Evaluation of cholinesterase inhibitory and antioxidant activity of Wedelia chinensis and isolation of apigenin as an active compound

Abstract

Background Wedelia chinensis has been reported as a folk medicine for the treatment of different diseases including neurodegenerative disease. Although the plant has been studied well for diverse biological activities, the effect of this plant in neurological disorder is largely unknown. The present study was undertaken to evaluate the cholinesterase inhibitory and antioxidant potential of W. chinensis. Methods The extract and fractions of the plant were evaluated for acetylcholinesterase and butyrylcholinesterase inhibitory activity by modified Ellman method. The antioxidant activity was assessed in several in vitro models/assays such as reducing power, total antioxidant capacity, total phenolic and flavonoid content, scavenging of 2,2′-diphenyl-1-picrylhydrazyl (DPPH) free radical and hydroxyl radical, and inhibition of brain lipid peroxidation. Chromatographic and spectroscopic methods were used to isolate and identify the active compound from the extract. Results Among the fractions, aqueous fraction (AQF) and ethylacetate fraction (EAF) exhibited high inhibition against acetylcholinesterase (IC50: 40.02 ± 0.16 μg/ml and 57.76 ± 0.37 μg/ml) and butyrylcholinesterase (IC50: 31.79 ± 0.18 μg/ml and 48.41 ± 0.05 μg/ml). Similarly, the EAF and AQF had high content of phenolics and flavonoids and possess strong antioxidant activity in several antioxidant assays including DPPH and hydroxyl radical scavenging, reducing power and total antioxidant activity. They effectively inhibited the peroxidation of brain lipid in vitro with IC50 values of 45.20 ± 0.10 μg/ml and 25.53 ± 0.04 μg/ml, respectively. A significant correlation was observed between total flavonoids and antioxidant and cholinesterase inhibitory activity. Activity guided chromatographic separation led to the isolation of a major active compound from the EAF and its structure was elucidated as apigenin by spectral analysis. Conclusions The potential ability of W. chinensis to inhibit the cholinesterase activity and peroxidation of lipids suggest that the plant might be useful for the management of AD.

In Vitro and in Silico Analysis of Phytochemicals From Fallopia dentatoalata as Dual Functional Cholinesterase Inhibitors for the Treatment of Alzheimer’s Disease

“…However, several compounds already have been evaluated for their potential anti-cholinesterase effects before, especially flavonoids ( Wu et al, 2017 ; Borowiec et al, 2022 ). For examples, compounds 1 , 5 and 19 showed over 50% inhibitions against AChE and BuChE, which further proved to be comparable with reported values ( Kim et al, 2016 ; Nugroho et al, 2018 ; Islam et al, 2021 ; Karatas et al, 2022 ). In addition, compounds 31 – 33 showed moderate inhibition of AChE, and were determined to be non-competitive inhibitors.…”

Compounds from the Petroleum Ether Extract of Wedelia chinensis with Cytotoxic, Anticholinesterase, Antioxidant, and Antimicrobial Activities

“…W. chinensis is a potential herb used in different traditional medical systems of Bangladesh to treat various ailments [ 3 , 4 , 5 , 6 ]. Until now only several flavonoid compounds have been identified as the major active compounds for anticancer and anticholinesterase activity which are mostly from the polar extract of the plant extract [ 8 , 15 ]. Although numerous compounds have been isolated from the nonpolar extract [ 14 , 16 ], their bioactive potentials are yet to be established.…”

“…Based on repression of androgen receptor activity in prostrate cancer cells, Lin et al identified three flavonoid compounds luteolin, wedelolactone, and apigenin for anticancer properties [ 8 ]. Aminul et al also identified the flavonoid apigenin as the active component for acetylcholinesterase and antioxidant activity [ 15 ]. All these compounds were found in the aqueous or other polar solvent extracts of the plant.…”

“…Huang et al [ 14 ] showed the most potent anti-angiogenic activity in the same petroleum ether extract. We also found good antioxidant and cholinesterase inhibitory properties in the petroleum ether extract [ 15 ]. These results revealed the petroleum ether extract has diverse biological activity.…”

Amelioration effects of the soybean lecithin–gallic acid complex on iron-overload-induced oxidative stress and liver damage in C57BL/6J mice

“…To the best of our knowledge, among of all antioxidant properties, radical scavenging, reducing power and inhibition effect upon linoleic acid autoxidation are most commonly used for the evaluation of antioxidant activity (Islam et al. 2021 ), including the determination of DPPH and ABTS which are synthetic stable free radicals in vitro . Our results showed that SL-GAC may offer resistance against the oxidative stress by scavenging the Fenton hydroxyl radicals, inhibiting peroxidation of linoleic acid, and enhancing ferric reducing power in vitro ( Figure 1 ).…”