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KMID : 0370220070510020150
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Yakhak Hoeji
2007 Volume.51 No. 2 p.150 ~ p.156
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Pharmacological Activities of Flavonoids (V): Spasmolytic Activities of Flavones and Flavonols on Rat Ileal Smooth Muscle Contraction Induced by Electrical Stimulation and Anaphylactic Reaction
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Ahn Hong-Zick
Lee Ji-Yun
Kim Chang-Jong
Park Sung-Hun
Kim Soo-Jeong
Kim Jung-Min
Park Ju-Hyun
Sim Sang-Soo
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Abstract
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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), IC50 of quercetin, apigenin, flavone and rutin were 0.98×10[-5], 1.20×10[-5], 1.55×10[-5] and 1.85×10[-5] M, respectively. Flavonoids at a concentration of 2×10[-5] M also significantly inhibited the anaphylactic contraction and decreased concentration-dependently the mast cell degranulation by anaphylactic reaction, IC50 of quercetin, apigenin, flavone and rutin were 4.0×10[-5], 7.5×10[-5], 8.0×10[-5] and 9.5×10[-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.
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KEYWORD
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flavone, apigenin, quercetin, rutin, flavonoids, rat ileal smooth muscle contraction, anaphylactic contraction
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