| Journal: | Brazilian Journal of Pharmaceutical Sciences |
| Database: | PERIÓDICA |
| System number: | 000452250 |
| ISSN: | 1984-8250 |
| Authors: | Xu, Qian1 Zhang, Luyun2 Xia, Guangqing2 Zhan, Dazhao2 Zhu, Junyi2 Zang, Hao1 |
| Institutions: | 1Yanbian University, College of Medicine, Yanji, Yanbian. China 2Tonghua Normal University, School of Pharmacy and Medicine, Tonghua, Jilin. China |
| Year: | 2022 |
| Volumen: | 58 |
| Country: | Brasil |
| Language: | Inglés |
| Document type: | Artículo |
| Approach: | Experimental, aplicado |
| English abstract | A series of Trolox amide derivatives were synthesized by modifying the carboxyl groups of Trolox. Thirty target compounds were obtained and characterized through nuclear magnetic resonance and mass spectrometry. Trolox derivatives were employed to explore the potential structure-antioxidant activity relationships. The antioxidant activities of these compounds were evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP) and hydroxyl radical assays. DPPH scavenging activity test results illustrated that compounds exhibited scavenging activities similar to L-ascorbic acid and Trolox, with compounds 14a, 18a, 24a and 26a in particular exhibiting higher scavenging activities than L-ascorbic acid. The results demonstrated that compounds displayed ABTS scavenging activities similar to L-ascorbic acid and Trolox, with compounds 26a and 29a in particular having potency twofold higher. FRAP assay results indicated that compounds 11a, 19a, 25a, 29a and 30a had activity similar to Trolox. The results revealed that compounds 6a and 19a had similarly high hydroxyl radical-scavenging activities as Trolox. The results of α-glucosidase experiments uncovered that compounds 10a, 25a, 28a and 29a had excellent inhibitory activity, which was similar to that of acarbose and different from Trolox. The results of acetylcholinesterase and butyrylcholinesterase experiments demonstrated that some compounds had weak anticholinesterase activities. 26a and 29a are important Trolox derivatives with better biological activity profiles and deserve further study |
| Disciplines: | Química |
| Keyword: | Química farmacéutica, Vitamina E, Trolox, Actividad antioxidante, Actividad hipoglucemiante, Actividad anticolinesterásica |
| Keyword: | Medicinal chemistry, Vitamin E, Trolox, Antioxidant activity, Hypoglycemic activity, Anticholinesterase activity |
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