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

Abstract

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

Electrochemically Enabled Total Syntheses of Natural Products

“…Perhaps more interestingly, preclinical data of lupinines shows promise as antiglycation agents in patients with diabetes. [136] Oxidation of the lactam 81 was achieved by CCE at a platinum anode in methanolic TEAClO 4 (Scheme 17). The resultant lactam hemiaminal 82 was then subjected to titanium(IV)-mediated cyclization to give bicyclic diester 83 in 77 % isolated yield.…”

“…Ban's studies in this arena also included the total syntheses of (±)‐lupinine ( 84 ) and (±)‐epilupinine ( 85 ) [134] which have exhibited multiple biological applications including mild acetylcholine receptor inhibition, partially hepatotoxicity, [135] and insect antifeedant activity. Perhaps more interestingly, pre‐clinical data of lupinines shows promise as antiglycation agents in patients with diabetes [136] . Oxidation of the lactam 81 was achieved by CCE at a platinum anode in methanolic TEAClO 4 (Scheme 17).…”

The Aza Diels‐Alder Reaction on Brominated Conjugated Dienes

“…The standard Diels-Alder reaction has been widely studied and new variants has been reported in recent years. One of these innovations is the aza Diels-Alder reaction (ADA), [8] which involves nitrogen atoms and has been successfully used in the synthesis of complex natural products, including (�)-lupinine [9] and (�)-epi-lupinine, [9] alkaloids with cytotoxic properties; [10] ipalbidine, [11] an analgesic; [12] and notapoditine B, [13] with cytotoxic activity [13] (Figure 2).…”

Alkaloids of narrow-leaved lupine as a factor determining alternative ways of the crop’s utilization and breeding

“…Lupinine demonstrates moderate antiglycation activity, without any cytotoxic effect (Abbas et al, 2017). It is also characterized by strong insecticidal activity (Campbell et al, 1933).…”