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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
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GONZALEZ PASTOR, REBECA EUGENIA
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Saskya E. Carrera Pacheco
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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
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Saskya E. Carrera-Pacheco
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GONZALEZ PASTOR, REBECA EUGENIA
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MAYORGA RAMOS, ARIANNA CAROLINA
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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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Graphene Quantum Dots from Natural Carbon Sources for Drug and Gene Delivery in Cancer Treatment
(MDPI AG, 2024-09-30)
Henrry M. Osorio
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Fabián Castillo-Solís
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Selena Y. Barragán
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Cristina Rodríguez-Pólit
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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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X-STR decaplex study in the population of Imbabura-Ecuador
(Elsevier BV, 2019-12)
ZAMBRANO ESPINOSA, ANA KARINA
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Michelle Vaca-Pólit
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Lissett Boada
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Margarita Vela
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Cristina Rodríguez-Pólit
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Genetic polymorphisms of 12 X-STRs in the Ecuadorian population
(Elsevier BV, 2019-12)
Aníbal Gaviria
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Lissett Boada
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Cristina Rodríguez-Pólit
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Margarita Vela
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Gisella Fiallos
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Genetic characterization of 12 STRs (Investigator® HDplex kit) in the Ecuadorian population
(Elsevier BV, 2019-12)
Aníbal Gaviria
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Gisella Fiallos
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Cristina Rodríguez-Pólit
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Lissett Boada
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Margarita Vela
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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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GONZALEZ PASTOR, REBECA EUGENIA
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Cristina Rodríguez-Pólit
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HEREDIA MOYA, JORGE HUMBERTO
<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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Current Landscape of Methods to Evaluate Antimicrobial Activity of Natural Extracts
(MDPI AG, 2023-01-20)
GONZALEZ PASTOR, REBECA EUGENIA
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Saskya E. Carrera-Pacheco
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ZUÑIGA MIRANDA, JOHANA JANINA
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Cristina Rodríguez-Pólit
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MAYORGA RAMOS, ARIANNA CAROLINA
<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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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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GONZALEZ PASTOR, REBECA EUGENIA
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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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GONZALEZ PASTOR, REBECA EUGENIA
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Roberto Vallejo-Imbaquingo
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Carlos Barba-Ostria
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HEREDIA MOYA, JORGE HUMBERTO
<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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