Objectives: Angina pectoris is usually due to spasm or obstruction of the coronary arteries that furnish blood to the heart muscle. Clinical symptoms include chest pain and discomfort, and the discomfort also can happen in patient's jaw, shoulders, arms, neck, or back. The medications in traditional Chinese medicine are a few for angina pectoris in clinical practice. Furthermore, the effect of Tribulus terrestris (T. terrestris) on coronary artery is unclear. Methods: T. terrestris and its active ingredients including kaempfrol, ruscogenin, protodioscin, protogracillin, and harmine were used in this study to examine their effect on porcine coronary artery. Results: The results showed T. terrestris can induce relaxation of porcine coronary artery in a dose dependent manner after U46619-induced contraction. Conclusions: The results provide a potential to develop T. terrestris for the treatment of angina pectoris in traditional Chinese medicine.