A b s t r a c tThis study was performed to identify new inhibitors of protein glycation glycation is one of the major causes of late diabetic complications. In this study, terpenoids and alkaloids, isolated from different medicinal plants, along with their derivatives, were evaluated for their antiglycation activity to assess their potential cytotoxicity. Among the tested compounds, gossypol (2,2 1,6,7 and its derivat gazolidone (6), showed a potent antiglycation activity (IC aminoantipyrine (5) showed a significant antiglycation activity with IC µM, in BSA methyl isolated from aphyllin significant inhibition activity with 110.203±4.816µM, respectively. Similarly, compounds gossypol deoxypeganine hydrochloride (8), with IC respectively. The results were compared with the = Cellular cytotoxicity assay showed only gossypol acetic acid (2) and gossypolidene thiocarbamide (3) as somewhat toxic to 3T3 (mouse fibroblast) cells with IC ±0.61 and 5.00 with IC