Novel cinnamic acid magnolol derivatives as potent α-glucosidase and α-amylase inhibitors: Synthesis, in vitro and in silico studies

被引：25
|
作者：
Hu, Chun-Mei [1 ]
Wang, Wen-Jing [1 ]
Ye, Yuan-Na [1 ]
Kang, Yu [1 ]
Lin, Jing [1 ]
Wu, Pan-Pan [1 ]
Li, Dong-Li [1 ]
Bai, Li-Ping [3 ]
Xu, Xue-Tao [1 ]
Li, Bao-Qiong [1 ]
Zhang, Kun [1 ,2 ]
机构：
[1] Wuyi Univ, Sch Biotechnol & Hlth Sci, Jiangmen 529020, Peoples R China
[2] Guangdong Univ Technol, Sch Biomed & Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
[3] Macau Univ Sci & Technol, Macau Inst Appl Res Med & Hlth, State Key Lab Qual Res Chinese Med, Macau 999078, Peoples R China
来源：
BIOORGANIC CHEMISTRY | 2021年 / 116卷
关键词：
Cinnamic acid; Magnolol; alpha-Glucosidase; alpha-Amylase; Enzyme inhibition; In silico study; DRUG SYNTHESIS BIODS; KINETICS; DOCKING;
D O I：
10.1016/j.bioorg.2021.105291
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
In this study, twenty novel cinnamic acid magnolol derivatives were synthesized, and screened for their anti hyperglycemic potential. All synthesized compounds exhibited good to moderate alpha-glucosidase and alpha-amylase inhibitory activities with IC50 values: 5.11 +/- 1.46-90.26 +/- 1.85 mu M and 4.27 +/- 1.51-49.28 +/- 2.54 mu M as compared to the standard acarbose (IC50: 255.44 +/- 1.89 mu M and 80.33 +/- 2.95 mu M, respectively). Compound 6j showed the strongest inhibitory activity against alpha-glucosidase (IC50 = 5.11 +/- 1.46 mu M) and alpha-amylase (IC50 = 4.27 +/- 1.51 mu M). Kinetic study indicated that compound 6j was reversible and a mixed type inhibitor against alpha-glucosidase and alpha-amylase. In silico studies revealed the binding interaction between 6j and two enzymes, respectively. Finally, cells cytotoxicity assay revealed that compound 6j showed low toxicity against 3 T3-L1 cells and HepG2 cells.
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页数：10
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