The discovery of potential anticholinesterase compounds from Achillea millefolium L.

Sevindik, Handan G.; Güvenalp, Zühal; Yerdelen, Kadir Özden; Yuca, Hafize; Demirezer, L. Ömür

doi:10.1016/j.indcrop.2015.05.088

Cited by 25 publications

(20 citation statements)

References 31 publications

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“…It was shown that 6-OH-luteolin 7-O-β-d-glucoside had significant in silico and in vitro BChE and AChE inhibitory effects with an IC 50 of 1.97 and 1.65 µM, respectively, in comparison with a standard of neostigmine (IC 50 4.36 and 1.08 µM). Collectively, these findings suggest that 6-OH-luteolin 7-O-β-d-glucoside might be developed as a novel therapeutic agent for AD management [240]. Another group has isolated 13 flavonoid derivatives along with two ginkgolides from the leaves of Ginkgo biloba.…”

Section: Role Of Flavonoids As Cholinesterase Inhibitorsmentioning

confidence: 96%

“…A research group has isolated and screened several potent flavonoids with cholinesterase inhibitors activity from the aerial part of Achillea millefolium (yarrow) [240]. It was shown that 6-OH-luteolin 7-O-β-d-glucoside had significant in silico and in vitro BChE and AChE inhibitory effects with an IC 50 of 1.97 and 1.65 µM, respectively, in comparison with a standard of neostigmine (IC 50 4.36 and 1.08 µM).…”

Section: Role Of Flavonoids As Cholinesterase Inhibitorsmentioning

confidence: 99%

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Molecular Insight into the Therapeutic Promise of Flavonoids against Alzheimer’s Disease

et al. 2020

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Alzheimer’s disease (AD) is one of the utmost chronic neurodegenerative disorders, which is characterized from a neuropathological point of view by the aggregates of amyloid beta (Aβ) peptides that are deposited as senile plaques and tau proteins which form neurofibrillary tangles (NFTs). Even though advancement has been observed in order to understand AD pathogenesis, currently available therapeutic methods can only deliver modest symptomatic relief. Interestingly, naturally occurring dietary flavonoids have gained substantial attention due to their antioxidative, anti-inflammatory, and anti-amyloidogenic properties as alternative candidates for AD therapy. Experimental proof provides support to the idea that some flavonoids might protect AD by interfering with the production and aggregation of Aβ peptides and/or decreasing the aggregation of tau. Flavonoids have the ability to promote clearance of Aβ peptides and inhibit tau phosphorylation by the mTOR/autophagy signaling pathway. Moreover, due to their cholinesterase inhibitory potential, flavonoids can represent promising symptomatic anti-Alzheimer agents. Several processes have been suggested for the aptitude of flavonoids to slow down the advancement or to avert the onset of Alzheimer’s pathogenesis. To enhance cognitive performance and to prevent the onset and progress of AD, the interaction of flavonoids with various signaling pathways is proposed to exert their therapeutic potential. Therefore, this review elaborates on the probable therapeutic approaches of flavonoids aimed at averting or slowing the progression of the AD pathogenesis.

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Section: Role Of Flavonoids As Cholinesterase Inhibitorsmentioning

confidence: 96%

Section: Role Of Flavonoids As Cholinesterase Inhibitorsmentioning

confidence: 99%

Molecular Insight into the Therapeutic Promise of Flavonoids against Alzheimer’s Disease

et al. 2020

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“…To get insights on the intermolecular interactions, four flavonoids contained in the Artemisia copa infusion: apigenin-7-O-glucoside, kaempferol-3-O-galactoside, kaempferol-3-O-acetyl-glucoside and kaempferol-7-rhamnoside (which are in high amount and proportion in this species), as well as the known cholinesterase inhibitor galantamine (Supplementary Figure S2), were selected and subjected to molecular docking studies over AChE (TcAChE) and BChE (hBChE) (Full description, Supplementary Material). The relationship between flavonoids and their potential as cholinesterase inhibitors have been reported (Sevindik et al, 2015;Khan et al, 2018). Table 4 shows the binding energies expressed in kcal/mol of every compound mentioned above.…”

Section: Molecular Docking Studiesmentioning

confidence: 99%

Chemical Profiling, Antioxidant, Anticholinesterase, and Antiprotozoal Potentials of Artemisia copa Phil. (Asteraceae)

Larrazábal

Fernández-Galleguillos

Palma-Ramírez

et al. 2020

Front. Pharmacol.

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Artemisia copa Phil. (Asteraceae) (known as copa-copa) is a native species of Chile used as an infusion in traditional medicine by Atacameños people in the Altiplano, highlands of northern Chile. In this research, we have investigated for the first time the cholinesterase inhibition potential against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and the chemical profiling of the infusions prepared from the aerial parts of A. copa by high resolution spectrometry. In addition, total phenolic, total flavonoid content, antioxidant (DPPH, FRAP, and ORAC) and antiprozoal activity were tested. Artemisia copa showed good inhibitory activity against AChE and BChE (3.92 ± 0.08 µg/ml and 44.13 ± 0.10 µg/ml). The infusion displayed a total phenolics content of 155.6 ± 2.9 mg of gallic acid equivalents/g and total flavonoid content of 5.5 ± 0.2 mg quercetin equivalents/g. Additionally, trypanocidal activity against Trypanosoma cruzi was found (LD50 of 131.8 µg/ml). Forty-seven metabolites were detected in the infusion of A. copa including several phenolic acids and flavonoids which were rapidly identified using ultrahigh performance liquid chromatography orbitrap mass spectrometry analysis (UHPLC-Orbitrap-MS) for chemical profiling. The major compounds identified in the infusions were studied by molecular docking against AChE and BChE. The UHPLC-MS fingerprints generated can be also used for the authentication of these endemic species. These findings reveal that A. copa infusions can be used as beverages with protective effects.

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“…Qiao-Qiao Lu and Ya-Ming Chen contributed equally to this work and should be regarded as co-first authors. Sevindik, Güvenalp, Erdelen, Yuca, & Demirezer, 2015). Among them some of flavonoid derivatives show better inhibition on AChE than their parent flavonoids (Luo, Chen, Wang, Hong, & Wang, 2015;Khan et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Nitrogen‐containing flavonoid and their analogs with diverse B‐ring in acetylcholinesterase and butyrylcholinesterase inhibition

Chen

Liu

et al. 2020

Drug Development Research

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In this study, a series of new flavones (2-phenyl-chromone), 2-naphthyl chromone, 2-anthryl-chromone, or 2-biphenyl-chromone derivatives containing 6 or 7-substituted tertiary amine side chain were designed, synthesized, and evaluated in acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition. The results indicated that the alteration of aromatic ring connecting to chromone scaffold brings about a significant impact on biological activity. Compared with flavones, the inhibitory activity of 2-naphthyl chromone, 2-anthryl-chromone derivatives against AChE significantly decreased, while that of 2-biphenyl chromone derivatives with 7-substituted tertiary amine side chain is better than relative flavones derivatives. For all new synthesized compounds, the position of tertiary amine side chain obviously influenced the activity of inhibiting AChE. The results above provide great worthy information for the further development of new AChE inhibitors. Among the newly synthesized compounds, compound 5a is potent in AChE inhibition (IC 50 = 1.29 ± 0.10 μmol/L) with high selectivity for AChE over BChE (selectivity ratio: 27.96). An enzyme kinetic study of compound 5a suggests that it produces a mixed-type inhibitory effect against AChE.

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The discovery of potential anticholinesterase compounds from Achillea millefolium L.

Cited by 25 publications

References 31 publications

Molecular Insight into the Therapeutic Promise of Flavonoids against Alzheimer’s Disease

Molecular Insight into the Therapeutic Promise of Flavonoids against Alzheimer’s Disease

Chemical Profiling, Antioxidant, Anticholinesterase, and Antiprotozoal Potentials of Artemisia copa Phil. (Asteraceae)

Nitrogen‐containing flavonoid and their analogs with diverse B‐ring in acetylcholinesterase and butyrylcholinesterase inhibition

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