Antioxidant Activity and Neuroprotective Activity of Stilbenoids in Rat Primary Cortex Neurons via the PI3K/Akt Signalling Pathway

作者：Wen, Haichao; Fu, Zheng; Wei, Yangji; Zhang, Xiaoxu; Ma, Liyan; Gu, Liwei; Li, Jingming^*

来源：Molecules, 2018, 23(9): 2328.

DOI：10.3390/molecules23092328

• Alzheimer's disease
• beta-amyloid
• rat primary cortex neurons
• stilbenoids
• secondary metabolites
• biological activity

Antioxidant activity and neuroprotective activity of three stilbenoids, namely, trans-4-hydroxystilbene (THS), trans-3,5,4'-trihydroxy-stilbene (resveratrol, RES), and trans-3',4',3,5-tetrahydroxy-stilbene (piceatannol, PIC), against beta-amyloid (A beta)-induced neurotoxicity in rat primary cortex neurons were evaluated. THS, RES, and PIC significantly scavenged DPPH center dot and center dot OH radicals. All three stilbenoids were able to inhibit A beta neurotoxicity by decreasing intracellular reactive oxygen species (ROS) via the PI3K/Akt signalling pathway. Specifically, stilbenoids significantly promoted Akt phosphorylation; suppressed Bcl-2/Bax expression; and inhibited caspase-9, caspase-3, and PARP cleavage. Molecular docking between stilbenoids with Akt indicated that stilbenoids could form hydrogen bond interactions with the COOH-terminal region of Akt. Additionally, the neuroprotective activity of stilbenoids correlated with the number and position of hydroxyl groups. The lack of meta-dihydroxyl groups on THS did not affect its neuroprotective activity in comparison with RES, whereas the ortho-dihydroxyl moiety on PIC significantly enhanced neuroprotective activity. These results provide new insights into the correlation between the biological activity and chemical structure of stilbenoids.

• 出版日期2018-9
• 单位天津科技大学; McGill; 中国农业大学