Advanced glycation end products (AGEs) play an important role in the development of chronic diabetic complications. Chlorogenic acid (CGA) is a phenolic compound formed by the esterification of caffeic and quinic acids. In this study, we evaluated the inhibitory effects of CGA against the formation of AGEs and AGEs protein cross-linking in vitro. An in vitro assay for glycation of bovine serum albumin by high glucose showed that CGA inhibited AGEs formation with an IC(50) value of 148.32 μM and was found to be more effective than aminoguanidine, a well-known AGEs inhibitor (IC(50); 807.67 μM). In an indirect AGE-ELISA assay, the CGA exhibited more potent inhibitory activity on the cross-linking of AGEs to collagen than aminoguanidine. In addition, the inhibitory effects of CGA on AGEs formation and on its cross-linking with collagen might be caused by its interactions with reactive decarbonyl compounds, such as methylglyoxal. These results suggest that CGA could be beneficial in the prevention of AGEs progression in patients with diabetes because CGA can attenuate AGEs deposition in glucose.