Abstract
BackgroundHawthorn fruit (HF) is a well-known traditional medicine in China with the effects of improving digestion and regulating qi-flowing for removing blood stasis. Modern pharmacological experiments showed that HF extract has various pharmaceutical properties and flavonoids are considered as the main bioactive compounds. In this paper, Diaion HP-20 adsorption chromatography was used to enrich flavonoids in PHF, and the phytochemical composition of EPHF was analyzed by high performance liquid chromatography (HPLC) and liquid chromatography tandem mass spectrometry (LC-MS). In addition, EPHF’s antioxidant capacity, acetylcholinesterase (AChE) inhibitory activity and cytotoxic activity were evaluated.MethodsEPHF was obtained by Diaion HP-20 adsorption chromatography. Phytochemical composition of EPHF was analyzed qualitatively and quantitatively using HPLC and LC-MS. Radical scavenging capacity of EPHF was estimated using 2,2-diphenyl-1-picryhydrazyl (DPPH) assay and oxygen radical absorbance capacity (ORAC) assay. The AChE inhibitory activity of EPHF was evaluated by Ellman method. Cytotoxic activity of EPHF was assessed by means of MTT assay.ResultsEight kinds of components were identified, in which ideain with the value of 179.4 mg/g was identified to be present in the highest level in EPHF, followed by (−)-epicatechin, chlorogenic acid, cyanidin 3-arabinoside, hyperoside and isoquercitrin at the concentrations of 40.9, 10.0, 1.4, 0.4 and 0.2 mg/g, respectively. The contents of these compounds in EPHF were much higher than those in PHF and HF. In addition, EPHF exhibited strong antioxidant and AChE inhibitory activity (ORAC value: 11.65 ± 2.37 μM Trolox equivalents (TE)/mg, DPPH IC50 value: 6.72 μg/mL, anti-AChE activity IC50 value: 11.72 μg/mL) compared with PHF and HF. Moreover, EPHF exhibited high levels of cytotoxicity on MCF-7 and SKOV-3 human tumour cell lines in a dose-dependent manner with the IC50 of 2.76 and 80.11 μg/mL, respectively.ConclusionsMacroporous resin is useful for the extraction and separation of the total flavonoids from PHF. The contents of flavonoids especially anthocyanin in EPHF were increased significantly compared with the PHF, and EPHF exhibited strong antioxidant, AChE inhibitory activity and cytotoxicity on human tumour cells.
Highlights
Hawthorn fruit (HF) is a well-known traditional medicine in China with the effects of improving digestion and regulating qi-flowing for removing blood stasis
The sample was eluted with water, 20%, and 60% ethanol all containing 0.1% (v/v) trifluoroacetic acid subsequently, and the corresponding eluents were analyzed by high performance liquid chromatography (HPLC)
The results showed that flavonoids with diversified structures were enriched in 20% ethanol eluent, while sugar was enriched in the fraction eluted by water, and little flavonoids were detected in 60% ethanol eluent
Summary
Hawthorn fruit (HF) is a well-known traditional medicine in China with the effects of improving digestion and regulating qi-flowing for removing blood stasis. Modern pharmacological experiments showed that HF extract has various pharmaceutical properties and flavonoids are considered as the main bioactive compounds. Hawthorn is distributed in the Northern Hemisphere mostly in China, Europe and North America [1] and has a long history of usage as a traditional medicine. In Europe and America, the extract of hawthorn leaves and flowers In China, hawthorn fruit (HF) has the effects of improving digestion and regulating qi-flowing for removing blood stasis. Modern pharmacological experiments showed that HF extract has anti-tumour, antioxidant [5], anti-aging and prevention of Alzheimer’s effects [6,7,8]. HF extract has the beneficial effects on the cardiovascular system [9,10,11,12]
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