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    Bioactivación del quimioterapéutico ciclofosfamida mediada por citocromos P450 con fines de uso en terapia génica de cáncer
    (Universidad Tecnica del Norte, 2025-01-31)
    Saskya Carrera-Pacheco
    ;
    Esta revisión examina el papel de las enzimas del citocromo P450 en la bioactivación del agente quimioterapéutico ciclofosfamida (CPA) para uso en la terapia génica del cáncer. El estudio explora enzimas específicas del citocromo P450, como CYP2B6, CYP2C9 y CYP3A4, encargadas de metabolizar la CPA en su forma activa, destacando su potencial en la terapia del gen suicida o GDEPT. La revisión también analiza las modificaciones genéticas realizadas para mejorar la eficiencia catalítica de estas enzimas y aborda los desafíos y las direcciones futuras de la integración de GDEPT con otras terapias contra el cáncer para mejorar la especificidad y eficacia del tratamiento.
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    Experimental and computational studies of Schiff bases derived from 4-aminoantipyrine as potential antibacterial and anticancer agents
    (Springer Science and Business Media LLC, 2025-01-31) ; ;
    Saskya E. Carrera Pacheco
    ;
    Cristina Rodríguez-Pólit
    ;
    Carlos Barba-Ostria
    Schiff bases are organic compounds recognized for their biological activities, including antiviral, antibacterial, antifungal, and anticancer properties, making them promising candidates in medicinal chemistry. In this studio, a series of Schiff bases derived from 4-aminoantipyrine and substituted cinnamaldehydes were evaluated in vitro against liver (HepG2) and thyroid (THJ29T) cancer cells, Gram-positive and Gram-negative multidrug-resistant bacteria, and biofilm-forming pathogens. Six compounds demonstrated anticancer activity, though some exhibited toxicity to non-tumor cells. Compounds showed notable anticancer potential, while also exhibited strong antibacterial effects, with being the most effective against multidrug-resistant bacteria strains. These Schiff bases also inhibit biofilm formation, suggesting their potential for treating biofilm-related infections. analyses of their ADME properties, global reactivity descriptors, and binding affinities corroborated these findings. The Schiff base has a strong binding affinity for DNA gyrase and vitamin D receptor, suggesting potential mechanisms for its antibacterial and anticancer activities.
    Scopus© Citations 17
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    Bioactive Phenolic Compounds from Rambutan - Nephelium lappaceum L. - Shell: Encapsulation, Structural Stability, and Multifunctional Activities
    (MDPI AG, 2025-11-09)
    Carlos Barba Ostria
    ;
    Orestes López
    ;
    Alexis Debut
    ;
    ;
    Rambutan (Nephelium lappaceum) shell, an agro-industrial by-product, is a rich source of phenolic acids and minor anthocyanins, but its direct use is limited by instability and low bioavailability. We extracted phenolic-rich fractions and produced maltodextrin microcapsules by spray drying, then confirmed chemical entrapment and amorphization by FTIR, SEM, and XRD. The formulation showed high encapsulation efficiency and high antioxidant capacity (DPPH), selective bactericidal activity against Pseudomonas aeruginosa and Burkholderia cepacia, and strong inhibition of Staphylococcus aureus and Listeria monocytogenes biofilms, while exhibiting negligible hemolysis (&lt;2%) across tested concentrations. Antitumor effects were moderate with low selectivity in vitro, indicating that phenolic-acid-driven redox modulation may require fractionation or delivery optimization for oncology applications. Overall, spray-dried microcapsules provided structural stability and safety while concentrating multifunctional activities relevant to food and biomedical uses. By valorizing a tropical waste stream into a bioactive, hemocompatible ingredient, this work aligns with societal goals on health and sustainable production (SDG 3 and SDG 12) and offers a scalable route to deploy underutilized phenolic resources.</jats:p>
    Scopus© Citations 8
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    Exploring the Multifaceted Biological Activities of Anthocyanins Isolated from Two Andean Berries
    (MDPI AG, 2024-08-21)
    Carlos Barba-Ostria
    ;
    Saskya E. Carrera-Pacheco
    ;
    ; ;
    Natural pigments extracted from plant species are used in foods, cosmetics, and pharmaceuticals. This study evaluates the comprehensive biological activities of anthocyanins isolated from Andean blueberry (Vaccinium floribundum Kunth) and Andean blackberry (Rubus glaucus Benth), focusing on their antimicrobial, antioxidant, antitumoral, anti-inflammatory, and hemolytic properties. Chemical characterization revealed significant anthocyanin content with complex mass spectrometric profiles indicating diverse glycosylation patterns that may influence their bioactivity. The antimicrobial assays showed that the extracts were particularly effective against Gram-positive bacteria, with minimal inhibitory concentrations (MICs) as low as 1 mg/mL for Rubus glaucus, indicating strong potential for therapeutic use. The antioxidant capacity of the berries was substantial, albeit slightly lower than that of ascorbic acid. The extracts also exhibited notable antitumoral activity in various cancer cell lines, showing promise as adjunctive or preventive treatments. The anti-inflammatory effects were confirmed by inhibiting nitric oxide production in macrophage cells, highlighting their potential in managing inflammatory diseases. In terms of hemolytic activity, Rubus glaucus exhibited dose-dependent effects, potentially attributable to anthocyanins and phenolics, while Vaccinium floribundum demonstrated no significant hemolytic activity, underscoring its safety. These findings suggest that anthocyanins from Andean berries possess potent biological activities, which could be leveraged for health benefits in pharmaceutical and nutraceutical applications. Further studies are needed to isolate specific bioactive compounds and investigate their synergistic effects in clinical and real-world contexts.
    Scopus© Citations 13
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    Current Landscape of Methods to Evaluate Antimicrobial Activity of Natural Extracts
    (MDPI AG, 2023-01-20) ;
    Saskya E. Carrera-Pacheco
    ;
    ;
    Cristina Rodríguez-Pólit
    ;
    <jats:p>Natural extracts have been and continue to be used to treat a wide range of medical conditions, from infectious diseases to cancer, based on their convenience and therapeutic potential. Natural products derived from microbes, plants, and animals offer a broad variety of molecules and chemical compounds. Natural products are not only one of the most important sources for innovative drug development for animal and human health, but they are also an inspiration for synthetic biology and chemistry scientists towards the discovery of new bioactive compounds and pharmaceuticals. This is particularly relevant in the current context, where antimicrobial resistance has risen as a global health problem. Thus, efforts are being directed toward studying natural compounds’ chemical composition and bioactive potential to generate drugs with better efficacy and lower toxicity than existing molecules. Currently, a wide range of methodologies are used to analyze the in vitro activity of natural extracts to determine their suitability as antimicrobial agents. Despite traditional technologies being the most employed, technological advances have contributed to the implementation of methods able to circumvent issues related to analysis capacity, time, sensitivity, and reproducibility. This review produces an updated analysis of the conventional and current methods to evaluate the antimicrobial activity of natural compounds.</jats:p>
    Scopus© Citations 93
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    Evaluation of Biological Activity of Natural Compounds: Current Trends and Methods
    (MDPI AG, 2022-07-13)
    Carlos Barba-Ostria
    ;
    Saskya E. Carrera-Pacheco
    ;
    ;
    Cristina Rodríguez-Pólit
    ;
    <jats:p>Natural compounds have diverse structures and are present in different forms of life. Metabolites such as tannins, anthocyanins, and alkaloids, among others, serve as a defense mechanism in live organisms and are undoubtedly compounds of interest for the food, cosmetic, and pharmaceutical industries. Plants, bacteria, and insects represent sources of biomolecules with diverse activities, which are in many cases poorly studied. To use these molecules for different applications, it is essential to know their structure, concentrations, and biological activity potential. In vitro techniques that evaluate the biological activity of the molecules of interest have been developed since the 1950s. Currently, different methodologies have emerged to overcome some of the limitations of these traditional techniques, mainly via reductions in time and costs. These emerging technologies continue to appear due to the urgent need to expand the analysis capacity of a growing number of reported biomolecules. This review presents an updated summary of the conventional and relevant methods to evaluate the natural compounds’ biological activity in vitro.</jats:p>
    Scopus© Citations 146
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    The Impact of Bioactive Molecules from Probiotics on Child Health: A Comprehensive Review
    (MDPI AG, 2024-10-30) ;
    Saskya E. Carrera-Pacheco
    ;
    ;
    Enrique Teran
    ;
    Cesar Erazo
    <jats:p>Background: This review investigates the impact of bioactive molecules produced by probiotics on child health, focusing on their roles in modulating gut microbiota, enhancing immune function, and supporting overall development. Key metabolites, including short-chain fatty acids (SCFAs), bacteriocins, exopolysaccharides (EPSs), vitamins, and gamma-aminobutyric acid (GABA), are highlighted for their ability to maintain gut health, regulate inflammation, and support neurodevelopment. Objectives: The aim of this review is to examine the mechanisms of action and clinical evidence supporting the use of probiotics and postbiotics in pediatric healthcare, with a focus on promoting optimal growth, development, and overall health in children. Methods: The review synthesizes findings from clinical studies that investigate the effects of probiotics and their metabolites on pediatric health. The focus is on specific probiotics and their ability to influence gut health, immune responses, and developmental outcomes. Results: Clinical studies demonstrate that specific probiotics and their metabolites can reduce gastrointestinal disorders, enhance immune responses, and decrease the incidence of allergies and respiratory infections in pediatric populations. Additionally, postbiotics—bioactive compounds from probiotic fermentation—offer promising benefits, such as improved gut barrier function, reduced inflammation, and enhanced nutrient absorption, while presenting fewer safety concerns compared to live probiotics. Conclusions: By examining the mechanisms of action and clinical evidence, this review underscores the potential of integrating probiotics and postbiotics into pediatric healthcare strategies to promote optimal growth, development, and overall health in children.</jats:p>
    Scopus© Citations 33
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    Bioactive Compounds, Antioxidant, Antimicrobial and Anticancerogenic Activity in Lacmellea edulis H. Karst., at Different Stages of Maturity
    (MDPI AG, 2025-10-14)
    Elena Coyago-Cruz
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    ;
    Gabriela Méndez
    ;
    Melany Alomoto
    ;
    Steven Vélez-Vite
    Lacmellea edulis, traditionally known as chicle, is a species that has received little attention despite its nutraceutical potential. This study aimed to evaluate the physicochemical characteristics (pH, soluble solids, titratable acidity, moisture, ash, and minerals) and the content of bioactive compounds (vitamin C, organic acids, carotenoids, and phenols) of fruits at different stages of ripeness, as well as their antimicrobial (against Candida albicans, Candida tropicalis, Escherichia coli, Staphylococcus aureus, and Streptococcus mutans), antiproliferative and antihaemolytic activity. Bioactive compounds were quantified using liquid chromatography, while biological activities were assessed via spectrophotometric assays. The results revealed a high concentration of ascorbic acid in the ripe pulp (3.0 mg/100 g DW), higher levels of organic acids in the unripe pulp (3947.6 mg/100 g DW), and a high total phenol content in the ripe peel (10,890.9 mg/100 g DW). The peel exhibited the highest antioxidant activity (63.3 mmol ET/100 g DW). Regarding antimicrobial activity, the pulp exhibited the lowest MIC values against E. coli (2.7 mg/mL) and S. mutans (2.6 mg/mL), the peel against S. aureus (21.3 mg/mL) and C. tropicalis (5.3 mg/mL), and the seeds against C. albicans (20.8 mg/mL). Additionally, the peel exhibited the greatest antiproliferative efficacy against cervical (HeLa) and hepatoma (HepG2) cancer cells. None of the evaluated extracts showed significant haemolytic effects, confirming their safety. Overall, L. edulis appears to be a promising source of bioactive metabolites with potential applications in functional foods and pharmaceutical products.
    Scopus© Citations 2
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    Antimicrobial, Antioxidant, Antitumor, and Anti-Inflammatory Properties of Gleichenella pectinata, a Bioprospecting of Medicinal Ferns
    (MDPI AG, 2025-11-12)
    Elena Coyago-Cruz
    ;
    ;
    Gabriela Méndez
    ;
    Mateo Moya Coyago
    ;
    Juan A. Puente Pineda
    Gleichenella pectinata, known as ‘Star fern’, is a species traditionally used by Amazonian indigenous communities to treat various diseases. The objective of this study was to evaluate the bioactive compounds and antioxidant, antimicrobial, antitumor, and anti-inflammatory activities of G. pectinata leaves. The study included the determination of physicochemical parameters (pH, soluble solids, titratable acidity, moisture, and ash), phytochemical screening, mineral analysis by atomic absorption and quantification of bioactive compounds (vitamin C, organic acids, carotenoids, chlorophylls, and phenols) by liquid chromatography (RRLC). Antioxidant (ABTS and DPPH), antimicrobial (ATCC bacteria and fungi, and multi-resistant strains), antitumor and anti-inflammatory activities were evaluated. The results showed the presence of acetogenins, high concentrations of malic acid (56,559.7 mg/100 g DW), β-carotene (266.6 mg/100 g DW), chlorophyll b (684.7 mg/100 g DW), ferulic acid (3163.5 mg/100 g DW) and quercetin glucoside (945.9 mg/100 g DW). The freeze-dried ethanolic extracts showed greater efficacy against Pseudomonas aeruginosa ATCC (12.0 mg/mL) and multidrug-resistant strains of E. coli (6.6 mg/mL) and P. aeruginosa (6.6 mg/mL). In addition, the extract exhibited moderate antiproliferative activity (IC50: 0.98–1.98 mg/mL) in hepatocellular and cervical carcinoma cell lines. In conclusion, this study provides the first evidence of the antitumor and bioactive potential of G. pectinata, supporting its value as a natural source of functional compounds with potential pharmacological applications.
    Scopus© Citations 2