Abstract

IntroductionOdontites serotina is a medicinal plant primarily distributed in northern China. To the best of our knowledge, no previous study has investigated the bioactivities of this plant. The present study investigated the active constituent contents and bioactivities of the 95% ethanol crude extract (ECE) of O. serotina and its fractions. MethodsThe total phenol/flavonoid/iridoid glycoside contents were examined by spectrophotometric methods. DPPH/ABTS assays were used to evaluate the antioxidant activities. α-Glycosidase/α-amylase/AChE/BChE-inhibitory assays were performed to evaluate antidiabetic and anticholinergic activities. Correlations were determined via Pearson's correlation analyses. ResultsThe total phenol/flavonoid contents of the ethyl acetate fraction (EAF) and n-butanol fraction (NBF) and the total iridoid glycoside content of the NBF were determined to be significantly higher than those of the ECE. The EAF and NBF exhibited strong antioxidant and potent inhibitory effects on acetylcholinesterase (AChE), and they also exhibited butylcholinesterase (BChE)/α-glucosidase-inhibitory effects. No sample demonstrated any effects against α-amylase. The correlation analyses indicated strong positive correlations between total phenol content and antioxidant activity and between total flavonoid content and antioxidant/AChE/BChE/α-glucosidase-inhibitory activities. The isolation of the EAF resulted in the acquisition of acteoside (1), emodin (2), benzoic acid (3) and β-sitosterol (4). Acteoside showed moderate antioxidant and BChE/α-glucosidase-inhibitory activities, and emodin exhibited moderate BChE-inhibitory activity. ConclusionThe EAF and NBF are rich in phenols, flavonoids and iridoid glycosides and have antioxidant and dual AChE/BChE and selective α-glycosidase-inhibitory activities. O. serotina has potential in the development of new drugs to treat Alzheimer's disease (AD) and diabetes.

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