Baicalein is a potential flavonoid for acetylcholinesterase inhibitor research to treat Alzheimer's disease. Six baicalein derivatives have been semi-synthesized via esterification and amino alkylation reactions. The in vitro acetylcholinesterase inhibitory activity of these derivatives was evaluated with the Ellman method, and certain improvement in the activity of some derivatives is observed. The methyl ester derivative shows the highest activity with an IC50 value of 51.64 µM.
- Dos Santos Picanco LC, Ozela PF, de Fatima de Bri-to Brito M, Pinheiro AA, Padilha EC, Braga FS, et al. Alzheimer's Disease: A Review from the Pathophysiology to Diagnosis, New Perspectives for Pharmacological Treatment. Current medicinal chemistry. 2018;25(26):3141-59. doi: https://doi.org/10.2174/0929867323666161213101126
- Alzheimer's Association. Medications For Memory. Available at: https://www.alz.org/alzheimers-dementia/treatments/medications-for-memory [Accessed 26 May 2020]
- Murray AP, Faraoni MB, Castro MJ, Alza NP, Cavallaro V. Natural AChE Inhibitors from Plants and their Contribution to Alzheimer's Disease Therapy. Current neuropharmacology. 2013;11(4):388-413. doi: https://doi.org/10.2174/1570159X11311040004
- Hoan DQ. Synthesis and biological activity evaluation of some derivatives synthesized from curcumin and curcumin analog. Hue University Journal of Science: Natural Science. 2017;126(1B):127-33. doi https://doi.org/10.26459/hueuni-jns.v126i1B.4139
- Kim JK, Kim YS, Kim Y, et al. Comparative analysis of flavonoids and polar metabolites from hairy roots of Scutellaria baicalensis and Scutellaria lateriflora. World Journal of Microbiology and Biotechnology. 2014;30(3):887‐892. doi: https://doi.org/10.1007/s11274-013-1498-7
- Han J, Ji Y, Youn K. Baicalein as a Potential Inhibitor against BACE1 and AChE: Mechanistic Comprehension through In Vitro and Computational Approaches. 2019;11(11). doi: https://doi.org/10.3390/nu11112694
- Sowndhararajan K, Deepa P, Kim M, Park SJ, Kim S. Baicalein as a potent neuroprotective agent: A review. Biomedicine & pharmacotherapy. 2017;95:1021-32. doi: https://doi.org/10.1016/j.biopha.2017.08.135
- Zhang S-Q, Obregon D, Ehrhart J, Deng J, Tian J, Hou H, et al. Baicalein reduces β-amyloid and promotes nonamyloidogenic amyloid precursor protein processing in an Alzheimer's disease transgenic mouse model. Journal of Neuroscience Research. 2013;91(9):1239-46. doi: https://doi.org/10.1002/jnr.23244
- Francis AC. Organic Chemistry. 10th ed. New York: McGraw-Hill Education; 2016.
- Ellman GL, Courtney KD, Andres V, Jr., Feather-Stone RM. A new and rapid colorimetric determination of acetylcholinesterase activity. Biochemical pharmacology. 1961;7:88-95. doi: https://doi.org/10.1016/0006-2952(61)90145-9
- Wu JY, Chung KT, Liu YW, Lu FJ, Tsai RS, Chen CH, et al. Synthesis and biological evaluation of novel C(6) modified baicalein derivatives as antioxidative agents. Journal of agricultural and food chemistry. 2008;56(8):2838-45. doi: https://doi.org/10.1021/jf073224a
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