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    Relationship Between Bioactive Compounds and Biological Activities (Antioxidant, Antimicrobial, Antihaemolytic) of ‘Colcas’ Fruits at Different Stages of Maturity
    (MDPI AG, 2025-09-10)
    Elena Coyago-Cruz
    ;
    ;
    Gabriela Méndez
    ;
    Aida Guachamin
    ;
    Ruth Escobar-Quiñonez
    The genus Miconia is used in traditional medicine, but there are few studies supporting the bioactive potential of Miconia crocea. This study aimed to evaluate the physicochemical properties, bioactive compound content, and antioxidant, antimicrobial and antihaemolytic activities at four different phenological stages of M. crocea. The pH, soluble solids, titratable acidity, moisture and ash content were determined. Mineral contents were determined by atomic absorption. Vitamin C, organic acids, carotenoids, chlorophylls and derivatives and phenols were determined by chromatography. Total anthocyanins were determined by spectrophotometry. The antioxidant capacity was evaluated using ABTS and DPPH assays, and the antimicrobial activity was tested against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus mutans, Candida albicans and Candida tropicalis. Potassium was the predominant mineral (>1000 mg/100 g DW), while malic acid was the predominant organic acid. Lutein was the most abundant carotenoid, as among the phenolic compounds, m-coumaric acid and chlorogenic acid were most abundant (>1000 mg/100 g DW). The optimal method for preparing the extract for antimicrobial and haemolytic activity, with a focus on phenols, involved using 50% ethanol, applying ultrasound for six minutes, and carrying out three extractions. The M0% extract exhibited the most potent antimicrobial activity against S. mutans (MIC: 7.8 mg/mL). Anti-haemolytic activity indicates biocompatibility. The results emphasise the bioactive and antimicrobial potential of M. crocea, suggesting its possible application in various industries. However, further research is needed in the form of in vivo studies.
    Scopus© Citations 6
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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
    ;
    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
    ;
    ;
    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
    ;
    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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    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
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    Scopus© Citations 3
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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
    ;
    ;
    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