Chemical Constituents from <i>Solenostemma argel</i> and their Cholinesterase Inhibitory Activity

Demmak, Rym Gouta; Bordage, Simon; Bensegueni, Abderrahmane; Boutaghane, Naima; Hennebelle, Thierry; Mokrani, El Hassen; Şahpaz, Sevser

doi:10.20307/nps.2019.25.2.115

Cited by 17 publications

(4 citation statements)

References 29 publications

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“…NMR analyses ( 1 H and 13 C) of these compounds led to the identification of emodin ( 1 ) kaempferol ( 2 ) ( Figure 2 ). The spectroscopic data from the NMR spectra ( Figures S3 and S4 ) corroborate those previously reported in the literature [ 29 , 30 ]. In addition, mass spectrometry analyses were performed to confirm the structures obtained ( Figures S5–S8 ).…”

Section: Resultssupporting

confidence: 88%

Bioguided Isolation of Active Compounds from Rhamnus alaternus against Methicillin-Resistant Staphylococcus aureus (MRSA) and Panton-Valentine Leucocidin Positive Strains (MSSA-PVL)

Zeouk¹,

Ouedrhiri

Sifaoui³

et al. 2021

Molecules

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Despite intensified efforts to develop an effective antibiotic, S. aureus is still a major cause of mortality and morbidity worldwide. The multidrug resistance of bacteria has considerably increased the difficulties of scientific research and the concomitant emergence of resistance is to be expected. In this study we have investigated the in vitro activity of 15 ethanol extracts prepared from Moroccan medicinal plants traditionally used for treatment of skin infections. Among the tested species I. viscosa, C. oxyacantha, R. tinctorum, A. herba alba, and B. hispanica showed moderate anti-staphylococcal activity. However, R. alaternus showed promising growth-inhibitory effects against specific pathogenic bacteria especially methicillin-susceptible Staphylococcus aureus Panton-Valentine leucocidin positive (MSSA-PVL) and methicillin-resistant S. aureus (MRSA). The bioguided fractionation of this plant using successive chromatographic separations followed by nuclear magnetic resonance (NMR) and mass spectrometry (MS) including EIMS and HREIMS analysis yielded the emodin (1) and kaempferol (2). Emodin being the most active with MICs ranging between 15.62 and 1.95 µg/mL and showing higher activity against the tested strains in comparison with the crude extract, its mechanism of action and the structure-activity relationship were interestingly discussed. The active compound has not displayed toxicity toward murine macrophage cells. The results obtained in the current study support the traditional uses of R. alaternus and suggest that this species could be a good source for the development of new anti-staphylococcal agents.

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Section: Resultssupporting

confidence: 88%

Bioguided Isolation of Active Compounds from Rhamnus alaternus against Methicillin-Resistant Staphylococcus aureus (MRSA) and Panton-Valentine Leucocidin Positive Strains (MSSA-PVL)

Zeouk¹,

Ouedrhiri

Sifaoui³

et al. 2021

Molecules

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“…This structural difference may contribute to the higher affinity of myricetin towards BChE. Molecular docking (MD) is a key technique in structural molecular biology, as confirmed by numerous literature reports [96][97][98][99][100]. MD was used to observe and confirm possible interactions between MYR and AChE/BChE, which are important targets for neuroprotection.…”

Section: Resultsmentioning

confidence: 99%

Myricetin Amorphous Solid Dispersions—Antineurodegenerative Potential

Rosiak,

Tykarska,

Cielecka-Piontek

2024

Molecules

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Our research aimed to develop an amorphous solid dispersion (ASD) of myricetin (MYR) with Polyvinylpyrrolidone K30 (PVP30) to enhance its solubility, dissolution rate, antioxidant, and neuroprotective properties. Employing a combination of solvent evaporation and freeze drying, we successfully formed MYR ASDs. XRPD analysis confirmed complete amorphization in 1:8 and 1:9 MYR-PVP weight ratios. DSC thermograms exhibited a single glass transition (Tg), indicating full miscibility. FT-IR results and molecular modeling confirmed hydrogen bonds stabilizing MYR’s amorphous state. HPLC analysis indicated the absence of degradation products, ensuring safe MYR delivery systems. Solubility, dissolution rate (pH 1.2 and 6.8), antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays), and in vitro neuroprotective activities (inhibition of cholinesterases: AChE and BChE) were significantly improved compared to the pure compound. Molecular docking studies revealed that MYR had made several hydrogen, hydrophobic, and π-π stacking interactions, which could explain the compound’s potency to inhibit AChE and BChE. MYR-PVP 1:9 w/w ASD has the best solubility, antioxidant, and neuroprotective activity. Stability studies confirmed the physical stability of MYR-PVP 1:9 w/w ASD immediately after dissolution and for two months under ambient conditions. Our study showed that the obtained ASDs are promising systems for the delivery of MYR with the potential for use in alleviating the symptoms of neurodegenerative diseases.

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“…These neuroprotective effects resulted from the plant’s bioactive compounds, quercetin and kaempferol. Kaempferol also inhibited AChE in a reversible mixed mode manner with an IC 50 value of 12.43 µM [ 33 ], exhibited 2-fold higher inhibitory activity against BChE than AChE [ 34 ], and also delayed memory loss by maintaining climbing ability and reducing AChE activity in a transgenic Drosophila model for AD [ 35 ]. Quercetin also acted as a reversible mixed inhibitor against AChE with an IC 50 value of 4.59 µM [ 36 ], while a 2.9-fold lower IC 50 value against BChE was observed [ 37 ], suggesting greater quercetin inhibitory capacity against BChE.…”

Section: Discussionmentioning

confidence: 99%

Enhancing Therapeutic Efficacy of Donepezil, an Alzheimer’s Disease Drug, by Diplazium esculentum (Retz.) Sw. and Its Phytochemicals

Inthachat,

Chantong,

Pitchakarn

et al. 2024

Pharmaceuticals

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Alzheimer’s disease (AD) is the most common type of dementia and a significant concern to global public health due to the prevalence of aging populations. Donepezil is one of only a few medications approved for use as an anti-AD agent but all have adverse side effects. Reducing the dosage of AD drugs with plant extracts (phytotherapy) while maintaining efficacy is one strategy to minimize adverse side effects. We previously reported the anti-AD properties of an edible fern, Diplazium esculentum (Retz.) Sw. (DE), which inhibited key enzymes involved in AD pathogenesis including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase 1 (BACE-1). This study aimed to determine whether DE exhibited a synergistic effect with donepezil. The enzyme inhibitory assay showed that DE extract and its bioactive compounds, kaempferol, and quercetin, slightly impeded AChE inhibition with donepezil, while DE extract and quercetin showed synergistic or additive effects with donepezil against BChE and BACE-1, respectively. DE extract combined with donepezil also improved eye phenotypes in a Drosophila model of AD by preventing ommatidia atrophia and bristle breakages. Furthermore, the DE extract exhibited no genotoxic activities, as determined by the Ames test. Our data revealed that DE extract showed promise when combined with donepezil during AD treatment by targeting BChE and BACE-1.

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Chemical Constituents from Solenostemma argel and their Cholinesterase Inhibitory Activity

Cited by 17 publications

References 29 publications

Bioguided Isolation of Active Compounds from Rhamnus alaternus against Methicillin-Resistant Staphylococcus aureus (MRSA) and Panton-Valentine Leucocidin Positive Strains (MSSA-PVL)

Bioguided Isolation of Active Compounds from Rhamnus alaternus against Methicillin-Resistant Staphylococcus aureus (MRSA) and Panton-Valentine Leucocidin Positive Strains (MSSA-PVL)

Myricetin Amorphous Solid Dispersions—Antineurodegenerative Potential

Enhancing Therapeutic Efficacy of Donepezil, an Alzheimer’s Disease Drug, by Diplazium esculentum (Retz.) Sw. and Its Phytochemicals

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