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

被引：31

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.

引用

页数：10

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