The antihyperglycaemic activity of berberine arises from a decrease of glucose absorption.
The mechanism of action of berberine as an antihyperglycaemic agent was investigated in the Caco-2 cell line. Berberine was found to effectively inhibit the activity of disaccharidases in Caco-2 cells. It also decreased sucrase activity after preincubation with Caco-2 cells for 72 hours. However gluconeogenesis and glucose consumption of Caco-2 cells were not influenced. 2-Deoxyglucose transporting through Caco-2 cell monolayers was decreased by berberine but the effect was not statistically significant. These results suggest that the antihyperglycaemic activity of berberine is at least partly due to its ability to inhibit alpha-glucosidase and decrease glucose transport through the intestinal epithelium.
Pan
Guo-Yu
GY
Center of Pharmacokinetics, China Pharmaceutical University, Nanjing, China.
Huang
Zhi-Jiang
ZJ
Wang
Guang-Ji
GJ
Fawcett
J Paul
JP
Liu
Xiao-Dong
XD
Zhao
Xiao-Chen
XC
Sun
Jian-Guo
JG
Xie
Yuan-Yuan
YY
D001599:Berberine / Q000494:pharmacology*; D018938:Caco-2 Cells; D004789:Enzyme Activation; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005943:Gluconeogenesis; D005947:Glucose / Q000096:biosynthesis / Q000378:metabolism*; D065089:Glycoside Hydrolase Inhibitors; D006801:Humans; D006943:Hyperglycemia / Q000517:prevention & control*; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007408:Intestinal Absorption; D013393:Sucrase / Q000378:metabolism; D000520:alpha-Glucosidases / Q000378:metabolism
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D001599:Berberine; D000520:alpha-Glucosidases; D013393:Sucrase; D005947:Glucose