Citation: Ning Cheng, Wen-Bin Yi, Qi-Qin Wang, Sheng-Ming Peng, Xiao-Qing Zou. Synthesis and α-glucosidase inhibitory activity of chrysin, diosmetin, apigenin, and luteolin derivatives[J]. Chinese Chemical Letters, ;2014, 25(7): 1094-1098. doi: 10.1016/j.cclet.2014.05.021 shu

Synthesis and α-glucosidase inhibitory activity of chrysin, diosmetin, apigenin, and luteolin derivatives

1.
a Key Laboratory of Environmentally Friendly Chemistry and Applications of Ministry of Education, College of Chemistry, Xiangtan University, Xiangtan 411105, China;
2.
b Postdoctoral Programme of Chemical Engineering & Technology, Xiangtan University, Xiangtan 411105, China

Corresponding author: Sheng-Ming Peng, Xiao-Qing Zou,
Received Date: 13 March 2014
Available Online: 30 April 2014
Fund Project: This work was financially supported by the Research Fund for the Doctoral Program of Higher Education of China (No. 20114301120004) (No. 20114301120004) Hunan Provincial Natural Science Foundation of China (No. 12JJ6081) (No. 12JJ6081) Dr.'s Start-up Foundation of Xiangtan University (No. 06KZjKZ08035) (No. 06KZjKZ08035)

Several derivatives have been synthesized from chrysin, diosmetin, apigenin, and luteolin, which were isolated from diverse natural plants. The a-glucosidase inhibitory activity of these compounds was evaluated. The glucosidase inhibitory activity of all derivatives (IC50 < 24.396 μmol/L) was higher compared with that of the reference drug, acarbose (IC₅₀=563.601±40.492 mmol/L), and 1-deoxynojirimycin (IC₅₀=226.912±12.573 μmol/L). O³',7-Hexyl diosmetin (IC₅₀=2.406 0.101 mmol/L) was the most potent inhibitor identified. These compounds showed a higher inhibitory ability compared with their precursors except the luteolin derivatives. In general, the inhibitory activity of the synthetic derivatives was enhanced with long alkyl chains at positions 3', 4' and 7 of the flavonoid.
- Derivatives,
- Flavonoid,
- α-ucosidase,
- Inhibition
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