title: Natural Prenylchalconaringenins and Prenylnaringenins as Antidiabetic Agents: α-Glucosidase and α-Amylase Inhibition and in Vivo Antihyperglycemic and Antihyperlipidemic Effects.
abstract: Inhibition of α-glucosidase and α-amylase decreases postprandial blood glucose levels and delays glucose absorption, making it a treatment strategy for type 2 diabetes. This study examined in vivo and in vitro antidiabetic activities of natural prenylchalconaringenins 1 and 2 and prenylnaringenins 3 and 4, found in hops and beer. 3'-Geranylchalconaringenin (2) competitively and irreversibly inhibited α-glucosidase (IC50= 1.08 μM) with activity 50-fold higher than that of acarbose (IC50= 51.30 μM) and showed moderate inhibitory activity against α-amylase (IC50= 20.46 μM). Docking analysis substantiated these findings. In addition, compound 2 suppressed the increase in postprandial blood glucose levels and serum levels of total cholesterol and triglycerides in streptozotocin-induced diabetic mice. Taken together, these results suggest that 2 has dual inhibitory activity against α-glucosidase and α-amylase and alleviates diabetic hyperglycemia and hyperlipidemia, making it a potential functional food ingredient and drug candidate for management of type 2 diabetes.
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Hua
authors.identifier: http://orcid.org/0000-0001-9920-6778
authors.initials: H
authors.lastname: Sun
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Wang
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Xiaotong
authors.initials: X
authors.lastname: Song
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Yazhou
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Weina
authors.initials: W
authors.lastname: Ding
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Xiaolin
authors.initials: X
authors.lastname: Peng
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Xiaoting
authors.initials: X
authors.lastname: Zhang
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Yashan
authors.initials: Y
authors.lastname: Li
authors.affiliation: School of Pharmacy, Tianjin Medical University , Tianjin 300070, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Ma
authors.affiliation: School of Pharmacy, Tianjin Medical University , Tianjin 300070, China.
authors.forename: Runling
authors.initials: R
authors.lastname: Wang
authors.affiliation: China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, Tianjin University of Science and Technology , Tianjin 300457, China.
authors.forename: Peng
authors.initials: P
authors.lastname: Yu
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D047188:Chalcones / Q000008:administration & dosage* / Q000737:chemistry; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics / Q000378:metabolism; D044950:Flavanones / Q000008:administration & dosage* / Q000737:chemistry; D065089:Glycoside Hydrolase Inhibitors / Q000008:administration & dosage*; D006801:Humans; D006943:Hyperglycemia / Q000188:drug therapy* / Q000201:enzymology / Q000235:genetics / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000008:administration & dosage*; D008297:Male; D051379:Mice; D010936:Plant Extracts / Q000008:administration & dosage*; D000516:alpha-Amylases / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D000520:alpha-Glucosidases / Q000235:genetics / Q000378:metabolism*
chemical_list: D001786:Blood Glucose; D047188:Chalcones; D044950:Flavanones; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D010936:Plant Extracts; C027329:naringenin chalcone; D000516:alpha-Amylases; D000520:alpha-Glucosidases; C005273:naringenin
keywords: diabetes; docking; prenylchalconaringenin; prenylnaringenin; α-amylase; α-glucosidase