Objective To study the mechanism of acute rejection of human renal transplantation and detect the sensitive markers for early diagnosis of acute rejection. Methods Immunohistochemistry was used to detect the expression of Perforin and Granzyme B molecules during acute rejection in the renal grafts. The immunocytochemical ABC assay and flow cytometry ways were used to detect the expression of Perforin and Granzyme B molecules in peripheral blood. Results Perforin and Granzyme B molecules were increased in all tissue specimens and lymphocytes of peripheral blood during acute rejection. There was a correlation between the Granzyme B and histological changes ( P 0.01 ). Granzyme B was increased about 3 days earlier than the appearance of symptoms, and intensive therapy of acute episodes decreased the expression of two markers. Conclusion Perforin and Granzyme B are useful for monitoring the clinical acute rejection, and they are valuable for diagnosis of earlier acute rejection.