Aim To study the effects of simvastatin,probucol and captopril on regression and stabilization of atherosclerosis, and to explore the expression of matrix metalloproteinase-1 (MMP-1) and tissue inhibitor of metalloproteinases-1 (TIMP-1). Methods 50 rabbits were induced to atherosclerosis by feeding cholesterol and then treated with simvastatin, probucol, captopril respectively for 12 weeks. The tissues of abdominal aorta were studied by reverse transcription polymerase chain reaction (RT-PCR), pathology and immunohistochemistry staining. Results The lipids were decreased in the drug-therapy groups significantly (p<0.05), especially in probucol and simvastatin groups. The atherosclerosis regressed significantly in the drug-therapy groups (p<0.05), and simvastatin had the best result. The expression of mRNA level of collagen Ⅰ, MMP-1 and TIMP-1 was decreased in drug-therapy groups, but was statistically significant only in the probucol group (p<0.01). Conclusion Simvastatin, probucol and captopril could regress the atherosclerosis and stabilize the plaque by reducing the expression of MMP-1.