Abstract: Five kinds of macroporous adsorbent resins including D101, AB-8, NKA-9, S-8, ADS-5 and AB-8resin were selected as a suitable material for the purification of sesame leaf polyphenols by static research, respectively. One factor-at-a-time method was used to determine the optimal operating conditions for purification of the polyphenols from sesame leaf. Then, the protein glycation inhibitory activity of polyphenols aqueous from sesame leaf was evaluated in vitro using the model system of bovine serum albumin and glucose. The results indicated that AB-8 macroporous resin has better adsorption and desorption ability to purify the raw polyphenols. The optimum conditions were as follows:sample solution 12.0mL, raw polyphenols concentration 3.5mg/mL, pH5.0. If the gradient elution was applied using 30% and 50% (v/v) ethanol for 3BV, purification products were named SPP1 and SPP2, the polyphenol contents were 28.43% (SPP1) and 45.71% (SPP2) , respectively, while in crude samples the yield was 16.88%. As to advanced glycation end products (AGEs) formation inhibition activities, the raw polyphenol, SPP1 and SPP2 showed strong inhibitory effect on the development of non-enzymatic glycation reaction, much stronger than that of the positive control (Aminoguanidine) , which suggests potential anti-diabetic properties.