Inhibitive Mechanism of Loquat Flower Isolate on Tyrosinase Activity and Melanin Synthesis in Mouse Melanoma B16 Cells.

Melanin naturally exists in organisms and is synthetized by tyrosinase (TYR); however, its over-production may lead to aberrant pigmentation and skin conditions. Loquat (Eriobotrya japonica (Thunb.) Lindl.) flowers contain a variety of bioactive compounds, while studies on their suppressive capabilities against melanin synthesis are limited. Loquat flower isolate product (LFP) was obtained by ethanol extraction and resin purification, and its inhibitory efficiency against TYR activity was investigated by enzyme kinetics and multiple spectroscopy analyses. In addition, the impact of LFP on melanin synthesis-related proteins' expression in mouse melanoma B16 cells was analyzed using Western blotting. HPLC-MS/MS analysis indicated that LFP was composed of 137 compounds, of which 12 compounds, including flavonoids (quercetin, isorhamnoin, p-coumaric acid, etc.) and cinnamic acid and its derivatives, as well as benzene and its derivatives, might have TYR inhibitory activities. LFP inhibited TYR activity in a concentration-dependent manner with its IC50 value being 2.8 mg/mL. The inhibition was an anti-competitive one through altering the enzyme's conformation rather than chelating copper ions at the active center. LFP reduced the expression of TYR, tyrosinase-related protein (TRP) 1, and TRP2 in melanoma B16 cells, hence inhibiting the synthesis of melanin. The research suggested that LFP had the potential to reduce the risks of hyperpigmentation caused by tyrosinase and provided a foundation for the utilization of loquat flower as a natural resource in the development of beauty and aging-related functional products.

Genome-wide identification of R2R3-MYB family in Eriobotrya japonica and functional analysis of EjMYB5 involved in proanthocyanidin biosynthesis.

Loquat (Eriobotrya japonica Lindl.) is a popular fruit and medicinal plant. Proanthocyanidins (PAs), as one of the main types of flavonoids, are the key components of loquat fruit quality and medicinal properties. However, the identification of transcription factors (TFs) involved in PA accumulation in loquat remains limited. R2R3-MYB TFs play key regulatory role in PA accumulation in plants. In this study, 190 R2R3-MYB TFs were identified in loquat genome. Combined with transcriptome data, R2R3-MYB TF EjMYB5 involved in PA accumulation in loquat was isolated. EjMYB5 was transcriptional activator localized to nucleus. Expression of EjMYB5 was closely related to PA accumulation in loquat fruits. Heterogenous overexpression of EjMYB5 in tomato (Solanum lycopersicum) inhibited anthocyanin accumulation and promoted PA accumulation. Additionally, transient overexpression of EjMYB5 in tobacco (Nicotiana benthamiana) leaves promoted PA accumulation by upregulating flavonoid biosynthesis genes (NtDFR, NtANS, and NtLAR). Transcriptome analysis of EjMYB5-overexpressing tomato fruits suggested that EjMYB5 was involved in several biological pathways, including lipid metabolism, MAPK signaling, phenylpropanoid biosynthesis, and flavonoid biosynthesis. Collectively, our findings provided basic data for further analysis the function of R2R3-MYB TFs in loquat, and revealed that EjMYB5 functioned as PA accumulation in loquat.

Corosolic acid delivered by exosomes from Eriobotrya japonica decreased pancreatic cancer cell proliferation and invasion by inducing SAT1-mediated ferroptosis.

BACKGROUND: In this study, we investigated whether Exo regulate the proliferation and invasion of PC. METHODS: In this study, we isolated the Eriobotrya japonica Exo using Ultra-high speed centrifugal method. Mass spectrum were used for Exo active components analysis. PC (Capan-1 and Bxpc-3) cells proliferation, migration, and apoptosis were detected using CCK8, ethynyldeoxyuridine, transwell, wound healing, and flow cytometry analyses. We also constructed a lung metastatic mouse model and subcutaneous tumor model to illustrate the regulation effect of Exo or active components. Proteomics were used to reveal the regulatory mechanism responsible for the observed effects. RESULTS: We isolated Eriobotrya japonica Exo and found that Exo treatment significantly suppressed cell migration and proliferation in both in vivo and in vitro using Capan-1. Mass spectrum for Exo active components analysis found that Exo contains high amounts of corosolic acid (CRA). The further study found that CRA treatment inhibit the proliferation, migration, and increased cell death of both Capan-1 and Bxpc-3 cells in a concentration-dependent manner. In vivo experiments confirmed that CRA inhibited pulmonary metastasis by decreasing the number of metastatic foci. Cell proteomics analysis showed that CRA treatment induced spermidine/spermine N1-acetyltransferase 1 (SAT1)-dependent ferroptosis. Treatment with the ferroptosis suppressor ferrostatin-1 significantly reversed CRA-induced cell apoptosis. CONCLUSION: The data suggested that corosolic acid delivered by exosomes from Eriobotrya japonica decreased pancreatic cancer cell proliferation and invasion by inducing SAT1-mediated ferroptosis.

Anti-Diabetic Potential of Polyphenol-Rich Fruits from the Maleae Tribe-A Review of In Vitro and In Vivo Animal and Human Trials.

The Maleae tribe consists of over one thousand species, including many well-known polyphenol-containing fruit crops with wide-ranging biological properties, e.g., apples (Malus), chokeberries (Aronia), pears (Pyrus), quinces (Cydonia, Chaenomeles), saskatoon (Amelanchier), loquats (Eriobotrya), medlars (Mespilus), rowans (Sorbus), and hawthorns (Crataegus). Considering the current interest in the concept of functional foods and the still-insufficient methods of diabetes management, the anti-diabetic potential of fruits has been studied intensively, including those of the Maleae tribe. This paper is the first comprehensive overview of this selected topic, covering articles published from 2000 to 2023 (131 articles in total). The first part of this review focuses on the potential mechanisms of action of fruits investigated so far (46 species), including their effects on tissue-specific glucose transport and the expression or activity of proteins in the insulin signalling pathway. The second part covers the phytocompounds responsible for particular fruits' activity-primarily polyphenols (e.g., flavonols, dihydrochalcones, proanthocyanidins, anthocyanins, phenolic acids), but also polysaccharides, triterpenes, and their additive and synergistic effects. In summary, fruits from the Maleae tribe seem promising as functional foods and anti-diabetic agents; however, their prospects for more expansive pro-health application require further research, especially more profound in vivo trials.

Effects of L-Cysteine and γ-Aminobutyric Acid Treatment on Postharvest Quality and Antioxidant Activity of Loquat Fruit during Storage.

Sichuan is the China's leading producer of loquat, with the largest cultivation area and yield ranked first in China. Loquat is a seasonal fruit highly appreciated by consumers; however, the fruit is prone to browning and lignification after harvest, affecting its storage quality. The effects of L-Cysteine (L-Cys, 0.01, 0.05, 0.1, 0.2%) and γ-aminobutyric acid (GABA, 0.025, 0.05, 0.075, 0.1%) on the sensory quality and antioxidant activity of loquat fruit during cold storage at 4 °C for 35 days and simulated shelf life for 5 days were investigated. The results showed that after 40 days of storage, compared with the control, 0.05% L-Cys and 0.05% GABA treatment of 'Zaozhong No. 6' loquat fruit effectively reduced the weight loss rate, browning index, decay index, respiratory rate, firmness, and lignin content and slowed the decreases in total soluble solids, soluble sugar, titratable acidityand vitamin C contents. The application of 0.05% L-Cys and 0.05% GABA significantly increased the contents of total phenols, total flavonoids, flavanols, and carotenoids; delayed the increase of relative electric conductivity, MDA, POD, and PPO activities; and significantly enhanced the activities of SOD and CAT, DPPH free radical scavenging ability, and FRAP, thereby improving antioxidant capacity. In summary, 0.05% L-Cys and 0.05% GABA treatment promotes the quality of loquat fruit after 40 days of storage, and significantly enhances antioxidant capacity, thus delaying senescence after harvest.

Loquat fruit peel extract regulates lipid metabolism and liver oxidative stress in mice: In vivo and in silico approaches.

ETHNOPHARMACOLOGICAL RELEVANCE: In Moroccan traditional medicine, fresh or dried loquat (Eriobotrya japonica (Thunb.) Lindl.) fruit peels infused in water and taken for 45 days are used as natural remedies against hypercholesterolemia, hyperglycemia and cardiovascular diseases. This is the first experimental study approving the folk medicinal use of loquat fruit peels originated from eastern Morocco. AIM OF THE STUDY: The study aims to investigate the effect of loquat fruit peel extract on lipid metabolism and liver oxidative status in mice as well as to predict the possible mechanisms. MATERIALS AND METHODS: The study was carried out using high fat/fructose diet-induced hyperlipidemic mice model treated with the loquat peel extract for 45 days at two doses (100 and 200 mg/kg/day) in comparison to fenofibrate drug. The plasma, tissue, fecal and biliary lipids and blood glucose were analyzed using enzymatic methods. The liver oxidative status was evaluated and the polyphenol profiling was conducted using the HPLC-DAD method. Possible mechanisms involved in the observed pharmacological effects were predicted by in silico method. RESULTS: The extract at a dose of 200 mg/kg possessed higher effect than at 100 mg/kg. It significantly reduced plasma total cholesterol (TC), triglycerides (TG), LDL-cholesterol, atherogenic index, LDL-C/HDL-C ratio and plasma glucose (-36%, -45%, -45%, -82%, -87%, 58%, respectively), while the HDL-cholesterol was increased (+172%). Moreover, the extract reduced TC and TG in the liver and adipose tissue by increasing their excretion in bile and fecal matter. It prevented the liver oxidative stress and decreased body weight and organ relative mass. The extract appears to be nontoxic (LD50 > 5000 mg/kg) and contains five polyphenols including ferulic acid (32.74 ± 0.71 mg/g), caffeic acid (21.48 ± 0.32 mg/g), 5-O-Caffeoylquinic acid (112.15 ± 1.86 mg/g), chlorogenic acid (42.05 ± 0.92 mg/g) and quercetin (32.69 ± 0.68 mg/g). These phenolics and/or their circulating metabolites presented differential interaction capacities with the potential enzymes and transcription factors implicated in lipid homeostasis such as HMG-CoA reductase, lipoprotein lipase, fatty acid synthase, Cyp7a1, ABCG, PPARs, RXR, FXR and RAR. CONCLUSION: Our findings justify the traditional use of loquat fruit peels and suggest that their aqueous extract could be used as substrate to produce phytotherapeutic drugs or dietary supplements to prevent hyperlipidemia, hyperglycemia and related cardiovascular diseases.

Exogenous Nitric Oxide-Induced Postharvest Gray Spot Disease Resistance in Loquat Fruit and Its Possible Mechanism of Action.

The effectiveness of nitric oxide (NO) for control of grey spot rot cause by Pestalotiopsis eriobotryfolia in harvested loquat fruit and its probable mechanisms have been investigated. The results showed that NO donor sodium nitroprusside (SNP) did not evidently inhibit mycelial growth and spore germination of P. eriobotryfolia, but resulted in a low disease incidence and small lesion diameter. SNP resulted in a higher hydrogen peroxide (H2O2) level in the early stage after inoculation and a lower H2O2 level in the latter period by regulating the activities of superoxide dismutase, ascorbate peroxidase and catalase. At the same time, SNP enhanced the activities of chitinase, ß-1,3-glucanase, phenylalanine ammonialyase, polyphenoloxidase, and total phenolic content in loquat fruit. However, SNP treatment inhibited the activities of cell wall-modifying enzymes and the modification of cell wall components. Our results suggested that NO treatment might have potential in reducing grey spot rot of postharvest loquat fruit.

Sorbitol induces flower bud formation via the MADS-box transcription factor EjCAL in loquat.

Sorbitol is an important signaling molecule in fruit trees. Here, we observed that sorbitol increased during flower bud differentiation (FBD) in loquat (Eriobotrya japonica Lindl.). Transcriptomic analysis suggested that bud formation was associated with the expression of the MADS-box transcription factor (TF) family gene, EjCAL. RNA fluorescence in situ hybridization showed that EjCAL was enriched in flower primordia but hardly detected in the shoot apical meristem. Heterologous expression of EjCAL in Nicotiana benthamiana plants resulted in early FBD. Yeast-one-hybrid analysis identified the ERF12 TF as a binding partner of the EjCAL promoter. Chromatin immunoprecipitation-PCR confirmed that EjERF12 binds to the EjCAL promoter, and ß-glucuronidase activity assays indicated that EjERF12 regulates EjCAL expression. Spraying loquat trees with sorbitol promoted flower bud formation and was associated with increased expression of EjERF12 and EjCAL. Furthermore, we identified EjUF3GaT1 as a target gene of EjCAL and its expression was activated by EjCAL. Function characterization via overexpression and RNAi reveals that EjUF3GaT1 is a biosynthetic gene of flavonoid hyperoside. The concentration of the flavonoid hyperoside mirrored that of sorbitol during FBD and exogenous hyperoside treatment also promoted loquat bud formation. We identified a mechanism whereby EjCAL might regulate hyperoside biosynthesis and confirmed the involvement of EjCAL in flower bud formation in planta. Together, these results provide insight into bud formation in loquat and may be used in efforts to increase yield.

Natural parasitism in fruit fly (Diptera: Tephritidae) and interaction with wild hosts surrounding apple orchards adjacent to Atlantic Forest fragments in Paraná State, Brazil / Parasitismo natural de mosca-das-frutas (Diptera: Tephritidae) e interação com hospedeiros silvestres em pomares de macieira adjacentes a fragmentos de Mata Atlântica no Estado do Paraná, Brasil

The South American fruit fly, Anastrepha fraterculus (Wiedemann, 1830) (Diptera: Tephritidae), is an important pest in the subtropical region of Brazil. This insect has tritrophic relation between wild fruits and parasitoids and is associated with apple (Malus domestica Borkh.) orchards adjacent to the Atlantic Forest in Paraná. We thus investigated the degree of infestation of the fruit fly and natural parasitism in wild and cultivated fruits surrounding apple orchards. For this purpose, we collected fruits of Acca sellowiana (Berg.) Burret, Campomanesia xanthocarpa (Mart), Eugenia uniflora L., Eugenia pyriformis Cambessèdes, Psidium cattleianum Sabine, Psidium guajava (L.), Annona neosericea Rainer and Eriobotrya japonica (Thumb) in apple orchards adjacent to the Atlantic Forest located in Campo do Tenente, Lapa and Porto Amazonas counties. In total, we collected 18,289 fruits during four growing years. The occurrence of A. fraterculus depends on the susceptible period of apple fruits. A. sellowiana and P. cattleianum were considered primary fruit fly multipliers and P. guajava was secondary, all occurring after the apple harvest (IS period). The group of parasitoids with A. fraterculus was Aganaspis pelleranoi (Brèthes, 1924) (Hymenoptera: Figitidae), Opius bellus (Gahan, 1930), Doryctobracon areolatus (Szépligeti, 1911) and Doryctobracon brasiliensis (Szépligeti, 1911) (Hymenoptera: Braconidae) all of which are first records in the Atlantic Forest in Paraná. First record of O. bellus occurring in the State of Paraná, as well as, first record of the tritrophic association between host plant A. neosericea, parasitoids D. areolatus and O. bellus and fruit fly A. fraterculus. The host P. cattleianum stood out among the Myrtaceae species in regard to the high diversity of parasitoid species (81% of parasitoids). The total number of Figitidae species (76.5%) was higher [...].

Mosca-das-frutas sul-americana, Anastrepha fraterculus (Wiedemann, 1830) (Diptera: Tephritidae), é uma importante praga da região subtropical do Brasil. Este inseto tem relação tritrófico entre frutos silvestres e parasitoides e está associado a pomares de macieiras (Malus domestica Borkh.) adjacentes à Mata Atlântica no Paraná. Assim, investigamos o grau de infestação da mosca-das-frutas e o parasitismo natural em frutas silvestres e cultivadas ao redor de pomares de maçã. Para tanto, foram coletados frutos de Acca sellowiana (Berg.) Burret, Campomanesia xanthocarpa (Mart), Eugenia uniflora L., Eugenia pyriformis Cambessèdes, Psidium cattleianum Sabine, Psidium guajava (L.), Annona neosericea Rainer e Eriobotrya japonica (Thumb) em pomares de maçã adjacentes à Mata Atlântica localizados nos municípios de Campo do Tenente, Lapa e Porto Amazonas. No total, coletamos 18.289 frutos durante quatro anos de cultivo. A ocorrência de A. fraterculus depende do período de suscetibilidade dos frutos da maçã. A. sellowiana e P. cattleianum foram considerados multiplicadores primários de mosca-das-frutas e P. guajava foi secundário, todos ocorrendo após a colheita da maçã (período IS). Os parasitóides a associados a A. fraterculus foram Aganaspis pelleranoi (Brèthes, 1924) (Hymenoptera: Figitidae), Opius bellus (Gahan, 1930), Doryctobracon areolatus (Szépligeti, 1911) e Doryctobracon brasiliensis (Szépligeti, 1911) (Hymenoptera: Braconidae), todos os quais são primeiros registros na Mata Atlântica no Paraná. Primeiro registro de O. bellus ocorrendo no Estado do Paraná, assim como, primeiro registro da associação tritrófica entre o hospedeiro A. neosericea, parasitoides D. areolatus e O. bellus e mosca-das-frutas A. fraterculus. O hospedeiro P. cattleianum se destacou entre as espécies de Myrtaceae pela alta diversidade de parasitóides associados (81% dos parasitóides). O número total de espécies de Figitidae (76,5%) foi superior [...].

Photosynthetic Efficiency and Glyco-Metabolism Changes in Artificial Triploid Loquats Contribute to Heterosis Manifestation.

Previous studies indicated that extensive genetic variations could be generated due to polyploidy, which is considered to be closely associated with the manifestation of polyploid heterosis. Our previous studies confirmed that triploid loquats demonstrated significant heterosis, other than the ploidy effect, but the underlying mechanisms are largely unknown. This study aimed to overcome the narrow genetic distance of loquats, increase the genetic variation level of triploid loquats, and systematically illuminate the heterosis mechanisms of triploid loquats derived from two cross combinations. Here, inter-simple sequence repeats (ISSRs) and simple sequence repeats (SSRs) were adopted for evaluating the genetic diversity, and transcriptome sequencing (RNA-Seq) was performed to investigate gene expression as well as pathway changes in the triploids. We found that extensive genetic variations were produced during the formation of triploid loquats. The polymorphism ratios of ISSRs and SSRs were 43.75% and 19.32%, respectively, and almost all their markers had a PIC value higher than 0.5, suggesting that both ISSRs and SSRs could work well in loquat assisted breeding. Furthermore, our results revealed that by broadening the genetic distance between the parents, genetic variations in triploids could be promoted. Additionally, RNA-Seq results suggested that numerous genes differentially expressed between the triploids and parents were screened out. Moreover, KEGG analyses revealed that "photosynthetic efficiency" and "glyco-metabolism" were significantly changed in triploid loquats compared with the parents, which was consistent with the results of physiological indicator analyses, leaf micro-structure observations, and qRT-PCR validation. Collectively, our results suggested that extensive genetic variations occurred in the triploids and that the changes in the "photosynthetic efficiency" as well as "glyco-metabolism" of triploids might have further resulted in heterosis manifestation in the triploid loquats.

Traditional uses, phytochemistry, pharmacology, and toxicity of Eriobotrya japonica leaves: A summary.

ETHNOPHARMACOLOGICAL RELEVANCE: Eriobotrya japonica Lindl. has been included in "The Plant List" (http://www.theplantlist.org) and is the most widely researched species in its genus. E. japonica is a subtropical evergreen fruit tree belonging to the Rosaceae family. Its dried leaves are widely used in traditional Chinese herbal medicine to treat coughing caused by pulmonary inflammation, dyspnea due to asthma and cough, nausea caused by stomach disorders, restlessness, and thirst. Furthermore, it is used to treat stomach ache, ulcers, chronic bronchitis, cancer, and diabetes mellitus in Japanese folk medicine. However, no systematic reports on E. japonica leaves have been published before. AIM OF THE STUDY: This review summarizes the available information on the traditional uses, phytochemistry, pharmacology, toxicity, and quality control of various extracts and phytoconstituents of E. japonica leaves. MATERIALS AND METHODS: Relevant publications between 1931 and 2022 were considered. Chinese and English studies on E. japonica leaves were collected from databases, including PubMed, Web of Science, Elsevier, ACS Publications, Springer, and CNKI (Chinese). The traditional uses, phytochemistry, pharmacology, toxicity, and quality control of E. japonica leaves were reviewed. RESULTS: Briefly, 164 compounds, including triterpenes, flavonoids, sesquiterpene glycosides, megastigmane derivatives, phenylpropanoids, and organic acids, have been identified from E. japonica leaves, in addition to 169 volatile oils. More than half of these compounds have not yet been reported to have pharmacological activities. Triterpenes and flavonoids are the most important bioactive compounds responsible for pharmacological activities, such as antidiabetic, anti-inflammatory, and antitumor activities. Other beneficial physiological effects such as antioxidant, hepatoprotective, bronchodilatory, antitussive, and expectorant effects and tracheal smooth muscle relaxation, protection against myocardial ischemia injury, and improved cognitive activities have also been reported. High doses of E. japonica leaf extracts have been used in laboratory animals, and no side effects or toxicity-symptoms have been observed. CONCLUSIONS: The pharmacological activities of E. japonica leaves support their use in traditional Chinese herbal medicine. However, several aspects, such as the bioavailability, pharmacodynamics, pharmacokinetics, mechanism of action, and structure-activity relationships of the pure compounds isolated from E. japonica leaves, have not been studied yet and warrant further studies.

Loquat (Eriobotrya japonica (Thunb) Lindl.): Evaluation of nutritional value, polyphenol composition, antidiabetic effect, and toxicity of leaf aqueous extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Loquat (Eriobotrya japonica (Thunb.) Lindl.) is an evergreen tree native to China, which is introduced in many Mediterranean countries. As in many ancient medical systems, loquat leaves have been used in Moroccan traditional medicine to treat diabetes and its complications. AIM OF THE STUDY: This study aims to determine the nutritional and polyphenol composition and to evaluate the in vivo antidiabetic, and antihyperlipidemic properties and oral toxicity of a leaf aqueous extract (LLE) derived from loquat grown in Morocco. MATERIALS AND METHODS: Energy value and fiber, fatty acids, minerals, vitamins, total carbohydrate, sugar, lipid, and protein contents were determined according to international methods committee guidelines. Polyphenol profiling was carried out using the HPLC-DAD method. Mice fed a high-fat and high-glucose (HFG) diet for 10 weeks were used as a model to assess the antidiabetic and antihyperlipidemic effects of a daily administration of LLE at three different doses (150, 200, 250 mg/kg body weight (BW)/day), in comparison with metformin (50 mg/kg BW/day) and pravastatin (20 mg/kg BW/day). The oral toxicity was determined following OECD 425 Guideline. RESULTS: Loquat leaves were found to be rich in fiber, minerals (potassium, calcium, magnesium, iron, and sodium), and vitamins (B2, B6, and B12) and lower in energy, sugar, and fat. Ten different phenolic compounds were characterized. Naringenin, procyanidin C1, epicatechin, and rutin were the more abundant compounds in LLE. The administration of the LLE dose-dependently ameliorated hyperglycemia, insulin resistance, oxidative stress, and hyperlipidemia in HFG diet-fed mice. The median lethal dose of LLE was higher than 5000 mg/kg BW. CONCLUSIONS: Loquat leaves are a potential source of micronutrients and polyphenols with beneficial effects on diabetes and its complications.

Residue analysis and dietary risk assessment of tebuconazole in loquat and sugarcane after open-field application in China.

Tebuconazole is an effective but potentially carcinogenic fungicide. Tebuconazole residues in loquat and sugarcane were investigated, together with an analysis of their dietary risk. Solid-phase extraction and high-performance liquid chromatography-tandem mass spectrometry showed fortified recoveries of 87% to 98%, with standard deviations ≤ 6.4%. The tebuconazole residues were below 6.34 mg kg-1 for whole loquat and 0.80 mg kg-1 for sugarcane. Based on the final residue test, the chronic hazard index was 90.74% in whole loquat and sugarcane, while the acute hazard index ranged from 66.32% to 109.49% for loquat and 33.37% to 76.93% for sugarcane. The assessment of potential dietary risk showed that while loquats may represent an acute risk to human health, whereas sugarcane consumption was safe. A 21-day pre-harvest interval is proposed to comply with maximum residue limit regulations and the observed risks when using 430 g/L tebuconazole for treating sugarcane. These findings offer guidance for tebuconazole formulation and use.

Effects of intercropping with Solanum photeinocarpum and its post-grafting generations on cadmium accumulation in loquat (Eriobotrya japonica).

Cadmium (Cd) contamination of orchard soils is a global problem that has been increasing. To decrease the Cd accumulation in fruits, intercropping the orchard crops with hyperaccumulator plants has been used for soil remediation. A pot and a field experiment were conducted to study the effects of intercropping the potential Cd-hyperaccumulator Solanum photeinocarpum and its post-grafting generations with loquat (Eriobotrya japonica) on the growth and Cd uptake of these two plant species. In the pot experiment, intercropping improved the biomass, Cd content, Cd extraction, and root-to-shoot Cd translocation in both species. Intercropping increased the DNA methylation levels, antioxidant enzyme activity, and soluble protein content of loquat seedlings. These results indicate that intercropping could improve the phytoremediation of S. photeinocarpum and its post-grafting generations and increase the Cd uptake in loquat seedlings. In the field experiment, intercropping increased the Cd contents in the old branches, while it decreased that in the young branches and fruits of loquat. These findings indicate that intercropping could increase the Cd uptake in old tissues but reduce the Cd uptake in young tissues and fruits of loquat. So, intercropping loquat with S. photeinocarpum and its post-grafting generations could be used in Cd-contaminated orchards.

Intercropping the potential Cd-hyperaccumulator Solanum photeinocarpum and its post-grafting generations with loquat mutually promoted the growth of two plant species, and also promoted the cadmium uptakes in S. photeinocarpum and old branches of loquat, while inhibited the Cd uptake in the loquat young tissues (young branches and fruits). These results are the new findings of the intercropping.

Cell suspension culture extract of Eriobotrya japonica attenuates growth and induces apoptosis in prostate cancer cells via targeting SREBP-1/FASN-driven metabolism and AR.

BACKGROUND: Castration-resistant prostate cancer (CRPC) is one of the main causes of male cancer mortality. There is currently no effective treatment to cure this deadly prostate cancer (PCa) progression. However, recent research showed that activation of lipogenesis leads to CRPC progression. It provides a rationale to target the highly lipogenic activity as a novel and promising therapy against lethal CRPC. PURPOSES: The present study aims to evaluate the anticancer efficacy and the molecular mechanism of cell suspension culture extract from Eriobotrya japonica (EJCE) in PCa, including CRPC. METHODS: Cell growth, migration and invasion analyses were performed by MTT method, a wound healing assay and the transwell method, respectively. Apoptosis was assessed by a flow cytometry-based Annexin V-FITC/PI assay, caspase enzymatic activity and Western blot analyses. Lipogenesis was determined by a Fatty Acid Quantification Kit and an Oil Red O staining. The in vivo experiment was conducted by a xenograft mouse model. RESULTS: PCa cell growth, migration and invasion were significantly affected by EJCE. EJCE decreased expression of sterol regulatory element-binding protein-1 (SREBP-1) and fatty acid synthase (FASN) in PCa cells, two main factors for lipogenesis. By inhibiting SREBP-1/FASN, EJCE reduced the intracellular fatty acid levels and lipid droplet accumulation in PCa. Moreover, EJCE down-regulated the androgen receptor (AR) and prostate-specific antigen (PSA) in PCa cells. Significantly, EJCE exhibited the potential anticancer activity by suppressing the growth and leading to apoptosis of CRPC tumors in a xenograft mouse model. CONCLUSION: These results reveal a novel therapeutic molecular mechanism of EJCE in PCa. Blockade of SREBP-1/FASN-driven metabolism and AR by EJCE could be employed as a potent opportunity to cure malignant PCa.

Structure features, selenylation modification, and improved anti-tumor activity of a polysaccharide from Eriobotrya japonica.

A homogeneous polysaccharide, EJP90-1, was isolated from the leaves of E. japonica by hot water extraction in this study. EJP90-1 (7702 Da) was a heteropolysaccharide mainly consisting of →5)-linked-α-L-Araf-(1→, →4)-linked-ß-D-Manp-(1→, →2,4)-linked-α-L-Rhap-(1→, →4)-linked-α-D-Xylp-(1→, →4)-linked-ß-D-Galp-(1→, →2)-linked-ß-D-Galp-(1→, →6)-linked-ß-D-Glcp-(1→, α-D-Glcp-(4→, and t-linked-α-L-Araf. EJP90-1 was found to show moderate anti-tumor activity at the cellular level. In order to improve the anti-tumor activity and the potential applications of EJP90-1, a typical sodium selenite-nitric acid (Na2SeO3-HNO3) modification on EJP90-1 was carried out. X-ray photoelectron spectroscopy (XPS) and energy dispersive spectrometer (EDS) analysis confirmed that Se was successfully introduced into the polymer chain of EJP90-1. The subsequent in vitro cytotoxicity evaluation showed the selenylation modification derivative (EJP90-1-Se) possessed significant antiproliferative activity against cancer cells (HepG2 and A549 cells) through inducing cell apoptosis. The anti-tumor activity of EJP90-1-Se was further confirmed by zebrafish models, which inhibited the proliferation and migration of HepG2 cells and the angiogenesis.

Polyploidy underlies co-option and diversification of biosynthetic triterpene pathways in the apple tribe.

Whole-genome duplication (WGD) plays important roles in plant evolution and function, yet little is known about how WGD underlies metabolic diversification of natural products that bear significant medicinal properties, especially in nonmodel trees. Here, we reveal how WGD laid the foundation for co-option and differentiation of medicinally important ursane triterpene pathway duplicates, generating distinct chemotypes between species and between developmental stages in the apple tribe. After generating chromosome-level assemblies of a widely cultivated loquat variety and Gillenia trifoliata, we define differentially evolved, duplicated gene pathways and date the WGD in the apple tribe at 13.5 to 27.1 Mya, much more recent than previously thought. We then functionally characterize contrasting metabolic pathways responsible for major triterpene biosynthesis in G. trifoliata and loquat, which pre- and postdate the Maleae WGD, respectively. Our work mechanistically details the metabolic diversity that arose post-WGD and provides insights into the genomic basis of medicinal properties of loquat, which has been used in both traditional and modern medicines.

A promiscuous fatty acid ω-hydroxylase CYP94A90 is likely to be involved in biosynthesis of a floral nitro compound in loquat (Eriobotrya japonica).

Nitro groups are often associated with synthetically manufactured compounds such as medicines and explosives, and rarely with natural products. Loquat emits a nitro compound, (2-nitroethyl)benzene, as a flower scent. The nitro compound exhibits fungistatic activity and is biosynthesised from l-phenylalanine via (E/Z)-phenylacetaldoxime. Although aldoxime-producing CYP79s have been intensively studied, it is unclear what enzymes form nitro groups from aldoximes either in plants or in other organisms. Here, we report the identification of two cytochrome P450s that are likely to be involved in (2-nitroethyl)benzene biosynthesis in loquat through differential gene expression analysis using RNA-seq and functional identification using yeast and tobacco. CYP79D80 and CYP94A90 catalysed the formation of (E/Z)-phenylacetaldoxime from l-phenylalanine and (2-nitroethyl)benzene from the aldoxime, respectively. Expression profiles of CYP79D80 and CYP94A90 were correlated with the emission of (2-nitroethyl)benzene from loquat flowers. CYP94A90 also functioned as a fatty acid ω-hydroxylase as do other CYP94A fatty acid ω-hydroxylases. The CYP94As tested from other plants were all found to catalyse the formation of (2-nitroethyl)benzene from (E/Z)-phenylacetaldoxime. CYP79D80 and CYP94A90 are likely to operate in concert to biosynthesise (2-nitroethyl)benzene in loquat. CYP94A90 and other CYP94As are 'promiscuous fatty acid ω-hydroxylases', catalysing the formation of nitro groups from aldoximes, and are widely distributed in dicot plants.

Anti-polyphenol oxidase properties of total flavonoids from young loquat fruits: inhibitory activity and mechanism.

This study investigated anti-polyphenol oxidase activity and mechanism of purified total flavonoids (PTF) from young loquat fruits. PTF remarkably inhibited the activity of polyphenol oxidase (PPO) with an IC50 value of 21.03 ± 2.37 µg/mL. Based on enzyme kinetics, PTF was found to be a potent, mixed-type, and reversible inhibitor of PPO. The fluorescence intensity of PPO was quenched by PTF through forming a PTF-PPO complex in a static procedure. Therefore, this study authenticated PTF as an efficient PPO inhibitor, which would contribute to their utilization in food industry.

Green synthesis of silver nanoparticles from Eriobotrya japonica extract: a promising approach against cancer cells proliferation, inflammation, allergic disorders and phagocytosis induction.

Nanoparticles (NPs) have biological activities like antibacterial, antifungal, drug delivery, immunomodulation and antitumor activities. The aim of the current study was to investigate some of biomedical applications of silver NP synthesis using extracts from leaves of Eriobotrya japonica. Colour changes, UV-visible spectroscopy, SEM, zeta potential, dynamic light scattering, FTIR and XRD were used to confirm AgNPs formation. The UV-vis spectrum absorption band was observed at almost 430 nm. The SEM image shows quasi-spherical shape of AgNPs. The zeta potential demonstrated the negative surface charge of NPs. FTIR results showed the functional groups of AgNPs. Crystalline nature of AgNPs was confirmed by XRD pattern. MTT assay was used to study the anti-proliferative activity against MCF-7 and HeLa cells. Apoptosis was tested using a DNA-fragmentation test, and expression of P53. AgNPs inhibited the proliferation of MCF-7 and HeLa cells, and reduced inflammation. Treatment with AgNPs significantly decreased allergic disorder. AgNPs stimulated the phagocytosis process in BMDMs. The results suggested that AgNPs could be a promising therapy for future and preventing inflammation, reduce allergic disorders and prevent bacterial infection through the up-regulation of phagocytosis. Hence, future work such as developed and improved NPs as adjuvants, immune-modulating substances and nano-drug delivery system is needed.