月橘烯碱抗着床作用及其激素活性的研究

小鼠于妊娠第1～3天,po或sc月橘烯碱(yuehchukene)2mg或4mg/kg·d有明显的抗着床作用。金黄地鼠于妊娠1～3天,sc月橘烯碱4mg/kg·d却无此作用。月橘烯碱有明显的雌激素活性,与雌二醇合用有协同作用。该化合物无雄激素或抗雄激素活性;无孕激素或抗孕激素活性。放射受体竞争实验测得月橘烯碱对³H]-雌二醇与雌激素受体特异性结合抑制50%的浓度(IC₅₀)为4.2×10^-6mol/L,表观解离常数(KI)为1.24×10^-6mol/L。说明月橘烯碱与雌激素受体有一定的亲和力。

STUDIES ON ANTI-IMPLANTATION AND HORMONE ACTIVITY OF YUEHCHUKENE, AN ALKALOID ISOLATED FROM THE ROOT OF MURRAYA PANICULATA

Oral or subcutaneous administration of yuehchukene to female mice at the dosage of 2 or 4 mg/kg.d on day 1-3 of gestation resulted in 100% anti-implantation effect. However, yuehchukene at 4 mg/kg.d was found to have no anti-implantation effect in hamsters. Allen-Doisy test showed that yuehchukene had obvious estrogenic activity. Treatment of immature mice with yuehchukene at the dosage of 2 or 4 mg/kg.d for 3 days caused an increase of uterine weight. Combined use of yuehchukene with estradiol was shown to have synergistic effect on promoting uterine growth. Experiments showed that the estrogenic activity of yuehchukene was weaker than that of estriol. The affinity of this compound for estrogen receptor was also found to be weaker than that of estriol.