The usefulness of traditional plants in Mexico to treat human ailments has been known since ancient times. This work evaluated the antimicrobial, anticoagulant, antioxidant, cytotoxic, and anti-inflammatory potential of ethanolic extracts of Aloe vera, Equisetum arvense, Mimosa tenuiflora, Lippia graveolens, and Syzygium aromaticum. The antimicrobial activity of the extracts was evaluated against Streptococcus mutans and Streptococcus sorbinus; a significant inhibitory effect of the L. graveolens extract on both bacteria was observed at concentration levels of 250 µg/mL and greater. The anticoagulant activity was evaluated in terms of prothrombin time (PT) and activated partial thromboplastin time (APTT), A. vera and M. tenuiflora extracts showed no significant difference (p ˂ 0.05) in PT compared with the control, and for APTT the extracts of A. vera, L. graveolens, and S. aromaticum decreased the APTT significantly (p ˂ 0.05) compared with the control. The antioxidant potential by DPPH assay indicated that the E. arvense extract behaved statistically the same as the control. The cytotoxic activity was evaluated in HGF-1 cells using the fluorometric microculture cytotoxicity assay technique, and none of the extracts was toxic at 125 and 250 µg/mL concentrations. Finally, the anti-inflammatory activity was evaluated using ELISA, where the A. vera extract showed the best anti-inflammatory capacity. Further research on the search for bioactive metabolites and elucidation of action mechanisms of the most promising extracts will be carried out.

Introducción: El uso indiscriminado de agentes antiparasitarios ha resultado en el establecimiento de resistencia a ellos. Por lo cual es necesario el desarrollo de nuevas alternativas de tratamiento. Los productos naturales poseen diversas cualidades como posibles coadyuvantes en terapias contra distintos agentes etiológicos, entre los que destaca sus efectos antiparasitarios. Objetivo: Evaluar la actividad antiparasitaria, antioxidante, citotóxica y citoprotectora de Berberina (Ber), Curcumina (Cur) y Quercetina (Qr). Metodología: Se prepararon soluciones de Ber, Cur y Qr grado analítico y se realizaron alícuotas a diferentes concentraciones para su evaluación en contra de: Entamoeba histolytica, Trichomonas vaginalis y Strongyloides venezuelensis, para ello, se determinó la concentración inhibitoria media (IC50), además se determinó la capacidad antioxidante (CE50) mediante la prueba de DPPH, ambos por la prueba de Probit. Mediante la técnica de hemólisis se determinó la actividad citotóxica y citoprotectora, se aplicó Anova y la prueba de Tukey para determinar la diferencia de las medias en los tratamientos evaluados. Resultados: Ber, Cur y Qr, presentaron actividad en contra de E. histolytica, T. vaginalis y S. venezuelensis in-vitro. Ber presentó IC50 de 1.7, 1.2 y 1.9 μM respectivamente siendo más efectivo en comparación de Cur con IC50 de 55.3, 40.6 y 13.7 μM o Qr con IC50 de 147.2, 93.2 y 110.9 μM, sin embargo, la mejor actividad antioxidante (EC50 = 1.1 μg/ml), citoprotectora y menos hemolítica, fue presentada por Qr (P < 0.001) en comparación con el control evaluado. Conclusiones: Los metabolitos de origen natural berberina, curcumina y quercetina, poseen actividad en contra de trofozoítos de E. histolytica, T. vaginalis y larvas de S. venezuelensis en dosis bajas comparables con los fármacos de referencia para el caso de Ber. Además, estos productos de origen natural, no sintético podrían ser objeto de futuras investigaciones para coadyuvar al tratamiento de parasitosis, ya que, en dosis bajas, mostraron actividad antioxidante sin mostrar hemólisis considerable en eritrocitos humanos.

One primary drawback of enzyme catalysis at industrial scale is the short-term service life of the enzymes, they lose their activity due to oxidation or other processes which results in less stability and a shorter lifetime thereby rendering them less efficient. An effective way to increase the stability of the enzymes is to attach them to nanoparticles. In this work, the polymer Eudragit^® L 100-55 sensitive to pH was used to prepare laccase polymeric nanoparticles by the double-emulsion solvent evaporation approach. The size and morphology of the nanoparticles obtained were evaluated—as well as the encapsulation efficiency and zeta potential. pH effect on activity and stability was compared between free and immobilized laccase. Their stability was also determined in a sequential assay involving acidic pHs up to alkaline ones. The nanoparticles had a spherical shape with a mean size of 147 nm, zeta potential of −22.7 mV at pH 7.0 and load efficiency of 87%. The optimum pH of both free and immobilized laccases was 3.0, being the nanoparticles more stable at acidic pHs. Thus, this would be the first report of obtaining laccase nanoparticles with potential application in animal feed due to the stability conferred to enzymatic activity at pHs similar to those present in the gastrointestinal tract of rabbits, which would allow their potential use in animal feed.

Eudragit^® polymers have proven their potential as a means to control the release of aqueous insoluble drugs in various delivery systems as polymer nanoparticles (PNPs). The size (S) and polydispersity index (PDI) of PNPs are crucial factors for their interaction with biological systems from a pharmaceutical standpoint. This study aimed to determine the impact of the volumes of the organic phase (OP) and aqueous phase (AP), as well as the polymer amount (PA), on the size and PDI of PNPs prepared using the nanoprecipitation method for encapsulating quercetin (Qr). The study also evaluated the toxic effects of PNPs on human erythrocytes. The PNPs were prepared using preformed polymers derived from methacrylic acid and polyvinyl alcohol (PVA) as a surfactant. The nanoprecipitation technique enabled the production of particles smaller than 200 nm with a PDI lower than 0.2, and the study established the significant impact (p < 0.05) of the three variables related to the polymers and solvents. The selected PNPs contained 5 mg of Qr and 50 mg of Eudragit polymers (1:10 w/w Eudragit^® EPO, E100, L100, and Eudragit L100-55) and diverse concentrations of PVA. The study found that including PVA in the AP increased the Qr encapsulation by up to 98%. The hemolytic potential of Eudragit^® PNPs and Qr was assessed in human erythrocytes, with no significant cytotoxic activity observed (p < 0.001) compared with the control. In conclusion, via the nanoprecipitation technique, preparing PNPs with defined and homogeneous S to entrap the flavonol Qr efficiently is possible.

Introduction: In tropical and developing countries, pathogenic protozoa are a major public health problem. Objective: The main objective of this study was the evaluation of ethanol extracts of Curcuma longa and Berberis vulgaris, as well as their main components curcumin (Cur) and berberine (Ber) in non-encapsulated form and encapsulated into polymeric nanoparticles (NPs) on Entamoeba histolytica and Trichomonas vaginalis trophozoites as well as to evaluate the hemolytic activity. Additionally, we studied the morphology of the NPs, average particle size, polydispersity index (PDI), and encapsulation percentages (%EE) of the formulations. Methods: For this purpose, the activity of the encapsulated and non-encapsulated treatments against E. histolytica and T. vaginalis was evaluated by the microassay technique (in-vitro). In addition, the cytotoxic capacity was determined by the hemolysis technique in healthy erythrocytes. The size and morphology of the NPs were determined by photon correlation spectroscopy and scanning electron microscopy (SEM). Results: Phytochemical analysis of the extracts showed that C. longa had mainly tannins, phenols and flavonoids, and B. vulgaris alkaloids. The NPs were significantly (P < 0.001) more effective compared to their non-encapsulated counterparts, but CurNPs and BerNPs were the most efficient treatments. CurNPs showed IC50 values (μg/mL) of 9.48 and 4.25, against E. histolytica and T. vaginalis respectively, and BerNPs 0.24 and 0.71. The respective particle sizes and encapsulation percentages for CurNPs and BerNPs were 66.5 and 73.4 nm, 83.59 and 76.48 %, respectively. SEM shows that NPs had a spherical morphology. Finally, we analyzed whether ethanolic extracts and NPs induced hemolytic activity and found that significantly NPs reduced hemolysis compared to the non-encapsulated extracts. Conclusions: Therefore, these findings suggest that the use of NPs represent a valuable and novel source of administration of bioactive compounds for the therapeutic treatment of diseases caused by protozoa of clinical interest since they potentiate the amebicidal and trichomonicidal activity of the administered products without significant hemolytic activity. Introducción: En los países tropicales y en desarrollo, los protozoos patógenos constituyen un importante problema de salud pública. Objetivo: El objetivo principal de este estudio fue la evaluación de los extractos etanólicos de Curcuma longa y Berberis vulgaris, y de sus componentes principales curcumina (Cur) y berberina (Ber) en forma no encapsulada y encapsulada en nanopartículas poliméricas (NPs) sobre los trofozoítos de Entamoeba histolytica y Trichomonas vaginalis, así como evaluar la actividad hemolítica. Además, se estudió la morfología de las NPs, el tamaño medio de las partículas, el índice de polidispersidad (PDI) y los porcentajes de encapsulación (%EE) de las formulaciones. Métodos: Para ello, se evaluó la actividad de los tratamientos encapsulados y no encapsulados frente a E. histolytica y T. vaginalis, mediante la técnica del microensayo (in-vitro). Además, se determinó la capacidad citotóxica mediante la técnica de hemólisis en eritrocitos sanos. El tamaño y la morfología de las NPs se determinó mediante espectroscopia de correlación fotónica y mediante microscopia electrónica de barrido (SEM). Resultados: El análisis fitoquímico de los extractos mostró que C. longa tenía principalmente taninos, fenoles y flavonoides, y B. vulgaris alcaloides. Las NPs fueron significativamente (P < 0.001) más eficaces en comparación con sus homólogas no encapsuladas, sin embargo, CurNPs y las BerNPs fueron los tratamientos más eficaces. CurNPs mostró valores de IC50 (μg/mL) de 9.48 y 4.25, contra E. histolytica y T. vaginalis respectivamente, y las BerNPs 0.24 y 0.71. Los tamaños de partícula respectivos y porcentajes de encapsulación para las CurNPs y BerNPs fueron de 66.5 y 73.4 nm, y de 83.59 y 76.48 %, respectivamente. La SEM muestra que las NPs tenían una morfología esférica. Finalmente, se analizó si los extractos etanólicos y las NPs inducían actividad hemolítica y encontramos que significativamente las NPs reducían la hemólisis en comparación con los extractos no encapsulados. Conclusiones: Estos hallazgos sugieren que el uso de las NPs representa una valiosa y novedosa fuente de administración de compuestos bioactivos para el tratamiento terapéutico de enfermedades causadas por protozoos de interés clínico ya que potencian la actividad amebicida y tricomonicida de los productos administrados sin actividad hemolítica significativa.