Potential Bioactive Ingredients Research Articles

Paper-based ligand fishing method for rapid screening and real-time capturing of α-glucosidase inhibitors from the Chinese herbs

Identifying medicinally relevant compounds from natural resources generally involves the tedious work of screening plants for the desired activity before capturing the bioactive molecules from them. In this work, we created a paper-based ligand fishing platform to vastly simplify the discovery process. This paper-based method exploits the enzymatic cascade reaction between α-glucosidase (GAA), glucose oxidase (GOx), and horseradish peroxidase (HRP), to simultaneously screen the plants and capture the GAA inhibitors from them. The designed test strip could capture ligands in tandem with screening the plants, and it features a very simply operation based on direct visual assessment. Multiple acylated flavonol glycosides from the leaves of Quercus variabilis Blume were newly found to possess GAA inhibitory activities, and they may be potential leads for new antidiabetic medications. Our study demonstrates the prospect of the newly discovered GAA ligands as potential bioactive ingredients as well as the utility of the paper-based ligand fishing method.

An integrated strategy of UPLC-Q-TOF-MS analysis, network pharmacology, and molecular docking to explore the chemical constituents and mechanism of Zixue Powder against febrile seizures

Febrile seizures (FS) are the most common type of seizures for children. As a commonly used representative cold formula for resuscitation, Zixue Powder (ZP) has shown great efficacy for the treatment of FS in clinic, while its active ingredients and underlying mechanism remain largely unclear. This study aimed to preliminarily elucidate the material basis of ZP and the potential mechanism for the treatment of FS through ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS), network pharmacology, and molecular docking. UPLC-Q-TOF-MS was firstly applied to characterize the ingredients in ZP, followed by network pharmacology to explore the potential bioactive ingredients and pathways of ZP against FS. Furthermore, molecular docking technique was employed to verify the binding affinity between the screened active ingredients and targets. As a result, 75 ingredients were identified, containing flavonoids, chromogenic ketones, triterpenes and their saponins, organic acids, etc. Through the current study, we focused on 13 potential active ingredients and 14 key potential anti-FS targets of ZP, such as IL6, STAT3, TNF, and MMP9. Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis showed that inflammatory response, EGFR tyrosine kinase inhibitor resistance, AGE-RAGE signaling pathway in diabetic complications, and neuroactive ligand-receptor interaction were the main anti-FS signaling pathways. Licochalcones A and B, 26-deoxycimicifugoside, and hederagenin were screened as the main potential active ingredients by molecular docking. In conclusion, this study provides an effective in-depth investigation of the chemical composition, potential bioactive components, and possible anti-FS mechanism of ZP, which lays the foundation for pharmacodynamic studies and clinical applications of ZP.

Indian gooseberry (Emblica officinalis) pomace: exploring its sustainable application as a functional ingredient with nutritional, technofunctional, rheological and in‐vitro antioxidant properties

SummaryAmla pomace (APO) is a valuable by‐product obtained during juice extraction from Amla. To facilitate its application in food systems, comprehensive knowledge regarding its nutritional, physicochemical and techno‐functional properties is essential. The present study aimed to investigate the potential of APO as a functional ingredient. The results revealed that APO powder contains a good content of total dietary fibre and insoluble fibre equal to 35.81/100 g and 28.00/100 g, respectively. An in vitro antioxidant assay depicted APO as a potential bioactive ingredient. Thermogravimetric analysis revealed that both amla pulp (AP) and pomace have higher thermal stability. Scanning electron micrographs were unstructured without exhibiting a well‐defined cellular structure. Reconstituted suspensions of AP and APO exhibited non‐Newtonian pseudoplastic behaviour with more elastic behaviour than viscous behaviour and weak gel‐forming ability. The study would provide a comprehensive overview of various properties of APO and will allow drawing conclusions regarding its applicability in complex food systems. APO represents an important source of dietary fibre and bioactive components to enhance the nutritional and technological properties, and therapeutic potential of foods.

Algal Nanoparticles and Their Antibacterial Activity: Current Research Status and Future Prospectives

Green nanotechnology is a promising technology that has a wide range of applications in pharmaceuticals today because they offer a higher surface-area-to-volume ratio. Algal-based nanoparticles (NPs) are the subject of intense research interest today for their potential to treat and prevent infections caused by infectious microorganisms that are antibiotic resistant. Algae contain a variety of therapeutically potential bioactive ingredients, including chlorophyll, phycobilin, phenolics, flavonoids, glucosides, tannins, and saponins. As a result, NPs made from algae could be used as therapeutic antimicrobials. Due to their higher surface-area-to-volume ratios compared to their macroscopic components, metallic nanoparticles are more reactive and have toxic effects on their therapy. For pharmaceutical and biomedical applications, green synthesis restricts the use of physical and chemical methods of metallic nanoparticle synthesis, and it can be carried out in an environmentally friendly and relatively low-cost manner. The majority of macroalgae and some microalgae have latent antimicrobial activity and are used in the synthesis of metallic nanoparticles. A potential application in the field of nanomedicine and the establishment of a potential pharmacophore against microorganisms may result from the synthesis of algal-based NPs. Only a few studies have been done on the potential antimicrobial, antifungal, and antibacterial activity of algae-based NPs. As a result, the study will concentrate on the environmentally friendly synthesis of various NPs and their therapeutic potential, with a focus on their antibacterial activity. Thus, the aim of this study is to review all the literature available on the synthesis and characterization of the algal nanoparticles and their potential application as an antibacterial agent.

Development and characterization of starch-based bioactive thermoplastic packaging films derived from banana peels

The present work deals with the development of cellulose-reinforced starch-based bioactive thermoplastic packaging films, from complete recycling of banana peel waste. The nanocellulose fibers, starch and bioactive compounds from banana peel were extracted and reconstituted to produce cellulose-reinforced starch-based bioactive thermoplastic packaging films. The banana peel starch was examined to have an abundance of amylopectin (88.55 ± 0.28% (w/w)) and high thermal stability (∼295 °C maximum degradation temperature), to serve as a matrix for the thermoplastic films. The ethanolic extract of the banana peel with major active compounds of β-sitosterol, and 1, 2 Benzenedicarboxylic acid mono (2-ethyl hexyl ester) was examined to be having high antioxidant (74.43 ± 0.26% DPPH inhibition) and antimicrobial properties, to serve as a potential bioactive ingredient for the development of bioactive thermoplastic films. The addition of banana peel-based nanocellulose fiber improved the mechanical (6-fold increase in tensile strength) and barrier properties (0.6-fold reduction in O2 permeability) of banana peel thermoplastic films (BPT). The developed bioactive BPT films were examined to have a UV blocking capacity of ∼98%. The produced Bioactive BPT films were found to be effective in the shelf life extension of bread by 10 days. The proposed methodology for the complete recycling of banana peel will take the state of research in agro-waste management one step closer to a green bio-circle economy.

Explored potential hypoglycemic, hypolipidemic, and anti‐hyperuricemic components from Rheum tanguticum combing affinity ultrafiltration with four enzyme targets

AbstractDue to its variety of biological activities, rhubarb has been widely applied worldwide with a long history. However, the potential bioactive compounds in Rheum tanguticum responsible for hypoglycemic, hypolipidemic, and anti‐hyperuricemic activities as well as their underlying mechanisms remain elusive. In order to explore these specific multifunctional ingredients, the in vitro α‐glucosidase and pancreatic lipase inhibitory assays were first determined, and the results indicated that R. tanguticum possessed remarkable hypoglycemic and hypolipidemic activities. Then, 14, 23, 15, and 10 active compounds in R. tanguticum were fast screened out by employing the bio‐affinity ultrafiltration with LC‐MS (Liquid Chromatograph‐Mass Spectrometer) strategy, which displayed various binding abilities to α‐glucosidase, α‐amylase, lipase, and xanthine oxidase enzymes, respectively. Further verifications of potential bioactive ingredients were implemented by molecule docking and the enzyme inhibitory assays in vitro. At last, the first interaction network between multifunctional components in R. tanguticum and their targets was further constructed facilitating to decipher the underlying mechanisms of action regarding R. tanguticum. The present work suggests that R. tanguticum may be a promising natural therapeutics and have good potential to be developed to prevent and treat diabetes, obesity, and gout in the near future.

Identification of the active compounds in the Yi-Fei-San-Jie formula using a comprehensive strategy based on cell extraction/UPLC-MS/MS, network pharmacology, and molecular biology techniques

BackgroundChinese herbal formulae has multiple active constituents and targets, and the good clinical response is encouraging more scientists to explore the bio-active ingredients in such complex systems. Yi-Fei-San-Jie formula (YFSJF) is commonly used to treat patients with lung cancer in South China; however, its bio-active ingredients remain unknown. PurposeWe investigated the bio-active ingredients of the YFSJF using a novel comprehensive strategy. MethodsA549 cell extraction coupled with ultra-high performance liquid chromatography-mass spectrometry (UPLC-MS/MS) was used for the screening of potential bio-active ingredients. Network pharmacology approach and molecular dynamics simulation were performed for the screening of targets. Surface plasmon resonance (SPR) assay and molecular biology techniques were used to verify the targets. ResultsNine A549 cell membrane-binding compounds were identified through cell extraction/UPLC-MS/MS. Five compounds, namely ginsenoside Ro, ginsenoside Rb1, ginsenoside Rc, peimisine, and peimine were cytotoxic to A549 cells, and they were considered the bio-active ingredients of the YFSJF in vitro. Network pharmacology analysis revealed that TGFBR2 is the key target and the TGFβ pathway is the key pathway targeted by YFSJF in non-small cell lung cancer. Peimisine showed an affinity to TGFBR2 using molecular docking and dynamic stimulation, which was confirmed using surface plasmon resonance spectroscopy. The molecular biology-based analysis further confirmed that peimisine targets TGFBR2 and can reverse A549 epithelial-mesenchymal transition by inhibiting the TGFβ pathway. ConclusionTaken together, cell extraction/UPLC-MS/MS, network pharmacology, and molecular biology-based analysis comprise a feasible strategy to explore active ingredients in YFSJF.

The potential bioactive ingredients and hub genes of five TCM prescriptions against lung adenocarcinoma were explored based on bioinformatics.

Analysis of the commonness of several prescriptions of traditional Chinese medicine (TCM) in the treatment of lung adenocarcinoma (LUAD) based on bioinformatics. Searched the TCM prescriptions for the treatment of LUAD in the literature published in the database, searched ingredients in the TCM through TCMSP and Swiss target prediction databases (OB ≥ 30%, DL > 0.18, Caco-2 > 0), and predicted the potential targets. GEO database retrieved LUAD gene chip data and screened (P < 0.05, | log2 (fold change) |> 1). The biological function, hub gene selection and survival period, immune infiltration, methylation, copy number variations (CNVs), and single-nucleotide variants (SNV) of hub genes were analyzed by DAVID, STRING, Kaplan-Meier plotter database, Cytoscape software, GSCALite database, and TIMER2.0. In this study, 5 TCM prescriptions were analyzed, and a total of 173 ingredients were obtained through database search, including 35 coincidence ingredients, a total of 603 potential targets, 621 LUAD-related genes, 16 up-regulated genes, and 31 down-regulated genes. A total of 61 terms of biological process (BP), 14 terms of cellular component (CC), and 14 terms of molecular function (MF) were obtained. Twenty core genes were obtained, including 15 genes with different survival periods, which were closely related to immune cells (B cell, CD8 + T cell, CD4 + T cell, macrophage, neutrophil, and dendritic cells). The low expression of ADRB2 and MAOA and the high expression of AUARK, CDK1, KIF11, MIF, TOP2A, and TTK were associated with the survival rate of LUAD patients (P < 0.05). Baicalein, Arachidonate, Hederagenin, and hub genes may become potential drugs and potential targets for LUAD treatment. Evaluated the efficacy of TCM in the treatment of LUAD from macro to micro, mined the hub genes, and predicted the mechanism of action, so as to lay the foundation for the development of new drugs of TCM, prescription optimization, or disease control.

Preparation of whey protein hydrolysates with ACE‐inhibitory activity using cysteine peptidases from Bromelia hieronymi Mez. (Bromeliaceae)

A proteolytic extract from fruits of Bromelia hieronymi was used to hydrolyse bovine whey proteins. The peptide profile obtained exhibited a gradual fading of the main whey proteins and a decrease in the content of hydrophobic peptides. The 180‐min hydrolysate showed a hydrolysis degree of 15.2% and inhibited the angiotensin‐converting enzyme (ACE), showing an IC50 of 0.17 mg/mL. By bioinformatics analysis, several theoretical sequences of possible ACE‐inhibitory peptides were deduced. These results showed that proteolytic extracts from B. hieronymi can be used to prepare whey hydrolysates that would serve as a potential bioactive ingredient of functional foods.

Variation of Saponins in Sanguisorba officinalis L. before and after Processing (Paozhi) and Its Effects on Colon Cancer Cells In Vitro.

The incidence of colon cancer is increasing year over year, seriously affecting human health and quality of life in recent years. However, traditional Chinese medicine (TCM) has been utilized for the treatment of colon cancer. S. officinalis Saponins (S-Saponins), the potential compound of TCM, displays multiple biological activities in colon cancer treatment. In our study, ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) combined with multivariate statistical analysis were performed to analyze and identify raw and processed saponins. Then, MTT and cell migration assays were used to preliminarily explore the effects of saponins in vitro on colon cancer cells. The results showed that 29 differential saponins compounds under Paozhi were identified by UHPLC-MS/MS. Moreover, in vitro validation showed that Sprocessed better inhibited the proliferation and migration of colon cancer cells than Sraw. This study provides a basis for the determination of the chemical fundamentals of the efficacy changes during Paozhi through inferring the changes in saponin components and its possible transformation mechanisms before and after processing S. officinalis. Meanwhile, it also provides new insights into potential bioactive ingredients for the treatment of colon cancer.

Investigation of the potential mechanism of the Shugan Xiaozhi decoction for the treatment of nonalcoholic fatty liver disease based on network pharmacology, molecular docking and molecular dynamics simulation.

Nonalcoholic fatty liver disease (NAFLD) is a metabolic disease, the incidence of which increases annually. Shugan Xiaozhi (SGXZ) decoction, a composite traditional Chinese medicinal prescription, has been demonstrated to exert a therapeutic effect on NAFLD. In this study, the potential bioactive ingredients and mechanism of SGXZ decoction against NAFLD were explored via network pharmacology, molecular docking, and molecular dynamics simulation. Compounds in SGXZ decoction were identified and collected from the literature, and the corresponding targets were predicted through the Similarity Ensemble Approach database. Potential targets related to NAFLD were searched on DisGeNET and GeneCards databases. The compound-target-disease and protein-protein interaction (PPI) networks were constructed to recognize key compounds and targets. Functional enrichment analysis of Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) was performed on the targets. Molecular docking was used to further screen the potent active compounds in SGXZ. Finally, molecular dynamics (MD) simulation was applied to verify and validate the binding between the most potent compound and targets. A total of 31 active compounds and 220 corresponding targets in SGXZ decoction were collected. Moreover, 1,544 targets of NAFLD were obtained, of which 78 targets intersected with the targets of SGXZ decoction. Key compounds and targets were recognized through the compound-target-disease and PPI network. Multiple biological pathways were annotated, including PI3K-Akt, MAPK, insulin resistance, HIF-1, and tryptophan metabolism. Molecular docking showed that gallic acid, chlorogenic acid and isochlorogenic acid A could combine with the key targets. Molecular dynamics simulations suggested that isochlorogenic acid A might potentially bind directly with RELA, IL-6, VEGFA, and MMP9 in the regulation of PI3K-Akt signaling pathway. This study investigated the active substances and key targets of SGXZ decoction in the regulation of multiple-pathways based on network pharmacology and computational approaches, providing a theoretical basis for further pharmacological research into the potential mechanism of SGXZ in NAFLD.

Potential application of natural bioactive compounds as skin-whitening agents: A review.

Melanin is a skin pigment that gives color to the skin, hair, and eyes. The accumulation or over production of melanin can lead to aesthetic problems as well as serious diseases associated with hyperpigmentation. Skin lightening is described as the procedure of using natural or synthetic products to lighten the skin tone or provide an even skin complexion by reducing the amount of melanin in the skin; therefore, skin lightening products help people to treat their skin problems. Ingredients such as hydroquinone, ascorbic acid, and retinoic acid were used as whitening agents to lighten the skin. However, they have many adverse effects on the skin and body health, such as skin irritation. In this review, firstly, discuss on the directly/indirectly target melanogenesis-related signal pathways. Secondly, summarize potential natural bioactive ingredients with skin lightening properties from plants, marine organisms, microorganisms. Finally, the remaining problems and future challenges are also discussed. For relevant literature, a literature search was conducted using Google Scholar and Web of Science. Natural bioactive compounds, tyrosinase inhibitors, and other related topics were researched and evaluated. Natural products isolated from plant and animal resources are potential active cosmetic candidates for lightening the skin tone and skin whitening and protection against UV irradiation. Natural bioactive ingredients as cosmetic whitening additives have attracted increasingly attention due to their safety and cost effectiveness, with few side effects. Although natural active substances have been advocated for use in whitening cosmetics in recent years, there are still many challenges due to the fact that traditional inhibitors are used perennial in cosmetics which cannot be easily changed and the research on natural active substances is still in its infancy. In the future, by improving the extraction technique of natural extracts, it is achieved to give a qualitative and quantitative analysis of the active ingredients of the extracts, to determine the effect of the active components of action, and to find the substances that have the best possible whitening effect in natural organisms.

Total glucosides of paeony alleviates scleroderma by inhibiting type I interferon responses

Ethnopharmacological relevanceType I interferon (IFN) is believed to play a pathogenic role in systemic sclerosis (SSc, also called scleroderma), which is an autoimmune rheumatic disease. Our previous studies have found that Chinese medicine formula Si–Ni-San (SNS, composed of Glycyrrhiza uralensis Fisch., Bupleurum chinense DC., Paeonia lactiflora Pall., and Citrus aurantium L.) had inhibitory effects on type I IFN responses. Among these herbal products, Paeonia lactiflora Pall. has been traditionally used to treat inflammation-related diseases, yet its therapeutic effects against type I IFN-related diseases and potential bioactive ingredients are not characterized. Aim of the studyWe aim to identify bioactive ingredient with anti-type I IFN activity from herbal products in SNS and further elucidate its therapeutic effect against scleroderma and underlying mechanisms. Materials and methodsWe constructed a Gaussia-luciferase (Gluc) reporter assay system to identify ingredients with anti-type I IFN activities from SNS. In RAW264.7 cells, real-time PCR (RT-PCR) and western blotting were used to investigate the induction of type I IFN pathway. Additionally, in a bleomycin (BLM)-induced experimental scleroderma model, the expression of fibrotic genes, type I IFN-related genes, inflammatory cytokines, and cytotoxic granules were measured by RT-PCR, and the histopathological changes were determined by H&E staining, Masson's staining and immunohistochemistry analysis. ResultsOur data demonstrated that total glucosides of paeony (TGP) was the bioactive component of SNS that selectively inhibited TLR3-mediated type I IFN responses and blocked type I IFN-induced downstream JAK-STAT signaling pathways. In the BLM-induced scleroderma mouse model, TGP ameliorated skin fibrosis by inhibiting multiple targets in the upstream and downstream of type I IFN signaling. Further research found that TGP hindered polarization of M2 macrophages and their profibrotic effects and reduced cytotoxic T lymphocytes and their cytotoxic granules by suppressing Cxcl9 and Cxcl10 in the skin tissue of scleroderma mice. ConclusionsOur study not only sheds novel lights into the immunoregulative effects of TGP but also provides convincing evidence to develop TGP-based therapies in the treatment of scleroderma and other autoimmune diseases associated with type I IFN signatures. ClassificationSkin

Integrating UPLC-HR-MS/MS, Network Pharmacology, and Experimental Validation to Uncover the Mechanisms of Jin'gan Capsules against Breast Cancer.

In the theory of traditional Chinese medicine (TCM), “liver-qi” stagnation and heat-induced toxicity represent the main etiologies of breast cancer. Recently, several TCMs with heat-clearing and detoxification efficacy have shown inhibitory effects on breast cancer. Jin’gan capsules (JGCs), initially approved to treat colds in China, are a heat-clearing and detoxification TCM formula. However, the anticancer activity of JGCs against breast cancer and its underlying mechanisms remain unclear. First, we assessed the antiproliferative activity of JGCs in breast cancer cell lines and evaluated their effects on cell apoptosis and the cell cycle by flow cytometry. Furthermore, we identified the potential bioactive components of JGCs and their corresponding target genes and constructed a bioactive compound–target interaction network by ultra-performance liquid chromatography–high-resolution tandem mass spectrometry (UPLC-HR-MS/MS) and network pharmacology analysis. Finally, the underlying mechanism was investigated through gene function enrichment analysis and experimental validation. We found that JGCs significantly inhibited breast cancer cell growth with IC50 values of 0.56 ± 0.03, 0.16 ± 0.03, and 0.94 ± 0.09 mg/mL for MDA-MB-231, MDA-MB-468, and MCF-7, respectively. In addition, JGC treatment dramatically induced apoptosis and S phase cell cycle arrest in breast cancer cells. Western blot analysis confirmed that JGCs could regulate the protein levels of apoptosis- and cell cycle-related genes. Utilizing UPLC-HR-MS/MS analysis and network pharmacology, we identified 7 potential bioactive ingredients in JGCs and 116 antibreast cancer targets. Functional enrichment analysis indicated that the antitumor effects of JGCs were strongly associated with apoptosis and the Janus kinase (JAK)-signal transducer and activator of transcription (STAT) signaling pathway. Western blot analysis validated that JGC treatment markedly decreased the expression levels of p-JAK2, p-STAT3, and STAT3. Our findings suggest that JGCs suppress breast cancer cell proliferation and induce cell cycle arrest and apoptosis partly by inhibiting the JAK2/STAT3 signaling pathway, highlighting JGCs as a potential therapeutic candidate against breast cancer.

Network analysis combined with pharmacological evaluation strategy to reveal the mechanism of Tibetan medicine Wuwei Shexiang pills in treating rheumatoid arthritis

Tibetan medicine is an important part of traditional Chinese medicine and a significant representative of ethnic medicine in China. Tibetan medicine is gradually recognized by the world for its unique curative effects. Wuwei Shexiang pills (WPW) has been widely used to treat “Zhenbu” disease (Also known as rheumatoid arthritis) in Tibetan medicine, however, its potential bioactive ingredients and mechanism for RA treatment remain unclear. In this study, we used a combination of gas chromatography-mass spectrometry (GC-MS), ultra-performance liquid chromatography coupled with quadrupole time-of-fight mass spectrometry (UPLC-Q-TOF/MS), network analysis and experimental validation to elucidate the potential pharmacodynamic substances and mechanisms of WPW in the treatment of rheumatoid arthritis (RA). The results showed that songoramine, cheilanthifoline, saussureanine C, acoric acid, arjunolic acid, peraksine, ellagic acid, arjungenin and other 11 components may be the main activities of WPW in the treatment of RA. PIK3CA, AKT, MAPK, IL-6, TNF, MMP1, MMP3, and CDK1 are considered as core targets. PI3K-AKT, MAPK, apoptosis, cell cycle, and other signaling pathways may be the key pathways for WPW to play a role in the treatment of RA. Furthermore, we validated the underlying molecular mechanism of WPW predicted by network analysis and demonstrated its possible mechanism through in vivo animal experiments. It was found that WPW could significantly improve the degree of paw swelling, and reduce ankle joint diameter and arthritis index. Further histomorphological analysis showed that WPW could reduce the degree of synovial tissue inflammation and ankle joint cartilage damage. Meanwhile, WPW could down-regulate the levels of IL-6, IL-1β, and IL-17, and increase the levels of IL-10 and IL-4 in the serum of AA rats. TUNEL staining confirmed that WPW could significantly promote the apoptosis of synovial cells. Moreover, the immunohistochemical results showed that WPW decreased the expression of PI3K, AKT, MAPK, MMP1, MMP3, CDK1, and Bcl-2, as well as increased the expression of Bax protein. In conclusion, we successfully combined GC-MS, UPLC-Q-TOF/MS, network analysis, and experimental validation strategies to elucidate the inhibition of inflammation by WPW in AA model rats via PI3K/AKT, MAPK, cell cycle and apoptotic pathways process. This not only provides new evidence for the study of potential pharmacodynamic substances and the mechanism of WPW in the treatment of RA, but also provides ideas for the study of other Tibetan medicine compound preparations.

Pomegranate juice ameliorates pulmonary fibrosis by regulating inflammatory response and epithelial mesenchymal transformation

POMJ could ameliorate pulmonary fibrosis in vivo and in vitro . Based on the analysis of the bioactive ingredients and the anti-oxidation ability of POMJ, we explored the potential role and underlying mechanisms of POMJ against PF both in in vivo and in vitro experimental model. POMJ could improve BLM-induced PF by alleviating the inflammatory response and the progression of EMT, and also could ameliorate EMT process in TGF-β1 stimulated cell model by inhibiting the activation of NF-κB pathway. • The potential bioactive ingredients in POMJ were analyzed using LC-HR/MS. • POMJ prevents bleomycin-induced lung injury by reducing inflammation response. • POMJ alleviated EMT in vivo and in vitro . • POMJ suppressed TGF‐β1‐induced NF‐κB pathway activation in EMT. Pulmonary fibrosis (PF) is a chronic, progressive interstitial pneumonia characterized by abnormal epithelial -mesenchymal transition (EMT) and persistent inflammatory injury. Pomegranate has multiple biological activities, including antioxidant, anti-inflammatory and anticancer activities. In this study, we evaluated the effect of pomegranate juice (POMJ) in ameliorating PF and explored the underlying mechanisms in vivo and in vitro . Compared to the Vehicle group, POMJ attenuated bleomycin (BLM)-induced histopathological changes and collagen deposition in the lungs and alleviated the inflammatory response. Western blot and immunohistochemistry results revealed that POMJ treatment reduced the expression of Collagen I and Vimentin and increased the expression of E-cadherin. In addition, in TGF-β1-treated A549 cells, it was further confirmed, which may be associated with inhibition of NF-κB pathway activation. Taken together, these findings suggest that POMJ ameliorates lung injury by regulating the inflammatory response and the process of EMT, exhibiting great potential to ameliorate pulmonary fibrosis.

Isolation and identification of immunomodulatory peptides from the protein hydrolysate of tuna trimmings (Thunnas albacares)

To improve the commercial value of underutilized fish-trade by-products, immunomodulatory peptides were detected and subsequently isolated from the trypsin hydrolysate of tuna trimmings. The gel-isolated fraction T1 of the hydrolysate showed the best enhancement of immune activity. The addition of T1 to RAW264.7 cells enhanced phagocytosis and promoted the secretion of NO, IL-1β, IL-6 and TNF-α. Moreover, T1 significantly accelerated the expression of TLR2 and TLR4, promoted the phosphorylation of IKK and p65, and further activated the NF-κB signalling pathway to promote the immune response of RAW264.7 cells. By analyzing computer-simulated docking with TLR2 and TLR4, key immunomodulatory peptides were identified. The immune activity of synthetic peptides was verified, with HIAEEADRK and AEQAESDKK exhibiting the strongest immune activity. Ultimately, the T1 fraction demonstrated the most potential as an immune-enhancing source of nutraceutical and functional foods, and peptides HIAEEADRK and AEQAESDKK were the potential bioactive ingredient of the T1 fraction.

Potential biocontrol mechanisms of Bacillus sp. TSO2 against Bipolaris sorokiniana, spot blotch in wheat

&lt;p class="Default"&gt;&lt;em&gt;Bipolaris sorokiniana &lt;/em&gt;is a pathogen of cereals such as wheat and barley, causing root rot, leaf blight, seedling blight, and spot blotch. This phytopathogen causes a considerable reduction in cereal yield of up to 85%. Thus, sustainable alternatives to the application of synthetic fungicides are determinants for the control of phytopathogens, such as the application of biological control agents. This study aims to identify the potential biocontrol mechanisms of the bacterial strain TSO2 by sequencing, annotation, and mining its genome. The draft genome of strain TSO2 was sequenced through the Illumina Miseq platform and presented 4,242,212 bp, 43.9% G+C content, 300,069 bp N50, 5 L50, 47 contigs, 96 RNAs, and 4,432 predicted coding DNA sequences. Besides, the presence of 86 CDS of agricultural importance involved in virulence, disease, defense, iron acquisition, and secondary and phosphate metabolisms was detected. On the other hand, seven putative secondary metabolite gene clusters involved in biocontrol activity were identified in the genome of strain TSO2. &lt;em&gt;Bacillus &lt;/em&gt;sp. TSO2 contains a great number of biosynthetic gene clusters which supports its biocontrol activity against phytopathogenic fungi. Thus, this strain needs to be further studied as a potential bioactive ingredient for the biopesticide formulation due to its high potential as a biological control agent.&lt;/p&gt;

A comprehensive strategy integrating metabolomics with multiple chemometric for discovery of function related active markers for assessment of foodstuffs: A case of hawthorn (Crataegus cuneata) fruits

There is a growing demand for functional foodstuffs naturally rich in nutrients and bioactive compounds associated with putative health benefits. This study followed a strategy integrating metabolomic with chemometric to identify quality markers that can be used to distinguish function related bioactivity of fruits, using hawthorn (Crataegus cuneata) fruit as an example. The integrated strategy was reduced to characterization of metabolic processes and discovered potential bioactive ingredients that were further investigated for functionalities. This comprehensive process provided guidance for discovery of function-related active markers for assessment of foodstuffs.

Anti-VEGF Effect of Bioactive Indolic Compounds and Hydroxytyrosol Metabolites.

Angiogenesis is a key process involved in both cancer and cardiovascular diseases, the vascular endothelial growth factor (VEGF) and its VEGF receptor-2 (VEGFR-2) being the main triggers. The aim of this study was to determine the molecular mechanism underlying the potent inhibition of VEGF signaling by hydroxytyrosol (HT) metabolites and indolic compounds and establish a relation between their structure and bioactivity. Experiments involved the evaluation of their potential to inhibit VEGF on human umbilical vein endothelial cells (HUVECs) by ELISA assay and their subsequent effect on the downstream signaling pathway (PLCγ1, Akt, and endothelial nitric oxide synthetase (eNOS)) by Western blot. Respectively, 3,4-dihydroxyphenylacetaldehyde (DOPAL) (100 µM) and indole pyruvic acid (IPy) (1 mM) were capable of inhibiting VEGFR-2 activation with an IC50 value of 119 µM and 1.037 mM. The anti-angiogenic effect of DOPAL and IPy is mediated via PLCγ1. Additionally, DOPAL significantly increases eNOS phosphorylation, while IPy maintained it. These data provide for the first time evidence of the anti-angiogenic effect of DOPAL and IPy for future use as potential bioactive food ingredients.