Bioactivity Profile Research Articles

Sour Jujube (Ziziphus jujuba var. spinosa): A Bibliometric Review of Its Bioactive Profile, Health Benefits and Trends in Food and Medicine Applications.

Research on the comprehensive utilization of sour jujube and its beneficial properties to human health has attracted extensive attention. This study aims to conduct a bibliometric analysis of the bioactive profile of sour jujube and future trends in applications. The research advancements within this field from 2000 to 2023 were addressed using the Web of Science database and VOSviewer. Among the 322 results, the most frequent keywords of bioactivity are flavonoids, antioxidants, saponins, insomnia, polyphenols, terpenoids and anti-inflammatory; the most studied parts of sour jujube are seeds, fruits and leaves; the published articles with high citations mainly focus on identification, biological effects and different parts distribution of bioactive compounds. The bioactivity of various parts of sour jujube was reviewed considering their application potential. The seeds, rich in flavonoids, saponins and alkaloids, exhibit strong effects on central nervous system diseases and have been well-developed in pharmacology, healthcare products and functional foods. The pulp has antioxidant properties and is used to develop added-value foods (e.g., juice, vinegar, wine). The leaves can be used to make tea and flowers are good sources of honey; their extracts are rich sources of flavonoids and saponins, which show promising medicinal effects. The branches, roots and bark have healing properties in traditional folk medicine. Overall, this study provides a reference for future applications of sour jujube in food and medicine fields.

Engineering a Hybrid Ti6Al4V-Based System for Responsive and Consistent Osteogenesis.

As the aging population increases worldwide, the incidence of musculoskeletal diseases and the need for orthopedic implants also arise. One of the most desirable goals in orthopedic reconstructive therapies is de novo bone formation. Yet, reproducible, long-lasting, and cost-effective strategies for implants that strongly induce osteogenesis are still in need. Nanoengineered titanium substrates (and their alloys) are among the most used materials in orthopedic implants. Although having high biocompatibility, titanium alloys hold a low bioactivity profile. The osteogenic capacity and osseointegration of Ti-based implantable systems are limited, as they critically depend on the body-substrate interactions defined by blood proteins adsorbed into implant surfaces that ultimately lead to the recruitment, proliferation, and differentiation of mesenchymal stem cells (MSCs) to comply bone formation and regeneration. In this work, a hybrid Ti6Al4V system combining micro- and nanoscale modifications induced by hydrothermal treatment followed by functionalization with a bioactive compound (fibronectin derived from human plasma) is proposed, aiming for bioactivity improvement. An evaluation of the biological activity and cellular responses in vitro with respect to bone regeneration indicated that the integration of morphological and chemical modifications into Ti6Al4V surfaces induces the osteogenic differentiation of MSCs to improve bone regeneration by an enhancement of mineral matrix formation that accelerates the osseointegration process. Overall, this hybrid system has numerous competitive advantages over more complex treatments, including reproducibility, low production cost, and potential for improved long-term maintenance of the implant.

Annulated Heterocyclic[g]Coumarin Composites: Synthetic Approaches and Bioactive Profiling.

Coumarins, widely abundant natural heterocyclic compounds, are extensively employed in creating various biologically and pharmacologically potent substances. The hybridization of heterocycles presents a key opportunity to craft innovative multicyclic compounds with enhanced biological activity. Fusing different heterocyclic rings with the coumarin structure presents an intriguing method for crafting fresh hybrid compounds possessing remarkable biological effects. In the pursuit of creating heterocyclic-fused coumarins, a wide range of annulated heterocyclic[g]coumarin composites has been introduced, displaying impressive biological potency. The influence of the linear attachment of heterocyclic rings to the coumarin structure on the biological performance of the resulting compounds has been investigated. This review centers on the synthetic methodologies, structural activity relationship investigation, and biological potentials of annulated heterocyclic[g]coumarin composites. We conducted searches across several databases, including Web of Science, Google Scholar, PubMed, and Scopus. After sieving, we ultimately identified and included 71 pertinent studies published between 2000 and the middle of 2023. This will provide valuable perspectives for medicinal chemists in the prospective design and synthesis of lead compounds with significant therapeutic effects, centered around heterocycle-fused coumarin frameworks.

African Under-Utilized Medicinal Leafy Vegetables Studied by Microtiter Plate Assays and High-Performance Thin-Layer Chromatography-Planar Assays.

Biological activities of six under-utilized medicinal leafy vegetable plants indigenous to Africa, i.e., Basella alba, Crassocephalum rubens, Gnetum africanum, Launaea taraxacifolia, Solanecio biafrae, and Solanum macrocarpon, were investigated via two independent techniques. The total phenolic content (TPC) was determined, and six microtiter plate assays were applied after extraction and fractionation. Three were antioxidant in vitro assays, i.e., ferric reducing antioxidant power (FRAP), cupric reduction antioxidant capacity (CUPRAC), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging, and the others were enzyme (acetylcholinesterase, butyrylcholinesterase, and tyrosinase) inhibition assays. The highest TPC and antioxidant activity from all the methods were obtained from polar and medium polar fractions of C. rubens, S. biafrae, and S. macrocarpon. The highest acetyl- and butyrylcholinesterase inhibition was exhibited by polar fractions of S. biafrae, C. rubens, and L. taraxacifolia, the latter comparable to galantamine. The highest tyrosinase inhibition was observed in the n-butanol fraction of C. rubens and ethyl acetate fraction of S. biafrae. In vitro assay results of the different extracts and fractions were mostly in agreement with the bioactivity profiling via high-performance thin-layer chromatography-multi-imaging-effect-directed analysis, exploiting nine different planar assays. Several separated compounds of the plant extracts showed antioxidant, α-glucosidase, α-amylase, acetyl- and butyrylcholinesterase-inhibiting, Gram-positive/-negative antimicrobial, cytotoxic, and genotoxic activities. A prominent apolar bioactive compound zone was tentatively assigned to fatty acids, in particular linolenic acid, via electrospray ionization high-resolution mass spectrometry. The detected antioxidant, antimicrobial, antidiabetic, anticholinesterase, cytotoxic, and genotoxic potentials of these vegetable plants, in particular C. rubens, S. biafrae, and S. macrocarpon, may validate some of their ethnomedicinal uses.

Kinetic simulation of convection drying for its effect on nutritional, functional, and phytochemical profiling of Colocasia antiquorum and Nasturtium officinale leaves of the Himalayan region

AbstractColocasia antiquorum (Taro) and Nasturtium officinale (Watercress) leaves are highly potent indigenous crops with rich nutritional and phytochemical profiles. The leaves were mathematically modeled, using thin‐layer models, to study the process kinetics for convection drying and its cumulative effect on the physico‐chemical, nutritional, functional, phytochemical, and targeted metabolite profiles. The best‐fit model for C. antiquorum was the two‐term model, whereas for N. officinale, Page model showed the best adequacy with the determination of least Chi‐square and high co‐efficient along with root mean square error. The color and pigment degradation were the prominent changes observed in the quality characteristics of C. antiquorum and N. officinale leaves depicted by the color degradation study. The nutritional composition was significantly affected by the convective drying with reduced ash, protein, and phenolic contents. The extraction yields were however higher along with some elevated metabolite contents estimated for convection drying in comparison to freeze‐dried leaves.Practical applicationsThis study explores the drying kinetic behavior for the progression of moisture loss occurring over the drying time and moderation of drying to achieve a desired moisture content at certain drying rates. The quality characterization before and after selected drying conditions revealed the sensitivity of the chlorophyll/carotenoid pigments, nutrients, and phenolics retained significantly after the end point of drying. Also, the effect of convective drying on the physicochemical, nutritional, and phytochemical contents was significant, which edifies the extent of alterations occurring due to convective drying on the quality characteristics of Colocasia antiquorum (Taro) and Nasturtium officinale (Watercress) leaves. Consequently, these two leafy vegetables hold good potential as crops to be promoted for nutritional security and health and wellness due to their rich bioactive profiles.

Alkyl deoxyglycoside-polymyxin combinations against critical priority carbapenem-resistant gram-negative bacteria

The escalating antimicrobial resistance crisis urges the development of new antibacterial treatments with innovative mechanisms of action, particularly against the critical priority carbapenem-resistant Acinetobacter baumannii (CRAB), Pseudomonas aeruginosa (CRPA) and Enterobacteriaceae (CRE). Membrane-disrupting dodecyl deoxyglycosides have been reported for their interesting phosphatidylethanolamine-associated bactericidal activity against Gram-positive strains; however, their inability to penetrate the Gram-negative outer membrane (OM) renders them useless against the most challenging pathogens. Aiming to repurpose alkyl deoxyglycosides against Gram-negative bacteria, this study investigates the antimicrobial effects of five reference compounds with different deoxygenation patterns or anomeric configurations in combination with polymyxins as adjuvants for enhanced OM permeability. The generation of the lead 4,6-dideoxy scaffold was optimized through a simultaneous dideoxygenation step and applied to the synthesis of a novel alkyl 4,6-dideoxy C-glycoside 5, herein reported for the first time. When combined with subtherapeutic colistin concentrations, most glycosides demonstrated potent antimicrobial activity against several multidrug-resistant clinical isolates of CRAB, CRE and CRPA exhibiting distinct carbapenem resistance mechanisms, together with acceptable cytotoxicity against human HEK-293T and Caco-2 cells. The novel 4,6-dideoxy C-glycoside 5 emerged as the most promising prototype structure for further development (MIC 3.1 μg/mL when combined with colistin 0.5 μg/mL against CRPA or 0.25 μg/mL against several CRE and CRAB strains), highlighting the potential of C-glycosylation for an improved bioactive profile. This study is the first to show the potential of IM-targeting carbohydrate-based compounds for the treatment of infections caused by MDR Gram-negative pathogens of clinical importance.

Hydrogel foam dressings with angiogenic and immunomodulatory factors from mesenchymal stem cells.

Stem cell therapy and skin substitutes address the stalled healing of chronic wounds in order to promote wound closure; however, the high cost and regulatory hurdles of these treatments limit patient access. A low-cost method to induce bioactive healing has the potential to substantially improve patient care and prevent wound-induced limb loss. A previous study reported that bioactive factors derived from apoptotic-like mesenchymal stem cells (MSCs) demonstrated anti-inflammatory and proangiogenic effects and improved ischemic muscle regeneration. In this work, these MSC-derived bioactive factors were loaded into a hydrogel foam to harness immunomodulatory and angiogenic properties from MSC components to facilitate chronic wound healing without the high cost and translational challenges of cell therapies. After incorporation of bioactive factors, the hydrogel foam retained high absorbency, moisture retention, and target water vapor transmission rate. High loading efficiency was confirmed and release studies indicated that over 90% of loaded factors were released within 24 h. Ethylene oxide sterilization and 4-week storage did not affect the bioactive factor release profile or physical properties of the hydrogel foam dressing. Bioactivity retention of the released factors was also confirmed for as-sterilized, 4°C-stored, and -20°C-stored bioactive hydrogel foams as determined by relevant gene expression levels in treated pro-inflammatory (M1) macrophages. These results support the use of the bioactive dressings as an off-the-shelf product. Overall, this work reports a new method to achieve a first-line wound dressing with the potential to reduce persistent inflammation and promote angiogenesis in chronic wounds.

A Long-Term Study on Chemical Compounds and Their Location in Sweet Basil Leaves from Organic and Conventional Producers

Bioactive compound profiles in organic and conventional sweet basil were analyzed by HPLC, and the enzymatic status and antioxidant status of plants cultivated with the two systems were also examined. Fluorescence microscopy was used for the determination of compounds’ locations in the basil leaves. The experiment was conducted from 2019 to 2021. Organic and conventional basil samples were obtained directly from Polish herb producers. The results showed that the chemical profiles of organic and conventional basil leaves are different. Not only the cultivation method but also the experimental year had a significant impact on the antioxidant content in basil leaves. Organic basil contained significantly more dry matter (11.97 g 100 g−1 FW) compared to conventional one (10.54 g 100 g−1 FW) and a higher tendency for total phenolic compounds (5.24 mg g −1 DW) accumulation. The higher bioactive compound content reflects the antioxidant activity (61.0%, 54.33%, and 46%) in organic basil compared to conventional (46.87%, 38.055, and 39.24%) with respect to the analysis method (ABTS, DPPH, and FRAP). Catalase activity (39 µmol H2O2 min−1 mg−1) in organic basil was higher compared to conventional (23.19 µmol H2O2 min−1 mg−1) ones. The obtained results are very unique and could be used by herb producers as a key for high-quality basil production. The higher concentration of bioactive compounds in organic basil gives a better nutraceutical status to this popular herb.

A randomized, placebo-controlled crossover trial to assess the influence of body weight on aspirin-triggered specialized pro-resolving mediators: Protocol for the DISCOVER Study.

Low-dose aspirin is ineffective for primary prevention of cardiovascular events in people with body weight greater than 70kg. While the prevalent explanation for this is reduced platelet cyclooxygenase-1 (COX-1) inhibition at higher body weights, supporting data are limited, thereby demanding further investigation of the reason(s) underlying this observation. We propose that aspirin-mediated cyclooxygenase-2 (COX-2) acetylation and the resulting synthesis of 15-epi-lipoxin A4, a specialized pro-resolving mediator, is suboptimal in higher weight individuals, which may contribute to the clinical trial findings. To test this hypothesis, we are conducting a double-blind, placebo-controlled, randomized, mechanistic crossover trial. Healthy men and women exhibiting a wide range of body weights take 81mg aspirin and 325mg aspirin for 3 weeks each, following 3-week placebo run-in and wash-out phases. Our target sample size is 90 subjects, with a minimum of 72 completing all visits estimated to be necessary to achieve power adequate to test our primary hypothesis. Our primary endpoint is the difference in change in plasma 15-epi-lipoxin A4 occurring with each dose of aspirin. Secondary endpoints include lipid mediator profiles, serum bioactive lipid profiles, and other endpoints involved in the resolution of vascular inflammation. Study enrollment began in November 2021 and is ongoing. The results of this study will improve our understanding of the mechanisms underlying aspirin's role(s) in the prevention of adverse cardiovascular outcomes. They may also lead to additional studies with the potential to inform dosing strategies for patients based on body weight.

Physicochemical and bioactive traits of black chickpea (Cicer arietinum) as affected by germination-induced modifications

ABSTRACT Foods with higher bioactive activities are being sought as a potential tool to prevent lifestyle-related disorders. In this context, germinated foods are preferred over conventional foods as they are rich in health promoting moieties. The current research was planned to assess the germination-induced modifications in physicochemical and bioactive profile of black chickpea (Cicer arietinum). For this purpose, black chickpeas (desi) were soaked for 12 h and germinated. The germinated black chickpeas were recovered after 24, 48, 72, 96, and 120 h of germination, separately, and their physicochemical and antioxidant profiles were studied. The phytochemical profiling of the germinated black chickpea revealed that germination time significantly influenced the chemical composition of black chickpea. It was observed that the phytochemical contents of the germinated chickpeas increased with an increase in germination time. However, the flavonoids such as rutin, luteolin, kaempferol, and quercetin were decreased, but isorhamnetin was increased as the germination time was extended. Moreover, the antioxidant capacity quantified by DPPH and ABTS activity of germinated chickpeas also increased with an increase in germination time. The highest content of DPPH antioxidant activity was observed at the 72 h of germination, while the highest concentration of ABTS was observed at the fourth day of germination. Conclusively, extended germination for 120 h can negatively influence the phytochemical and antioxidant profile of black chickpea, whereas optimum germination for 72 h was found satisfactory.

Investigations on the chemical and bioactivity profile of Bromeliaceae Juss

Bromeliaceae Juss., in several cultures for thousands of years it has been used for food, fibers, in ceremonies, medicines and ornamental plants. The phytochemical composition of the species of the family is chemodiverse, with the presence of fatty acids, phenolic compounds, vitamins, triterpenes and enzymes, exerting antibacterial, antimicrobial, hypoglycemic, antileukemic, proteolytic activities, non-polar natural products and production of bioactive peptides. As a result, the family has great chemical and pharmacological potential in order to contribute to scientific knowledge and the development of new drugs.

Profile Assessment of Bioactive Peptides in the Greek Traditional Cheese “Tsalafouti”

In the Greek regions of Agrafa and Tzoumerka, Tsalafouti, a traditional spreadable cheese made from goat’s and sheep’s milk is produced. This product has emerged in recent years as a result of the campaign to acquire Geographical Indication. This study aimed to assess the biopeptide profile of Tsalafouti cheese in order to highlight its nutritional value. Using HPLC-MS, bioactive peptides in Tsalafouti cheese samples were identified and classified according to their bioactivity. The biopeptides detected are known to present antibacterial, anti-diabetic, anti-hypertensive, anti-thrombotic, antioxidant, and immunomodulatory activities, while ACE enzyme and dipeptidyl-4 (DPP-IV) inhibitors were also identified. Based on these results, Tsalafouti cheese presents an interesting bioactive peptides profile that may act as special motivation for consumers to choose this specific cheese.

Discovery of Repurposable Drugs in the Combination Therapy of Breast Cancer: A Virtual Drug Screening Study

Cathepsin D (Cat D) is a lysosomal aspartic acid protease encoded by CTSD gene and has significant biological roles such as degradation of extracellular and intracellular proteins, regulation of apoptosis, hormone processing, antigen processing etc. Furthermore, it is overexpressed by breast cancer cells and it acts a role in many processes affecting the cancer prognosis such as metastasis, angiogenesis, invasion, and drug resistance through regulation of the metabolic pathways and digesting the extracellular matrix (ECM) proteins. Due to that there is no drug targeting Cat D in clinical trial phases, a virtual drug screening in order to reveal possible drugs with high Cat D inhibitory activity from a library composed of 12,111 ligands is carried out with this study. Results have demonstrated that ZINC000003922429 (Adozelesin), ZINC000012358610 (Phthalocyanine), ZINC000051951669 (Bemcentinib), ZINC000003786250 (YM022), and ZINC000150338819 (Ledipasvir) have high binding affinity to Cat D. Among these chemical ligands, YM022 from Drugs in Clinical Trials dataset has been evaluated as most promising one that might be repurposed in the treatment of breast cancer due to its high affinity, convenient ADME and Toxicity properties, and highest bioactivity profiles. However, the possible activity of YM022 should be analyzed with further molecular dynamics (MD) simulations, in vitro and in vivo studies.

Antifungal and Antiproliferative Activity of Pistagremic Acid and Flavonoids Extracted from the Galls of Pistacia chinensis subsp. integerrima.

Pistacia chinensis subsp. integerrima (J.L. Stewart) Rech. f. is a plant known for its therapeutic applications in traditional medicine, which are related to its antimicrobial, anticancer, antioxidant, anti-inflammatory, analgesic, antidiarrheal, and muscle relaxant properties. The galls of P. chinensis are rich in triterpenes and flavonoids, and we here report the extraction of pistagremic acid (1), apigenin (2) and sakuranetin (3) from this source. The isolated compounds were tested against Aspergillus flavus, Candida albicans, Candida glabrata, Fusarium solani, Microsporum canis and Trichoderma longibrachiatum. The results highlighted the antimicrobial activity of flavonoids 2 and 3, suggesting that this class of molecules may be responsible for the effect related to the traditional use. On the other hand, when the compounds and the extract were tested for their antiproliferative activity on a panel of 4 human cancer cell lines, the triterpene pistagremic acid (1) showed a higher potential, thus demonstrating a different bioactivity profile. Structure-based docking and molecular dynamics simulations were used to help the interpretation of experimental results. Taken together, the here reported findings pave the way for the rationalization of the use of P. chinensis extracts, highlighting the contributions of the different components of galls to the observed bioactivity.

Investigating bioactive phytochemicals in bulb and shoot of Allium longisepalum Bertol. from Iran

This study investigated a wide range of bioactive compounds in bulb and shoot of Allium longisepalum Bertol. from Iran. The organs were first extracted with methanol, followed by hexane, dichloromethane, chloroform, ethyl acetate, and butanol, and phytochemicals in fractions were analysed using GC/MS. Butanol exhibited the highest yield percentages in both organs. Palmitic and oleic acid were found in all fractions, while heptadecene-(8)-carboxylic acid, stearic acid, and myristic acid were detected in at least three fractions. Each fraction contained exclusively unique metabolites found only in itself. Hexane, dichloromethane, and chloroform fractions contained specific metabolites with potential antioxidant, allelopathic, antibacterial, and anti-inflammatory effects. Ethyl acetate and butanol fractions revealed significant compounds that have potential in terms of their anticarcinogenic, anti-inflammatory, hair growth-enhancing, and antimicrobial properties, in addition to containing compounds not previously identified in plants. The study analyzes bioactive compound profiles in A. longisepalum, highlighting its chemical diversity and therapeutic potential.

Ionic Liquid-Catalyzed Multicomponent Synthesis of Isoxazole-5(4H)-ones: in vitro Activities and Principal Component Analysis

Heterocycles of the isoxazolone class stand out in the pharmaceutical field because they have numerous biological properties, such as antioxidant, antifungal and antibacterial properties. Thus, isoxazole derivatives have attracted the attention of organic researchers, and several procedures have been developed to obtain these compounds. The present study aimed to synthesize 17 derivatives of isoxazol-5(4H)-ones using a multicomponent reaction catalyzed by an acidic ionic liquid, which allowed yields from 20-96% of the products. To evaluate the bioactivity of the compounds, the synthesized derivatives were analyzed at various concentrations against bacteria and fungi; the derivatives, in general, showed a moderate activity of 125 μg mL-1 against the fungus Candida tropicalis (ATCC 13803) and four derivatives showed an inhibition of < 15.62 μg mL-1 for Gram-positive Staphylococcus epidermidis (ATCC 12228). Furthermore, the antioxidant potential of the derivatives was evaluated by measuring their ability to scavenge 2,2-diphenyl1-picryl-hydrazyl (DPPH) free radicals, resulting in a remarkable reduction percentage of up to 81.06%. To gain further insights into the structure-activity relationships, a principal component analysis was conducted to classify the compounds into active and inactive classes, providing a comprehensive understanding of their bioactivity profiles.

Characteristics of bioactive components in fermented Sargassum and Ulva Seaweed using SCOBY as potential anti-diabetic candidates

Sargassum and Ulva are abundant seaweeds in Indonesia, renowned for their bioactive compounds with diverse biological activities, including anti-diabetic properties. However, the full utilization of these seaweeds, particularly in the form of functional beverages, has not been achieved. Fermentation using Symbiotic Culture of Bacteria and Yeast (SCOBY) presents a promising method for producing functional seaweed beverages. This study aimed to analyze the chemical composition of Sargassum sp. and Ulva sp., assess their anti-diabetic properties, and investigate the effects of fermentation with SCOBY on their bioactive profile. Hot water extracts of Sargassum sp., Ulva sp., and a combination of both were fermented with SCOBY for 8 days at room temperature. The results revealed that Sargassum sp. contains hydroquinone phenols, steroids, triterpenoids, tannins, and saponins, whereas Ulva sp. contains hydroquinone phenols, steroids, and saponins. The combined seaweed extracts exhibited a higher total phenolic content (69.63 ppm) and demonstrated stronger anti-diabetic activity, with a low IC50 value for alpha-amylase inhibition (4.04±0.09 ppm). LC/MS profiling of extracts and fermented combinations highlighted differences attributed to SCOBY fermentation, suggesting the potential for enhanced anti-diabetic activity.

Microwave-Assisted Rearrangement of Costunolide Catalyzed by Palladium(II)

The structure of costunolide was modified before conducting the Cope rearrangement under thermal conditions. This modification was undertaken to block the highly reactive Michael acceptor α-methylene-γ-lactone, thus preventing side reactions at high temperatures. In this work, the reaction was performed under heating or microwave irradiation using costunolide, not its modified version. Rates of Cope reactions catalyzed by palladium(II) assisted by microwave were substantially enhanced. The rearrangements of costunolide to elemanolide, eudesmanolides, and germacranolide were catalyzed by palladium acetate, bis(benzonitrile)palladium dichloride, and a mixture of both organometallics. Rates of microwave promoted rearrangements of costunolide were six times faster than the reactions assisted by heating. The best success rate for elemanolide (7) was obtained using a mixture of Pd(OAc)2 and (NCPh)2PdCl2. In this case, compound 7 was obtained in a yield of 34%, while the other sesquiterpene lactones were formed only in trace amounts. The reaction products were isolated using semi-preparative high performance liquid chromatography and further purified through sequential analytical high performance liquid chromatography. Bioactivity profiles that used etiolated wheat coleoptiles were conducted for compounds 6, 7, and 9. The tested compounds presented very high phytotoxicity, with inhibition up to 97%.

Identification of bioactive compounds and ADMET profile of stem bark of Syzygium samarangense and their potential as antibreast cancer and antiinflammatory

Identification of bioactive compounds and ADMET profile of stem bark of Syzygium samarangense and their potential as antibreast cancer and antiinflammatory

Probiotic-fermented tomato with hepatic lipid metabolism modulation effects: analysis of physicochemical properties, bioactivities, and potential bioactive compounds.

Lactiplantibacillus plantarum NCUH001046 (LP)-fermented tomatoes exhibited the potential to alleviate obesity in our previous study. This subsequent study further delves deeper into the effects of LP fermentation on the physicochemical properties, bioactivities, and hepatic lipid metabolism modulation of tomatoes, as well as the analysis of potential bioactive compounds exerting obesity-alleviating effects. Results showed that after LP fermentation, viable bacterial counts peaked at 9.11 log CFU mL-1 and sugar decreased, while organic acids, umami amino acids, total phenols, and total flavonoids increased. LP fermentation also improved the inhibition capacities of three digestive enzyme activities and Enterobacter cloacae growth, as well as antioxidant activities. Western blot results indicated that fermented tomatoes, especially live probiotic-fermented tomatoes (LFT), showed improved effects compared to unfermented tomatoes in reducing hepatic lipid accumulation by activating the AMPK signal pathway. UHPLC-Q-TOF/MS-based untargeted metabolomics analysis showed that chlorogenic acid, capsiate, tiliroside, irisflorentin, and homoeriodictyol levels increased after fermentation. Subsequent cell culture assays demonstrated that irisflorentin and homoeriodictyol reduced lipid accumulation via enhancing AMPK expression in oleic acid-induced hyperlipidemic HepG2 cells. Furthermore, Spearman's correlation analysis indicated that the five phenols were positively associated with hepatic AMPK pathway activation. Consequently, it could be inferred that the five phenols may be potential bioactive compounds in LFT to alleviate obesity and lipid metabolism disorders. In summary, these findings underscored the transformative potential of LP fermentation in enhancing the bioactive profile of tomatoes and augmenting its capacity to alleviate obesity and lipid metabolism disorders. This study furnished theoretical underpinnings for the functional investigation of probiotic-fermented plant-based foods.