Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer’s disease

Li, Renshi; Wang, Xiaobing; Hu, Xiaojun; Kong, Ling–Yi

doi:10.1016/j.bmcl.2013.02.095

Cited by 83 publications

(23 citation statements)

References 35 publications

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“…(IC 50 = 0.28 mg/ml for AChE) leaves (Ndhlala, Aderogba, Ncube, & Van Staden, 2013), or Lavandula viridis L'Her essential oil (IC 50 = 0.42 mg/ml and 0.75 mg/ml for AChE and BuChE, respectively). Moreover, some flavonoids derivatives have demonstrated potential for acetylcholinesterase inhibition (Li, Wang, Hu, & Kong, 2013), but the LP and LN are not purified extracts: they are natural juices enriched with powdered fruits that can be taken regularly. Due to this fact, these results are of interest for developing natural foods using lemon juice Fig.…”

Section: Ache and Buche Inhibitory Activitymentioning

confidence: 99%

Beverages of lemon juice and exotic noni and papaya with potential for anticholinergic effects

et al. 2015

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Section: Ache and Buche Inhibitory Activitymentioning

confidence: 99%

Beverages of lemon juice and exotic noni and papaya with potential for anticholinergic effects

et al. 2015

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“…In the recent years, some research groups selected flavonoids and optimized their chemical structures to develop new anti-AD agents (Fig. 1, A A A A and B B B B' [8,9].…”

Section: Inmentioning

confidence: 99%

Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents

Luo

Wang

Chen

et al. 2016

European Journal of Medicinal Chemistry

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“…However, these drugs have side-effects issues which are exacerbated by their long term used as required for AD treatment in addition to the cost of therapy (Wollen, 2010;Anand & Singh, 2013;Tayeb, Yang, Price, & Tarazi, 2012). affected tissues associated with AD (Li, Wang, Hu, & Kong, 2013).…”

Section: Introductionmentioning

confidence: 99%

Screening Flavonoids for Inhibition of Acetylcholinesterase Identified Baicalein as the Most Potent Inhibitor

Balkis¹,

Tran²,

Lee³

et al. 2015

JAS

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Screening phenolic and polyphenolic compounds for inhibitory activity against electric eels acetylcholinesterase (AChE) identified baicalein, a major flavone derived from the roots of Scutellaria baicalensis, as the most potent inhibitor with IC50 (concentration required for 50% inhibition) of 0.61 µM. None of the hydroxybenzoic and hydroxycinnamic acids screened showed inhibitory activity measured at 100 µM. Structure-activity relationships based on IC50 values of the active flavonoids showed that inhibitory activity (a) required the unsaturated 2-phenyl-chroman structure, (b) has strong requirement for the A-ring A5-OH, A6-OH and A7-OH groups (b) does not depend on B-ring hydroxyl groups, and (d) was reduced by bulky sugar substitution of the saturated C-ring C3-OH. Enzyme kinetic analysis showed that baicalein is a mixed inhibitor of AChE with K 1 (equilibrium constant of dissociation of the inhibitor bound enzyme complex) and K 2 (equilibrium constant of dissociation of the inhibitor bound enzyme-substrate complex) of 0.91 and 1.98 µM, respectively.

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Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer’s disease

Cited by 83 publications

References 35 publications

Beverages of lemon juice and exotic noni and papaya with potential for anticholinergic effects

Beverages of lemon juice and exotic noni and papaya with potential for anticholinergic effects

Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents

Screening Flavonoids for Inhibition of Acetylcholinesterase Identified Baicalein as the Most Potent Inhibitor

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