1.School of Chemistry & Chemical Engineering��Shihezi University��Shihezi 832003��China�� 2. School of Medicine��Shihezi University��Shihezi 832003��China
Abstract��
OBJECTIVE To screen the activity of thiazolidine-4-carboxylic acid ethyl ester with cell membrane chromatography(CMC).METHODS The conditions of CMC consisted of cardiac muscle CMC column(50 mm��2 mm) at 37 ��.The mobile phase was 25 mmol��L-1 phosphate buffer(pH 7.4) at the flow-rate of 0.30 mL��min-1.Captopril was used as positive control in the screening.The capacity factors or retention time was used as the chromatographic parameters.The pharmacological effect of compounds was tested by the antihypertensive experiment in SD rats.RESULTS The compounds,except 2-(4-chloro-phenyl)-thiazolidine-4-carboxylic acid ethyl ester,were adsorbed well on cell membrane stationary phase.It was indicated these compounds had physiological activities.The antihypertensive activity of compounds determined in rats showed the compounds,except 2-(4-dimethylamino-phenyl)-thiazolidine-4-carboxylic acid ethyl ester,2-(3-nitro-phenyl)-thiazolidine-4-carboxylic acid ethyl ester and 2-(4-chloro-phenyl)-thiazolidine-4-carboxylic acid ethyl ester,had antihypertensive activity.CONCLUSION The interactions between the compounds and the membrane or membrane receptor were reflected in the cardiac muscle CMC model.The CMC could be used as a good method of qualitative analysis and screen.Most of synthesized compounds could be adsorbed well on cell membrane and had antihypertensive effect.
2008, Vol. 43 