[Synthesis, preliminary antigastrelcosis activity and the protective effect on acute liver injury of zinc chlorin E4].

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 x 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.