Advances in screening assays for identifying cholinesterase ligands

de Oliveira, Pamella C.O.; Tinoco, Luzineide W.; Cardoso, Carmen L.; Cass, Quezia B.; de Moraes, Marcela C.

doi:10.1016/j.trac.2023.117362

Cited by 6 publications

(1 citation statement)

References 55 publications

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“…In Alzheimer's patients, ACh levels are lower than in healthy people. From this point on, inhibiting AChE can increase ACh levels in Alzheimer's patients and thus increase cognitive functions [36]. Likewise, α-amylase and α-glucosidase are the most important enzymes for the hydrolysis of carbohydrates.…”

Section: Enzymes Inhibition Propertiesmentioning

confidence: 99%

Evaluating Phytochemical Profiles, Cytotoxicity, Antiviral Activity, Antioxidant Potential, and Enzyme Inhibition of Vepris boiviniana Extracts

Bakar,

Nilofar,

Mohamed

et al. 2023

Molecules

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In the present study, we performed comprehensive LC-MS chemical profiling and biological tests of Vepris boiviniana leaves and stem bark extracts of different polarities. In total, 60 bioactive compounds were tentatively identified in all extracts. The 80% ethanolic stem bark extract exhibited the highest activity in the ABTS assay, equal to 551.82 mg TE/g. The infusion extract of stem bark consistently demonstrated elevated antioxidant activity in all assays, with values ranging from 137.39 mg TE/g to 218.46 mg TE/g. Regarding the enzyme inhibitory assay, aqueous extracts from both bark and leaves exhibited substantial inhibition of AChE, with EC50 values of 2.41 mg GALAE/g and 2.25 mg GALAE/g, respectively. The 80% ethanolic leaf extract exhibited the lowest cytotoxicity in VERO cells (CC50: 613.27 µg/mL) and demonstrated selective cytotoxicity against cancer cells, particularly against H1HeLa cells, indicating potential therapeutic specificity. The 80% ethanolic bark extract exhibited elevated toxicity in VERO cells but had reduced anticancer selectivity. The n-hexane extracts, notably the leaves’ n-hexane extract, displayed the highest toxicity towards non-cancerous cells with selectivity towards H1HeLa and RKO cells. In viral load assessment, all extracts reduced HHV-1 load by 0.14–0.54 log and HRV-14 viral load by 0.13–0.72 log, indicating limited antiviral activity. In conclusion, our research underscores the diverse bioactive properties of Vepris boiviniana extracts, exhibiting potent antioxidant, enzyme inhibitory, and cytotoxicity potential against cancer cells.

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Section: Enzymes Inhibition Propertiesmentioning

confidence: 99%