Antioxidant and Antidiabetic Activity of Cornus mas L. and Crataegus monogyna Fruit Extracts.

The present study evaluated three green extraction methods, accelerated solvent extraction (ASE), ultrasound-assisted extraction (UAE), and laser irradiation extraction (LE), for the polyphenolic compounds and vitamin C extraction of Cornus mas L. and Crataegus monogyna fruit extracts. The polyphenols and vitamin C of extracts were quantified using HPLC-DAD, and the total phenolic content, flavonoid content, antioxidant activity (DPPH and reducing power), and antidiabetic activity were also studied. The antidiabetic activity was examined by the inhibition of α-amylase and α-glucosidase, and in vitro on a beta TC cell line (ß-TC-6). The results showed significant differentiation in the extraction yield between the methods used, with the ASE and LE presenting the highest values. The C. mas fruit extract obtained by ASE exhibited the best antioxidant activity, reaching an IC50 value of 31.82 ± 0.10 µg/mL in the DPPH assay and 33.95 ± 0.20 µg/mL in the reducing power assay. The C. mas fruit extracts obtained by ASE and LE also have the highest inhibitory activity on enzymes associated with metabolic disorders: α-amylase (IC50 = 0.44 ± 0.02 µg/mL for the extract obtained by ASE, and 0.11 ± 0.01 µg/mL for the extract obtained by LE at combined wavelengths of 1270 + 1550 nm) and α-glucosidase (IC50 of 77.1 ± 3.1 µg/mL for the extract obtained by ASE, and 98.2 ± 4.7 µg/mL for the extract obtained by LE at combined wavelengths of 1270 + 1550 nm). The evaluation of in vitro antidiabetic activity demonstrated that the treatment with C. mas and C. monogyna fruit extracts obtained using ASE stimulated the insulin secretion of ß-TC-6 cells, both under normal conditions and hyperglycemic conditions, as well. All results suggest that C. mas and C. monogyna fruit extracts are good sources of bioactive molecules with antioxidant and antidiabetic activity.

A New Alternative Nutritional Source Hawthorn Vinegar: How It Interacts with Protein, Glucose and GLP-1.

(1) Background: There is a balance between nutrition, glycemic control, and immune response. Their roles in physiological mechanisms are essential for maintaining life quality. This study aimed to evaluate hawthorn vinegar's metabolic effects, and describe its possible mechanism. We also pointed out several vinegar production methods to clarify the antioxidant features. (2) Methods: In the study, three vinegar techniques were applied to vinegar: traditional production of hawthorn vinegar (N), thermal pasteurization (P), and ultrasound method (U). Thirty-two female adult Wistar albino rats were randomly separated into four groups: Control, N1 (regular vinegar; 1 mL/kg bw), P1 (pasteurized vinegar; 1 mL/kg bw), and U1(ultrasound treated vinegar; 1 mL/kg bw). Vinegar was administered by oral gavage daily for 45 days. Initial and final weights, the percentage changes of body weight gains, and Gamma-Glutamyl Transferase (GGT) values of plasma and liver were measured. The total protein, globulin, and albumin values of plasma, liver, and intestinal tissue were determined. In addition, plasma glucagon-like peptide-1 (GLP-1) and glucose concentrations were evaluated. (3) Results: There was a statistical increase in total intestinal protein value and an increasing tendency in total protein in plasma and liver in group U1 compared to group Control. However, the GGT concentrations in plasma and liver were slightly lower in group U1 than in group Control. In addition, there were significant increases in plasma GLP-1 values in all experimental groups compared to the Control group (p: 0.015; 576.80 ± 56.06, 773.10 ± 28.92, 700.70 ± 17.05 and 735.00 ± 40.70; respectively groups control, N1, P1, and U1). Also, liver GLP-1 concentrations in groups P1 and U1 were higher than in group Control (p: 0.005; 968.00 ± 25.54, 1176 ± 17.54 and 1174.00 ± 44.06, respectively groups control, P1 and U1). On the other hand, significant decreases were found in plasma glucose concentrations in groups N1 and U1 as to the Control group (p: 0.02; Control: 189.90 ± 15.22, N1: 133.10 ± 7.32 and U1: 142.30 ± 4.14). Besides, liver glucose levels were lower in all experimental groups than in group Control statistically (p: 0.010; 53.47 ± 0.97, 37.99 ± 1.46, 44.52 ± 4.05 and 44.57 ± 2.39, respectively groups control, N1, P1, and U1). (4) Conclusions: The findings suggest that hawthorn vinegar can balance normal physiological conditions via intestinal health, protein profiles, and glycemic control. Additionally, ultrasound application of vinegar may improve the ability of hawthorn vinegar, and have positive effects on general health.

Metabolomics analysis of physicochemical properties associated with quality deterioration in insect-infested hawthorn berries.

The sliced and dried hawthorn berries are easily infested by insects during storage. This study aimed to determine the effect of insect infestation on the quality of hawthorn berries and assess the change at metabolite level by analyzing physicochemical property and metabolomics profiling. A total of 184 shared differential metabolites were obtained, mainly including flavonoids, fatty acids, carboxylic acids and derivatives, and nitrogenous compounds. Through receiver operating characteristic curve assessment, 9 significant differential markers were screened out to distinguish insect infestation of hawthorn berries. Correlation analysis showed that the color, total organic acids, total phenolics, and total flavonoids were effective indicators for quality evaluation of insect infestation, and uric acid and hippuric acid can serve as biomarkers for the quality deterioration of hawthorn berries during storage. This study demonstrated that insect infestation could decrease the quality of hawthorn berries from macro and micro perspectives.

Dynamic transformation in flavor during hawthorn wine fermentation: Sensory properties and profiles of nonvolatile and volatile aroma compounds coupled with multivariate analysis.

Fermentation stage is a crucial factor for flavor profiles formation of hawthon wine. Thus, comprehensive knowledge of dynamic relationship between nonvolatile (NVOCs) and volatile aroma compounds (VOCs) from hawthorn wine at different fermentation stages was investigated by GC-MS and HPLC coupled with multivariate analysis. The increase of alcohols/esters/acids but decrease of terpenes/aldehydes/ketones was observed as fermentation extension. Specifically, OAV of ethyl acetate, ethyl caprylate, and ethyl caprate was > 50 from the 3rd day to 10th day, giving more fruity properties. Multivariate analysis showed that 1-hexanol, ethyl myristate, isobutyric acid, et al., were linked to the sensory evaluation of "sweet", "floral" and "fruity", and fructose, glucose and bitter amino acids were responsible for reduction of "bitterness" and "astringency". Additionally, VOCs were positively correlated with organic acids while negative to amino acids/soluble sugars, probably due to metabolization as precursors, providing references for aroma enhancement by regulating NVOCs precursors.

Physicochemical properties of pectin-Fe(III) gained by HG-type hawthorn with different esterification degree.

In this study, the complexation ability of HG-type hawthorn pectin with trivalent iron ions after de-esterification was investigated. The moderate esterification reaction could significantly increase the iron content in HG-type hawthorn pectin. Fourier transform infrared spectroscopy (FT-IR) and X-ray photoelectron spectroscopy (XPS) experiments proved that -OH and -COOH in the pectin acted as a bridge connecting Fe3+ leading to the formation of ß-FeOOH structure, and the trivalent iron ions were successfully complexed into the HG-type hawthorn pectin. In addition, infrared and ultraviolet spectroscopic scans, particle size, and potentiometric measurements were carried out to demonstrate the complexation coordination mechanism of hawthorn pectin with Fe3+, and there were differences in the complexation effect of HG-type hawthorn pectin with different degrees of esterification. The gelling properties of HG-type hawthorn pectin were subsequently verified by in vitro gastrointestinal tract simulation experiments to aid the smooth passage of ferric ions through the gastric juices and reduce irritation. The success of the experiments demonstrated that HG-type hawthorn pectin is an excellent raw material for metal complexation, and the degree of esterification is one of the important factors affecting its complexation effect, which proves its potential application value as an iron supplement.

Hawthorn (Crataegus pinnatifida) berries ripeness induced pectin diversity: A comparative study in physicochemical properties, structure, function and fresh-keeping potential.

The effect of hawthorn berries ripeness on the physicochemical, structural and functional properties of hawthorn pectin (HP) and its potential in sweet cherry preservation were investigated. With the advanced ripeness of hawthorn berries, the galacturonic acid (GalA) content decreased from 59.70 mol% to 52.16 mol%, the molecular weight (Mw) reduced from 368.6 kDa to 284.3 kDa, the microstructure exhibited variable appearance from thick lamella towards porous cross-linked fragment, emulsifying activity and emulsions stability, antioxidant activities, α-amylase and pancreatic lipid inhibitory capacities significantly increased. The heated emulsion stored for 30 d presented higher creaming index and more ordered oil droplets compared to the unheated emulsion. With the extended berries ripeness, the firmness of HP gels remarkably decreased from 225.69 g to 73.39 g, while the springiness increased from 0.78 to 1.16, HP exhibited a superior inhibitory effect in water loss, browning, softening, and bacterial infection in sweet cherries preservation.

Hawthorn Vinegar in Health with a Focus on Immune Responses.

BACKGROUND: The hawthorn fruit is an interesting medicinal plant that has several biological features, especially related to anti-inflammatory, antioxidant and immune-modulating actions, and boosting general health. In this study, we aimed to clarify the immunological effects of hawthorn vinegar on immunity and general health. We also focused on three different production processes to improve the antioxidant activity of hawthorn vinegar (2) Methods: In the study, besides the traditional production of hawthorn vinegar (N), thermal pasteurization (P) and ultrasound (U) techniques were applied to vinegars. A total of 56 female adult Wistar albino rats were randomly allocated into seven groups; Control, N0.5 (regular vinegar; 0.5 mL/kgbw), N1 (regular vinegar; 1 mL/kgbw), P0.5 (pasteurized vinegar; 0.5 mL/kgbw), P1 (pasteurized vinegar; 1 mL/kgbw), U0.5 (ultrasound treated vinegar; 0.5 mL/kgbw), and U1 (ultrasound treated vinegar; 1 mL/kgbw). Vinegars were administered by oral gavage daily. The average weight gains, body mass index, and blood hematological parameters were measured, and the Neutrophil Lymphocyte ratio was calculated. The plasma IL-1ß and TNF-α values, and MDA, IL-1ß and TNF-α values of intestinal tissue, were determined. Also, the streptavidin-biotin-peroxidase complex method was applied to determine the expressions of TNF-α and IL-1ß in duodenum. (3) Results: There was a decreasing tendency in the average weight gains in all vinegar groups compared to the control group. In addition, there was an increase in NL ratio in all vinegar groups, although not significant. There were no statistical differences among all vinegar groups, although decreases were observed in plasma IL-1ß. Also, the plasma TNF-α values showed slight increases in high-dose-of-vinegar groups (N1, P1 and U1), although not significant. In addition, the intestinal tissue IL-1ß value tended to increase in groups N0.5, N1 and P0.5, while it tended to decrease in P1, U0.5 and U1. On the other hand, there were slight increases in the TNF-α values of intestinal tissue in all groups compared to control, although these were not significant. Furthermore, the intensive expressions of TNF-α and IL-1ß were determined in groups U0.5 and U1. (4) Conclusions: The results suggest that either high doses or ultrasound applications of hawthorn vinegar have positive effects on intestinal health, boosting immunity and general health.

Targeting Non-Alcoholic Fatty Liver Disease with Hawthorn Ethanol Extract (HEE): A Comprehensive Examination of Hepatic Lipid Reduction and Gut Microbiota Modulation.

Recent studies have highlighted the lipid-lowering ability of hawthorn ethanol extract (HEE) and the role played by gut flora in the efficacy of HEE. Our study sought to explore the effects of HEE on non-alcoholic fatty liver disease (NAFLD) in normal flora and pseudo germ-free mice. The results showed that HEE effectively diminished hepatic lipid accumulation, ameliorated liver function, reduced inflammatory cytokine levels and blood lipid profiles, and regulated blood glucose levels. HEE facilitated triglyceride breakdown, suppressed fatty acid synthesis, and enhanced intestinal health by modulating the diversity of the gut microbiota and the production of short-chain fatty acids in the gut. In addition, HEE apparently helps to increase the presence of beneficial genera of bacteria, thereby influencing the composition of the gut microbiota, and the absence of gut flora affects the efficacy of HEE. These findings reveal the potential of hawthorn for the prevention and treatment of NAFLD and provide new perspectives on the study of functional plants to improve liver health.

Inhibitory effect of homemade hawthorn vinegar-based marinade on Nε-(carboxymethyl)lysine and Nε-(carboxyethyl)lysine formation in beef tenderloins.

In this study, the inhibitory effects of homemade hawthorn vinegar-based marinade on the formation of Nε-(carboxymethyl) lysine (CML) and Nε-(carboxyethyl) lysine (CEL) during the cooking of beef tenderloins investigated. Additionally, the goal was to determine the bioactive compounds present in hawthorn vinegar that could contribute to these effects, both quantitatively and qualitatively. For this purpose, hawthorn vinegar was first produced from hawthorn fruit and characterized. Then, beef tenderloins were marinated at two different concentrations (25% and 50%) and three different marination times (2, 6 and 24 h) and cooked in a airfryer at 200 °C for 12 min. After the cooking process, analyses were conducted for CML, CEL, thiobarbituric acid reactive substances (TBARS), sensory and color. Hawthorn vinegar was found to have high phytochemical and bioactivity properties. It was found that hawthorn vinegar significantly altered the color properties (L*, a*, and b*) of raw beef tenderloin samples (P < 0.05). The marinating process did not adversely affect the sensory properties of the beef tenderloin, other than odour, and even improved its texture and appearance. Increasing the marination concentration and time significantly inhibited CML and CEL formation (P < 0.05), marinating the meat for 24 h reduced CML formation from 13.75 µg/g to 2.5 µg/g, while CEL formation decreased from 17.58 µg/g to 16.63 µg/g. Although CEL was inhibited at low levels during marination, it remained stable. In conclusion, this study showed that hawthorn vinegar contains bioactive compounds that significantly inhibit the formation of CML and stabilize the formation of CEL.

Study on the hypotensive effect and mechanism of hawthorn (Crataegus pinnatifida) fruits and hyperoside in spontaneously hypertensive rats.

Hawthorn fruits have a sweet and sour taste, besides having beneficial therapeutic effects on hyperlipidemia, hypertension, and coronary heart disease, making them widely used in food and clinical medicine. However, their hypotensive effects and potential mechanisms of anti-hypertension still need to be elucidated. This study aims to explore the antihypertensive effect of hawthorn and its monomer hyperoside on spontaneously hypertensive rats through pharmacodynamics, serum metabolomics, and in vivo mechanism studies. After 7 weeks of intervention with hawthorn extract and hyperoside, the blood pressure was significantly reduced. Aortic vascular staining results showed that the injury was significantly improved after intervention with hawthorn extract and hyperoside. According to the serum metabolomics study, the main metabolic pathway regulating blood pressure in hawthorn extract and hyperoside groups was the primary bile acid biosynthesis pathway. Quantitative experiments confirmed that the level of bile acid in the model group was significantly different from that in the normal group, while that in the hawthorn group and the hyperoside group was close to that in the normal group. Based on the prediction of bile acid-hypertension related targets and the literature, nine genes involved in bile acid metabolism and inflammatory pathways were selected for further study. The FXR, TGR5, ET-1, NOS3, Akt1, TNF-α, Ptgs2, ACE2 and Kdr mRNA expression levels in the hawthorn extract and hyperoside groups were significantly different from those in the model groups. In summary, hawthorn extract and hyperoside have a hypotensive effect on spontaneously hypertensive rats through bile acid and inflammation related targets. Hence, hawthorn extract has the potential to become a functional food or an alternative therapy for hypertension.

Characterizations of White Mulberry, Sea-Buckthorn, Garlic, Lily of the Valley, Motherwort, and Hawthorn as Potential Candidates for Managing Cardiovascular Disease-In Vitro and Ex Vivo Animal Studies.

Cardiovascular diseases are a broadly understood concept focusing on vascular and heart dysfunction. Lack of physical exercise, type 2 diabetes, obesity, hypertension, dyslipidemia, thromboembolism, and kidney and lung diseases all contribute to the development of heart and blood vessel dysfunction. Although effective and important, traditional treatment with diuretics, statins, beta blockers, calcium inhibitors, ACE inhibitors, and anti-platelet drugs remains a second-line treatment after dietary interventions and lifestyle changes. Scientists worldwide are still looking for an herbal product that would be effective and free from side effects, either taken together with or before the standard pharmacological intervention. Such herbal-originated medication therapy may include Morus alba L. (white mulberry), Elaeagnus rhamnoides (L.) A. Nelson (sea-buckthorn), Allium sativum L. (garlic), Convallaria majalis L. (lily of the valley), Leonurus cardiaca L. (motherwort), and Crataegus spp. (hawthorn). Valuable herbal raw materials include leaves, fruits, seeds, and even thorns. This short review focuses on six herbs that can constitute an interesting and potential therapeutic option in the management of cardiovascular disorders.

Investigation on the lipid-lowering effect and mechanism by combining turmeric with hawthorn in C57BL/6 obese mice.

Study on the hypolipidemic effect of turmeric combined with hawthorn on C57BL/6 obese mice and its possible mechanism. C57 mice were fed with 60% high-fat diet for 8 weeks to establish an obesity model, and 4 mice were slaughtered to verify whether the modeling was successful. The successful mice were divided into model group (HFD), positive group (high fat feed group [HFD] + simvastatin group [SIM]), turmeric group (HFD + TUR), hawthorn group (HFD + HAW), and para-medicine group (HFD + para-drug group [DOU]) for 4 weeks by gavage intervention. Different intervention groups had certain lipid-lowering effects, and the para-medicine group showed significant differences (p < 0.05, p < 0.01, p < 0.001) in reducing serum total cholesterol, triglycerides, low-density lipoprotein cholesterol, glutamic acid transaminase (ALT), glutamic acid transaminase (AST), and increasing high-density lipoprotein cholesterol. In the para-medicine group, the protein expression of peroxisome proliferator-activated receptor γ, fatty acid synthase, platelet-reactive protein receptor 36, and CCAAT/enhancer binding protein α were significantly downregulated, and the protein expression of carnitine palmitoyl transferase1 and peroxisome proliferator-activated receptor α protein expression (p < 0.01, p < 0.001), thus suggesting that turmeric and hawthorn are superior to turmeric and hawthorn alone in enhancing lipid metabolism-related mechanisms. Combined effects of turmeric and hawthorn improve lipid metabolism in mice, protect the liver, and improve the protein expression of liver-related genes. This study can lay the theoretical basis for the future association of medicinal food products and the development of related weight loss products.

Characterization, antioxidant activity and in vitro digestion of hawthorn pectin prepared by gradient ethanol precipitation.

Four modified hawthorn pectin fractions (MHPs), named MHP-30, MHP-50, MHP-70 and MHP-90, were obtained by ultrasonic-assisted pectin methyl esterase modification and gradient ethanol precipitation. The results indicated that all four MHPs were composed of galacturonic acid, galactose, xylose, arabinose, glucose and mannose in different proportions. With the increase of the ethanol concentration, the molecular weight, esterification degree and galacturonic acid content of MHPs all decreased, whereas the arabinose content and branching degree increased. The structural characterization from XRD, SEM, and FT-IR showed that four MHPs exhibited amorphous structure, similar functional groups, diverse surface morphologies. Besides, in vitro antioxidant assays confirmed that MHP-70 and MHP-90 exhibited stronger total antioxidant activities than MHP-30 and MHP-50. The results of simulated saliva-gastrointestinal digestion showed that the molecular weight of MHP-70 and MHP-90 remained stable, yielded small amounts of reducing sugars, and were resistant to digestion in the human upper digestive tract. Overall, MHP-70 and MHP-90 shown great potential as novel natural antioxidants, which are expected to be good carbon sources for the utilization of intestinal microorganisms.

Structurally diverse 1,2-diarylpropanes from the fruit of Crataegus pinnatifida and the investigation on their mirror-image ECD spectra with the same absolute configurations.

1,2-diarylpropanes are a kind of abundant natural products formed by radical coupling. On account of molecular flexibility, it was challenged in the identifications of relative and absolute configurations of the 1,2-diarylpropanes. In this research, fourteen pairs of enantiomeric 1,2-diarylpropanes (1a/1b-14a/14b), comprising twelve previously undescribed pairs (1a/1b-4a/4b, 6a/6b-10a/10b, and 12a/12b-14a/14b), were isolated from the fruit of Crataegus pinnatifida. Their structures were determined through multiple NMR spectral analyses, empirical NMR rules, X-ray crystallography, and the comparison of experimental ECD spectra with calculated data. In addition, the analysis of ECD spectra revealed that substituent effects could generate an inverted chiroptical response, exhibiting in mirror-image ECD signals. This phenomenon was investigated by conformational analysis, molecular orbital analysis, the transition density matrix and hole/electron distributions. Moreover, a potential experimental rule was proposed for the rapid determination of the absolute configurations of the 1,2-diarylpropanes.

Hawthorn leaf flavonoids alleviate the deterioration of atherosclerosis by inhibiting SCAP-SREBP2-LDLR pathway through sPLA2-â ¡A signaling in macrophages in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Hawthorn leaves are a combination of the dried leaves of the Rosaceae plants, i.e., Crataegus pinnatifida Bge. or Crataegus pinnatifida Bge. var. major N. E. Br., is primarily cultivated in East Asia, North America, and Europe. hawthorn leaf flavonoids (HLF) are the main part of extraction. The HLF have demonstrated potential in preventing hypertension, inflammation, hyperlipidemia, and atherosclerosis. However, the potential pharmacological mechanism behind its anti-atherosclerotic effect has yet to be explored. AIM OF THE STUDY: The in vivo and in vitro effects of HLF on lipid-mediated foam cell formation were investigated, with a specific focus on the levels of secreted phospholipase A2 type IIA (sPLA2-II A) in macrophage cells. MATERIALS AND METHODS: The primary constituents of HLF were analyzed using ultra-high performance liquid chromatography and liquid chromatography-tandem mass spectrometry. In vivo, HLF, at concentrations of 5 mg/kg, 20 mg/kg, and 40 mg/kg, were administered to apolipoprotein E knockout mice (ApoE-/-) fed by high-fat diet (HFD) for 16 weeks. Aorta and serum samples were collected to identify lesion areas and lipids through mass spectrometry analysis to dissect the pathological process. RAW264.7 cells were incubated with oxidized low-density lipoprotein (ox-LDL) alone, or ox-LDL combined with different doses of HLF (100, 50, and 25 µg/ml), or ox-LDL plus 24-h sPLA2-IIA inhibitors, for cell biology analysis. Lipids and inflammatory cytokines were detected using biochemical analyzers and ELISA, while plaque size and collagen content of plaque were assessed by HE and the Masson staining of the aorta. The lipid deposition in macrophages was observed by Oil Red O staining. The expression of sPLA2-IIA and SCAP-SREBP2-LDLR was determined by RT-qPCR and Western blot analysis. RESULTS: The chemical profile of HLF was studied using UPLC-Q-TOF-MS/MS, allowing the tentative identification of 20 compounds, comprising 1 phenolic acid, 9 flavonols and 10 flavones, including isovitexin, vitexin-4″-O-glucoside, quercetin-3-O-robibioside, rutin, vitexin-2″-O-rhamnoside, quercetin, etc. HLF decreased total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and non-high-density lipoprotein cholesterol (non-HDL-C) levels in ApoE-/- mice (P < 0.05), reduced ox-LDL uptake, inhibited level of inflammatory factors, such as IL-6, IL-8, TNF-α, and IL-1ꞵ (P < 0.001), and alleviated aortic plaques with a thicker fibrous cap. HLF effectively attenuated foam cell formation in ox-LDL-treated RAW264.7 macrophages, and reduced levels of intracellular TC, free cholesterol (FC), cholesteryl ester (CE), IL-6, TNF-α, and IL-1ß (P < 0.001). In both in vivo and in vitro experiments, HLF significantly downregulated the expression of sPLA2-IIA, SCAP, SREBP2, LDLR, HMGCR, and LOX-1 (P < 0.05). Furthermore, sPLA2-IIA inhibitor effectively mitigated inflammatory release in RAW264.7 macrophages and regulated SCAP-SREBP2-LDLR signaling pathway by inhibiting sPLA2-IIA secretion (P < 0.05). CONCLUSION: HLF exerted a protective effect against atherosclerosis through inhibiting sPLA2-IIA to diminish SCAP-SREBP2-LDLR signaling pathway, to reduce LDL uptake caused foam cell formation, and to slow down the progression of atherosclerosis in mice.

Crataegus pentagyna willd. Fruits, leaves and roots: phytochemicals, antioxidant and antimicrobial potentials.

BACKGROUND: The hawthorn has recently been used as a popular herbal medicine in food applications and phytotherapy, especially for the cardiovascular system. METHODS: In this study, phytochemicals were evaluated by LC-ESI-MS, GC-MS, and biological activity, including antioxidant (DPPH test) and antibacterial (broth dilution assay), in different extracts of Crataegus pentagyna fruit, leaf, and root. RESULTS: Globally, 49 phenolics were tentatively identified using HPLC-ESI-MS/MS in the hydro-methanolic extract of the fruit (major apigenin, caffeoylquinic acid derivative, and 4-O-(3'-O-glucopyranosyl)-caffeoyl quinic acid), 42 in the leaf (major salicylic acid, naringenin-6-C-glucoside, and naringin), and 33 in the root (major naringenin-7-O-neohesperidoside, isovitexin-2″-O-rhamnoside, and 4-O-(3'-O-glucopyranosyl)-caffeoyl quinic acid). The major group compounds analyzed by GC-MS in petroleum ether extracts were hydrocarbons (63.80%) and fatty acids and their derivatives (11.77%) in fruit, hydrocarbons (49.20%) and fatty acids and their derivatives (13.85%) in leaf, and hydrocarbons (53.96%) and terpenes (13.06%) in root. All samples exhibited promising phytochemical profile (total phenol, flavonoid, phenolic acid, and anthocyanin), antioxidant and antibacterial capacities, especially in hydro-methanolic extract of fruit (210.22 ± 0.44 mg GAE/g DE; 79.93 ± 0.54 mg QE/g DE; 194.64 ± 0.32 mg CAE/g DE; 85.37 ± 0.13 mg cyanidin 3-glucoside/100 g FW; DPPH: 15.43 ± 0.65 µg/mL; MIC: 0.15-0.62 µg/mL; and MBC: 0.62-1.25 mg/mL), followed by the leaf and root extracts, respectively. The PCA and heatmap analysis results distinguished metabolite profile differences for samples. CONCLUSION: The results of the present work provide scientific support for C. pentagyna as antimicrobial agents and natural antioxidants in human health and food preservation.

Hawthorn Fruit (Crataegus spp.) Polysaccharides Exhibit Immunomodulatory Activity on Macrophages via TLR4/NF-κB Signaling Activation.

The immunostimulatory effects and the involved molecular mechanisms of polysaccharides from hawthorn fruit (Crataegus spp.) have not been well understood. In this study, the chemical composition, monosaccharide composition, uronic acid content, and structural features of hawthorn fruit polysaccharides (HFP) and the two collected fractions were analyzed. Both AF1-2 and AF2 have pectic-like structural features rich in galacturonic acid. AF2 showed superior proinflammatory effects on macrophages which significantly increased the secretion of pro-inflammatory cytokines interleukin-1ß, interleukin-6, and tumor necrosis factor-α, but not AF1-2. AF2 was found to activate the nuclear factor-κB signaling pathway with suppressed expression of IκBα but up-regulated expression of p-IκBα and nuclear factor-κB P65. The surface binding site of AF2 on macrophage cells was characterized and toll like receptor-4 was responsible for AF2 induced activation of down-stream nuclear factor-κB signaling pathways. AF2 from hawthorn fruit could be potentially used as a natural source of immunomodulator in functional foods.

Determination and analysis of patulin in apples, hawthorns, and their products by high-performance liquid chromatography.

This study aimed to establish a high-performance liquid chromatography (HPLC) method to investigate the residues of patulin in apples, hawthorns, and their products. A total of 400 samples were collected from online shopping plats and supermarkets in China, including apples (n = 50), hawthorns (n = 50), and their products (apple juice, apple puree, apple jam, hawthorn juice, hawthorn chips, and hawthorn rolls, n = 300). In this experiment, this method had good linearity and a recovery of 82.3-94.4% for patulin. The limit of detection (LOD) was 0.2 µg/kg for liquid samples, while it was 0.3 µg/kg for solid and semi-fluid samples. The frequencies of patulin were 79.8% in 400 samples, and the patulin concentration is from 0.6 to 126.0 µg/kg. Two samples (0.5%) for patulin exceeded the regulatory limit (50 µg/kg) in 400 samples. The frequencies of patulin in kinds of samples were 32.0-98.0% (p < 0.05), and the percentage of samples exceeding the limit was not more than 2.0%. The frequencies of patulin in domestic samples were 83.0%, while they were 57.7% in imported samples. Two domestic samples (0.6%) contained patulin above the regulatory limit, while none of the imported samples exceeded the limit. Among the online and offline samples, the frequencies of patulin were 76.4 and 82.1%. Two online samples (1.0%) for patulin exceeded the regulatory limit, whereas none of the offline samples exceeded the limit. These results showed it is important to monitor regularly the content of patulin in apples, hawthorns, and their products to ensure consumer food safety.

[Screening of bioactive components endowing hawthorn with turbidity-eliminating and lipid-lowering functions and development of quality control method of hawthorn].

Hawthorn has the efficacy of eliminating turbidity and lowering the blood lipid level, and it is used for treating hyperlipidemia in clinic. However, the bioactive components of hawthorn are still unclear. In this study, the spectrum-effect relationship was employed to screen the bioactive components of hawthorn in the treatment of hyperlipidemia, and then the bioactive components screened out were verified in vivo. Furthermore, the quality control method for hawthorn was developed based on liquid chromatography-mass spectrometry(LC-MS). The hyperlipidemia model of rats was built, and different polar fractions of hawthorn extracts and their combinations were administrated by gavage. The effects of different hawthorn extract fractions on the total cholesterol(TC), triglycerides(TG), and low-density lipoprotein-cholesterol(LDL-C) in the serum of model rats were studied. The orthogonal projections to latent structures(OPLS) algorithm was used to establish the spectrum-effect relationship model between the 24 chemical components of hawthorn and the pharmacodynamic indexes, and the bioactive components were screened out and verified in vivo. Finally, 10 chemical components of hawthorn, including citric acid and quinic acid, were selected to establish the method for evaluating hawthorn quality based on LC-MS. The results showed that different polar fractions of hawthorn extracts and their combinations regulated the TG, TC, and LDL-C levels in the serum of the model rats. The bioactive components of hawthorn screened by the OPLS model were vitexin-4″-O-glucoside, vitexin-2″-O-rhamnoside, rutin, citric acid, malic acid, and quinic acid. The 10 chemical components of hawthorn, i.e., citric acid, quinic acid, rutin, gallic acid, vitexin-4″-O-glucoside, vitexin-2″-O-rhamnoside, malic acid, vanillic acid, neochlorogenic acid, and fumaric acid were determined, with the average content of 38, 11, 0.018, 0.009 5, 0.037, 0.017, 8.1, 0.009 5, 0.073, and 0.98 mg·g~(-1), respectively. This study provided a scientific basis for elucidating the material basis of hawthorn in treating hyperlipidemia and developed a content determination method for evaluating the quality of hawthorn.

Four pairs of neolignan enantiomers with distinctive isochroman moiety from the fruits of Crataegus pinnatifida and their protective activities against H2O2-induced SH-SY5Y cells.

Four pairs of neolignan enantiomers (±)-1- (±)-4 with a distinctive isochroman moiety, including seven undescribed compounds, were isolated and identified from the fruits of Crataegus pinnatifida. Structural characterization of these compounds was established through comprehensive spectroscopic analyses, as well as quantum chemical calculations of ECD and NMR data. The preliminary bioassay displayed that compounds (+)-2 and (±)-3 exerted protective activities against H2O2-induced human neuroblastoma SH-SY5Y cells compared with the positive control. These bioactive compounds could be potential candidates for further pharmaceutical applications.