Objective:To investigate the effect of TG-6 on myocardial ischemia reperfusion injury in rats and the underlying mechanism. Methods:The drugs were administered by intravenous injection 5 min before ischemia reperfusion(I/R)injury. Myocardial ischemia reperfusion injury(MI/RI)model was treated by 45 min of left anterior descending(LAD)occlusion followed by 24 h of reperfusion. Measurement of rat electrocardiogram(ECG),hematoxylin-eosin(HE)staining of cardiac tissue,serum lactate dehydrogenase(LDH),creatine kinase(CK),superoxide dismutase(SOD)and malondialdehyde(MDA). Serum inflammatory cytokines,such as tumor necrosis factor-α(TNF-α),interleukin-6(IL-6)and interleukin -1β(IL-1β)were measured by ELISA kits. The protein expression of TLR4,IκBα and NF-κB were measured by Western blot. Results:Compared with the I/R group,TG-6 decreased S-T elevation,reduced myocardial pathological lesions,significantly decreased serum LDH,CK,MDA,TNF-α,IL-6,IL-1β content,and increased SOD activity. TG-6 reduced TLR4,IκBα and NF-κB protein expression in cardiac tissue. Conclusion:TG-6 exerts strong favorable cardioprotective function on myocardial I/R injury, which may be related to anti-inflammatory and antioxidant activity.