α-Glucosidase inhibitors from Brickellia cavanillesii. Escandón-Rivera, S., González-Andrade, M., Bye, R., Linares, E., Navarrete, A., & Mata, R. Journal of Natural Products, 2012.
abstract   bibtex   
An aqueous extract from the aerial parts of Brickellia cavanillesii attenuated postprandial hyperglycemia in diabetic mice during oral glucose and sucrose tolerance tests. Experimental type-II DM was achieved by treating mice with streptozotocin (100 mg/kg) and β-nicotinamide adenine dinucleotide (40 mg/kg). These pharmacological results demonstrated that B. cavanillesii is effective for controlling fasting and postprandial blood glucose levels in animal models. The same aqueous extract also showed potent inhibitory activity (IC 50 = 0.169 vs 1.12 mg/mL for acarbose) against yeast α-glucosidase. Bioassay-guided fractionation of the active extract using the α-glucosidase inhibitory assay led to the isolation of several compounds including two chromenes [6-acetyl-5-hydroxy-2,2-dimethyl-2H-chromene (1) and 6-hydroxyacetyl-5-hydroxy-2,2-dimethyl-2H-chromene (2)], two sesquiterpene lactones [caleins B (3) and C (4)] , several flavonoids [acacetin (5), genkwanin (6), isorhamnetin (7), kaempferol (8), and quercetin (9)], and 3,5-di-O-caffeoylquinic acid (10). Chromene 2 is a new chemical entity. Compounds 2, 4, 7, and 9 inhibited the activity of yeast α-glucosidase with IC 50 0.42, 0.28, 0.16, and 0.53 mM, respectively, vs 1.7 mM for acarbose. Kinetic analysis revealed that compounds 4 and 7 behaved as mixed-type inhibitors with K i values of 1.91 and 0.41 mM, respectively, while 2 was noncompetititive, with a K i of 0.13 mM. Docking analysis predicted that these compounds, except 2, bind to the enzyme at the catalytic site. © 2012 The American Chemical Society and American Society of Pharmacognosy.
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 title = {α-Glucosidase inhibitors from Brickellia cavanillesii},
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 year = {2012},
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 abstract = {An aqueous extract from the aerial parts of Brickellia cavanillesii attenuated postprandial hyperglycemia in diabetic mice during oral glucose and sucrose tolerance tests. Experimental type-II DM was achieved by treating mice with streptozotocin (100 mg/kg) and β-nicotinamide adenine dinucleotide (40 mg/kg). These pharmacological results demonstrated that B. cavanillesii is effective for controlling fasting and postprandial blood glucose levels in animal models. The same aqueous extract also showed potent inhibitory activity (IC 50  = 0.169 vs 1.12 mg/mL for acarbose) against yeast α-glucosidase. Bioassay-guided fractionation of the active extract using the α-glucosidase inhibitory assay led to the isolation of several compounds including two chromenes [6-acetyl-5-hydroxy-2,2-dimethyl-2H-chromene (1) and 6-hydroxyacetyl-5-hydroxy-2,2-dimethyl-2H-chromene (2)], two sesquiterpene lactones [caleins B (3) and C (4)] , several flavonoids [acacetin (5), genkwanin (6), isorhamnetin (7), kaempferol (8), and quercetin (9)], and 3,5-di-O-caffeoylquinic acid (10). Chromene 2 is a new chemical entity. Compounds 2, 4, 7, and 9 inhibited the activity of yeast α-glucosidase with IC 50  0.42, 0.28, 0.16, and 0.53 mM, respectively, vs 1.7 mM for acarbose. Kinetic analysis revealed that compounds 4 and 7 behaved as mixed-type inhibitors with K i  values of 1.91 and 0.41 mM, respectively, while 2 was noncompetititive, with a K i  of 0.13 mM. Docking analysis predicted that these compounds, except 2, bind to the enzyme at the catalytic site. © 2012 The American Chemical Society and American Society of Pharmacognosy.},
 bibtype = {article},
 author = {Escandón-Rivera, S. and González-Andrade, M. and Bye, R. and Linares, E. and Navarrete, A. and Mata, R.},
 journal = {Journal of Natural Products},
 number = {5}
}
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