姚建忠, 刘建飞, 张万年, 周有骏, 朱驹, 吕加国, 王小燕. 锌二氢卟吩e4的合成及初步抗胃溃疡活性和对急性肝损伤的保护作用J. 药学学报, 2001, 36(3): 188-191.
引用本文: 姚建忠, 刘建飞, 张万年, 周有骏, 朱驹, 吕加国, 王小燕. 锌二氢卟吩e4的合成及初步抗胃溃疡活性和对急性肝损伤的保护作用J. 药学学报, 2001, 36(3): 188-191.
YAO Jian-zhong, LIU Jian-fei, ZHANG Wan-nian, ZHOU You-jun, ZHU Ju, LU Jia-guo, WANG Xiao-yan. SYNTHESIS, PRELIMINARY ANTIGASTRELCOSIS ACTIVITY AND THE PROTECTIVE EFFECT ON ACUTE LIVER INJURY OF ZINC CHLORIN E4J. Acta Pharmaceutica Sinica, 2001, 36(3): 188-191.
Citation: YAO Jian-zhong, LIU Jian-fei, ZHANG Wan-nian, ZHOU You-jun, ZHU Ju, LU Jia-guo, WANG Xiao-yan. SYNTHESIS, PRELIMINARY ANTIGASTRELCOSIS ACTIVITY AND THE PROTECTIVE EFFECT ON ACUTE LIVER INJURY OF ZINC CHLORIN E4J. Acta Pharmaceutica Sinica, 2001, 36(3): 188-191.

锌二氢卟吩e4的合成及初步抗胃溃疡活性和对急性肝损伤的保护作用

SYNTHESIS, PRELIMINARY ANTIGASTRELCOSIS ACTIVITY AND THE PROTECTIVE EFFECT ON ACUTE LIVER INJURY OF ZINC CHLORIN E4

  • 摘要: 目的 研究锌二氢卟吩e4(1)的合成及实验性抗溃疡活性和对急性肝损伤的保护作用。方法 蚕沙叶绿素粗品经酸碱降解反应制得二氢卟吩e6(3),3经吡啶回流降解制得二氢卟吩e4(2),2与醋酸锌络合制得1;并测定1对消炎痛诱发的大鼠胃溃疡的保护作用及对硫代乙酰胺、四氯化碳所致小鼠急性肝损伤的防治作用。结果 1为新化合物。生物活性实验结果表明,1能显著降低消炎痛诱发的大鼠胃溃疡指数和溃疡个数;能显著降低小鼠硫代乙酰胺或四氯化碳急性肝损伤后升高的SGPT活性。结论 1对消炎痛诱发的大鼠胃溃疡和硫代乙酰胺、四氯化碳所致小鼠急性肝损伤具有显著的保护作用。

     

    Abstract: AIM To study the synthesis of zinc chlorin e4 (1), its experimental antigastrelcosis activity as well as the protection against acute liver injuries. METHODS Chlorin e6 (3) was prepared through acidic and alkaline oxidative degradation using silkworm excrement crude chlorophyll extracts as starting material. Compound 1 was synthesized via Zn(OAc)2 complex action with Chlorin e4 (2) which was prepared by refluxing 3 in pyridine. Gastric ulcers were induced by abdominal injection of 0.2% indomethacin at 20 mg.kg-1 in rats. The ulcer indexes and ulcer numbers in gastric mucosa were determined. Acute liver injuries were induced by abdominal injection of 0.3% thioacetamide (TAA) or 0.3% CCl4 at 20 mg.kg-1 in mice, and activities of SGPT in mice were determined. RESULTS Compound 1 is previously unknown. Compared with control group, abdominal administration of 1 at 100 mg.kg-1 reduced significantly the gastric ulcer index (P<0.001) and the number of ulcer (P<0.001) induced by indomethacin in rats. Abdominal administration of 1 at 100 mg.kg-1×3 exhibited marked inhibitory effects on elevated activities of SGPT induced by TAA (P<0.02) or CCl4 (P<0.01) in mice. CONCLUSION These results show that 1 has significant protective effect against indomethacin-induced gastric lesion in rats and TAA or CCl4 induced acute liver injuries in mice. It is suggested that 1 may be a promising new drug candidate for antigastrelcosis and liver injury protection.

     

/

返回文章
返回