alpha-Glucosidase and alpha-Amylase Inhibitors from Arcytophyllum thymifolium

作者:Milella Luigi; Milazzo Stella; De Leo Marinella; Vera Saltos Mariela Beatriz; Faraone Immacolata; Tuccinardi Tiziano; Lapillo Margherita; De Tommasi Nunziatina*; Braca Alessandra
来源:Journal of Natural Products, 2016, 79(8): 2104-2112.
DOI:10.1021/acs.jnatprod.6b00484

摘要

Three new coumarins (1-3), a prenylated flavanone (4), and two iridoids (5 and 6), together with 17 known secondary metabolites, were isolated from the aerial parts of Arcytophyllum thymifolium. The structures of the new compounds were elucidated on the basis of their spectroscopic data. The potential hypoglycemic properties of the new and known compounds were evaluated by measuring their alpha-amylase and alpha-glucosidase inhibitory effects. The iridoid asperulosidic acid (15) and the flavonoid rhamnetin (13) showed the highest activities versus alpha-amylase (IC50 = 69.4 +/- 3.1 and 73.9 +/- 5.9 mu M, respectively). In turn, the new eriodictyol derivative 4 exhibited the most potent effect as an alpha-glucosidase inhibitor, with an IC50 value of 28.1 +/- 2.6 mu M, and was more active than acarbose, used as a positive control. Modeling studies were also performed to suggest the interaction mode of compound 4 in the alpha-glucosidase enzyme active site.

  • 出版日期2016-8