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


  • Ghulam Abbas Department of Biological Sciences and Chemistry, University of Nizwa, P.O Box 33, Postal Code 616, Birkat Al Mauz, Nizwa, Sultanate of Oman.
  • Ahmed Suliman Al-Harrasi UoN, Chair of Oman’s Medicinal Plants and Marine Natural Products, University of Nizwa, P.O Box 33, Postal Code 616, Birkat Al Mauz, Nizwa, Sultanate of Oman.
  • Hidayat Hussain UoN, Chair of Oman’s Medicinal Plants and Marine Natural Products, University of Nizwa, P.O Box 33, Postal Code 616, Birkat Al Mauz, Nizwa, Sultanate of Oman.
  • Samina Abdul Sattar H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
  • M. Iqbal Choudhary H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan. Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah-21589, Saudi Arabia


Protein glycation, diabetic complications, antiglycation agents, medicinal plants, cytotoxicity, terpenoids, alkaloids


This study was performed to identify new inhibitors of protein glycation in 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 activity in 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 < 16 µM), while gossypolidene-4-aminoantipyrine (5) showed a significant antiglycation activity with IC50 value 82.934±2.924 µM, 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 from Papaver 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 with IC50 values 152.662±5.432, 393.758 ±4.001 µM and 110.203±4.816µM, respectively. Similarly, compounds gossypolidene thiocarbamide (3), deoxypeganine hydrochloride (8), lupinine (10) and cytisine (12) showed moderate inhibition with IC50 values of 401.865 ±18.450, 863.322 ±6.415, 712.176±7.745, and 728.462±2.331 µM, respectively. The results were compared with the standard antiglycation agent, rutin (13) (IC50 =98.012±2.030 µM). Cellular cytotoxicity assay showed only gossypol acetic acid (2) and gossypolidene thiocarbamide (3) as somewhat toxic to 3T3 (mouse fibroblast) cells with IC50 values 2.07 ±0.61 and 5.00 ±1.89 µM, respectively. Cycloheximide was used as a standard in this assay with IC50 value 0.3 ± 0.089 μM


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How to Cite

Ghulam Abbas, Ahmed Suliman Al-Harrasi, Hidayat Hussain, Samina Abdul Sattar, M. Iqbal Choudhary. Identification of natural products and their derivatives as promising inhibitors of protein glycation with non-toxic nature against mouse fibroblast 3T3 cells. ijp [Internet]. 2016 Dec. 31 [cited 2024 Jul. 15];8(4):533-9. Available from:



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