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    Protective role of butyrate in obesity and diabetes: New insights
    (Frontiers Media SA, 2022-11-24) ;
    Carlos Barba-Ostria
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    SIMANCAS RACINES, DANIEL ALEJANDRO
    ;
    <jats:p>Studies in human microbiota dysbiosis have shown that short-chain fatty acids (SCFAs) like propionate, acetate, and particularly butyrate, positively affect energy homeostasis, behavior, and inflammation. This positive effect can be demonstrated in the reduction of butyrate-producing bacteria observed in the gut microbiota of individuals with type 2 diabetes (T2DM) and other energy-associated metabolic alterations. Butyrate is the major end product of dietary fiber bacterial fermentation in the large intestine and serves as the primary energy source for colonocytes. In addition, it plays a key role in reducing glycemia and improving body weight control and insulin sensitivity. The major mechanisms involved in butyrate regulation include key signaling pathways such as AMPK, p38, HDAC inhibition, and cAMP production/signaling. Treatment strategies using butyrate aim to increase its intestine levels, bioavailability, and improvement in delivery either through direct supplementation or by increasing dietary fiber in the diet, which ultimately generates a higher production of butyrate in the gut. In the final part of this review, we present a summary of the most relevant studies currently being carried out in humans.</jats:p>
    Scopus© Citations 117
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    Microencapsulation of Anthocyanins from Zea mays and Solanum tuberosum: Impacts on Antioxidant, Antimicrobial, and Cytotoxic Activities
    (MDPI AG, 2024-11-27)
    Carlos Barba-Ostria
    ;
    Yenddy Carrero
    ;
    Jéssica Guamán-Bautista
    ;
    Orestes López
    ;
    Christian Aranda
    Objectives: This study investigates the biological activities of microencapsulated anthocyanins extracted from two Andean ancestral edible plants, Solanum tuberosum, and Zea mays, with a focus on their potential applications in functional foods and therapeutics. The primary objective was to evaluate their antioxidant, antimicrobial, and cytotoxic properties alongside structural and functional analyses of the microencapsulation process. Methods: Anthocyanins were extracted and microencapsulated using maltodextrin as a carrier. Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) were employed to analyze the stability and structure of the microencapsulated particles. The antioxidant, antimicrobial, and cytotoxic activities of the microencapsulated were assessed through established assays. Results:S. tuberosum exhibited superior antioxidant capacity and potent anticancer activity against HepG2 and THJ29T cell lines, while Z. mays demonstrated significant antimicrobial efficacy against multidrug-resistant bacterial strains and biofilm-forming pathogens. Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) confirmed the stabilization of anthocyanins within a maltodextrin matrix, enhancing their bioavailability and application potential. Conclusions: These results highlight the versatility of microencapsulated anthocyanins as bioactive agents for industrial and therapeutic applications. Future studies should explore in vivo validation and synergistic formulations to optimize their efficacy and broaden their use in nutraceutical and pharmaceutical fields.
    Scopus© Citations 7
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    Gene silencing based on RNA-guided catalytically inactive Cas9 (dCas9): a new tool for genetic engineering in Leptospira
    (Springer Science and Business Media LLC, 2019-02-12)
    L. G. V. Fernandes
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    S. A. Vasconcellos
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    Marcos B. Heinemann
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    M. Picardeau
    <jats:title>Abstract</jats:title><jats:p>Leptospirosis is a worldwide zoonosis caused by pathogenic bacteria of the genus <jats:italic>Leptospira</jats:italic>, which also includes free-living saprophyte strains. Many aspects of leptospiral basic biology and virulence mechanisms remain unexplored mainly due to the lack of effective genetic tools available for these bacteria. Recently, the type II CRISPR/Cas system from <jats:italic>Streptococcus pyogenes</jats:italic> has been widely used as an efficient genome engineering tool in bacteria by inducing double-strand breaks (DSBs) in the desired genomic targets caused by an RNA-guided DNA endonuclease called Cas9, and the DSB repair associated machinery. In the present work, plasmids expressing heterologous <jats:italic>S. pyogenes</jats:italic> Cas9 in <jats:italic>L. biflexa</jats:italic> cells were generated, and the enzyme could be expressed with no apparent toxicity to leptospiral cells. However, <jats:italic>L. biflexa</jats:italic> cells were unable to repair RNA-guided Cas9-induced DSBs. Thus, we used a catalytically dead Cas9 (dCas9) to obtain gene silencing rather than disruption, in a strategy called CRISPR interference (CRISPRi). We demonstrated complete gene silencing in <jats:italic>L. biflexa</jats:italic> cells when both dCas9 and single-guide RNA (sgRNA) targeting the coding strand of the β-galactosidase gene were expressed simultaneously. Furthermore, when the system was applied for silencing the <jats:italic>dnaK</jats:italic> gene, no colonies were recovered, indicating that DnaK protein is essential in <jats:italic>Leptospira</jats:italic>. In addition, flagellar motor switch FliG gene silencing resulted in reduced bacterial motility. To the best of our knowledge, this is the first work applying the CRISPRi system in <jats:italic>Leptospira</jats:italic> and spirochetes in general, expanding the tools available for understanding leptospiral biology.</jats:p>
    Scopus© Citations 40
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    Crystal Structure, Hirshfeld Surface Analysis, and Biological Activities of Schiff-Base Derivatives of 4-Aminoantipyrine
    (American Chemical Society (ACS), 2023-10-31)
    Esteban Aguilar-Llanos
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    Saskya E. Carrera-Pacheco
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    Juan Carlos Romero-Benavides
    ;
    Carlos Cevallos-Morillo
    Scopus© Citations 32
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    Designing cytochrome P450 enzymes for use in cancer gene therapy
    (Frontiers Media SA, 2024-05-24)
    Saskya E. Carrera-Pacheco
    ;
    Alexander Mueller
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    Juan A. Puente-Pineda
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    Cancer is a significant global socioeconomic burden, as millions of new cases and deaths occur annually. In 2020, almost 10 million cancer deaths were recorded worldwide. Advancements in cancer gene therapy have revolutionized the landscape of cancer treatment. An approach with promising potential for cancer gene therapy is introducing genes to cancer cells that encode for chemotherapy prodrug metabolizing enzymes, such as Cytochrome P450 (CYP) enzymes, which can contribute to the effective elimination of cancer cells. This can be achieved through gene-directed enzyme prodrug therapy (GDEPT). CYP enzymes can be genetically engineered to improve anticancer prodrug conversion to its active metabolites and to minimize chemotherapy side effects by reducing the prodrug dosage. Rational design, directed evolution, and phylogenetic methods are some approaches to developing tailored CYP enzymes for cancer therapy. Here, we provide a compilation of genetic modifications performed on CYP enzymes aiming to build highly efficient therapeutic genes capable of bio-activating different chemotherapeutic prodrugs. Additionally, this review summarizes promising preclinical and clinical trials highlighting engineered CYP enzymes’ potential in GDEPT. Finally, the challenges, limitations, and future directions of using CYP enzymes for GDEPT in cancer gene therapy are discussed.
    Scopus© Citations 11
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    Phytochemical Composition and Biological Properties of Macleania rupestris Fruit Extract: Insights into Its Antimicrobial and Antioxidant Activity
    (MDPI AG, 2025-03-27) ; ;
    Elena Coyago-Cruz
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    ;
    Jéssica Guamán-Bautista
    Macleania rupestris, a fruit-bearing species of the Ericaceae family, has traditionally been used for its potential medicinal properties. Background/Objectives: This study investigates the phytochemical composition and antimicrobial activity of M. rupestris fruit extract, focusing on its antibacterial, antibiofilm, and antifungal effects. Methods: M. rupestris (Kunth) A.C.Sm. berries (code: 4456, Herbario QUPS-Ecuador) were collected from the cloud forest Montano Alto, Cuenca-Ecuador, and the extract was obtained using an ethanolic-based extraction and chemically characterized. The antibacterial and antifungal activity of the fruit extract was assessed against seven multidrug-resistant bacteria strains and four fungal strains using the microdilution method. The biofilm inhibition potential was evaluated using a microplate assay with the crystal violet staining method. The antioxidant activity was evaluated using DPPH and ABTS assays. Results: The bioactive compounds showed 853.9 mg phenols/100 g DW, 573.2 mg organic acid/100 g DW, and 21.5 mg C-3-gl/100 g DW of anthocyanins. The antibacterial assays demonstrated significant inhibitory activity against Enterococcus faecalis, Enterococcus faecium, Escherichia coli, and Staphylococcus epidermidis, with MIC values ranging from 1.25 to 5 mg/mL. Additionally, the biofilm inhibition assays confirmed the potential of M. rupestris extract to disrupt bacterial biofilms, particularly in S. aureus and L. monocytogenes. Nevertheless, no significant antifungal activity was observed against Candida spp., suggesting selective antimicrobial properties. Finally, the antioxidant activity was strong (1.62 mmol TE/100 g DW by DPPH and 3.28 mmol TE/100 g DW by ABTS). Conclusions: These findings indicate that M. rupestris possesses promising antibacterial, antibiofilm, and antioxidant properties, which may be attributed to its phenolic and organic acid composition. Further fractionation and targeted bioassays are required to elucidate the specific bioactive compounds responsible for these effects and explore their potential applications in antimicrobial formulations.
    Scopus© Citations 9
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    Green Synthesis of Silver Oxide Nanoparticles from Mauritia flexuosa Fruit Extract: Characterization and Bioactivity Assessment
    (MDPI AG, 2024-11-22) ;
    David Vaca-Vega
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    Karla Vizuete
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    Saskya E. Carrera-Pacheco
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    The increasing prevalence of multidrug-resistant (MDR) pathogens, persistent biofilms, oxidative stress, and cancerous cell proliferation poses significant challenges in healthcare and environmental settings, highlighting the urgent need for innovative and sustainable therapeutic solutions. The exploration of nanotechnology, particularly the use of green-synthesized nanoparticles, offers a promising avenue to address these complex biological challenges due to their multifunctional properties and biocompatibility. Utilizing a green synthesis approach, Mauritia flexuosa Mf-Ag2ONPs were synthesized and characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), X-ray diffraction (XRD), energy-dispersive X-ray spectroscopy coupled with scanning electron microscopy (EDS-SEM), UV-Vis spectroscopy, and Fourier transform infrared spectroscopy (FTIR). The Mf-Ag2ONPs exhibited potent antibacterial effects against both non-resistant and MDR bacterial strains, with minimum inhibitory concentrations (MICs) ranging from 11.25 to 45 µg/mL. Mf-Ag2ONPs also demonstrated significant antifungal efficacy, particularly against Candida glabrata, with an MIC of 5.63 µg/mL. Moreover, the nanoparticles showed strong biofilm inhibition capabilities and substantial antioxidant properties, underscoring their potential to combat oxidative stress. Additionally, Mf-Ag2ONPs exhibited pronounced anticancer properties against various cancer cell lines, displaying low IC50 values across various cancer cell lines while maintaining minimal hemolytic activity at therapeutic concentrations. These findings suggest that Mf-Ag2ONPs synthesized via an eco-friendly approach offer a promising alternative for biomedical applications, including antimicrobial, antifungal, antioxidant, and anticancer therapies, warranting further in vivo studies to fully exploit their therapeutic potential.
    Scopus© Citations 15
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    Chemical Properties and Biological Activity of Bee Pollen
    (MDPI AG, 2023-11-25)
    Cristina Rodríguez-Pólit
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    ;
    Roberto Vallejo-Imbaquingo
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    Carlos Barba-Ostria
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    <jats:p>Pollen, a remarkably versatile natural compound collected by bees for its abundant source of proteins and nutrients, represents a rich reservoir of diverse bioactive compounds with noteworthy chemical and therapeutic potential. Its extensive biological effects have been known and exploited since ancient times. Today, there is an increased interest in finding natural compounds against oxidative stress, a factor that contributes to various diseases. Recent research has unraveled a multitude of biological activities associated with bee pollen, ranging from antioxidant, anti-inflammatory, antimicrobial, and antifungal properties to potential antiviral and anticancer applications. Comprehending the extensive repertoire of biological properties across various pollen sources remains challenging. By investigating a spectrum of pollen types and their chemical composition, this review produces an updated analysis of the bioactive constituents and the therapeutic prospects they offer. This review emphasizes the necessity for further exploration and standardization of diverse pollen sources and bioactive compounds that could contribute to the development of innovative therapies.</jats:p>
    Scopus© Citations 57
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    Mxenes as a versatile nanoplatform: Synthesis and emerging biomedical applications
    (Elsevier BV, 2025-09-25)
    Ali Mohammad Amani
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    Ehsan Vafa
    ;
    Maryam Mirzae
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    Milad Abbasi
    ;
    Ahmad Vaez
    Recently, MXenes have garnered significant attention in academic research due to their remarkable structural, electrical, magnetic, optical, mechanical, and chemical properties. New advancements and emerging findings indicate that MXene, classified as a two-dimensional (2D) layered material, exhibits significantly more potential in the field of biomedicine and biotechnology compared to existing nanosystems. These applications include acting as antibacterial agents, biosensor systems, the delivery and loading of drugs, bioimaging, and therapeutic interventions. The unique characteristics of MXenes, such as their significant electrical conductivity, large surface area, low toxicity, magnetism, luminescence, and high biocompatibility, make them highly promising candidates for diagnostic, therapeutic, and theranostic applications. Surface modifications of MXenes exhibit biocompatibility and have multifunctional functions, including the ability to direct ligands towards specific spots for preferential aggregation, hence enabling their utilization in specialized applications. This paper provides an overview of the characteristics, modifications, and synthesis methods of MXene nanomaterials. The present article also delivers a comprehensive assessment of the practical uses of MXene-based nanomaterials in biomedicine, with a particular focus on biosensing, bioimaging, antibacterial effects, implants, and multifunctional therapeutic platforms. This paper also presents a discussion of the future prospects and challenges associated with the applications of MXenes in the biomedicine field.
    Scopus© Citations 38
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    Bioactive Properties of Microencapsulated Anthocyanins from Vaccinium floribundum and Rubus glaucus
    (MDPI AG, 2024-11-21)
    Carlos Barba-Ostria
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    ;
    Castillo-solís Fabián
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    Saskya E. Carrera-Pacheco
    ;
    Orestes Lopez
    Anthocyanins, widely recognized for their antioxidant properties and potential health benefits, are highly susceptible to degradation due to environmental factors such as light, temperature, and pH leading to reduced bioavailability and efficacy. Microencapsulation, which involves entrapment in a matrix to enhance stability and bioavailability. This study aims to investigate the bioactive properties of microencapsulated anthocyanins derived from Vaccinium floribundum (Andean blueberry) and Rubus glaucus (Andean blackberry). The extracts from V. floribundum and R. glaucus were microencapsulated using maltodextrin as the carrier agent due to its film-forming properties and effectiveness in stabilizing sensitive compounds through a spray-drying process. The microcapsules were characterized using Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM) to assess their chemical and morphological properties. The biological activities of these microencapsulated anthocyanins were evaluated using in vitro assays for their antibacterial, antioxidant, and anti-inflammatory effects. The results indicated enhanced bioactivity of the microencapsulated anthocyanins, suggesting their potential use in developing functional foods and pharmaceuticals. This study provides valuable insights into the effectiveness of microencapsulation in preserving anthocyanins’ functional properties and enhancing their health-promoting effects, highlighting the potential for application in the food and pharmaceutical industries.
    Scopus© Citations 12