SYNTHESIS, PRELIMINARY ANTIGASTRELCOSIS ACTIVITY AND THE PROTECTIVE EFFECT ON ACUTE LIVER INJURY OF ZINC CHLORIN E4
- VernacularTitle: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
- Author:
Jianzhong YAO
;
Jianfei LIU
;
Wannian ZHANG
;
Youjun ZHOU
;
Ju ZHU
;
Jiaguo LU
;
Xiaoyan WANG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2001;36(3):188-191
- CountryChina
- Language:Chinese
-
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.
