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ABSTRACT: Context
Bryophyllum pinnatum (Lam.) Oken (Crassulaceae) is used traditionally to treat many ailments.Objectives
This study characterizes the constituents of B. pinnatum flavonoid-rich fraction (BPFRF) and investigates their antioxidant and anticholinesterase activity using in vitro and in silico approaches.Materials and methods
Methanol extract of B. pinnatum leaves was partitioned to yield the ethyl acetate fraction. BPFRF was isolated from the ethyl acetate fraction and purified. The constituent flavonoids were structurally characterized using UPLC-PDA-MS2. Antioxidant activity (DPPH), Fe2+-induced lipid peroxidation (LP) and anticholinesterase activity (Ellman's method) of the BPFRF and standards (ascorbic acid and rivastigmine) across a concentration range of 3.125-100 μg/mL were evaluated in vitro for 4 months. Molecular docking was performed to give insight into the binding potentials of BPFRF constituents against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE).Results
UPLC-PDA-MS2 analysis of BPFRF identified carlinoside, quercetin (most dominant), luteolin, isorhamnetin, luteolin-7-glucoside. Carlinoside was first reported in this plant. BPFRF significantly inhibited DPPH radical (IC50 = 7.382 ± 0.79 µg/mL) and LP (IC50 = 7.182 ± 0.60 µg/mL) better than quercetin and ascorbic acid. Also, BPFRF exhibited potent inhibition against AChE and BuChE with IC50 values of 22.283 ± 0.27 µg/mL and 33.437 ± 1.46 µg/mL, respectively compared to quercetin and rivastigmine. Docking studies revealed that luteolin-7-glucoside, carlinoside and quercetin interact effectively with crucial amino acid residues of AChE and BuChE through hydrogen bonds.Discussion and conclusions
BPFRF possesses an excellent natural source of cholinesterase inhibitor and antioxidant. The material could be further explored for the potential treatment of oxidative damage and cholinergic dysfunction in Alzheimer's disease.
SUBMITTER: Ogidigo JO
PROVIDER: S-EPMC8871626 | biostudies-literature | 2021 Dec
REPOSITORIES: biostudies-literature
Pharmaceutical biology 20211201 1
<h4>Context</h4><i>Bryophyllum pinnatum</i> (Lam.) Oken (Crassulaceae) is used traditionally to treat many ailments.<h4>Objectives</h4>This study characterizes the constituents of <i>B. pinnatum</i> flavonoid-rich fraction (BPFRF) and investigates their antioxidant and anticholinesterase activity using <i>in vitro</i> and <i>in silico</i> approaches.<h4>Materials and methods</h4>Methanol extract of <i>B. pinnatum</i> leaves was partitioned to yield the ethyl acetate fraction. BPFRF was isolated ...[more]