37 research outputs found

    Tucumanin, a β-hydroxy-γ-lactone bistetrahydrofuranic acetogenin from Annona cherimolia, is a potent inhibitor of mitochondrial complex I

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    A new β-hydroxy-γ-methyl-γ-lactone bistetrahydrofuranic acetogenin, tucumanin, with the infrequent symmetrical threo/trans/threo/trans/ threo relative configuration at the tetrahydrofuran rings was isolated from Annona cherimolia (Annonaceae) seeds. The inhibitory potency on the mitochondrial complex I of acetogenins with this relative configuration (tucumanin and asimicin) was compared with that shown by the corresponding pairs with an asymmetrical threo/trans/threo/trans/erythro relative configuration (laherradurin/rolliniastatin-2, and itrabin/molvizarin). All these compounds act as selective inhibitors of mitochondrial complex 1 in the 0.18 - 1.55 nM range.Fil: Barrachina, Isabel. Universidad de Valencia; EspañaFil: Neske, Adriana. Universidad Nacional de Tucumán; ArgentinaFil: Granell, Susana. Universidad de Valencia; EspañaFil: Bermejo, Almudena. Universidad de Valencia; EspañaFil: Chahboune, Nadia. Universidad de Valencia; EspañaFil: El Aouad, Noureddine. Universidad de Valencia; EspañaFil: Alvarez, Olga. Universidad Nacional de Tucumán; ArgentinaFil: Bardon, Alicia del Valle. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán. Instituto de Química del Noroeste. Universidad Nacional de Tucumán. Facultad de Bioquímica, Química y Farmacia. Instituto de Química del Noroeste; Argentina. Universidad Nacional de Tucumán; ArgentinaFil: Zafra Polo, M. Carmen. Universidad de Valencia; Españ

    Exploring the potential anti-inflammatory and wound-healing proprieties of Cepaea hortensis snail mucin

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    Long before its popularization as a skincare ingredient, snail slime was reported to have a variety of health-promoting attributes. Its medicinal use involved the treatment of ailments, such as anthrax, hernias, stomach pain, chest pain, as well as tuberculosis. The main aim of this study was to investigate the anti-inflammatory and wound-healing properties of snail slime from Cepaea hortensis (Müller, 1774) (brown garden snail). The slime was extracted by a mild method, and the anti-inflammatory characteristics were determined by croton-oil-induced mouse-ear edema. The histological study showed that the snail slime exerts its action at the level of inflammatory mediators, explaining the drastic decrease of edema (59% in comparison to the 47% of indomethacin). The daily application of 50 µL (15 mg/kg) of snail slime on excision wounds in rabbits proved to induce an almost full tissue repair after 24 days of treatment (87.80–92.7% wound closure in width and length, respectively). Analysis of the slime’s safety aspect allowed affirming the nontoxicity of snail slime on both the skin and eyes.info:eu-repo/semantics/publishedVersio

    Valorization of dairy and fruit/berry industry by-products to sustainable marinades for broilers’ wooden breast meat quality improvement

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    The study aims to improve the quality of wooden breast meat (WBM) via the use of newly developed marinades based on selected strains of lactic acid bacteria (LAB) in combination with the by-products of the dairy and fruit/berry industries. Six distinct marinades were produced based on milk permeate (MP) fermented with Lacticaseibacillus casei (Lc) and Liquorilactobacillus uvarum (Lu) with the addition of apple (ApBp) and blackcurrant (BcBp) processing by-products. The microbiological and acidity parameters of the fermented marinades were evaluated. The effects of marinades on the microbiological, technical, and physicochemical properties of meat were assessed following 24 and 48 h of WBM treatment. It was established that LAB viable counts in marinades were higher than 7.00 log10 colony-forming units (CFU)/mL and, after 48 h of marination, enterobacteria and molds/yeasts in WBM were absent. Marinated (24 and 48 h) WBM showed lower dry-matter and protein content, as well as water holding capacity, and exhibited higher drip loss (by 8.76%) and cooking loss (by 12.3%) in comparison with controls. After WBM treatment, biogenic amines decreased; besides, the absence of spermidine and phenylethylamine was observed in meat marinated for 48 h with a marinade prepared with Lu. Overall, this study highlights the potential advantages of the developed sustainable marinades in enhancing the safety and quality attributes of WBM.info:eu-repo/semantics/publishedVersio

    Contribution to the characterization of the seed endophyte microbiome of Argania spinosa across geographical locations in Central Morocco using metagenomic approaches

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    Microbial endophytes are microorganisms that live inside plants, and some of them play important yet understudied roles in plant health, growth, and adaptation to environmental conditions. Their diversity within plants has traditionally been underestimated due to the limitations of culture-dependent techniques. Metagenomic profiling provides a culture-independent approach to characterize entire microbial communities. The argan tree (Argania spinosa) is ecologically and economically important in Morocco, yet its seed endophyte microbiome remains unexplored. This study aimed to compare the bacterial and fungal endophyte communities associated with argan seeds collected from six sites across Morocco using Illumina MiSeq sequencing of the 16S rRNA gene and ITS regions, respectively. Bacterial DNA was extracted from surface-sterilized seeds and amplified using universal primers, while fungal DNA was isolated directly from seeds. Bioinformatics analysis of sequencing data identified taxonomic profiles at the phylum to genus levels. The results indicated that bacterial communities were dominated by the genus Rhodoligotrophos, while fungal communities exhibited varying degrees of dominance between Ascomycota and Basidiomycota depending on site, with Penicillium being the most abundant overall. Distinct site-specific profiles were observed, with Pseudomonas, Bacillus, and Aspergillus present across multiple locations. Alpha diversity indices revealed variation in endophyte richness between seed sources. In conclusion, this first exploration of the argan seed endophyte microbiome demonstrated environmental influence on community structure. While facing limitations due to small sample sizes and lack of ecological metadata, it provides a foundation for future mechanistic investigations into how specific endophyte–host interactions shape argan adaptation across Morocco’s diverse landscapes

    Semisynthetic roxburghin tetra­methyl ether

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    The title mol­ecule, (E)-2,3′,4,5-tetra­methoxy­stilbene, C18H20O4, is virtually planar. The angle between the two benzene rings is 4.06 (6)°. The inter­molecular inter­actions present in the structure are weak. There are C—H⋯O hydrogen bonds and C—H⋯π-electron ring inter­actions. The mol­ecules are ordered into planes that are parallel to (01). The distance between adjacent planes is about 3.3 Å and therefore π–π electron inter­actions between the aromatic planes are also plausible

    Discovery of New Compounds Active against Plasmodium falciparum by High Throughput Screening of Microbial Natural Products

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    Due to the low structural diversity within the set of antimalarial drugs currently available in the clinic and the increasing number of cases of resistance, there is an urgent need to find new compounds with novel modes of action to treat the disease. Microbial natural products are characterized by their large diversity provided in terms of the chemical complexity of the compounds and the novelty of structures. Microbial natural products extracts have been underexplored in the search for new antiparasitic drugs and even more so in the discovery of new antimalarials. Our objective was to find new druggable natural products with antimalarial properties from the MEDINA natural products collection, one of the largest natural product libraries harboring more than 130,000 microbial extracts. In this work, we describe the optimization process and the results of a phenotypic high throughput screen (HTS) based on measurements of Plasmodium lactate dehydrogenase. A subset of more than 20,000 extracts from the MEDINA microbial products collection has been explored, leading to the discovery of 3 new compounds with antimalarial activity. In addition, we report on the novel antiplasmodial activity of 4 previously described natural productsThis work was supported by the Junta de Andalucía [BIO-199, P09-CVI- 5367], the VI Plan Nacional de Investigación Científica, Desarrollo e Innovación Tecnológica 2008-2011, Instituto de Salud Carlos III-Subdirección General de Redes y Centros de Investigación Cooperativa-Red de Investigación Cooperativa en Enfermedades Tropicales (RICET FIS Network: RD12/0018/0017),the Plan Nacional (SAF2013-48999-R), the FEDER funds from the EU and the PARAMET network (FP7-PEOPLE-2011-ITN. GA290080) to DG-P. Research of FV and OG was supported by the Instituto de Salud Carlos III-Subdirección General de Redes y Centros de Investigación Cooperativa-Red de Investigación Cooperativa en Enfermedades Tropicales (RICET FIS Network: RD12/0018/0005) and the FEDER funds from the EU and the PARAMET network (FP7-PEOPLE-2011-ITN. GA290080). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.Peer reviewe

    In Vitro and In Silico Evaluations of <i>Boswellia carterii</i> Resin Dermocosmetic Activities

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    Boswellia carterii is a plant species belonging to the Burseraceae family. It grows up in trees or shrubs, and it is known for producing an aromatic resin commonly named frankincense or olibanum. This resin has been used in traditional medicine to treat various conditions such as inflammations, gastrointestinal disorders and traumatic injuries. Virtual screening and molecular docking are two in silico approaches used to predict potential interactions between ligands and the active site of a protein. These approaches are mainly used in natural product chemistry and pharmacology as a screening tool to select plant extracts or fractions for in vitro testing, as well as for the prediction of mechanisms of action. The aim of this research is the in silico and in vitro evaluations of the potential collagenase and elastase inhibitory activities of Boswellia carterii resin organic extracts (viz., methanol, n-hexane and ethyl acetate). The obtained results revealed that methanol and n-hexane exhibited the best collagenase inhibitory activity with values superior to 85%, whereas the methanol and ethyl acetate showed the highest elastase inhibition activity with inhibition values ranging between 40 and 60%. The molecular docking prediction confirmed the experimental results; moreover, the visualization of the ligand–protein interactions showed that the main compounds of the organic extracts may have mechanisms of action similar to the positive controls. Those findings are very promising and open new perspectives for the exploitation of Boswellia carterii resin as active agents for the development of anti-aging cosmeceuticals

    In Vitro and In Silico Evaluations of Boswellia&nbsp;carterii Resin Dermocosmetic Activities

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    Boswellia carterii is a plant species belonging to the Burseraceae family. It grows up in trees or shrubs, and it is known for producing an aromatic resin commonly named frankincense or olibanum. This resin has been used in traditional medicine to treat various conditions such as inflammations, gastrointestinal disorders and traumatic injuries. Virtual screening and molecular docking are two in silico approaches used to predict potential interactions between ligands and the active site of a protein. These approaches are mainly used in natural product chemistry and pharmacology as a screening tool to select plant extracts or fractions for in vitro testing, as well as for the prediction of mechanisms of action. The aim of this research is the in silico and in vitro evaluations of the potential collagenase and elastase inhibitory activities of Boswellia carterii resin organic extracts (viz., methanol, n-hexane and ethyl acetate). The obtained results revealed that methanol and n-hexane exhibited the best collagenase inhibitory activity with values superior to 85%, whereas the methanol and ethyl acetate showed the highest elastase inhibition activity with inhibition values ranging between 40 and 60%. The molecular docking prediction confirmed the experimental results; moreover, the visualization of the ligand&ndash;protein interactions showed that the main compounds of the organic extracts may have mechanisms of action similar to the positive controls. Those findings are very promising and open new perspectives for the exploitation of Boswellia carterii resin as active agents for the development of anti-aging cosmeceuticals

    Molecular Docking, Tyrosinase, Collagenase, and Elastase Inhibition Activities of Argan By-Products

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    The argan tree (Argania spinosa (L.) Skeels) is one of the most important floristic resources in Morocco. This Moroccan endemic tree is known for its numerous therapeutic and medicinal uses. In addition to some medicinal and cosmetic uses, argan fruit pulp and press cake are traditionally used by the Berber population for heating and feeding livestock. Molecular docking is an in silico approach that predicts the interaction between a ligand and a protein. This approach is mainly used in chemistry and pharmacology of natural products as a prediction tool with the purpose of selecting plant extracts or fractions for in vitro tests. The aim of this research is to study the evaluation of potential tyrosinase, collagenase, and elastase inhibitory activities of argan fruit press-cake and pulp extracts. Extracts were evaluated for their total phenolic content (TPC), and the major polyphenols of both press-cake and pulp extracts were submitted to molecular docking in order to determine the mechanisms of action of these compounds. Obtained results revealed that fruit pulp had the strongest dermocosmetic activities, as well as the highest TPC, with values above 55 mg gallic-acid equivalent per gram of dry matter (mgeq AG/gDM). Moreover, those results were positively correlated with the docking findings, suggesting that the pulp lead compounds have higher affinity with tyrosinase, collagenase, and elastase action sites. The results here presented are very promising and open new perspectives for the exploitation of argan-tree by-products as cosmetic agents towards the development of new anti-aging products

    Phytochemical Screening, and In Vitro Evaluation of the Antioxidant and Dermocosmetic Activities of Four Moroccan Plants: <i>Halimium antiatlanticum</i>, <i>Adenocarpus artemisiifolius</i>, <i>Pistacia lentiscus</i> and <i>Leonotis nepetifolia</i>

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    In this study, four Moroccan plants, Halimium antiatlanticum, Adenocarpus artemisiifolius, Pistacia lentiscus and Leonotis nepetifolia, were evaluated for their phytoconstituents and biological activities. Methanolic extracts of these plants were obtained by Soxhlet apparatus, phytochemical screening was performed, and the total phenolic and flavonoid contents were determined. Then, the antioxidant and dermocosmetic activities of the methanolic extracts were evaluated. The obtained results revealed that the leaves and/or aerial parts contained tannins, polyphenols, flavonoids, coumarins, carotenoids, terpenoids and saponins. The higher total phenolic content values were recorded on Pistacia lentiscus and Halimium antiatlanticum with 396.64 ± 30.79 and 304.96 ± 55.61 mgGAE/gDW, respectively. The antioxidant activity was measured by DPPH, ABTS and FRAP assays, and showed that Pistacia lentiscus and Halimium antiatlanticum were the most active extracts, with, respectively, IC50 values of 3.705 ± 0.445 and 5.037 ± 0.122 µg/mL for DPPH. The same results were observed for the FRAP and ABTS assays. Those extracts also showed a strong collagenase inhibitory activity at 200 µg/mL, with 78.51 ± 2.27% for Pistacia lentiscus and 73.10 ± 8.52% for Halimium antiatlanticum. Adenocarpus artemisiifolius showed the highest elastase inhibition rate, with 76.30 ± 5.29%. This study disclosed the dermocosmetic potential of Halimium antiatlanticum and Adenocarpus artemisiifolius, two Moroccan endemic plants that can be traditionally used by local populations or exploited by the cosmetic industry
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