Kapil A, Koul I B, Banerjee S K, Gupta B D
Department of Pharmacology, Regional Research Laboratory, Jammu, India.
Biochem Pharmacol. 1993 Jul 6;46(1):182-5. doi: 10.1016/0006-2952(93)90364-3.
The diterpenes andrographolide (I), andrographiside (II) and neoandrographolide (III) isolated from Andrographis paniculata were investigated for their protective effects on hepatotoxicity induced in mice by carbon tetrachloride or tert-butylhydroperoxide (tBHP) intoxication. Pretreatment of mice with the diterpenes (I, II & III; 100 mg/kg, i.p.) for 3 consecutive days produced significant reduction in malondialdehyde formation, reduced glutathione (GSH) depletion and enzymatic leakage of glutamic-pyruvate transaminase (GPT) and alkaline phosphatase (AP) in either group of the toxin-treated animals. A comparison with the known hepatoprotective agent silymarin revealed that I exhibited a lower protective potential than II and III, which were as effective as silymarin with respect to their effects on the formation of the degradation products of lipid peroxidation and release of GPT and AP in the serum. GSH status was returned to normal only by III. The greater protective activity of II and III could be due to their glucoside groups which may act as strong antioxidants.
研究了从穿心莲中分离得到的二萜类化合物穿心莲内酯(I)、穿心莲苷(II)和新穿心莲内酯(III)对四氯化碳或叔丁基过氧化氢(tBHP)中毒诱导的小鼠肝毒性的保护作用。连续3天给小鼠腹腔注射二萜类化合物(I、II和III;100 mg/kg)进行预处理,可使两组毒素处理动物的丙二醛生成显著减少、谷胱甘肽(GSH)消耗降低以及谷丙转氨酶(GPT)和碱性磷酸酶(AP)的酶泄漏减少。与已知的肝保护剂水飞蓟宾相比,I的保护潜力低于II和III,II和III在对脂质过氧化降解产物形成以及血清中GPT和AP释放的影响方面与水飞蓟宾一样有效。只有III能使GSH状态恢复正常。II和III具有更强的保护活性可能是由于它们的糖苷基团,这些基团可能作为强抗氧化剂起作用。