Luteolin, a flavone, does not suppress postprandial glucose absorption through an inhibition of alpha-glucosidase action.
In order to clarify the postprandial glucose suppression via alpha-glucosidase (AGH) inhibitory action by natural compounds, flavonoids were examined in this study. Among the flavonoids (luteolin, kaempferol, chrysin, and galangin), luteolin showed the potent maltase inhibitory activity with the IC50 of 2.3 mM, while less inhibitions were observed against sucrase. In addition, the effects of maltase inhibition by flavonoids were observed in the descending order of potency of luteolin > kaempferol > chrysin > galangin. Apparently, the AGH inhibition power greatly increased with the replacement of hydroxyl groups at 3' and 4'-position of the B-ring. However, the inhibitory power of luteolin was poorer than a therapeutic drug (acarbose: IC50; 430 nM). As a result of a single oral administration of maltose or sucrose (2 g/kg) in SD rats, no significant change in blood glucose level with the doses of 100 and 200 mg/kg of luteolin was observed. These findings strongly suggested that luteolin given at less than 200 mg/kg did not possess the ability to suppress the glucose production from carbohydrates through the inhibition of AGH action in the gut.
Matsui
Toshiro
T
Department of Bioscience and Biotechnology, Faculty of Agriculture, Graduate School, Kyushu University, Fukuoka, Japan. tmatsui@agr.kyushu-u.ac.jp
Kobayashi
Mio
M
Hayashida
Sachiko
S
Matsumoto
Kiyoshi
K
D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005419:Flavonoids / Q000494:pharmacology*; D005947:Glucose / Q000493:pharmacokinetics*; D065089:Glycoside Hydrolase Inhibitors; D007408:Intestinal Absorption / Q000187:drug effects*; D047311:Luteolin; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
D001786:Blood Glucose; D004791:Enzyme Inhibitors; D005419:Flavonoids; D065089:Glycoside Hydrolase Inhibitors; D005947:Glucose; D047311:Luteolin