OBJECTIVE To study the effect and mechanism of saffor injection on renal ischemia/reperfusion (I/R) injury in rats. METHODS Seventy-five SD rats were randomly divided into five groups (n = 15, in each), normal control groups, I/R control groups, low-dose treatment groups, middle-dose treatment groups and high-dose treatment groups. After rat's I/R injury model was established, renal function was assessed by measuring serum creatinine, blood urea nitrogen, urine osmotic pressure and urine osmotic pressure/blood osmotic pressure, the apoptosis rate in I/R renal tissure was measured by TUNEL method and caspase-3 concentration was measured by immunohistochemistry. RESULTS Reperfusion of the ischemic kidney induced marked renal dysfunction. Saffor injection significantly inhibited the reperfusion-associated increase in apoptosis rate and caspase-3 protein absorbance value. Moreover, the renal dysfunction at all treatment groups was markedly ameliorated by Saffor injection. (P < 0.01). CONCLUSIONS The results show that saffor injection significantly reduces the renal dysfunction and injury caused by I/R of the kidney, And the protective effect of Saffor injection may be related to the inhibition of cell apoptosis and caspase-3 gene expression following renal I/R.