This study is to investigate the effects of ceramide on GSTA1 expression in Caco-2 cells.  After being exposed to ceramide for a fixed time, GSTA1 protein expression was detected by Western blotting analysis; GSTA1 mRNA expression was detected by real time PCR; dual luciferase assay was used to analyze GSTA1 transcriptional activity and GSTA1 activity was determined toward androstanedione (AD) as substrate.  The data showed that ceramide can significantly induce the expression of protein and GSTA1 mRNA, and increase transcriptional activity and enzyme activity of GSTA1.  The results demonstrated that ceramide may increase resistance to chemotherapeutics in Caco-2 cells by up-regulating the expression of GSTA1.