Smilax aristolochiifolia Root Extract and Its Compounds Chlorogenic Acid and Astilbin Inhibit the Activity of α-Amylase and α-Glucosidase Enzymes

Abstract

Regulating activities of α-amylase and α-glucosidase through the use of specific inhibitors is a main strategy for controlling type 2 diabetes. Smilax aristolochiifolia root decoctions are traditionally used in Mexico as hypoglycemic and for weight loss, but the active principles and mechanisms underlying such putative metabolic effects are yet unknown. Here, we isolated the major bioactive compounds from a hydroethanolic extract of S. aristolochiifolia root by fast centrifugal partition chromatography and evaluated their effects against pancreatic α-amylase and yeast α-glucosidase. A chlorogenic acid-rich fraction (CAF) inhibited α-amylase activity with an IC ₅₀ value of 59.28  μg/mL in an uncompetitive manner and α-glucosidase activity with an IC ₅₀ value of 9.27  μg/mL in a noncompetitive mode. Also, an astilbin-rich fraction (ABF) inhibited α-glucosidase activity with an IC ₅₀ value of 12.30  μg/mL, in a noncompetitive manner. CAF inhibition α-amylase was as active as acarbose while both CAF and ABF were 50-fold more potent inhibitors of α-glucosidase than acarbose. The molecular docking results of chlorogenic acid and astilbin with α-amylase and α-glucosidase enzymes correlated with the inhibition mechanisms suggested by enzymatic assays. Our results prove that S. aristolochiifolia roots contain chlorogenic acid and astilbin, which inhibit carbohydrates-hydrolyzing enzymes, suggesting a new mechanism for the hypoglycemic effect reported for this plant.