Synthesis, Anticholinesterase, Antioxidant, and Anti‐Aflatoxigenic Activity of Novel Coumarin Carbamate Derivatives. Issue 14 (14th April 2018)

• Record Type: Journal Article
• Authors: Kurt, Belma Zengin; Gazioglu, Isil; Kandas, Nur Ozten; Sonmez, Fatih
• Is Part Of: ChemistrySelect. Volume 3:Issue 14(2018)
• Page Start: 3978
• Page End: 3983
• Publication Date: 2018-04-14
• Subjects: Aflatoxin B1 -- antioxidant activity -- carbamate -- coumarin -- glutathione-s-transferase -- western blot; Chemistry -- Periodicals; 540.5
• DOI: 10.1002/slct.201800142
• Languages: English
• ISSNs: 2365-6549

Abstract

Abstract: New coumarin derivatives with the carbamate moiety were synthesized and their inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 4‐methyl‐2‐oxo‐2H‐chromen‐7‐yl cycloheptylcarbamate (4 h ) showed the strongest inhibition against AChE with IC50 values of 2.30 μM, and 2‐oxo‐2H‐chromen‐7‐yl‐(cyclohexylmethyl)carbamate (4 c ) and 4‐methyl‐2‐oxo‐2H‐chromen‐7‐yl‐(cyclohexylmethyl)carbamate (4 g ) were found to be the most potent BuChE inhibitors with IC50 value of 0.003 μM and 0.004 μM, respectively. Moreover antioxidant, anti‐aflatoxigenic activities, protective effects against aflatoxin‐B1 (AFB1) in H4IIE−C3 cells and effects on glutathione s‐transferase of the synthesized compounds were investigated. The synthesized coumarin carbamates inhibited AFB1 in H4IIE−C3 cells. Western blot analyses confirmed that GSTα protein was induced in cells treated with coumarin carbamates and AFB1. These results showed that the synthesized coumarin carbamates possess a potent protective effect against AFB1. Abstract : Novel coumarin carbamate derivatives was synthesized and their in vitro inhibitory effects on the acetyl‐butyryl cholinesterase enzymes, antiaflatoxigenic, antioxidant properties were evaluated. compound4 h showed the strongest inhibition against AChE with IC50 of 2.30 μM, and compound4 c and compound4 g were found to be the most potent BuChE inhibitors with IC50 of 0.003 μM and 0.004 μM, respectively.4 f showed significantly the best ABTS +. scavenging ability (IC50 = 23.15 μM) and had the highest inhibition against to aflatoxin B1 (71%).