土荆皮甲酸的抗生育作用和毒性

ANTIFERTILITY EFFECTS AND TOXICITY OF PSEUDOLARIC ACID A

土荆皮甲酸(Pseudolaric acid A),是从金钱松(Pseudolarix kamepferi)的根皮中分离得到的一个新型的二萜类化合物,将其混悬于1%羧甲基纤维素中,经口服给药,对大鼠、仑鼠及狗均可产生明显的抗早孕作用,其抗早孕的有效剂量各为7.5mg/kg,60mg/kg,0.5mg/kg qd×3d,土荆皮甲酸经皮下及阴道给药也能产生明显的抗早孕作用,其对大鼠口服的ED_(50),LD_(50)及95%可信限是14.5(11.7～17.7)mg/kg和219.8(193～250)mg/kg,得治疗指数10.2。狗的亚急性毒性试验表明,土荆皮甲酸对狗的中毒作用主要为呕吐、腹泻、便血等消化道的症状,显微镜下可见胃肠道粘膜及粘膜下组织广泛的出血点,其它器官未见到明显的病理变化。

Pseudolaric acid A, a novel diterpenoid, is the active constituent isolated from the root of Pseudolarix kaempferi Gorde. Pseudolaric acid A was suspended in 1%CMC and diluted to the desired concentration for administration and was given orally daily at the doses of 7.5 mg/kg, 60 mg/kg, 0.5 mg/kg on days. 7～9 after mating in rats, hamsters and dogs respectively. Early pregnancies were terminated in all treated animals.In rats and hamsters, subcutaneous or vaginal administrations of pseudolaric acid A were also effective in terminating early pregnancies. It possesses mid-pregnancy termination effect in rats but implantation was not prevented in this species when pseudolaric acid A 20 mg/kg was given orally daily on days 1～3 after mating.In the poisoning effects of pseudolaric acid A, gastrointestinal side-effects play a dominant role.