Cholinesterase inhibitory, anti-amyloidogenic and neuroprotective effect of the medicinal plant Grewia tiliaefolia - An in vitro and in silico study

药用植物 Grewia tiliaefolia 的胆碱酯酶抑制、抗淀粉样变性和神经保护作用 - 体外和计算机模拟研究

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作者:Dicson Sheeja Malar, Rajamohamed Beema Shafreen, Shunmugiah Karutha Pandian, Kasi Pandima Devi

Conclusion

Grewia tiliaefolia can be considered as a promising therapeutic agent for the treatment of AD.

Results

Antioxidant assays demonstrated that the MEGT showed significant free radical scavenging activity at the IC50 value of 71.5 ± 1.12 μg/mL. MEGT also exhibited significant dual cholinesterase inhibition with IC50 value of 64.26 ± 2.56 and 54 ± 0.7 μg/mL for acetyl and butyrylcholinesterase (BChE), respectively. Also, MEGT showed significant anti-aggregation activity by preventing the oligomerization of Aβ25-35. Further, MEGT increased the viability of Neuro2a cells up to 95% against Aβ25-35 neurotoxicity. LC-MS analysis revealed the presence of 16 compounds including vitexin, ellagic acid, isovitexin, etc. In silico analysis revealed that vitexin binds effectively with AChE through strong hydrogen bonding. These results were further confirmed by evaluating the activity of vitexin in vitro, which showed dual cholinesterase inhibition with IC50 value of 15.21 ± 0.41 and 19.75 ± 0.16 μM for acetyl and butyrlcholinesterase, respectively.

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