Synthesis and biological evaluation of berberine–thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and Aβ aggregation and antioxidant activity

Wu, Kai; Xie, Shishun; Wei, Hui; Yan, Jun; Huang, Ling; Li, Xingshu

doi:10.1016/j.bmc.2013.07.011

Cited by 46 publications

(22 citation statements)

References 31 publications

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“…stably expressing human Swedish mutant APP (Asai et al, 2007;Su et al, 2013;Durairajan et al, 2012;Durairajan et al, 2014). Moreover, berberine reduces learning deficits and increases the long-term spatial memory retention of TgCRND8 transgenic AD mice compared to controls.…”

Section: Berberine Inhibits the Formation Of Pathogenic Aβ And Aβ Aggmentioning

confidence: 92%

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Plant alkaloids as drug leads for Alzheimer's disease

2015

Neurochemistry International

194

114

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Section: Berberine Inhibits the Formation Of Pathogenic Aβ And Aβ Aggmentioning

confidence: 92%

“…Several studies demonstrate that berberine inhibits both AChE and BChE (Abd El-Wahab et al, 2013;Bonesi et al, 2013;Su et al, 2013) with IC 50 of 0.37 and 18.21 µM, respectively.…”

Section: Berberinementioning

confidence: 99%

Plant alkaloids as drug leads for Alzheimer's disease

2015

Neurochemistry International

194

114

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“…3b derivative of berberine with o‐chlorothiophenyl was found not only as a potent AChE inhibitor (IC 50 of 0.042 μM) but also as a potent BuChE inhibitor (IC 50 of 0.662) (Figure ). These hybrids also inhibit βA aggregation and have antioxidant properties (Su et al, ).…”

Section: Natural Productsmentioning

confidence: 99%

Natural products and their derivatives as multifunctional ligands against Alzheimer's disease

Patil

Thakur

Sharma

et al. 2019

Drug Development Research

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Alzheimer's disease (AD), a complex neurodegenerative disorder causing multiple cellular changes including impaired cholinergic system, beta‐amyloid (βA) aggregation, tau hyperphosphorylation, metal dyshomeostasis, neuroinflammation, and many other pathways are involved in the pathogenesis of the disease. However, the exact cause of the disease is not known. Natural products such as flavonoids, alkaloids, resveratrol, and curcumin have multifunctional properties, and have drawn the attention of the researchers because these molecules are capable of interacting concurrently with the multiple targets of AD. Therefore, natural products and their derivatives with proven efficacy could be used in the management of the neurodegenerative disorders. This review focuses on the natural product based multitarget directed ligands like tacrine‐coumarin, tacrine‐huperzine A, harmine‐isoxazoline, berberine‐thiophenyl, galantamine‐indole, pyridoxine‐resveratrol, donepezil‐curcumin and their mode of action.

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“…Dimethyl methylated flavonoid derivatives also exhibited significant inhibition of self‐assembly of Aβ peptide as well as AChE activity . Substituted berberine‐thiophenyl compounds reported as potential inhibitors of Aβ peptide aggregation and AChE activity . Protriptyline‐based compounds interact with monomeric Aβ peptide and prevent aggregation of Aβ peptide as well as inhibit AChE activity by inducing conformational changes in the active site of AChE .…”

Section: Introductionmentioning

confidence: 99%

Thiosemicarbazone Moiety Assist in Interaction of Planar Aromatic Molecules with Amyloid Beta Peptide and Acetylcholinesterase

et al. 2017

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Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder. Aggregation of Aβ peptide, Aβ‐induced cytotoxicity and deficit of the neurotransmitter acetylcholine are strongly linked to the progression of AD. Herein, we synthesized aromatic thiosemicarbazone (TSC) analogues with two, three and four phenyl rings. Result obtained from docking studies showed that hydrophobic aromatic moieties are essential for interaction with aggregation prone region of Aβ peptide while thiosemicarbazone forms hydrogen bonding contacts with peptide residues. Docking studies also demonstrated that phenyl rings and thiosemicarbazone moiety present in TSC 3 forms hydrophobic interactions as well as hydrogen bonding interactions with CAS region of AChE respectively. Results of turbidity assay and ThT assay revealed that TSC 3 with four phenyl rings exhibited improved inhibition of Aβ (1‐42) peptide aggregation. Interestingly, TSC 3 also showed reversal of rough eye phenotype even at 20 μM concentration in the Drosophila model of AD.

show abstract

Synthesis and biological evaluation of berberine–thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and Aβ aggregation and antioxidant activity

Cited by 46 publications

References 31 publications

Plant alkaloids as drug leads for Alzheimer's disease

Plant alkaloids as drug leads for Alzheimer's disease

Natural products and their derivatives as multifunctional ligands against Alzheimer's disease

Thiosemicarbazone Moiety Assist in Interaction of Planar Aromatic Molecules with Amyloid Beta Peptide and Acetylcholinesterase

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