Isoliquiritigenin, a flavonoid from licorice, plays a dual role in regulating gastrointestinal motility in vitro and in vivo.
Licorice root has been used for years to regulate gastrointestinal function in traditional Chinese medicine. This study reveals the gastrointestinal effects of isoliquiritigenin, a flavonoid isolated from the roots of Glycyrrhiza glabra (a kind of Licorice). In vivo, isoliquiritigenin produced a dual dose-related effect on the charcoal meal travel, inhibitory at the low doses, while prokinetic at the high doses. In vitro, isoliquiritigenin showed an atropine-sensitive concentration-dependent spasmogenic effect in isolated rat stomach fundus. However, a spasmolytic effect was observed in isolated rabbit jejunums, guinea pig ileums and atropinized rat stomach fundus, either as noncompetitive inhibition of agonist concentration-response curves, inhibition of high K(+) (80 mM)-induced contractions, or displacement of Ca(2+) concentration-response curves to the right, indicating a calcium antagonist effect. Pretreatment with N(omega)-nitro-L-arginine methyl ester (L-NAME; 30 microM), indomethacin (10 microM), methylene blue (10 microM), tetraethylammonium chloride (0.5 mM), glibenclamide (1 microM), 4-aminopyridine (0.1 mM), or clotrimazole (1 microM) did not inhibit the spasmolytic effect. These results indicate that isoliquiritigenin plays a dual role in regulating gastrointestinal motility, both spasmogenic and spasmolytic. The spasmogenic effect may involve the activating of muscarinic receptors, while the spasmolytic effect is predominantly due to blockade of the calcium channels.
Chen
Gang
G
Department of Pharmacology, School of Medicine, Wuhan University, Donghu Road, Wuhan 430071, China.
Zhu
Lingxin
L
Liu
Yang
Y
Zhou
Qian
Q
Chen
Hao
H
Yang
Jing
J
D000818:Animals; D047188:Chalcones / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005748:Gastric Fundus / Q000187:drug effects; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006035:Glycyrrhiza / Q000737:chemistry*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007583:Jejunum / Q000187:drug effects; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010276:Parasympatholytics / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D018675:Toxicity Tests
D047188:Chalcones; D010276:Parasympatholytics; C040920:isoliquiritigenin