Handa S S, Sharma A
Department of Pharmaceutical Sciences, Panjab University, Chandigarh.
Indian J Med Res. 1990 Aug;92:276-83.
Andrographolide, a diterpenoid lactone, was isolated (yield 0.78% w/w) from A. paniculata (whole plant). Its LD50 in male mice was 11.46 g/kg, ip. Antihepatotoxic activity of andrographolide (100 mg/kg, ip) was compared with 861.33 mg/kg, ip, of the methanolic extract (equivalent to 100 mg/kg of andrographolide) and 761.33 mg/kg ip, of the andrographolide-free methanolic extract (equivalent to 861.33 mg/kg of the methanolic extract) of the plant, using CCl4-intoxicated rats. Biochemical parameters like serum transaminases--GOT and GPT, serum alkaline phosphatase, serum bilirubin and hepatic triglycerides were estimated to assess the liver function. Overall inhibition of CCl4-induced increase in the five biochemical parameters was found to be 48.6 per cent (andrographolide), 32.0 per cent (methanolic extract) and 15.0 per cent (andrographolide-free methanolic extract). These biochemical observations were supplemented by histopathological examination of the liver slices. Further, andrographolide (100 mg/kg, ip) was found to normalize completely the CCl4-induced increase in the pentobarbitone induced sleep time of mice. The results suggest that andrographolide is the major active antihepatotoxic principle present in A. paniculata.
穿心莲内酯,一种二萜类内酯,从穿心莲(全株)中分离得到(产率0.78% w/w)。其对雄性小鼠的半数致死量为11.46 g/kg,腹腔注射。将穿心莲内酯(100 mg/kg,腹腔注射)的抗肝毒性活性与该植物的甲醇提取物(861.33 mg/kg,腹腔注射,相当于100 mg/kg穿心莲内酯)以及无穿心莲内酯的甲醇提取物(761.33 mg/kg,腹腔注射,相当于861.33 mg/kg甲醇提取物)进行比较,使用四氯化碳中毒的大鼠。通过检测血清转氨酶——谷草转氨酶和谷丙转氨酶、血清碱性磷酸酶、血清胆红素和肝甘油三酯等生化参数来评估肝功能。结果发现,四氯化碳诱导的这五项生化参数升高的总体抑制率分别为:穿心莲内酯48.6%、甲醇提取物32.0%、无穿心莲内酯的甲醇提取物15.0%。这些生化观察结果通过肝脏切片的组织病理学检查得到补充。此外,还发现穿心莲内酯(100 mg/kg,腹腔注射)能使四氯化碳诱导的小鼠戊巴比妥诱导睡眠时间增加完全恢复正常。结果表明,穿心莲内酯是穿心莲中主要的具有抗肝毒性活性的成分。