Biological and Pharmaceutical Bulletin p. 231 - 246 (2019)
Update date:2022-08-03
Topics:
Chen, Jiangang
Lu, Wenfang
Chen, Hao
Bian, Xiaoli
Yang, Guangde
In this study, a series of salicylic acid derivatives were designed and synthesized as novel non-saccharide α-glucosidase inhibitors. Biological evaluation indicated that when compared to acarbose, compounds T9, T10, and T32 exhibited a higher potency of α-glucosidase inhibitory activity with IC50 values of 0.15±0.01, 0.086±0.01 and 0.32±0.02mM, respectively. Evaluation of the inhibition kinetics indicated that T9, T10, T32, and acarbose interacted with α-glucosidase in a mixed non-competitive inhibitory manner. Moreover, T9, T10, and T32 statically quenched the fluorescence of α-glucosidase by formation of an inhibitor-α-glucosidase complex. The docking results showed that hydrogen bonds were generated between the test compounds and α-glucosidase. The antioxidant study revealed that compound T10 exhibited a higher antioxidant activity via scavenging 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), thereby inhibiting lipid peroxidation and the total reduction capacity. In brief, the salicylic acid derivatives identified in this study were promising candidates for development as novel non-saccharide α-glucosidase inhibitors.
View MoreJiangsu King Road New Materials Co., Ltd.
website:http://www.jskingroad.com
Contact:0519-85720726 0519-85720721 13584535752
Address:No.1,Weihua Road,Xinbei District,Changzhou City,Jiangsu Province
Contact:86-25-84683399
Address:605, Phoenix Herui Plaza, No.389, South Taiping Road, Nanjing, China 210002
website:http://www.weichichem.com
Contact:+8613912949432
Address:Fine Chemical Industrial Base,Wujiang town,He County,Anhui China.
Suzhou HeChuang Chemical Co.,Ltd.
Contact:+86-512-88800520
Address:No.9 Guanchao Rd,Changshu Advanced Materials Industy Park
Contact:+1-284-4950244
Address:Box 3069, Road Town, Tortola, British Virgin Islands
Doi:10.1021/ja00404a024
(1981)Doi:10.1002/hlca.19510340425
(1951)Doi:10.1248/cpb.23.133
(1975)Doi:10.3390/molecules22111924
(2017)Doi:10.1080/00397910008087086
(2000)Doi:10.1016/j.jfluchem.2005.12.020
(2006)