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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)
ZUÑIGA MIRANDA, JOHANA JANINA
;
GONZALEZ PASTOR, REBECA EUGENIA
;
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.
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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)
ZUÑIGA MIRANDA, JOHANA JANINA
;
Saskya E. Carrera-Pacheco
;
GONZALEZ PASTOR, REBECA EUGENIA
;
MAYORGA RAMOS, ARIANNA CAROLINA
;
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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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
;
Selena Y. Barragán
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Cristina Rodríguez-Pólit
;
GONZALEZ PASTOR, REBECA EUGENIA
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.

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