Identification of natural products and their derivatives as promising inhibitors of protein glycation with non-toxic nature against mouse fibroblast 3T3 cells

This study was performed to identify new inhibitors of protein glycationin vitro. Protein 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 activityin vitro, while MTT assay on mouse fibroblast 3T3 cells was used to assess their potential cytotoxicity. Among the tested compounds, gossypol (2,2 ′-bis-(formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene) (1), isolated from Gossypium herbaceum,and its derivatives,gossypol acetic acid (2), gossypolidene- 4-aminoantipyrine (4), and gazolidone (6), showed a potent antiglycation activity (IC50< 16µM), while gossypolidene-4-aminoantipyrine (5) showed a significant antiglycation activity with IC50value 82.934 ±2.924µM, in BSA-fluorescence assay. Alkaloid, noscapine (3S)-6,7-Dimethoxy-3-[(5R)-4-methoxy-6-methyl-5,6,7,8-tetrahy-dro-1,3-dioxolo[4,5-g]isoquinolin-5-yl] isobenzofuran-1(3H)-one (7), isolated fromPapaver somniferum, N-nitrosoaphyllinic acid (9), a derivative of alkaloid aphylline,and 2H-quinolizine, octahydro salt (11), a salt of alkaloid lupinine, exhibited significant inhibition activity withIC50values 152.662 ±5.432, 393.758 ±4.001 µM and 110.203±4.816µM, respectively. Similarly, compoundsgossypolidene thiocarbamide (3), deoxypeganine hydrochloride (8),lupinine (10) and cytisine (12) showed moderate inhibition with IC50 values of 401.865...
Source: International Journal of Phytomedicine - Category: Science Authors: Source Type: research