Anti-Alzheimer’s Potential of Different Varieties of Piper betle Leaves and Molecular Docking Analyses of Metabolites

Abstract

Introduction: Acetylcholinesterase inhibitors are used to prevent symptoms of Alzheimer's disease which is initiated due to oxidative stress. Piper betle L. is a tropical evergreen perennial vine whose leaves are widely consumed as masticator in Asia and has medicinal properties. Objectives: The present study is aimed to investigate acetylcholinesterase inhibitory property of methanolic extracts of different varieties of Piper betle leaves and chemometrically identify different bioactive ingredients in vitro and in silico. Materials and Methods: Methanol extracts of the leaves collected in February and October from eight varieties of P. betle (Chhanchi, Bagerhati, Manikdanga, Kalibangla, Bangla, Ghanagete, Meetha and Haldi) were studied for acetylcholinesterase inhibitory properties. Chemical components were analyzed by Gas Chromatography -Mass spectrometry and High Performance Thin Layer Chromatography. Active metabolites were identified chemometrically. The activities were proved in vitro and in silico. Results: All the extracts inhibited acetylcholinesterase. Statistical analysis suggested that several phenolic compounds were correlated to anti-cholinesterase activity. Piceatannol, hydroxychavicol, benzene-1,2,4-triol, and 4-methylcatechol are reported here to have such enzyme inhibitory properties. These four small molecules were further subjected to molecular docking analysis to explore their binding mechanism with the acetylcholinesterase enzyme. All the four small molecules are found to interact with the targeted enzyme in similar fashion like the molecular interactions observed for the standard inhibitor, Donepezil, at the active site of acetylcholiesterase. Conclusion: Thus, consumption of P. betle leaves may have a beneficial effect in the prevention and treatment of this neurodegenerative disease.

Anti-Parkinson Potential of Indian Ocimum species in Relation to Active Components as Revealed Using Metabolites Profiling, in vitro and in silico Enzyme Inhibition Studies

“…In contrast, O. gratissimum showed the lowest inhibitory activity. Galantamine, the standard drug as reported previously, 28 exhibited IC 50 at 0.008 mg/mL. Activities of Ocimum leaf extracts were significantly lower than that of galantamine.…”

An overview of Betel vine (Piper Betle L.): Nutritional, pharmacological and economical promising natural reservoir

“…Indigestion, constipation, congestion, cough, and asthma are treated (Peddapalli et al, 2020). The antialzheimer bioactive compounds were found in various varieties of betel vine (De et al, 2021). The following bio chemical roles of phytochemicals from leaves are depicted in figure 5.…”

Isolation, Identification, and Antibacterial Testing of Essential Oil from Green Betel Leaf (Piper Betle L.) Using Well Diffusion Method

“…In particular, the essential oil derived from green betel leaves predominantly comprises terpenoid and phenol derivative compounds [6]. This essential oil from green betel leaves possesses a wide array of important biological properties, including antifungal, antibacterial, antiamoebic [7], antidiabetic, anti-inflammatory [8], antioxidant, antitumor, anti-carcinogenic [9], anti-Alzheimer [10] and antihelminthic [11]. Furthermore, essential oils can be applied to various industries, such as food, perfume, pharmaceutical, and others [12].…”