Flower opening dynamics, pollen-ovule ratio, stigma receptivity and stigmatic pollen germination (in-vivo) in Chaenomeles speciosa (Sweet) Nakai.

Although Chaenomeles is widely used in horticulture, traditional Chinese medicine and landscape greening, insufficient research has hindered its breeding and seed selection. This study investigated the floral phenology, floral organ characteristics, palynology, and breeding systems of Chaenomeles speciosa (Sweet) Nakai. The floral characteristics of C. speciosa were observed both visually and stereoscopically. The microstructures of the flower organs were observed using scanning electron microscopy. Pollen stainability was determined using triphenyl tetrazolium chloride staining. Stigma receptivity was determined using the benzidine-H2O2 method and the post-artificial pollination pollen germination method. The breeding system was assessed based on the outcrossing index and pollen-ovule ratio. The flowers of C. speciosa were bisexual with a flowering period from March to April. The flowering periods of single flowers ranged from 8 to 19 d, and those of single plants lasted 18-20 d. The anthers were cylindrical, with the base attached to the filament, and were split longitudinally to release pollen. The flower had five styles, with a connate base. The ovaries had five carpels and five compartments. The inverted ovules were arranged in two rows on the placental axis. The stigma of C. speciosa was dry and had many papillary protrusions. In the early flowering stage (1-2 d of flowering), the pollen exhibited high stainability (up to 84.24%), but all stainability was lost at 7 d of flowering. Storage at - 20 °C effectively delayed pollen inactivation. The stigma receptivity of C. speciosa lasted for approximately 7 days, and the breeding system was classified as outcrossing with partial self-compatibility.

Pulp or Peel? Comparative Analysis of the Phytochemical Content and Selected Cosmetic-Related Properties of Annona cherimola L., Diospyros kaki Thumb., Cydonia oblonga Mill. and Fortunella margarita Swingle Pulp and Peel Extracts.

Fruit peels might be a valuable source of active ingredients for cosmetics, leading to more sustainable usage of plant by-products. The aim of the study was to evaluate the phytochemical content and selected biological properties of hydroglycolic extracts from peels and pulps of Annona cherimola, Diospyros kaki, Cydonia oblonga, and Fortunella margarita as potential cosmetic ingredients. Peel and pulp extracts were compared for their antiradical activity (using DPPH and ABTS radical scavenging assays), skin-lightening potential (tyrosinase inhibitory assay), sun protection factor (SPF), and cytotoxicity toward human fibroblast, keratinocyte, and melanoma cell lines. The total content of polyphenols and/or flavonoids was significantly higher in peel than in pulp extracts, and the composition of particular active compounds was also markedly different. The HPLC-MS fingerprinting revealed the presence of catechin, epicatechin and rutoside in the peel of D. kaki, whereas kaempferol glucoside and procyanidin A were present only in the pulp. In A. cherimola, catechin, epicatechin and rutoside were identified only in the peel of the fruit, whereas procyanidins were traced only in the pulp extracts. Quercetin and luteolinidin were found to be characteristic compounds of F. margarita peel extract. Naringenin and hesperidin were found only in the pulp of F. margarita. The most significant compositional variety between the peel and pulp extracts was observed for C. oblonga: Peel extracts contained a higher number of active components (e.g., vicenin-2, kaempferol rutinoside, or kaempferol galactoside) than pulp extract. The radical scavenging potential of peel extracts was higher than of the pulp extracts. D. kaki and F. margarita peel and pulp extracts inhibited mushroom and murine tyrosinases at comparable levels. The C. oblonga pulp extract was a more potent mushroom tyrosinase inhibitor than the peel extract. Peel extract of A. cherimola inhibited mushroom tyrosinase but activated the murine enzyme. F. margarita pulp and peel extracts showed the highest in vitro SPF. A. cherimola, D. kaki, and F. margarita extracts were not cytotoxic for fibroblasts and keratinocytes up to a concentration of 2% (v/v) and the peel extracts were cytotoxic for A375 melanoma cells. To summarize, peel extracts from all analyzed fruit showed comparable or better cosmetic-related properties than pulp extracts and might be considered multifunctional active ingredients of skin lightening, anti-aging, and protective cosmetics.

Modified Chinese quince oligomeric proanthocyanidin protects deep-frying oil quality by inhibiting oxidation.

Chinese quince (Chaenomeles sinensis) fruit is an underutilized resource, rich in proanthocyanidins with antioxidant ability but poor lipid solubility. In this study, a novel modified oligomeric proanthocyanidin (MOPA) was prepared, which exhibited favorable lipid solubility (354.52 mg/100 g). It showed higher radical scavenging abilities than commercial antioxidant-BHA (butylated hydroxyanisole), both at 0.4-0.5 mg/mL. The addition of MOPA (0.04 %wt.) significantly increased the oxidative stability index of the soybean oil from 5.52 to 8.03 h, which was slightly lower than that of BHA (8.35 h). Analysis of the physicochemical properties and composition of oil during deep-frying showed that MOPA demonstrated significant antioxidant effects and effectively restricted the oil oxidation. This inhibition also delays the formation of heterocyclic amines (HAs) in fried food, thereby reducing the migration of HAs from food to deep-frying oil. Therefore, MOPA is a promising novel liposoluble antioxidant for protecting the quality of deep-frying oil.

One-step enrichment of phenolics from Chaenomeles speciosa (Sweet) Nakai fruit using macroporous resin: Adsorption/desorption characteristics, process optimization and UPLC-QqQ-MS/MS-based quantification.

Chaenomeles speciosa (Sweet) Nakai fruit is a good source of phenolics with many health benefits. In this work, the enrichment of C. speciosa fruit total phenolics (CSFTP) using macroporous resins was studied. NKA-Ⅱ resin was selected for enriching CSFTP due to its highest adsorption/desorption quantity. Adsorption characteristics of CSFTP on NKA-Ⅱ resin exhibited a good fit with the Langmuir isotherm model and pseudo-second order kinetics model. This adsorption was spontaneous, exothermic, and entropy-decreasing through a physisorption mechanism. The breakthrough-elution curves were studied to optimize CSFTP enrichment conditions. One-step enrichment increased CSFTP content in the extracts from 26.51 % to 78.63 %, with a recovery of 81.03 %. A UPLC-QqQ-MS/MS method in multiple reaction monitoring (MRM) mode was established and validated for the simultaneous quantification of seven phenolic compounds. This study demonstrates the feasibility of industrial enrichment of CSFTP using NKA-Ⅱ resin and proposes a reliable method for quality control of CSFTP-rich products.

Polyphenol-enriched extracts of Sarcopoterium spinosum fruits for counteracting lipid accumulation and oxidative stress in an in vitro model of hepatic steatosis.

Sarcopoterium spinosum (L.) Spach is a Rosaceae shrub employed in the folk medicine in the Eastern Mediterranean basin. The previous few studies have focused on the S. spinosum roots, while the fruits have been poorly investigated. The present study aims to assess the biological properties of S. spinosum fruits collected in Lebanon and subjected to ethanolic, water or boiling water extraction. The extracts were compared for the phenol and flavonoid contents, and for the in vitro radical scavenging ability. The ethanolic extract (SEE) was selected and characterized by high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS/MS) showing a phenolome rich in tannins (ellagitannins), flavonoids (quercetin derivatives), and triterpenes. The biological activity of SEE was tested on a cellular model of moderate steatosis consisting of lipid-loaded hepatic cells treated with increasing concentrations of SEE (1-25 µg/mL), or with corilagin or quercetin as comparison. In steatotic hepatocytes the SEE was able (i) to ameliorate the hepatosteatosis; (ii) to counteract the excess ROS and lipid peroxidation; (iii) to restore the impaired catalase activity. The results indicate that the ethanolic extract from S. spinosum fruits is endowed with relevant antisteatotic and antioxidant activities and might find application as nutraceutical product.

Exploring the potential of phenolic and antioxidant compounds in new Rosaceae fruits.

BACKGROUND: Rosaceae fruits have been used in traditional medicine for the prevention and treatment of diseases. However, these fruits have not extensively been studied regarding their phenolic composition. Thus, this research focuses on the determination of phenolic compounds by high-performance liquid chromatography electrospray ionization time-of-flight mass spectrometry, flavan-3-ols by high-performance liquid chromatography with fluorescence detection, and the antioxidant activity by 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and ferric reducing antioxidant power of the fruits of five species of genera Crataegus and Sorbus (Rosaceae). RESULTS: We found a total of 71 phenolic compounds from which 30 were identified in these berries for the first time. Crataegus monogyna and Crataegus laciniata revealed higher total phenolic and flavan-3-ol contents than the other species and the highest antioxidant activities. CONCLUSIONS: Therefore, the fruits evaluated have demonstrated to be important sources of bioactive compounds with huge potential for being used in nutraceutical or food scopes. Additional studies could be needed to evaluate the influence of the different production areas on the phenolic content. © 2023 The Authors. Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Phytochemistry and pharmacology of plants in the genus Chaenomeles.

Chaenomeles plants belong to the Rosaceae family and include five species, Chaenomeles speciosa (Sweet) Nakai, Chaenomeles sinensis (Thouin) Koehne, Chaenomeles japonica (Thunb.) Lindl, Chaenomeles cathayensis (Hemsl.) Schneid and Chaenomeles thibetica Yu. Chaenomeles plants are found and cultivated in nearly every country worldwide. China serves as both the origin and distribution hub for the plants in the Chaenomeles genus, and all Chaenomeles species except for C. japonica are indigenous to China. Chaenomeles spp. is a type of edible medicinal plant that has been traditionally used in China to treat various ailments, such as rheumatism, cholera, dysentery, enteritis, beriberi, and scurvy. A variety of chemical constituents have been extracted from this genus, including terpenoids, phenolics, flavonoids, phenylpropanoids and their derivatives, benzoic acid derivatives, biphenyls, oxylipins, and alkaloids. The biological activity of some of these constituents has already been evaluated. Pharmacological investigations have demonstrated that the plants in the genus Chaenomeles exhibit anti-inflammatory, analgesic, antioxidant, antihyperglycemic, antihyperlipidemic, gastrointestinal protective, antitumor, immunomodulatory, antibacterial, antiviral, hepatoprotective, neuroprotective and other pharmacological activities. The objective of this review is to provide a comprehensive and up-to-date summary of the available information on the genus Chaenomeles to serve as a valuable reference for further investigations.

A High-Quality Reference Genome Assembly of Prinsepia uniflora (Rosaceae).

This study introduces a meticulously constructed genome assembly at the chromosome level for the Rosaceae family species Prinsepia uniflora, a traditional Chinese medicinal herb. The final assembly encompasses 1272.71 megabases (Mb) distributed across 16 pseudochromosomes, boasting contig and super-scaffold N50 values of 2.77 and 79.32 Mb, respectively. Annotated within this genome is a substantial 875.99 Mb of repetitive sequences, with transposable elements occupying 777.28 Mb, constituting 61.07% of the entire genome. Our predictive efforts identified 49,261 protein-coding genes within the repeat-masked assembly, with 45,256 (91.87%) having functional annotations, 5127 (10.41%) demonstrating tandem duplication, and 2373 (4.82%) classified as transcription factor genes. Additionally, our investigation unveiled 3080 non-coding RNAs spanning 0.51 Mb of the genome sequences. According to our evolutionary study, P. uniflora underwent recent whole-genome duplication following its separation from Prunus salicina. The presented reference-level genome assembly and annotation for P. uniflora will significantly facilitate the in-depth exploration of genomic information pertaining to this species, offering substantial utility in comparative genomics and evolutionary analyses involving Rosaceae species.

Production and evaluation of total phenolics, antioxidant activity, viscosity, color, and sensory attributes of quince tea infusion: Effects of drying method, sonication, and brewing process.

This study aimed to examine the influence of drying approaches (convective and infrared (IR)), sonication, and brewing time on the total phenolic content (TPC), antioxidant activity (AA), viscosity, color indexes, and sensory attributes of quince tea infusion (QTI). The AA and TPC in the QTI dried in the IR dryer were higher than in the convective dryer. The TPC and AA of QTI prepared by convective and IR dryers increased when the ultrasound treatment and brewing time were increased. In terms of viscosity and Brix, there was no differences between the QTIs and the average viscosity and density of the samples were 1.79 ± 0.28 mPa.s and 3.18 ± 0.07°Brix, respectively. The QTI prepared by the IR has a reddish-brown hue (higher a* value), but the samples prepared with the convective dryer were yellow (higher b* value). The sensory attributes scores of QTI prepared by IR were higher than those of convection-dried samples. In general, the use of an IR dryer for drying grated quince, ultrasound treatment for 8 min, and brewing time for 30 min is a promising condition for the production of QTI with higher TPC and AA, and with appropriate color and sensorial acceptance.

Biodegradable nano-reinforced packaging with improved functionality to extend the freshness and longevity of Plums Oemleria cerasiformis.

Food packaging reinforced with Zn-doped TiO2 nanoparticles with enhanced prerequisite film-forming and biodegradable traits was prepared to augment fresh food storage. Pure and tailored metal (Zinc, Copper, and Selenium) doped TiO2 nanoparticles were synthesized and analyzed through multiple characterization techniques (optical spectra, XRD patterns (X-Ray Diffraction), Dynamic Light Scattering, and Scanning Electron Microscopy). The synthesized nanoparticles were tested for their Minimum Inhibitory Concentrations, antimicrobial potential against common lethal food pathogens, and cytotoxicity. Compared to Cu- and Se-doped nanoparticles, Zn-doped TiO2 nanoparticles displayed the most potent antimicrobial activity with insignificant cytotoxicity and were incorporated into the food packaging materials. The developed nano-reinforced food packaging efficaciously augmented the freshness of plums (Oemleria cerasiformis) for 16 days (42 ± 2 °C). The physicomechanical characterization of the nano-reinforced packaging establishes its utility in food packaging applications. The developed biodegradable packaging undergoes complete decomposition within 12 days of storage in natural soil.

Non-Targeted Screening of Metabolites in Aqueous-Ethanol Extract from Spiraea hypericifolia (Rosaceae) Using LC-HRMS.

By means of liquid chromatography combined with high-resolution mass spectrometry, metabolite profiling was performed on an aqueous-ethanol extract from Spiraea hypericifolia (Rosaceae) collected in Siberia (Russia). Up to 140 compounds were found in the extract, of which 47 were tentatively identified. The identified compounds were amino acids, sugars, phenylpropanoids, fatty acids and their derivatives, triterpenoids, flavonoids, and others. A quantitative analysis showed the predominance of phenolcarboxylic acids and flavonoids in the studied extract, but a qualitative analysis revealed the higher structural diversity of flavonoids. Of the 23 identified flavonoids, 13 were flavonols: quercetin, hyperoside, isoquercitrin, reynoutrin, avicularin, rutin, quercetin-3-O-(6″-O-malonyl)-ß-D-glucoside, 3-O-methylquercetin-3'-O-ß-D-glucopyranoside, isorhamnetin, rhamnetin-3-O-ß-D-xylopyranosyl-ß-D-glucopyranoside, kaempferol, tiliroside, and trifolin; six were catechins: catechin, (-)-epicatechin, (+)-epicatechin, (+)-catechin-7-O-ß-D-xyloside, (2S,3R)-3,5-dihydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-7-yl-ß-D-glucopyranoside, and catechin 7-O-apiofuranoside; two are isoflavones: genistin and genistein; and one was a flavone (luteolin-4'-O-ß-D-glucopyranoside) and another was an anthocyanidin (pelargonidin). The aqueous-ethanol extract from S. hypericifolia showed antioxidant activity (half-maximal inhibitory concentration 102.95 µg/mL), which was likely related to the high concentrations of phenolcarboxylic acids (229.6 mg/g), flavonoids (118.3 mg/g), and tannins (62.9 mg/g).

Green synthesis of quince/pectin cross-linked superporous hydrogel sponges for pH-regulated sustained domperidone delivery.

The present study aims to utilize green synthesis to fabricate stimuli-responsive, smart, quince/pectin cross-linked hydrogel sponges for the pH-regulated conveyance of domperidone. The designed hydrogel sponges were evaluated for a sol-gel fraction (%), swelling studies and kinetics, drug loading (%), electrolyte-responsive character, scanning electron microscopy (SEM), thermal analysis, drug-excipient compatibility studies (FTIR), X-ray diffraction (XRD) analysis, mechanical testing, in-vitro drug release studies, and acute oral toxicity studies. The drug loading (%) ranged from 67 to 85%. Hydrogel sponges displayed pH-responsive swelling potential, with optimum swelling in a phosphate buffer (pH 7.4) and insignificant swelling in an acidic buffer of pH 1.2. The prepared hydrogel sponges displayed second-order swelling dynamics. The FTIR data revealed the successful fabrication of the hydrogel sponges with the primary drug peaks remaining unchanged, demonstrating excipients-drug compatibility. SEM confirmed the rough, porous surface of hydrogel sponges with numerous cracks. XRD measurements revealed the transformation of the crystalline nature of domperidone into an amorphous one within the developed hydrogel sponges. Dissolution studies revealed little domperidone release in an acidic environment. However, hydrogel sponges exhibited release up to 10 h in phosphate buffer.The sponge's non-toxic or biocompatible character was confirmed through toxicological studies. Thus, the finding indicates that quince/pectin cross-linked hydrogel sponges are durable enough to deliver the domperidone to the gut for a longer time.

Microwave drying of quince coated with seed gum and pectin: A Taguchi optimization, techno-functional properties, and aromatic compounds.

In this study, the effects of coating quince slices with CaCl2 and pectin (C + P) followed by drying with microwave (MWD-C + P) or with hot air (HAD-C + P) were investigated to determine the physicochemical, techno-functional, textural, and volatile components of dried quince slices. A Taguchi orthogonal experimental design was set up with 18 points (L18 ), and the best conditions for drying were obtained using signal/noise ratio method. Coating quince slices with C + P and then drying with microwave at 450 W displayed the higher results compared to other points in terms of color, total phenolic, antioxidant activity, antimicrobial activity, and water holding capacity. MWD-C + P application dramatically changed the textural properties of dried quince slices in terms of hardness, gumminess, and chewiness. Moreover, MWD, lasted 12-15 min, was superior to HAD in the context of drying time. Ultrasonication as a pretreatment had no positive impact on dried products. GC-MS analyses revealed that MWD-C + P had positive effects on dried quince slices in terms of ethyl hexanoate and octanoic acid. However, MWD-C + P application triggered the formation of furfural in dried products.

Exploring the chondroprotective effect of Chaenomeles speciosa on Glucose-6-Phosphate Isomerase model mice using an integrated approach of network pharmacology and experimental validation.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional Chinese medicine (TCM) has been used in China for a long time and is gradually gaining more and more recognition worldwide. Chaenomeles speciosa (CSP) (Chinese Pinyin: mugua) is a medicinal and food herb that has long been used as a folk medicine for rheumatic diseases, yet its bioactive components and therapeutic mechanisms are not clear. AIM OF THE STUDY: Exploring anti-inflammatory and chondroprotective effects of CSP on rheumatoid arthritis (RA) and its possible targets of action. MATERIALS AND METHODS: In this study, we performed an integrated approach of network pharmacology, molecular docking and experimental studies to explore the potential mechanism of action of CSP in the treatment of cartilage damage in RA. RESULTS: Studies have shown that Quercetin, ent-Epicatechin and Mairin may be the main active compounds of CSP in the treatment of RA, while AKT1, VEGFA, IL-1ß, IL-6, MMP9 etc. are considered as core target proteins to which the main active compounds in CSP bind, as further confirmed by molecular docking. In addition, the potential molecular mechanism of CSP for the treatment of cartilage damage in RA predicted by network pharmacology analysis was validated by in vivo experiments. CSP was found to downregulate the expression of AKT1, VEGFA, IL-1ß, IL-6, MMP9, ICAM1, VCAM1, MMP3, MMP13 and TNF-α and increase the expression of COL-2 in the joint tissue of Glucose-6-Phosphate Isomerase (G6PI) model mice. Thus CSP contributes to the treatment of rheumatoid arthritis cartilage destruction. CONCLUSION: This study showed that CSP has multi-component, multi-target and multi-pathway characteristics in treating cartilage damage in RA, which can achieve the effect of treating RA by inhibiting the expression of inflammatory factors, reducing neovascularization and alleviating the damage to cartilage caused by the diffusion of synovial vascular opacities, and reducing the degradation of cartilage by MMPs to play a protective role in RA cartilage damage. In conclusion, this study indicates that CSP is a candidate Chinese medicine for further research in treating cartilage damage in RA.

Surfactant-Free Pickering Emulsification Using Chinese Quince Fruit Fiber.

Quince fruit powder can be obtained from the waste of the edible product. In this study, we modified the powder with various solvents and investigated its application in Pickering emulsification. The crushed Chinese quince fruit possessed excellent Pickering emulsifying abilities when the water-soluble components were removed. In addition to cellulose, the powder contains hydrophilic pectin and hydrophobic lignin fibers. Similarly, a powder consisting of cellulose and a small amount of lignin without pectin, which was obtained by further solvent treatment, also showed high emulsification performance. Although these two powders had different fiber compositions, their water contact angles were almost equal, and their surface hydrophilicity was lower than that of the cellulose-only powder without emulsification ability.

Investigation of the mixing ratio of quince seed gum, potato starch and gellan gum on the properties of the resulting film by Mixture Design.

In this study, the impact of three different biopolymers, namely, quince seed gum, potato starch and gellan gum, at levels of zero to three, on optimizing the biodegradable film was investigated. In order to prepare the mixed edible film, the textural properties of the films, water vapor permeability, water-solubility, transparency, thickness, color parameters, acid solubility and microstructure of the made films were investigated. Numerical optimization of method variables was performed based on the maximum Young's modulus and minimum solubility in water, minimum solubility in acid and minimum water vapor permeability by mixed design, using the Design-Expert software. The results showed that the increase of the quince seed gum directly affected the Young's modulus, tensile strength, elongation to break, solubility in acid, and a* and b* values. However, the rise of the potato starch and gellan gum levels increased the thickness, solubility in water, water vapor permeability, transparency, L* value and Young's modulus, tensile strength, elongation to break, solubility in acid and a* and b* values. The optimal conditions for the production of the biodegradable edible film were selected at the levels of 1.623 %, 1.637 % and 0 % for quince seed gum, potato starch and gellan gum, respectively. The results of scanning electron microscopy showed that the film had more uniformity, coherence and smoothness, as compared to other films studied. The results of this study, thus, showed that there was no statistically significant difference between the predicted and laboratory results (p < 0.05), indicating the good fit of the model designed for producing a quince seed gum/potato starch/gellan gum composite film.

Integrated untargeted metabolome, full-length sequencing, and transcriptome analyses reveal insights into the fruit quality at different harvest times of Chaenomeles speciosa.

Chaenomeles speciosa fruit is a homologous medicine and food plant with a long history of multiple uses. It could be harvested near maturity and last for a long time. However, the optimal harvest strategy of Chaenomeles speciosa for various uses is currently unavailable. Here, untargeted metabolome at different harvest times during maturation was investigated for the first time, and 896 metabolites, including sugars, organic acids, amino acids, and phenylpropanoids, were identified. Optimal harvesting methods were proposed for different purposes. During the early maturation stages (before 105 days after full bloom), Ch. speciosa fruit could be harvested as Chinesemedicine. Whereas as snacks and food, Ch. speciosa fruit might be harvested at late maturity (after 120 days after full bloom). In addition, the overall network was revealed by integrating full-length Iso-seq and transcriptomics (RNA-seq) to investigate the association between quality-associated metabolites and Chaenomeles speciosa fruit gene expression during maturation. A few putative genes were captured via screening, dissecting and correlation analysis with the quality-associated metabolites (including d-glucose, catechin, gallocatechin, and succinic acid). Overall, in addition to providing a harvesting strategy for food and medicine, we also investigated the metabolism and gene expression pattern of Chaenomeles speciosa fruit during maturation. This comprehensive data and analyses laid the foundation for further investigating potential regulatory mechanisms during harvest and provided a new possibility for its development and utilization.

Quince extract resists atherosclerosis in rats by down-regulating the EGFR/PI3K/Akt/GSK-3ß pathway.

We identified the effective components and the underlying mechanisms of Quince (Cydonia oblonga Mill, COM) extract against atherosclerosis. The effective components of COM extract were identified with UHPLC-Q-TOF-MS/MS. Network pharmacology was performed. A rat model of atherosclerosis induced by high-fat emulsion combined with vitamin D3 was established. The anti-atherosclerosis effect of COM extract was evaluated from various aspects such as blood lipid regulation, anti-oxidative stress, anti-inflammatory response, and vascular protection function. We identified 14 serum components of COM extract using UHPLC-Q-TOF-MS/MS. Through prediction, 573 targets were obtained, among which 224 targets were atherosclerosis specific targets. The key targets included GSK3ß, ESR1, EGFR, and HSP90AA1. The key signaling pathway was PI3K-Akt signaling pathway. Pharmacodynamics analysis showed that COM extract reduced the levels of TC, TG, and LDL-C as well as ALT and AST, while increased the level of HDL-C. Mechanistically, COM extract significantly increased serum SOD and GSH-Px activities, but decreased MDA content in atherosclerosis rats, showing antioxidant effects. Meanwhile, COM extract significantly down-regulated the levels of pro-inflammatory factors IL-1ß, IL-6, TNF-α and CRP, but up-regulated anti-inflammatory factor IL-10. Additionally, COM extract increased the levels of NO, eNOS, and 6-keto-PGF1α; whereas, decreased the levels of ET-1 and TXB2. Furthermore, COM extract significantly inhibited the mRNA and protein levels of EGFR, p-PI3K, p-AKT, GSK-3ß, Bax, and Caspase-3 as well as the Bax/Bcl-2 ratio. Conclusively, COM extract exerts hypolipidemic, anti-oxidative, anti-inflammatory, anti-thrombotic and vascular endothelium protective effects on atherosclerosis rat model, which may be related to the inhibition of EGFR/PI3K/AKT/GSK-3ß signaling pathway.

Prinsepia utilis Royle leaf extract: Ameliorative effects on allergic inflammation and skin lesions in allergic contact dermatitis and polyphenolic profiling through UPLC-MS/MS coupled to chemometric analysis.

ETHNOPHARMACOLOGICAL RELEVANCE: Allergic contact dermatitis (ACD) is a common allergic inflammatory disease that is concomitant with skin swelling, redness, dry itching, and relapses. Prinsepia utilis Royle, a Chinese and Indian folk medicine, is rich in polyphenols with potential anti-inflammatory and skin-protective activities. However, the underlying mechanism of P. utilis leaf (PUL) in the treatment of ACD and its functional basis remains unclear. AIM OF THE STUDY: This study is aimed to explore and reveal the active substances and mechanism of PUL against ACD. MATERIALS AND METHODS: Hyaluronidase inhibitory assay and fluorescein isothiocyanate (FITC)-induced ACD mouse model were performed to assess the antiallergic effects of PUL in vitro and in vivo. Different solvents were applied to obtain multiple PUL extracts. The extracts were further tested for total phenolic content (TPC) and total flavonoid content (TFC) by using spectrophotometric assays. Polyphenolic profiles were analyzed by using ultrahigh-performance liquid chromatography coupled with time-of-flight mass spectrometry (UPLC-QTOF-MS/MS), and a simultaneous quantification method was established using UPLC-QTrap-MS/MS through multiple reaction monitoring (MRM) and applied to analyze the pharmacokinetics of the multiple major polyphenols of PUL in mice. RESULTS: The water extract of PUL with the highest TPC/TFC exhibited the strongest antihyaluronidase effect (IC50 = 231.93 µg/mL). In vivo assays indicated that the oral administration of PUL water extract dose-dependently attenuated ACD-like symptoms by decreased interleukin (IL)-4, IL-5, IL-13, IL-33, thymic stromal lymphopoietin, and IgE production, suppressed eosinophil and basophil secretion, and increasing the expression of tight junction (TJ) proteins (claudin-1 [CLDN-1] and occludin). Concomitantly, UPLC-QTOF-MS/MS analysis enabled the identification of 60 polyphenols and the pharmacokinetic parameters of seven quantified constituents of PUL were characterized. Four compounds, trans-p-coumaric acid 4-O-ß-D-glucopyranoside (11), vicenin-2 (21), isoschaftoside (31), and kaempferol 3-O-(2″,6″-di-O-α-L-rhamnopyransoyl)-ß-D-glucopyranoside (38) which displayed satisfactory pharmacokinetic features, were considered as potential effective substances in PUL. CONCLUSIONS: PUL water extract ameliorated the allergic inflammation of ACD by repairing the epithelial barrier and alleviating Th2-type allergic inflammation. The anti-allergic effect of PUL is closely related to its phenolic substances, and compounds 11, 21, 31, and 38 were the active substances of PUL. It revealed that P. utilis could be developed as a new source of antiallergic agents for ACD therapy.

The African cherry: A review of the botany, traditional uses, phytochemistry, and biological activities of Prunus africana (Hook.f.) Kalkman.

ETHNOPHARMACOLOGICAL RELEVANCE: Prunus africana (Hook.f.) Kalkman (Rosaceae), commonly known as "Pygeum" or "African cherry", occurs in mainland montane forests scattered across sub-Saharan Africa, Madagascar, and some surrounding islands. Traditionally, decoctions of the stem-bark are taken orally for the treatment of a wide variety of conditions, such as benign prostatic hyperplasia (BPH), stomach ache, chest pain, malaria, heart conditions, and gonorrhoea, as well as urinary and kidney diseases. The timber is used to make axe handles and for other household needs. The dense wood is also sawn for timber. AIM: The fragmented information available on the ethnobotany, phytochemistry, and biological activities of the medicinally important P. africana was collated, organised, and analysed in this review, to highlight knowledge voids that can be addressed through future research. MATERIALS AND METHODS: A bibliometric analysis of research output on P. africana was conducted on literature retrieved, using the Scopus® database. The trend in the publications over time was assessed and a network analysis of collaborations between countries and authors was carried out. Furthermore, a detailed review of the literature over the period 1971 to 2021, acquired through Scopus, ScienceDirect, SciFinder, Pubmed, Scirp, DOAJ and Google Scholar, was conducted. All relevant abstracts, full-text articles and various book chapters on the botanical and ethnopharmacological aspects of P. africana, written in English and German, were consulted. RESULTS: A total of 455 documents published from 1971 to 2021, were retrieved using the Scopus search. Analysis of the data showed that the majority of these documents were original research articles, followed by reviews and lastly a miscellaneous group comprising conference papers, book chapters, short surveys, editorials and letters. Data were analysed for annual output and areas of intense research focus, and countries with high research output, productive institutions and authors, and collaborative networks were identified. Prunus africana is reported to exhibit anti-inflammatory, analgesic, antimicrobial, anti-oxidant, antiviral, antimutagenic, anti-asthmatic, anti-androgenic, antiproliferative and apoptotic activities amongst others. Phytosterols and other secondary metabolites such as phenols, triterpenes, fatty acids, and linear alcohols have been the focus of phytochemical investigations. The biological activity has largely been ascribed to the phytosterols (mainly 3-ß-sitosterol, 3-ß-sitostenone, and 3-ß-sitosterol-glucoside), which inhibit the production of prostaglandins in the prostate, thereby suppressing the inflammatory symptoms associated with BPH and chronic prostatitis. CONCLUSIONS: Many of the ethnobotanical assertions for the biological activity of P. africana have been confirmed through in vitro and in vivo studies. However, a disparity exists between the biological activity of the whole extract and that of single compounds isolated from the extract, which were reported to be less effective. This finding suggests that a different approach to biological activity studies should be encouraged that takes all secondary metabolites present into consideration. A robust technique, such as multivariate biochemometric data analysis, which allows for a holistic intervention to study the biological activity of a species is suggested. Furthermore, there is a need to develop rapid and efficient quality control methods for both raw materials and products to replace the time-consuming and laborious methods currently in use.