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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
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    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.
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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
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    Carlos Cevallos-Morillo
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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>
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    Phytosynthesis of Silver Nanoparticles Using Mansoa alliacea (Lam.) A.H. Gentry (Bignoniaceae) Leaf Extract: Characterization and Their Biological Activities
    (MDPI AG, 2024-09-25) ;
    Saskya E. Carrera-Pacheco
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    ; ;
    Cristina Rodríguez-Pólit
    Background. Mansoa alliacea is a native plant renowned for its medicinal properties in traditional healing in the Amazon Region. This plant is rich in polyphenols, flavonoids, anthocyanins, phenolic acids, tannins, ketones, triterpenes, as well as other bioactive compounds. Objectives. This study aims to develop an innovative, eco-friendly method for synthesizing silver nanoparticles using an aqueous extract of M. alliacea (Ma-AgNPs), enhancing the biological activities of AgNPs by leveraging the therapeutic potential of the plant’s bioactive compounds. Methods. Silver nanoparticles were synthesized using the aqueous extract of M. alliacea. The biological activities of Ma-AgNPs were assessed, including antibacterial, anti-inflammatory, antioxidant, antitumor, and anti-biofilm effects, along with evaluating their hemolytic activity. Results. Quantitative analysis revealed that Ma-AgNPs exhibit potent antibacterial activity against multidrug and non-multidrug-resistant bacteria, with MIC values ranging from 1.3 to 10.0 µg/mL. The Ma-AgNPs significantly reduced NO production by 86.9% at 4 µg/mL, indicating strong anti-inflammatory effects. They demonstrated robust antioxidant activity with an IC50 of 5.54 ± 1.48 µg/mL and minimal hemolytic activity, with no hemolysis observed up to 20 µg/mL and only 4.5% at 40 µg/mL. Their antitumor properties were notable, with IC50 values between 2.9 and 5.4 µg/mL across various cell lines, and they achieved over 50% biofilm inhibition at concentrations of 30–40 µg/mL. Conclusions. These findings underscore the potential of Ma-AgNPs for biomedical applications, particularly in developing new antimicrobial agents and bioactive coatings with reduced toxicity. This research highlights a sustainable approach that not only preserves but also amplifies the inherent biological activities of plant extracts, paving the way for innovative therapeutic solutions.
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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
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    Orestes López
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    Alexis Debut
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    ;
    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>
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    Phytochemical nanoencapsulation and microfluidics drive gene and tumor microenvironment modulation
    (Frontiers Media SA, 2025-09-29) ;
    Criollo, Mishell
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    Phytochemicals are plant-derived bioactive compounds with promising anticancer properties, but their clinical use is limited by poor solubility, instability, rapid metabolism, and restricted tumor penetration. Nanoencapsulation strategies address these barriers by enhancing bioavailability, stability, and tissue-specific delivery, thereby improving therapeutic efficacy and reducing systemic toxicity. This mini-review summarizes recent progress in nanoscale phytochemical delivery systems engineered for gene modulation and tumor microenvironment targeting, including lipid-based, polymeric, hybrid, and biogenic nanocarriers that improve biodistribution and enhance cellular uptake. Notably, the functional performance of nanoscale delivery systems depends on precisely controlled physicochemical characteristics. Consequently, microfluidics has emerged as a powerful tool to fine-tune and fabricate phytochemical-based nanocarriers in a reproducible manner. Beyond fabrication, microfluidic lab-on-a-chip platforms recreate physiological and tumor-specific microenvironments, providing dynamic, real-time assessment of drug transport, metabolism, and tumor–vascular interactions in biomimetic conditions that surpass conventional static models. These innovations expand mechanistic understanding and support more predictive preclinical evaluations. Remaining challenges include variability of natural sources, limited pharmacokinetic and toxicological data, and hurdles in scale-up and standardization. By integrating nanoscale engineering with microfluidic innovation, phytochemical-based nanomedicine is positioned to advance toward more effective, safer, and clinically translatable cancer therapies.
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    Current Landscape of Methods to Evaluate Antimicrobial Activity of Natural Extracts
    (MDPI AG, 2023-01-20) ;
    Saskya E. Carrera-Pacheco
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    ;
    Cristina Rodríguez-Pólit
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    <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>
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    Evaluation of Biological Activity of Natural Compounds: Current Trends and Methods
    (MDPI AG, 2022-07-13)
    Carlos Barba-Ostria
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    Saskya E. Carrera-Pacheco
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    Cristina Rodríguez-Pólit
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    <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>
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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
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    Cristina Rodríguez-Pólit
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    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.
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    Dimerocostus strobilaceus (Caña Agria) as an Emerging Reservoir of Bioactive Metabolites with Potential Antioxidant, Antimicrobial, Anticancer and Anti-Inflammatory Health Benefits
    (MDPI AG, 2025-10-29)
    Coyago Cruz Elena Del Rocío
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    Gabriela Méndez
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    Jeico Usinia-Carranza
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    The Amazon region is home to a wide variety of plant species that are of interest for their medicinal and nutritional properties. This study aimed to evaluate the physicochemical properties, bioactive compound profile, and antioxidant, antimicrobial, anticancer and anti-inflammatory activity of Dimerocostus strobilaceus leaves, stems, and seeds. Vitamin C, organic acids, carotenoids, and phenolic compounds were quantified using RPLC. Antioxidant activity was determined using ABTS and DPPH, while antimicrobial activity was assessed against pathogenic and multidrug-resistant bacteria. Anticancer activity was evaluated in tumour cell lines (HeLa, HCT116, HepG2, and THJ29T), and anti-inflammatory activity was examined in RAW 264.7 macrophages. The seeds stood out for their content of ferulic, caffeic and chlorogenic acids, while kaempferol and quercetin predominated in the leaves. The leaves exhibited greater antimicrobial efficacy and antiproliferative activity (IC50 &lt; 0.2 mg/mL), albeit with limited selectivity. These findings suggest that ‘caña agria’ is a promising source of bioactive metabolites with biotechnological and therapeutic applications.