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    Graphene Quantum Dots from Natural Carbon Sources for Drug and Gene Delivery in Cancer Treatment
    (MDPI AG, 2024-09-30)
    Henrry M. Osorio
    ;
    Fabián Castillo-Solís
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    Selena Y. Barragán
    ;
    Cristina Rodríguez-Pólit
    ;
    Cancer therapy is constantly evolving, with a growing emphasis on targeted and efficient treatment options. In this context, graphene quantum dots (GQDs) have emerged as promising agents for precise drug and gene delivery due to their unique attributes, such as high surface area, photoluminescence, up-conversion photoluminescence, and biocompatibility. GQDs can damage cancer cells and exhibit intrinsic photothermal conversion and singlet oxygen generation efficiency under specific light irradiation, enhancing their effectiveness. They serve as direct therapeutic agents and versatile drug delivery platforms capable of being easily functionalized with various targeting molecules and therapeutic agents. However, challenges such as achieving uniform size and morphology, precise bandgap engineering, and scalability, along with minimizing cytotoxicity and the environmental impact of their production, must be addressed. Additionally, there is a need for a more comprehensive understanding of cellular mechanisms and drug release processes, as well as improved purification methods. Integrating GQDs into existing drug delivery systems enhances the efficacy of traditional treatments, offering more efficient and less invasive options for cancer patients. This review highlights the transformative potential of GQDs in cancer therapy while acknowledging the challenges that researchers must overcome for broader application.
    Scopus© Citations 36
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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
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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
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    ;
    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 139
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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
    ;
    ; ;
    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.
    Scopus© Citations 12
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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 49
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    Phytochemical nanoencapsulation and microfluidics drive gene and tumor microenvironment modulation
    (Frontiers Media SA, 2025-09-29) ;
    Criollo, Mishell
    ;
    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.
    Scopus© Citations 9
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    Complexing the Oncolytic Adenoviruses Ad∆∆ and Ad-3∆-A20T with Cationic Nanoparticles Enhances Viral Infection and Spread in Prostate and Pancreatic Cancer Models
    (MDPI AG, 2022-08-10)
    Yang Kee Stella Man
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    Carmen Aguirre-Hernandez
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    Adrian Fernandez
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    Pilar Martin-Duque
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    <jats:p>Oncolytic adenoviruses (OAd) can be employed to efficiently eliminate cancer cells through multiple mechanisms of action including cell lysis and immune activation. Our OAds, AdΔΔ and Ad-3∆-A20T, selectively infect, replicate in, and kill adenocarcinoma cells with the added benefit of re-sensitising drug-resistant cells in preclinical models. Further modifications are required to enable systemic delivery in patients due to the rapid hepatic elimination and neutralisation by blood factors and antibodies. Here, we show data that support the use of coating OAds with gold nanoparticles (AuNPs) as a possible new method of virus modification to help augment tumour uptake. The pre-incubation of cationic AuNPs with AdΔΔ, Ad-3∆-A20T and wild type adenovirus (Ad5wt) was performed prior to infection of prostate/pancreatic cancer cell lines (22Rv, PC3, Panc04.03, PT45) and a pancreatic stellate cell line (PS1). Levels of viral infection, replication and cell viability were quantified 24–72 h post-infection in the presence and absence of AuNPs. Viral spread was assessed in organotypic cultures. The presence of AuNPs significantly increased the uptake of Ad∆∆, Ad-3∆-A20T and Ad5wt in all the cell lines tested (ranging from 1.5-fold to 40-fold), compared to virus alone, with the greatest uptake observed in PS1, a usually adenovirus-resistant cell line. Pre-coating the AdΔΔ and Ad-3∆-A20T with AuNPs also increased viral replication, leading to enhanced cell killing, with maximal effect in the most virus-insensitive cells (from 1.4-fold to 5-fold). To conclude, the electrostatic association of virus with cationic agents provides a new avenue to increase the dose in tumour lesions and potentially protect the virus from detrimental blood factor binding. Such an approach warrants further investigation for clinical translation.</jats:p>
    Scopus© Citations 15
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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
    ;
    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.
    Scopus© Citations 2
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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
    Scopus© Citations 25
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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
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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>
    Scopus© Citations 5