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士槿乙酸甙(PAG)对小鼠有明显的抗早孕作用。其抗早孕作用的ED_(50)=128.83±4.27mg/kg,p=0.95。PAG的抗早孕作用可被甲地孕酮所拮抗。用250mg/kg的PAG能明显抑制假孕小鼠的蜕膜反应,外源性甲地孕酮能对抗其抑制假孕小鼠的蜕膜反应。早孕大鼠给予皮下注射PAG 24h后,其血浆孕酮值没有明显下降。PAG既没有雌激素样活性,也没有抗雌激素活性。其抗早孕的有效剂量能使蜕膜细胞变性坏死。此外,低浓度的PAG对早孕大鼠离体子宫肌的收缩活动没有兴奋作用,而高浓度时表现为抑制作用。
The gentian acetic acid glycoside (PAG) has a significant anti-pregnancy effect in mice. The effect of early pregnancy on ED_(50) was 128.83±4.27 mg/kg, p=0.95. The anti-pregnancy effects of PAG can be antagonized by megestrol. With PAG of 250 mg/kg, the decidual reaction of pseudopregnant mice can be significantly inhibited. Exogenous megestrol can counteract the decidual reaction in mice that inhibit pseudopregnant mice. The plasma progesterone levels in early pregnancy rats did not decrease significantly after subcutaneous injection of PAG for 24 hours. PAG has neither estrogen-like activity nor anti-estrogen activity. Its anti-pregnancy effective dose can make the decidual cells degeneration and necrosis. In addition, low concentrations of PAG had no stimulatory effect on the contractile activity of isolated uterine muscles in early pregnancy rats, but showed inhibitory effect at high concentrations.