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Background Endophytes promote the survival of the host plants affected by unfavorable environment. To confirm the endophytes role in Chaenomeles speciosa pathogenic resistance, fungal isolates were derived from both fruit peel and pulp, and presumptively identified using macroscopic and microscopic techniques. Antifungal potential of the isolates was assayed by dual culture method and agar disc method against Alternaria alternata, Fusarium culmorum, and Fusarium oxysporum strains. Two most active fungal isolates were cultured in Czapek's liquid medium to obtain metabolites. The crude ethyl acetate extracts of metabolites were characterized for antibacterial activity against Basillus subtilis and Erwinia dissolvens, and for component composition by GC–MS technique. Results Nine fungal endophytic isolates were derived from the peel and pulp of C. speciosa fruits and tentatively attributed to Penicillium spp. (seven isolates), Aspergillus spp. (one isolate), Mucor spp. (one isolate). Two fungal isolates, one each of the fruit peel and pulp, were designated as Penicillium sp. I and Penicillium sp. II respectively, and selected for further research. Both isolates showed similar activity against A. alternata; however, Penicillium sp. I activity against F. culmorum and F. oxysporum exceeded the activity of Penicillium sp. II. Cultural medium ethyl acetate extracts of both endophytes exhibited higher antibacterial activity against Gram-positive B. subtilis, while mycelium extracts were more active against Gram-negative E. dissolvens. In general, Penicillium sp. I antibacterial activity was higher in cultural medium extracts, while activity of Penicillium sp. II dominated in mycelium extracts. GC–MS analysis of the fungal metabolites component composition revealed the identity of 27 and 17 compounds, respectively in the ethyl acetate extracts of Penicillium sp. I and Penicillium sp. II cultural medium. Basic compounds produced by the first isolate, were represented by 3-Furanacetic acid, 4-hexyl-2,5-dihydro-2,5-dioxo, Diisooctyl phthalate, 11-Hexadecyn-1-ol, and Propanedioic acid, dihydroxy. At the same time, Phthalic acid diisooctyl ester and other phthalates constituted the main part of the second isolate metabolites, followed by Hexadecanoic acid, Eicosyl isopropyl ether, and 4-Butoxy-2-butanone at a lower content. Conclusions The findings showed that the antimicrobial potential of Chaenomeles fruits endophytic fungi is promising and deserves further investigation.

Chaenomeles speciosa (Sweet) Nakai is a dual-purpose Chinese herbal medicine and functional food favored by minorities in Southwest China, and its fruits are used for the treatment of dyspepsia, dysentery, enteritis, and rheumatism inflammation. Some diseases may be related to microbial infection; however, it is not known how the fruits possess antimicrobial activity. We evaluated the antimicrobial bioctivity of different evaluation extracts of C. speciosa fruits by in vitro and in vivo with colony-forming unit assays, and the strongest bioactive-guided fraction was selected for column chromatography (CC), UHPLC-QTOF-MS/MS, and NMR spectroscopy to confirm the chemical constituents. The most possible antimicrobial mechanism of C. speciosa fruits was explored by metabolomics approach, fluorescence microscopy imaging, and scanning electron microscopy (SEM). Thirty compounds, which were major characteristic ions of the bioactive fraction, were determined precisely. The bioactive fraction could inhibit 18 pathogenic microorganisms, significantly reduced, especially drug-resistant bacteria, compared to ampicillin sodium salt, fluconazole, and berberine chloride form; and the minimum inhibitory concentration (MIC) or minimum fungicidal concentration (MFC) values were in the range of 0.1-1 mg/mL. The compounds 2'-methoxyaucuparin (1) and oleanolic acid (20) not only have antibacterial activity but also may have synergistic effects. Further, the bioactive fraction might inhibit the biofilm formation, enhance immunity, and restore bacterial infection damage in vitro and in vivo to kill microorganisms. The data indicated that C. speciosa fruits' major bioactive fraction enriched with triterpenes, flavonoids, and phenolics could be developed as a functional supplement for individuals to prevent and treat microbial infection.

Background Extracts from the Rosaceae family fruits are rich in natural, biologically active polyphenols, but their antibacterial properties are still poorly understood. Therefore, we focused our research on their activity against uropathogenic Escherichia coli strains. This research also concerned the proof of their ability to reduce oxidative stress and modulate the activity of lipoxygenase-1 (LOX-1). It is well-known that plants represent a source of bioactive compounds whose antioxidant activity may be useful in protecting against oxidative damage in cells, which have been linked to the pathogenesis of many oxidative diseases. Objectives The study determined the biological activity of methanol (ME) and water (WE) extracts rich in polyphenols from the hawthorn (Crataegus monogyna Jacq.), dog rose (Rosa canina L.), quince (Cydonia oblonga Mill.), and Japanese quince (Chaenomeles speciosa (Sweet) Nakai). Material and methods The antioxidant capacity was evaluated using 1,1diphenyl-2-picrylhydrazyl (DPPH▪) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS+▪) radical scavenging methods. The inhibition of liposome membrane oxidation was studied using the thiobarbituric acid reactive substances assay. Lipoxygenase-1 inhibitory activity was measured using the spectrophotometric method. Bacterial growth was determined by evaluating the number of colony forming units per milliliter (CFU/mL). Hydrophobicity was established with salt aggregation hydrophobicity test (SAT). Swimming and swarming motilities were evaluated using soft-agar plates. Production of curli fimbriae was estimated on CFA agar. The P fimbriae were detected using the hemagglutination of erythrocytes. Adhesion of bacteria to human uroepithelial cells was assessed. The amount of biofilm was determined spectrophotometrically. Results We showed that most of these extracts are effective antioxidants and free radical scavengers, possess reasonable potential anti-inflammatory activity, reduce the adhesion of E. coli to uroepithelial cells, and reduce the ability of these bacteria to form biofilm. Conclusions The extracts examined, showing very promising biological properties, seem to be able to join the list of substances that can be used as dietary supplements aimed at preventing, for example, urinary tract infections, or as support of drug treatment in many diseases.

Our previous studies have demonstrated that the total triterpenes from the fruits of Chaenomeles speciosa (CSTT) exhibit effective therapeutic effects on gastric ulcer patients and animals. The present aim is to further investigate the mechanisms involved. The results indicated that CSTT could ameliorate IND-induced gastric injury, which was related to promoting IND-damaged GES-1 cell proliferation and migration, improving the IND-damaged rat GBF, ulcer area, inhibition rate and pathologic changes of gastric mucous tissue, increasing the amount of adhered gastric mucus, attenuating the volume and total acidity of the gastric effluents, and augmenting the gastric pH; further studies showed that CSTT obviously downregulated miR-423-5p mRNA, NAG-1 mRNA and protein expression, Bax, Bad, cytosol cytochrome C, Apaf-1, cleaved-caspase-3, and cleaved-caspase-9 protein expression and cytosol cytochrome C concentration, and upregulated TFF1, TFF2 and TFF3 mRNA and protein expression, Bcl-2, Bcl-xl, pro-caspase-3, and pro-caspase-9 protein expression, mitochondrial viability, mitochondrial cytochrome C concentration and Bcl-2/Bax, Bcl-xl/Bad ratios. These findings demonstrated that CSTT protected against IND-induced gastric damage by depressing miR-423-5p expression and modulating the TFF/NAG-1 pathway, which in turn restrained mitochondrion-mediated apoptosis.

Background The dried fruit of Chaenomeles speciosa, known as Chaenomelis Fructus or Zhoupi Mugua, is a type of traditional Chinese medicine (TCM) that is widely used to treat many diseases. Guangpi Mugua, the dried fruit of the Chaenomeles sinensis, is its most commonly known adulterant. Objective To establish a robust approach for the quality control and identification of Chaenomelis Fructus. Method Thin-layer chromatography (TLC) was optimized and used to discriminate Chaenomelis Fructus from Guangpi Mugua. High-performance liquid chromatography (HPLC) combined with fingerprint analysis and partial least-squares (PLS) discrimination analysis (DA) was employed to study the chemical differences between Chaenomelis Fructus and Guangpi Mugua. The single standard to determine multi-components (SSDMC) method, with credible precision, repeatability, stability, and durability, was developed for quantitative analysis of the abundant markers. Results The developed TLC and HPLC methods were effective in the authentication of Chaenomelis Fructus. Moreover, oleanolic acid, ursolic acid, pomolic acid, corosolic acid, 3-O-acetylpomolic acid, and one unknown compound were identified to be critical markers for the discrimination of Chaenomelis Fructus from Guangpi Mugua. Conclusion Adulteration has always been a challenge in the development of TCM. This study presents useful insights that may help solve the problem of adulteration during the preparation of Chaenomelis Fructus. Highlights The present study provides a systematic method for the quality control of Chaenomelis Fructus. This is therefore the first step towards solving the problem of adulteration to improve the clinical safety and effectiveness of Chaenomelis Fructus.

Production of minor crop varieties often requires intensive pesticide use, which raises serious concerns over food safety and human health. Chaenomeles speciosa (Sweet) Nakai as one of the representative of this kind of crops is therefore used for investigating the residue behavior of fenpropathrin and emamectin benzoate, a synthetic pyrethroid and macrocyclic lactone widely used as an insecticide, respectively, from cultivation to C. speciosa postharvest processing. Results showed that the degradation trends of those selected insecticides in C. speciosa followed first-order kinetics with an average half-life (t1/2) of 3.7–4.1 days and a dissipation rate of 97% over 14 days. The terminal residues of fenpropathrin and emamectin benzoate at 120 and 3 g a.i./ha were below the U.S Environmental Protection Agency (FAD, 1.00 mg/kg) and European Union (EU, 0.01 mg/kg) maximum residue limits (MRLs) in papaya species, respectively, when measured 14 days after the final application, which suggested that the use of these insecticides was safe for humans. Postharvest processing procedure resulted in a |90% reduction of the insecticides. Moreover, the hazard quotient (HQ) for C. speciosa decoction (with processing factors) indicated an acceptable risk for human consumption. These findings provide the scientific evidence of reasonable application and risk assessment of the selected pesticide residues in C. speciosa.

Purification and structural characterization of a novel polysaccharide fraction from Chaenomeles speciosa seeds were investigated. After hot water extraction and ethanol precipitation, the crude polysaccharide was sequentially purified with Cellulose DEAE-52 and gel-filtration chromatography, and a highly purified polysaccharide fraction (F3) was obtained. The structure of F3 was characterized by high-performance gel permeation chromatography (HPGPC), high performance liquid chromatography (HPLC), ultraviolet-visible (UV), Fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR) spectrum, together with methylation, scanning electron microscopy (SEM), atomic force microscope (AFM), and Congo-red test analysis. The results indicated that F3 was a homogeneous polysaccharide fraction with a molecular weight of 8.65 × 106 Da, and it was composed of Rha, GlcA, Gal, and Ara in a molar ratio of 6.34:5.73:47.14:40.13. The backbone of F3 was consisted of →3,6)-Galp-(1→, and the side chains of F3 were composed of Araf-(1→, →4)-GlcpA-(1→, →4)-Galp-(1→ and →3)-Rhap-(1→. The hypoglycemic assays demonstrated F3 had good α-amylase and α-glucosidase inhibition activities, and their IC50 values were 6.24 mg/mL and 4.59 mg/mL respectively. Thus, the polysaccharide from Chaenomeles speciose could be applied as a potential natural source in retarding postprandial hyperglycemia effects.

Heat treatment was used to extend the shelf life of postharvest Chaenomeles speciosa (Sweet) Nakai (C. speciosa), its effects on the quality and physiological properties of C. speciosa were studied. The results showed that heat treatment reduced the weight loss, inhibited the decline of titratable acids (TA), maintained a higher activity of peroxidase (POD) and catalase (CAT), compared to untreated C. speciosa. Treatment in hot water dipping at 50℃ for 2-4 min maintained the better quality of postharvest C. speciosa stored at 0℃ for 120 days, which indicated that heat treatment is an effective preservation technology to prolong the shelf life of C. speciosa.

Solvents effect of water, methanol aqueous, and ethanol aqueous on the active compositions (TFc, TPc, TTc, TCc, TPs and contents of eleven selected compounds) in Chaenomeles speciosa were studied, as well as effects on antioxidant activity, anti-α-glucosidase activity, and inhibit effect on Ach induced smooth muscle contraction of isolated rat jejunum. The results indicate that compositions and activities of extracts prepared with different solvents vary, and methanol, 60% methanol, 40% methanol, 20% methanol and 60% ethanol would be good choices for the industrial production of Chaenomeles speciosa extracts. Water extract displays the highest inhibit activity on the contraction of smooth muscle of isolated rat jejunum, and the result also indicates that condensed tannin is responsible for the inhibit activity. In summary, our study presents the solvents effect on chemical compositions and biological activities of Chaenomeles speciosa, and gives an insight into the potential application of Chaenomeles speciosa.

Natural dyes are more eco-friendly alternatives to synthetic dyes. This research focuses on natural dyes and improved dye craft using plants employed by various ethnic groups in Southwestern China. In this study, we assessed the suitability of dried extracts from Buddleja officinalis flowers for dyeing hemp fabric. and valuated indicators including color strength (K/S), color characteristics, and fastness properties in response to washing, rubbing, and perspiration using metallic and natural mordants under pre-, post-, and simultaneous mordanting conditions. Specifically, we investigated the pigment compound crocin by ultraviolet-visible spectroscopy and Fourier transform–infrared spectroscopy analysis before using it to dye hemp fabric. Optimum dyeing conditions including staining temperature, staining duration, and pH have been identified using an orthogonal array experimental design. Optimum results were achieved when dyeing at pH 5, and at 60 °C for 90 min. Hemp fabric dyed without mordant had a shade of yellowness, while fabric mordanted with gum rosin, plant ash, KAl(SO4)2, and Chaenomeles speciosa had a variety of pale to dark yellowness color shades. A darker yellow–green color shade was obtained with FeSO4 mordant. The color change of washing fastness was mostly very poor, while the color stain of washing and perspiration fastness were good to excellent, and rubbing fastness was also good to excellent. The color fastness was kept and improved by the three natural mordants, especially gum rosin and plant ash, but reduced by FeSO4. Those results show that the use of aqueous extract from B. officinalis flowers combined with natural mordants represents a promising approach for textile dyeing, revealing an alternative method that could improve and extend the dyeing properties of this indigenous dye plant. In addition, our findings lay the foundation for further basic studies and demonstrate the utility of preserving natural dye plants, along with the related traditional knowledge of indigenous groups in Yunnan, China.

In our continuing search for bioactive constituents of Korean medicinal sources, we investigated an 80% MeOH extract of the twigs of Chaenomeles speciosa. Column chromatographic purification of the CHCl3 fraction resulted in the isolation of a new biphenyl derivative (1), along with four known biphenyl compounds (2-5) and six triterpenes (6-11). The chemical structure of the new compound was determined on the basis of spectroscopic analyses including 1D and 2D NMR data. Among isolates, compound 3 exhibited potent cytotoxic activities against SK-OV-3, SK-MEL-2, and XF498 cell lines (IC50=5.91, 4.22, and 6.28μM, respectively). Also, Compounds 9 and 10 showed strong anti-neuroinflammatory activities (IC50 2.38, and 6.70μM, respectively).

A water-soluble polysaccharide named as CSP-2 was isolated and purified from Chaenomeles speciosa by DEAE-Sepharose and Sephadex G-100 column chromatography. CSP-2 was composed of galactose (Gal), rhamnose (Rha), glucose (Glc) and xylose (Xyl) with a relative molar ratio of 3.8:1.6:1.2:0.4. The average molecular weight of CSP-2 was estimated to be about 4.6×104Da. The in vitro antioxidant assay showed that CSP-2 exhibited remarkable antioxidant activities to scavenge the DPPH radical, superoxide radical, hydroxyl radical and ABTS radical and significant cytoprotective effects on H2O2-induced PC12 cells injury in a concentration-dependent manner. Overall, CSP-2 may be useful as a naturally potential antioxidant agent for application in food and medicinal fields.

In the present study, the antimicrobial activities of methanol extracts obtained from the flowers Muscari neglectum Punica granatum, Tussilago farfara, Taraxacum officinal, Wisteria sinensis, Syringa vulgaris, Cyclamen coum, Chaenomeles speciosa, Ornithogalum umbelatum, Allium siculum, Viburnum tinus and Eryngium bithynicum were evaluated. Extracts with methanol were prepared in soxhlet device. The evaluation process of the antimicrobial activities was performed using the disc diffusion method. The highest antimicrobial activity has been detected at the strain of S. aureus. The detected inhibition zone diameters of the flower extracts were evaluated to be 15.5 mm for V. tinus, 15 mm for Eryngium bithynicum and 14.5 mm for Punica granatum. It has also been found that the flower extracts of C. coum and M. neglectum only affect the C. albicans strain. The flowers of P. granatum has been found to be effective on all the test microorganisms . The extracts obtained from W. sinensis, T. farfara, T. officinal and O. umbelatum have no antimicrobial effect on any test microorganisms. It was found that 7 of the 12 plant species used in the study showed antimicrobial activity. In our study, it was observed that the extracts obtained from flowers were also effective in inhibiting microorganisms. To our knowledge, this is the first study to elucidate the antimicrobial acitivity of E. bithynicum, V. tinus and A. siculum’s flowers and our results how that the flowers of these species have the potential that can be used as antimicrobial natural sources.

Chaenomeles plants are adapted to diverse ecological zones particularly the temperate areas of Korea, Japan and China. In China, Chaenomeles speciosa mainly planted in Chongqing, Anhui and Hubei provinces. Most of the studies till date have been focused on the anti-inflammatory activities of C. speciosa fractions. The present study aimed to review the maximum literature reported for the presence of various phytochemicals in C. speciosa. In addition, the pharmacological properties of these chemical compounds of this plant shall also be discussed. The extracts of the various parts of the plant are rich in diversity of antioxidants, organic acids, phenolics, terpenoides and many different phytochemicals that bear strong anticancer, antioxidant, anti-viral, antibacterial properties, anti-inflammation, anti-hyperlipidemic, anti-hyperglycemic and anti-parkinson properties. C. speciosa fruits have broad scope in industry as well as in medicines. Not only the leaves and fruits of C. speciosa plant, but various other parts including roots, seeds, bark twigs, and flowers all have long history of clinical trials in curing many human ailments. However, the maximum accessible data concerning the chemical composition and their broad pharmacological properties of C. speciosa plant parts is pretty restricted that make it more appealing for indepth investigations.

There is limited research focusing on the effects of human gut microbiota on the oral bioaccessibility and intestinal absorption of pesticide residues in food. In the present study, we use a modified setup of the Simulator of the Human Intestinal Microbial Ecosystem for the determination of pesticide residue bioaccessibility in Chaenomeles speciosa, and a Caco-2 cell model of human intestinal absorption. Results showed that gut microbiota played a dual role based their effects on contaminant release and metabolism in the bioaccessibility assay, and Lactobacillus plantarum was one of key bacterial species in the gut microbiota that influenced pesticide stability significantly. The addition of L. plantarum to the system reduced the relative amounts (by 11.40-86.51%) of six pesticides. The interaction between the food matrix and human gut microbiota led to different absorption rates, and the barrier effects increased with an increase in incubation time.

Contents of total flavonoids, total phenolics, total triterpenes, total condensed tannin and total saponins in peels, flesh and endocarps of Chaenomeles speciosa (CSP) and Chaenomeles sinensis (CSS) were determined by colorimetric method, while 5 phenolics (vanillic, gallic, chlorogenic, ferulic and p-coumaric acids), 2 triterpenes (oleanolic and ursolic acids), and 3 flavonoids (rutin, catechin and epicatechin) were identified and quantified by high-performance liquid chromatography-mass spectrometry (HPLC-MS) and HPLC, and antioxidant and α-glucosidase inhibitory activities of them also were evaluated as well as their digestive characteristics. In the correlation analysis, total phenolics, vanillic acid, catechin, ursolic acid and oleanolic acid all contribute to DPPH(·) scavenge capacity, gallic acid contributes to total ferric reducing antioxidant power, while total triterpenes, total saponins, chlorogenic acid and ferullic acid contribute to α-glucosidase inhibitory activity. In the principal component analysis, endocarps of CSP and CSS both show better quality than their peels and flesh, respectively. In vitro digestion can increase contents of total flavonoids, total condensed tannin and total saponins, while contents of total phenolics and total triterpenes decreased greatly. Our study would contribute to the full use of discarded parts of the 2 Chaenomeles and be helpful to establish a good foundation for further research of CSP and CSS.

The aim of this study was to compare the antioxidant activity of crude extracts of differing polarities of the fruits of Chaenomeles speciosa (Sweet) Nakai. The antioxidant compositions of the extracts were analyzed qualitatively and quantitatively, respectively. The 75% ethanol extract of the dried fruits was fractionated by sequential extraction using petroleum ether, ethyl acetate, and n-butyl alcohol. The antioxidant effectiveness of the components of differing polarities was examined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging method and compared with two reference substances: ascorbic acid and butylated hydroxytoluene (BHT). The total phenolic content of the extracts was analyzed using the Folin—Ciocalteu method and expressed as gallic acid equivalents. The active compounds were analyzed by thin-layer chromatography (TLC)—bioautography and ultra-performance liquid chromatography (UPLC). The order of antioxidant capacities of various solvent extracts from the fruit of C. speciosa was found to be ethyl acetate ≥ n-butyl alcohol > petroleum ether. The ethyl acetate extract was more active than the reference substances ascorbic acid and BHT. The radical-scavenging capacity of the extracts decreased as the total phenolic content decreased. TLC—bioautography revealed that the ethyl acetate extract contained many antioxidant spots that can remove DPPH radical, and protocatechuic acid and chlorogenic acid were the major antioxidant components. UPLC analysis confirmed that protocatechuic acid and chlorogenic acid were mainly distributed in the ethyl acetate fraction. The study demonstrated that the ethyl acetate extract had excellent antioxidant capacity. The total phenolic, protocatechuic acid, and chlorogenic acid contents of this extract were higher than those of the other two solvent extracts. These results showed that the ethyl acetate extract from the fruit of C. speciosa could be considered as a potential source of natural antioxidant agent.

In this study, a water-soluble polysaccharide (CSP) was successfully purified from Chaenomeles speciosa by DEAE-Sepharose and Sephadex G-100 column chromatography. CSP had a weight-average molecular weight of about 6.3 × 10(4)Da and was composed of glucose (Glc), galactose (Gal), rhamnose (Rha) and arabinose (Ara) with a relative molar ratio of 4.6:1.3:0.8:0.5. CSP could not only inhibit the growth of S180 tumor transplanted in mice, but also increase the relative spleen index and body weight of tumor bearing mice. Moreover, concanavalin A (ConA) and lipopolysaccharide (LPS) induced splenocyte proliferation and peritoneal macrophage phagocytosis were also enhanced after CSP administration. Furthermore, CSP treatment could improve delayed type hypersensitivity (DTH) and promote the secretion of IL-2, TNF-α and IFN-γ in serum. The overall findings suggest that the antitumor effect of CSP is might be associated with its potent immunostimulatory activity.

This study aimed to identify and quantify carotenoids, chlorophylls, tocopherols, tocotrienols and the free amino acid profile of 19 fruit cultivars of Chaenomeles × superba, Chaenomeles japonica, and Chaenomeles speciosa. For this purpose ultra-performance liquid chromatography (UPLC) with a photodiode array (PDA) and fluorescence (FL) detector coupled with quadrupole time-of-flight electrospray ionization mass spectrometry (QToF–ESI–MS) was used. Most of the Chaenomeles species and cultivars analyzed in this study have not been examined in this respect until now. Fruits contained 32.44–314.94 mg of carotenoids, 19.27–227.19 mg of chlorophylls, 5.51–37.58 mg of tocopherols, and 2.06–42.30 mg of tocotrienols per kg of dry weight (dw). Analysis of the amino acid profile revealed the presence of 10 amino acids, three of them essential ( l -threonine, l -valine and l -isoleucine). The highest content of total amino acids was shown by C. × superba ˈJet Trailˈ (2326.33 mg/100 g dw). Among tested species, C. speciosa was characterized by the highest content of all analyzed compounds, except for chlorophylls, present in the highest concentration in C. × superba fruits. These results indicate that Chaenomeles fruits could be regarded as a promising source of bioactive functional food containing vitamins A and E and indispensable amino acids.

Phytochemical investigation of fruits of Chaenomeles speciosa Lindley (Rosaceae) led to the isolation of 20 compounds including 5 flavonoids (1-5), 5 phenylpropanoids (6-10), 3 benzoic acid derivatives (11-13), 2 phloroglucinols (14 and 15), 2 purines (16 and 17), and 3 terpenoids (18–20). Their structures were elucidated by nuclear magnetic resonance analyses and from mass spectrometry data. These compounds were confirmed as catechin (1), epicatechin (2), catechin-5- O-β-d-glucoside (3), procyanidin B1 (4), quercetin-3- O-β-d-glucoside (5), p-coumaric acid (6), ferulic acid (7), caffeic alcohol (8), 1- O-p-coumaroyl-β-d-glucose (9), 1- O-cinnamoyl-β-d-glucose (10), p-hydroxybenzonic acid (11), protocatechuic acid (12), benzoic acid-β-d-gentiobioside (13), phloracetophenone 4′-glucoside (14), 3,5-dihydroxyphenyl β-d-glucopyranoside (15), adenine (16), adenosine (17), betulalbuside A (18), vomifoliol (19), and roseoside (20). Compounds 3-5, 8, 10, and 13-18 were isolated from the genus Chaenomeles and C. speciosa for the first time. Out of all these, compound 17 showed the best anti-inflammatory properties, comparable with those of the already known minocycline.

This study aimed to identify and quantify the chemical composition and polyphenolic profile of 19 cultivars of Chaenomeles &times, superba, Chaenomeles japonica, and Chaenomeles speciosa by liquid chromatography coupled with photodiode array detector and quadrupole time-of-flight electrospray ionization mass spectrometry (LC-PDA-QTOF-ESI-MS). Antioxidant (ABTS on-line, ABTS, FRAP, and ORAC), as well as in vitro biological activities, i.e., the ability to inhibit &alpha, amylase, &alpha, glucosidase, pancreatic lipase, acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and 15-lipoxygenase (15-LOX) were determined. Most of the Chaenomeles species and cultivars analyzed in this study have not been examined in this respect until now. Fruits contained 30.26 to 195.05 mg of vitamin C, 0.65 to 1.69 g of pectin, 0.32 to 0.64 g of ash, 0.60 to 3.98 g of sugars, and 41.64 to 110.31 g of organic acids in 100 g fresh weight. The lowest content of total polyphenols showed C. speciosa &lsquo, Rubra&rsquo, (57.84 g/kg dry weight, dw) while C. &times, superba &rsquo, Nicoline&rsquo, (170.38 g/kg dw) exhibited the highest concentration of those compounds. In the phenolic compounds, polymeric procyanidin fraction predominated (65%) with procyanidin B2, C1, and (&minus, )-epicatechin the most abundant. The antioxidant capacity measured by ABTS assay was mainly formed by polymeric procyanidins and flavan-3-ols, which was confirmed by ABTS on-line profiling. Chaenomeles fruits showed high potential for inhibition of &alpha, glucosidase and pancreatic lipase. The analyzed cultivars displayed greater potential for acetylcholinesterase (AChE) inhibition than for butyrylcholinesterase (BuChE). The data indicate that Chaenomeles fruits could be regarded as a promising source of bioactive functional food.

Chaenomeles speciosa (Sweet) Nakai is a medicinal plant. Until date, there are no studies focusing on comparing the chemical profiles, antioxidant activity and &alpha, glucosidase inhibitory activity of the dried fruits of C. speciosa from different production regions. In the study, we investigated the chemical components of dried fruits of C. speciosa from Yunnan, Chongqing, Zhejiang and Anhui provinces in China in relation to the antioxidant activity and &alpha, glucosidase inhibitory activity. C. speciosa from Yunnan had higher total flavonoid (47.92 &plusmn, 3.79 mg/g), total polyphenol (29.15 &plusmn, 0.29 mg/g) and polysaccharide (27.60 &plusmn, 1.56 mg/g) contents than plants from other production areas. Samples from Yunnan, Zhejiang and Anhui (all &gt, 3200 mg/kg) had higher free amino acid contents than those from Chongqing (2286.66 mg/kg). Oleanolic acid and ursolic acid levels were highest in samples from Zhejiang (555.98 &plusmn, 20.88 &mu, g/g) and Anhui (321.06 &plusmn, 14.64 &mu, g/g), respectively. C. speciosa from Chongqing had low total flavonoid, total polyphenol, polysaccharide, free amino acid, oleanolic acid and ursolic acid contents but high levels of palmitic acid (12.04 &plusmn, 0.02 mg/g) and stearic acid (2.23 &plusmn, 0.08 mg/g). Among four production areas, Yunnan represented the highest antioxidant activity and &alpha, glucosidase inhibitory activity. In addition, correlation analysis revealed that total flavonoid, total polyphenol, polysaccharide and ursolic acid were the major components responsible for the antioxidant activity of C. speciosa, while total flavonoid and polysaccharide were the main contributors for &alpha, glucosidase inhibitory activity of the plant. These results would be helpful for evaluating the quality of C. speciosa in the different production areas.

Chaenomeles plants are adapted to diverse ecological zones particularly the temperate areas of Korea, Japan, and China. In China, Chaenomeles speciosa is mainly planted in Chongqing, Anhui, and Hubei provinces. Most of the studies till date have been focused on the anti-inflammatory activities of C. speciosa fractions. The present study aimed to review the maximum literature reported for the presence of various phytochemicals in C. speciosa. In addition, the pharmacological properties of these chemical compounds of this plant shall also be discussed. The extracts of the various parts of the plant are rich in diversity of antioxidants, organic acids, phenolics, terpenoids, and many different phytochemicals that bear strong anticancer, antioxidant, antiviral, antibacterial properties, anti-inflammation, antihyperlipidemic, antihyperglycemic, and anti-Parkinson properties. C. speciosa fruits have broad scope in industry as well as in medicines. Not only the leaves and fruits of C. speciosa plant, but various other parts including roots, seeds, bark twigs, and flowers all have long history of clinical trials in curing many human ailments. However, the maximum accessible data concerning the chemical compositions and their broad pharmacological properties of C. speciosa plant parts is pretty restricted that make it more appealing for in-depth investigations.

Ministry of Science and Technology of China (2008BAD98B06); Foundation of Study Abroad Returnees from Ministry of Personnel (Y11G221261); Tufts University TEACRS Program (NIGMS IRACDA– K12GM074869)

A new sesquiterpenoid glycoside, called speciosaoside A ( 1 ), and a known sesquiterpenoid glycoside, (1′R,3′R,5′R,8′S)-epi-dihydrophaseic acid β-D-glucoside ( 2 ), were isolated from the fruits of Chaenomeles speciosa (Sweet) Nakai (Rosaceae) using column chromatography and preparative HPLC. The structure of compound 1 was deduced from comprehensive spectroscopic analysis including IR, HR-ESI-MS, 1D NMR, and 2D NMR. The structure of compound 2 was identified by comparison of its spectral data with those reported in the literature.

Amplified fragment length polymorphism (AFLP) analysis was performed to evaluate genetic relationships among 52 Chaenomeles speciosa accessions grown in China. A total of 208 polymorphic markers were generated from eight selective primer pair combinations. Genetic variations were remarkably observed in a wide range of dissimilarities, percent polymorphisms, and average polymorphism information. Genetic similarity values were calculated using Jaccard's coefficient between individuals of different flowering quince accessions; these values ranged from 0.296 to 0.931 with a mean of 0.597. Cluster analysis and principal coordinate analysis were then performed on the basis of AFLP profiles. In our generated dendrogram, accessions were clustered into seven major groups. Mantel's test was performed to determine cophenetic correlation ( r = 0.9); this result indicated a very good fit of the dendrogram. We conducted analysis of molecular variance and found greater variations within cultivars than among cultivars. AFLP analysis results further revealed relevant information regarding the genetic background of flowering quince accessions essential for future breeding programs related to plant improvement.

Chemical composition and antioxidant activity of fresh and boiled Chaenomeles speciosa (CS) slices dried by different drying methods were determined. Data were analyzed by principle component analysis and cluster analysis. All dried boiled CS from dried fresh CS slices form main cluster. The results also demonstrated that both drying methods, freeze drying and hot air drying at 60 °C had good potential in the industrial drying of fresh and boiled CS. Fresh CS dried by hot air drying at 60 °C was more suitable for the industrial production.

Phytochemical research on the anti-inflammatory activities of Chaenomeles speciosa (Sweet) Nakai (Rosaceae) to investigate the main components of 10% ethanol fraction of the crude extract of C. speciosa fruit in an attempt to find bioactive compounds or new compounds from this medicinal plant. The phytochemical investigation succeeded in isolating two new phenolic compounds, specpolyphenol A (1) and specphenoside A (2), together with three known phenyl glycosides (3–5) from the fraction. The structures of the new compounds were deduced from comprehensive spectroscopic analyses including IR, EI-MS, 1H NMR, 13C NMR, DEPT, COSY, HMBC and HMQC. The structures of the three known compounds 3, 4 and 5 were identified by comparison of their spectral data with those reported in the literature.

Chaenomeles speciosa (Sweet) Nakai (C. speciosa, Rosaceae family) is an effective medicinal plant, which has long been used in China to treat various diseases, such as rheumatism, cholera, dysentery, enteritis, beriberi and vitamin C deficiency syndrome. A series of chemical constituents, including triterpenoid, phenolic and phenylpropionic acids, flavonoids, saccharides, essential oils and alkaloids, have been isolated from this plant and some have already been evaluated for their biological activities. Pharmacological investigations demonstrated that C. speciosa possesses anti-inflammatory, antinociceptive, antimicrobial, antioxidant, immunoregulatory, antiparkinsonian, hepatoprotective and antitumor properties. The objective of this review was to summarise available up-to-date and comprehensive information on C. speciosa and provide a relevant reference for further investigations.

Chaenomeles speciosa Nakai is commonly used in traditional Chinese medicine for a variety of health-promoting effects. The present study aimed to investigate the antitumor effects of Chaenomeles speciosa Nakai. The tumor-inhibitory activity of the ethanol extract of Chaenomeles speciosa Nakai (EEC) was evaluated by in vitro growth assays of tumor cells and in vivo H22 tumor formation assays in mice. Mitochondrial membrane potential and DNA ladder assays were used to detect tumor cell apoptosis in the presence of EEC. To investigate the cellular targets of EEC, the immunomodulatory genes PD-L1, Foxp3 and TGF-β were detected in the tumor tissue using reverse transcription polymerase chain reaction (RT-PCR). Immune responses were determined by hemolysis and lymphocyte proliferation assays. EEC markedly inhibited the proliferation of the H22 cells in a dose-dependent manner. Moreover, it induced DNA fragmentation and decreased the mitochondrial membrane potential. In vivo, EEC inhibited tumor growth and enhanced the immune responses in mice, while the expression of PD-L1, Foxp3 and TGF-β was inhibited in the tumor tissue. These results provide the first evidence that EEC may inhibit tumor growth by directly killing tumor cells and enhancing immune function. Thus, it is a natural source for safe anticancer medicine.

Ethnopharmacological relevance Chaenomeles speciosa fruits have been widely used in traditional Chinese medicine for treatment of diseases related to inflammatory reaction. This study aims to identify anti-inflammatory and immunomodulatory components of Chaenomeles speciosa fruit and unravel their potential mechanisms. Materials and methods Ethanolic extract and its n-hexane, chloroform, ethyl acetate and n-butanol fractions, as well as water-soluble polysaccharide, were prepared from dry fruits of Chaenomeles speciosa . The mouse macrophage-like RAW264.7 cells were induced by lipopolysaccharide (LPS) and used as an inflammatory cell model. Production of nitric oxide in the cells was determined by the Griess assay, and cell viability was tested by the MTT method. Cellular apoptosis was evaluated by fluorescence-activated cell sorting. Relative quantification of inflammation-related genes was analyzed by real-time PCR. Results LPS-induced production of nitric oxide in RAW264.7 cells was significantly inhibited by the ethyl acetate fraction (EAF) at 200–800 μg/ml, while Chaenomeles speciosa polysaccharide (CPS) promoted nitric oxide production at 250–750 μg/ml either alone or in an additive fashion with LPS. Both EAF and CPS did not provoke noticeable cytotoxicity and apoptosis at the above effective concentrations. EAF significantly reduced LPS-induced upshift of iNOS mRNA level but showed no significant effect on the induction of IFN-γ and G-CSF , while CPS reduced the gene induction of TNF-α , IFN-γ and G-CSF by LPS. Conclusions EAF was able to inhibit nitric oxide production by reducing LPS-induced upshift of iNOS mRNA level. CPS was an activator of nitric oxide production through cytokines such as TNF-α , IFN-γ and G-CSF . These results demonstrate the therapeutic effects of both ethanolic and aqueous extracts of Chaenomeles speciosa fruit, a traditional edible medicine used in health maintenance and disease treatment.

The quality of Chinese quince fruit is a significant factor for medicinal materials, influencing the quality of the medicine. However, it is difficult to distinguish different types of Chinese quince fruit. The main objective of this work was to use near-infrared (NIR) spectroscopy, which is a rapid and non-destructive analysis method, to classify the varieties of Chinese quince fruits. Raw spectra in the range of 1000 to 2500 nm were combined with linear discriminant analysis (LDA), quadratic discriminant analysis (QDA), and support vector machines (SVMs) for classification. The first three principal component analysis (PCA) scores were used as input variables to build LDA, QDA, and SVM discriminant models. The results indicate that all three of these methods are effective for distinguishing the different types of Chinese quince fruit. The classification accuracies for LDA, QDA, and SVM are 94, 96, and 98 %, respectively. QDA led to high-level classification accuracy of Chinese quince fruit.

Gingivitis and periodontial disease are inflammatory disorders that lead to the progressive destruction of gingival tissues and alveolar bone. The mechanisms underlying the destructive processes involve both direct tissue damage, resulting from periodontal pathogens, and indirect damage through host inflammatory reaction. Invasive pathogenic anerobic bacteria are believed to be responsible for this inflammatory response. Fourteen botanical extracts, used in traditional medicine for oral health, were tested against three of the most important anerobic peridontal pathogens including Porphyromonas gingivalis (PG), Fusobacterium nucleatum (FN) and Streptococcus mutans (SM). Of the 14 extract tested six were active and minimal inhibitory concentrations (MICs) were obtained. 95% EtOH extracts of Punica granatum L. (Punicaceae) peel, Moringa oleifera Lam. (Moringaceae) bark or Aegle marmelos (L.) Correa (Rutaceae) fruit inhibited the growth of PG with an MIC of 64 µg/mL, 128 µg/mL, and 128 µg/mL, respectively; a 95% extract of Chaenomeles speciosa (Sweet) Nak. (Rosaceae) quince fruit inhibited the growth of FN with an MIC of 128 µg/mL. Boesenbergia rotunda (L.) Mansfield (Zingiberaceae) rhizome extract inhibited the growth of FN and PG with an MIC of 128 µg/mL for both. Litsea elliptica Blume (Lauraceae) leaf extract inhibited the growth of inhibited the growth of FN with an MIC of 64 µg/mL and PG with an MIC of 32 µg/mL. None of the extracts inhibited the growth of S. mutans. The results indicate that several botanical extracts used in traditional medicine have activity against anerobic oral pathogens and maybe useful for the treatment of gingivitis or peridontal disease. Acknowledgements: Partial support for this work was made possible by a grant from the Wm. Wrigley Company.

The fruit of Chaenomeles speciosa is a traditional Chinese medicine used for the treatment of dyspepsia and various inflammatory diseases. In the present study, we evaluated the potential radical scavenging capacity, and activity against nitrous oxide, inflammatory cytokines production and neuramindase (NA) of its isolates. The results showed that 3,4-dihydroxybenzoic acid (1) displayed higher inhibitory activities on DPPH and NA with IC50 values of 1.02 mg/mL and 1.27 mg/mL respectively, and quercetin (2) also showed significant inhibitory action on DPPH and NA, with IC50 values of 3.82 mg/mL and 1.90 mg/mL. Compounds 1, 2 and methyl 3-hydroxybutanedioic ester (3) could inhibit the production of TNF-a by 22.73%, 33.14% and 37.19% at 5 mg/mL (P < 0.05) compared with the control. In addition, compound 2 was found to be active on the release of IL-6 in RAW264.7 macrophage cells, with an inhibitory rate of 39.79% (P < 0.05). The anti-inflammatory effect of compound 3 is disclosed for the first time in this study. Avian influenza is usually accompanied by virus invasion followed by the occurrence of oxidative stress and serious inflammation, so the multiple effects of the isolates may play a cocktail-like role in the treatment of avian influenza, and C. speciosa components, especially quercetin, might be a potent source for anti-viral and anti-inflammatory agents.

Objective:To investigate the chemical constituents of Chaenomeles speciosa.Methods:The chemical constituents of Chaenomeles speciosa was analyzed by various chromatographic methods.The structures of the compounds were identified based on physicochemical properties and spectral data.Results:Nine compounds were obtained from the ethyl acetate fraction of C.speciosa and were identified as methyl chlorogenate (Ⅰ),5-O-cafeoyl quinic acid butyl ester (Ⅱ),quinic acid butyl ester (Ⅲ),5-hydroxymethyl-furan-2-carbaldehyde (Ⅳ),triacontanoic acid (Ⅴ),(-)-epicatichin (Ⅵ),7,8-dihydroxy-coumanrin (Ⅶ),protocatechuic acid ethyl ester (Ⅷ),and protocatechuic acid (Ⅸ).Conclusion:Compounds Ⅲ-Ⅷ have been obtained from this genus for the first time.

The prescription of current existing anti-inflammatory drugs is hampered by their adverse effects over time. Botanical extracts are thought to be a potential source of a natural anti-inflammatory property with fewer adverse effects. Chaenomeles speciosa has long been used as an herbal medicine for treatment of various diseases such as rheumatoid arthritis, prosopalgia, and hepatitis. Until now there have been no reports on the specific anti-inflammatory fractions of extract of C. speciosa (ECS). In the present study the anti-inflammatory activities of different fractions of ECS were evaluated using carrageenan-induced paw edema in rats. The 10% ethanol fraction (C3) was found to have stronger anti-inflammatory effects compared with other fractions at the same dose. We also found that chlorogenic acid was one of the active constituents responsible for the anti-inflammatory effect using bioassay-guided fractionation by means of high-performance liquid chromatography. Compared with controls, fraction C3 demonstrated significant anti-inflammatory activity in the xylene-induced ear edema test (P.01), acetic acid-induced peritoneal capillary permeability test, and the cotton pellet granuloma test in mice or rats (P.01); it also showed marked analgesic activity in the acetic acid-induced abdominal contraction test and formalin-induced paw licking test in mice and rats (P.05 or .01). However, fraction C3 showed no significant effect in the hot plate test in mice. These findings justify the use of the C. speciosa for treating pain and inflammation. These results support the proposal of C. speciosa fraction C3 as a potential anti-inflammatory agent.

The oxynitrilase in Chaenomeles Speciosa seed meal was used as the biocatalyst to synthesize a series of chiral methyl ketone cyanohydrins with satisfactory conversion and conspicuous enantiomeric excess. The optimized reaction conditions including the organic solvent, the ratio of biphasic solvents as well as the pH of the reaction system were investigated.

Objective To establish reliable methods for evaluating the quality of Chinese herb fructus chaenomelis. Methods Qualitative analysis by Thin layer chromatography (TLC), reference substances were Chaenomeles speciosa (Sweet) Nakai and oleanolic acid, a mixed solvent of chloroform-methanol (40:1) was employed as the mobile phase, color developing agent was 10% sulfuric acid-ethanol solution. In the system of high performance liquid chromatography (HPLC), a Prontosil Eurobond C18 column (250 mmx4.0 mm, 5 μm) was used, the mobile phase was composed of acetonitrile-methanol-0.4% ammonium acetate solution (55:25:20), the flow rate was 1.0 ml/min with UV detected at 210 nm, the column temperature was maintained at room temperature. Results In the system of TLC, oleanolic acid was separated successfully. In HPLC, the linear ranges of oleanolic acid and ursolic acid were 5.89±13.73 μg (R=0.9990) and 6.84±15.96 μg (R=0.9990), respectively. The average recoveries of oleanolic acid and ursolic acid were 97.52% (RSD=2.58%), 98.21% (RSD=2.23%), respectively. Conclusion The established TLC method can easily distinguish Chinese herb fructus chaenomelis from other commonly used crude drugs of the same family. The HPLC method for determining oleanolic acid and ursolic acid is simple, reproducible, accurate and feasible. The methods reported in this paper can be used scientifically and effectively to evaluate the quality of Chinese herb fructus chaenomelis.

The chemical composition of essential oil obtained by hydrodistillation from the dried fruits of Chaenomeles speciosa was analyzed by GC–MS. Forty compounds, constituting about 85.13% of the total oil, were identified. The main constituents were β-caryophyllene (12.52%), α-terpineol (5.41%), terpinen-4-ol (4.56%) and 1,8-cineole (4.31%). The antimicrobial activity of the oil was evaluated against 10 microorganisms using disc diffusion and broth microdilution methods. The essential oil was found to show a broad spectrum of antimicrobial activity against all the tested bacterial strains. The essential oil had more sensitivity to gram-positive than gram-negative bacteria.

The aim of this study was to evaluate several plant extracts with a view to developing melanogenesis inhibitors. In this study, 100 plant extracts were screened to elucidate their whitening effects using in vitro inhibition of tyrosinase and DOPA auto-oxidation activity. Several plant extracts such as Chaenomeles speciosa, Dryopteris crassirhizoma, Gastrodia ellata, Glycyrrhiza glabra, Morus alba, Myristica fragrans, Rheum palmatum and Sophora japonica showed inhibition of mushroom tyrosinase activity. Plant extracts including Bupleurum falcatum, Caragana sinica, Morus alba and Tussilago farfara showed inhibition of DOPA auto-oxidation activity. L'objet de cette etude etait d'evaluer plusieurs extraits vegetaux dans le but de developper des inhibiteurs de la melanogenese. Dans cette etude, on a crible 100 extraits vegetaux pour connaitre leurs effets blanchissants en utilisant in vitro l'inhibition de la tyrosinase et de l'activite auto-oxydante de la DOPA. Plusieurs extraits vegetaux tels que Chaenomeles speciosa, Dryopteris crassirhizoma, Gastrodia ellata, Glycyrrhiza glabra, Morus alba, Myristica fragrans, Rheum palmatum et Sophora japonica presentent une activite d'inhibition de la tyrosinase du champignon. Des extraits vegetaux comprenant Bupleurum falcatum, Caragana sinica, Morus alba et Tussilago farfara montrent une inhibition de l'activite d'auto-oxydation de la DOPA.

Fire blight, caused by the bacterium Erwinia amylovora (Burrill) Winslow et al., is one of the most destructive diseases of plants in the Rosaceae subfamily Maloideae. Artificial inoculations, using E. amylovora strain E2002a, were conducted to determine levels of resistance to fire blight among taxa of flowering pears (Pyrus L. spp.) and quince (Chaenomeles Lindl. spp.). The level of resistance was measured as the length of the fire blight lesion as a percentage of overall shoot length. Considerable variation in resistance was observed among both pears and quince. Pyrus ussuriensis Maxim. `Prairie Gem' was highly resistant with a lesion length of 1% of the total shoot length. Pyrus calleryana Decne. `Bradford' was intermediate with a 50% lesion length while P. calleryana `Chanticleer' was significantly more resistant with a lesion length of 31%. Nine pear taxa were highly susceptible and did not differ significantly from 100% disease severity (total shoot death). Chaenomeles speciosa (Sweet) Nak. `Contorta' was highly resistant with a lesion length of 15%. Six quince taxa, including C. × superba (Frahm) Rehd. `Cameo', `Texas Scarlet', and `Jet Trail' were highly susceptible while nine other taxa showed intermediate resistance.

Mugua, fruit of the genus Chaenomeles, is a valuable source of health food and Chinese medicine. To elu- cidate the bioactive compounds of five wild Chaenomeles species, extracts from fresh fruits were investi- gated by HPLC-DAD/ESI-MS/MS. Among the 24 polyphenol compounds obtained, 20 were flavan-3-ols (including catechin, epicatechin and procyanidin oligomers). The mean polymerisation degree (mDP) of procyanidins was examined by two acid-catalysed cleavage reactions; the mDP value was the highest in Chaenomeles sinensis and the lowest in Chaenomeles japonica. Total polyphenol content (TPC) reached 46.92 and 46.28 mg/g gallic acid equivalents (GAE) in Chaenomeles speciosa and Chaenomeles thibetica, respectively, although their main bioactive compounds were different (being epicatechin and procyani- din B2 in the former, and catechin and procyanidin B1 in the latter). These two species also exhibited equally strong free radical scavenging activities. Our results further showed that the antioxidant ability of Chaenomeles fruits was significantly correlated to their total polyphenol contents. Two triterpenes (ole- anolic acid and ursolic acid) were the highest quantity in Chaenomeles cathayensis and C. thibetica, respectively.

This study was conducted to explore antioxidative property and antiatherosclerotic effects of the powder processed from Chaenomeles speciosa. Chaenomeles speciosa powder (CSP) was rich in vitamin C and polyphenols. The ferric reducing antioxidant power of CSP was 173 ± 7 µmol Fe2+/g and the scavenging activity on 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH•) andwere 945 ± 20 µg DPPH•/g and 700 ± 21 U/mL, respectively. We further tested antiatherosclerotic effects of CSP in ApoE–/– mice which was fed a high-fat diet for 16 weeks. Both 5 and 10% CSP dietary supplement significantly reduced serum low-density lipoprotein cholesterol and total cholesterol levels (P

In order to develop a model for screening the agonists of human beta(2)-adrenoceptor from Chinese medicinal herbs extracts, we used a cell-based functional assay based on a common G protein-coupled receptor (GPCR) regulation mechanism and destabilized enhanced green fluorescent protein (d(2)EGFP) reporter gene technique. The positive cell clone was confirmed by real-time polymerase chain reaction (PCR) and imaging analysis. To assess the value of this model, we screened over 2000 high performance liquid chromatography (HPLC)-fractionated samples from the ethanol extracts of Chinese medicinal herbs. Six fractions (isolated from Panax japonicus, Veratrum nigrum, Phellodendron amurense, Fructus Aurantii Immaturus, Chaenomeles speciosa, and Dictamnus dasycarpus) showed significant effects on active reporter gene expression, three of which (isolated from Phellodendron amurense, Fructus Aurantii Immaturus, and Chaenomeles speciosa) were selected for further concentration response analysis and the half maximal effective concentration (EC(1/2 max)) values were 4.2, 2.7, and 4.8 microg/ml, respectively. Therefore, this reporter gene assay was suitable for screening beta(2)-adrenoceptor agonists. The results suggest that the six herbal extracts are the possible agonists of beta(2)-adrenoceptor.

Investigation on the EtOH extract of the fruits of Chaenomeles speciosa led to the isolation of a new triterpene acid bearing an unusual hydroperoxyl substitute group at C-11, speciosaperoxide (1), along with six known triterpenoids, 3beta-acetoxyurs-11-en-13beta,28-olide (2), 3-O-acetyl ursolic acid (3), oleanolic acid (4), ursolic acid (5), masilinic acid (6), and tormentic acid (7), and three known norsesquiterpenoids, roseoside (8), vomifoliol (9) and (6S,7E,9R)-6,9-dihydroxy-4,7-megastigmadien-3-one 9-O-[beta-d-xylopyranosyl (1 --> 6)-glucopyranoside] (10). Their structures were elucidated on the basis of spectroscopic data and comparison with reference data. Besides compound 1, compounds 2, 8-10 were obtained from this genus for the first time. None of these compounds exhibited inhibitory activity against T-and B-lymphocyte proliferation.

Enterotoxigenic Escherichia coli (ETEC) is responsible for millions of deaths in developing countries. Heat-labile enterotoxin (LT), the virulence factor of ETEC, induces diarrhea by initially binding to the G(M1) on the surface of intestinal epithelial cells and consequently leading to the massive loss of fluid and ions from cells. Fruit of Chaenomeles (FC), the dried fruit of Chaenomeles speciosa, has been used for diarrhea in China. However, the anti-diarrheal mechanism of FC is still unclear. In this study, we demonstrated that FC extract (FCE) inhibited the LT-induced diarrhea in mice by blocking the binding of the B subunit of LT (LTB) to G(M1). The ethyl acetate (EA) soluble fraction was the most active fraction of FC that significantly abolished the LTB and G(M1) interaction. Furthermore, the oleanolic acid, ursolic acid, and betulinic acid from EA fraction, blocked the toxin binding effects, resulting in the suppression of LT-induced diarrhea. Moreover, by docking techniques, these compounds fitted LTB well via hydrogen bonds and hydrophobic contacts with amino acid residues of LTB. In conclusion, our findings suggested that oleanolic acid, ursolic acid, and betulinic acid were the active constituents from FC and might be considered as lead therapeutic agents in the treatment of LT-induced diarrhea.

The volatile components isolated from Flowering Quince fruit were analyzed by capillary GC and GC/MS. Nineteen compounds were identified of which hexanal, ethyl butyrate, (E)-2-hexenal, (Z)-3-hexenyl acetate, ethyl hexanoate, linalool, trans-linalool oxide (furanoid), cis-linalool oxide (furanoid), α-terpineol, ethyl octanoate, Edulan I, ethyl (Z)-4-decenoate and ethyl p-methoxybenzoate were the major constituents.

The dietary fibre in the fruits of 12 genotypes of Japanese quince (Chaenomeles japonica) and 1 genotype of flowering quince (Chaenomeles speciosa) were prepared using two different methods: the alcohol insoluble solid (AIS) preparation; and the Association of Official Analytical Chemists (AOAC) method for total as well as for soluble and insoluble fibre. The two methods resulted in similar but significantly different estimates. No interaction was revealed between the methods and the genotypes studied. For content of total dietary fibre, three main groups could be distinguished: a group containing a low amount of fibre (three genotypes, 28–30 g/100 g dry matter), a group containing a medium amount of fibre (nine genotypes, 30–36 g/100 g dry matter) and an isolated genotype (Chaenomeles speciosa) that contained a considerable amount of fibre (38 g/100 g dry matter). The amount and the nature of monomeric sugars in the constitutive polysaccharides of the fibres were determined after total hydrolysis of the AIS or the total dietary fibre (TDF). The fibre contained mostly pectic and cellulosic polysaccharides. Analysis of the fibre from different parts of the fruits of two genotypes showed that they differed in their proportion of constituent polysaccharides (cellulose, hemicelluloses and pectic polysaccharides).