Pharmacological Activities of Flavonoids (V): Spasmolytic Activities of Flavones and Flavonols on Rat Ileal Smooth Muscle Contraction Induced by Electrical Stimulation and Anaphylactic Reaction

Some flavonoids have spasmolytic activities in various smooth muscles, but structure-activity relationships on their spasmolytic activity and its mechanism are unclear. In this study, effects of flavones (flavone and apigenin) and flavonols (quercetin and rutin) on the rat ileal smooth muscle contraction were studied in vitro and in vitro. In the electric stimulation-induced contraction, all of four flavonoids inhibited concentration-dependently the rat ileal smooth muscle contraction induced by electric stimulation (10 mV, 0.1 cps, 0.1 msec duration), IC$_{50}$ of quercetin, apigenin, flavone and rutin were 0.98${\times}$10$^{-5}$, 1.20${\times}$10$^{-5}$, 1.55${\times}$10$^{-5}$ and 1.85${\times}$10$^{-5}$ M, respectively. Flavonoids at a concentration of 2${\times}$10$^{-5}$ M also significantly inhibited the anaphylactic contraction and decreased concentration-dependently the mast cell degranulation by anaphylactic reaction, IC$_{50}$ of quercetin, apigenin, flavone and rutin were 4.0${\times}$10$^{-5}$, 7.5${\times}$10$^{-5}$, 8.0${\times}$10$^{-5}$ and 9.5${\times}$10$^{-5}$ M, respectively. These results indicated that flavones and flavonols inhibited the rat ileal smooth muscle contraction induced by electric stimulation because of their antagonism against acetylcholine and have spasmolytic activities on anaphylactic contraction which may be due to their mast cell-stabilizing activities. Furthermore, double bond of C$_{2,3}$ in benzene ring of flavonoids may be important in the their antispasmodic activities on the rat ileal smooth muscle contraction induced by electric stimulation and anaphylactic reaction.

Flavonoids의 약리작용(V) - 전기자극 및 과민반응으로 유발된 흰쥐 회장의 평활근수축에서 Flavones 및 Flavonols의 진경효과 -