UPLC-PDA-ESI-QTOF-MS/MS fingerprint of purified flavonoid enriched fraction of ; antioxidant properties, anticholinesterase activity and in studies.

CONTEXT

(Lam.) Oken (Crassulaceae) is used traditionally to treat many ailments.

OBJECTIVES

This study characterizes the constituents of flavonoid-rich fraction (BPFRF) and investigates their antioxidant and anticholinesterase activity using and approaches.

MATERIALS AND METHODS

Methanol extract of 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-MS. Antioxidant activity (DPPH), Fe-induced lipid peroxidation (LP) and anticholinesterase activity (Ellman's method) of the BPFRF and standards (ascorbic acid and rivastigmine) across a concentration range of 3.125-100μg/mL were evaluated 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-MS 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 (IC = 7.382 ± 0.79 µg/mL) and LP (IC = 7.182 ± 0.60 µg/mL) better than quercetin and ascorbic acid. Also, BPFRF exhibited potent inhibition against AChE and BuChE with IC 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.