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Objective: To study the effect of levocitine (L-CN) on tissue inhibitor of metalloproteinase-1 (TIMP-1) and intercellular adhesion molecule-1 (ICAM-1) expression of rats with coronary heart disease and evaluate the protective effect of L-CN on myocardial cells. Methods: High-fat diet feeding and intraperitoneal injection of pituitrin was performed on rats in model group and CHD Model of rats was built. Rats with successful model-building were selected and divided into L-CN group and Ctrl group randomly. Rats in L-CN group were given L-CN treatment, with intraperitoneal injection of 200 mg?kg-1?d-1 and successive administration for 3 d. Rats in Ctrl group were given equal volumes of normal saline. Blood was collected from carotid artery at different time and expression quantity of creatine kinase-MB (CK-MB) and Troponin Ⅰ (TnⅠ)in serum was detected. Rats in each group were put to death and were separated to obtain the myocardial tissue. Real-time PCR and West Blotting hybridization were performed to detect the TIMP-1, ICAM-1 expression in myocardial tissue in each group. Statistical analysis was employed to explore the expression changes of TIMP-1 and ICAM-1, and ELISA test was used to analyse the expression changes of myocardial necrosis marker- CK-MB and TnⅠ to le the effect of L-CN and its myocardial protective effect. Results: The total cholesterol, triglyceride and blood glucose levels of rats in model group were significantly higher than that in control group, which indicated that due to high-fat diet feeding, blood lipid of rats in model group was obviously higher than that in control group. In myocardial tissue of rats in model group, TIMP-1 level significantly reduced and ICAM-1 level significantly increased (P<0.01). In model group, after L-CN treatment, TIMP-1 level had double increase, while ICAM-1 level had 43% of decrease in L-CN group compared with Ctrl group. After L-CN intervention treatment, CK-MB and TnⅠ contentin L-CN group relatively reduced compared with Ctrl group. The difference among groups was obvious (P<0.01). Conclusions: L-CN could increase the TIMP-1 expression level and inhibit the ICAM-1 expression level. L-CN has a certain myocardial protective effect.