Anti-5-hydroxytryptamine3 effect of galanolactone, diterpenoid isolated from ginger.

摘要: It has been reported that an acetone extract of ginger and its fractions have anti-5-HT (5-hydroxytryptamine; serotonin) effects. In the present study, guinea pig ileum, rat stomach fundus rabbit aortic strips are used in order to determined constituents fraction 2 which responsible for effect examine their pharmacological properties.The analysis 2-3 indicated galanolactone, a diterpenoid, is one active constituents. galanolactone inhibited contractile responses 5-HT with pIC50 value 4.93. against response 2-methyl-5-HT, selective 5-HT3 agonist, presence methysergide at 1×10-5M was 5.10. values ICS 205-930, antagonist, were 5.30 7.49, respectively. The concentration-response curve shown as biphasic caused shift right second phase.In same preparations, 205-930 carbamylcholine (CCh) 4.45 4.46.The inhibitory on less than ileum.In addition, thoracic aorta precontracted 50 mM K+, relaxing about 1/10 papaverine.These results suggest diterpenoid isolated from ginger, related antagonism receptors.