg). This infusion showed poor hypoglycemic and antihyperglycemic effects (100-570 mg/kg) when tested in normal and hyperglycemic mice using acute and oral glucose tolerance tests, respectively. However, this infusion possessed antihyperglycemic action in vivo during an oral sucrose tolerance test (31.6-316 mg/kg), suggesting the presence of α-glucosidase inhibitors in S. circinata. Fractionation of a nonpolar extract of the aerial parts of the plant yielded a new biflavone (1) and four new neoclerodane diterpenoid glucosides (2-5) along with the known compounds amarisolide (6), pedalitin (7), apigenin-7-O-β-d-glucoside (8), and the flavone 2-(3,4-dimethoxyphenyl)-5,6-dihydroxy-7-methoxy-4H-chromen-4-one (9). Compounds 1 and 6-9 were active against mammalian α-glucosidases; 6 and 7 were also active against a recombinant α-glucosidase from Ruminococcus obeum and reduced significantly the postprandial peak during an oral sucrose tolerance test in healthy mice, consistent with their α-glucosidase inhibitory activity. Molecular docking and dynamic studies revealed that compounds 6 and 7 might bind to α-glucosidases at the catalytic center of the enzyme.},
bibtype = {article},
author = {Flores-Bocanegra, L. and González-Andrade, M. and Bye, R. and Linares, E. and Mata, R.},
journal = {Journal of Natural Products},
number = {5}
}
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