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Synthesis Of Ethyl Ferulate And Study On Its Pharmacological

Posted on:2003-08-13Degree:MasterType:Thesis
Country:ChinaCandidate:R T WangFull Text:PDF
GTID:2144360062490701Subject:Pharmacology
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Ethyl ferulate was synthesized with ferulic acid as starting material and its synthetic technics was studied. The activies of ethyl ferulate were investigated in comparison with those of ferulic acid.Section 1 Synthesis of ethyl ferulate.AIM: To esterify ferulic acid and synthesize ethyl ferulate. METHODS: Ethyl ferulate was synthesized from ferulic acid. RESULT: The melting point of ethyl ferulate was 41~42癈 which was in accord with literature. CONCLUSION: This method is feasible for the successful synthesis of ethyl ferulate Section 2 Study on the pharmacological activities of ethyl ferulate The inhibitory effect and mechanism of ethyl ferulate on plateletcongregation induced by ADPAIM: To investigate the inhibitory effect of ethyl ferulate on platelet congregate induced by ADP and platelet intracellular calcium oscillations. METHODS: To observe platelet congregate rate induced by congregater TYXN-91. Platelet intracellular calcium oscillation was observed by laserscanning .RESULTS: The inhibition rates of ethyl ferulate were 26.3 + 3.3, 33.4 ?2.4, 73.4 ?3.1 and 94.9 ?2.7% respectively at different concentrations 0.1,0.5,1.5 ,3.0 niniol-L"1 , higher than that of the group of ferulic acid. The change of API 4.6?.7 induced by ethyl ferulate was much lower than control 10.3+2.6 (n=8, P<0.01). CONCLUSION: Theinhibitory effect of ethyl ferulate on platelet congregation induced by ADP was much more than that of ferulic acid.HI . Protective effect of ethyl ferulate on acute liver injury of miceAIM: To investigate the effect of ferulic acid and ethyl ferulate on acute liver injury of mice. METHODS: (1) To divide 64 mices into 8 group .control , models , ferulic acid 25 mg-kg"1, 50 mg-kg"1,100 mg-kg"1 respectively and ethyl ferulate 25 mg-kg"1 ,50 mg-kg" ^lOOmg-kg"1 ig for 5 days respectively. In all other groups except group control , acute liver injury models of mice were made by CCL4 (156mg kg"1) ip The serum ALT , AST , SGST activities were measured. (2) To divide 48 mices into 6 group, control, models, ferulic acid 50 mg kg^and ethyl ferulate 50 mg- kg"1, 100 mg-kg"1, 200mg kg"1 ig for 5 days respectively. In all other groups except control, acute liver injury models of mice were made by CCL4 (156 mg-kg"1) ip and the level of liver MDA and SOD were measured. Liver mitochondria was observed under electronmicroscope. RESULTS: The AST, ALT, SGST levels in serum and MDA in liver tissue were significantly inhibited. It was also shown that ethyl ferulate could obviously enhanced activities of SOD. CONCLUSION: The protective effect of ethyl ferulate on mice against CCL4 acute liver injury was much better than that of ferulic acid.H . Protective effects of ethyl ferulate on injured vascular endothelialcells (EC) by H2O2.Aim: To observe protective effect of ethyl ferulate on injured vascularendothelial cells (EC) by F^Oi. METHODS: Experiments were divided into control group, model group , ferulic acid group and ethyl ferulate group. The proliferation of vascular endothelial cells was assessed by methyl thiazolyl tetrazolium (MTT) assay. RESULTS: Ethyl ferulate at concentration of0.1 umol-I/'jO.Ol umol-L"1, nmol-L"1 ,0.1 nmol-L"1 could significantly protect vascular endothelial cells from the injure by fyCh . CONCLUSION: ethyl ferulate exerted the protective effects on injured vascular endothelial cells by H2O2.
Keywords/Search Tags:ferulic acid, ethyl ferulate, blood platelets, Ca2+
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