In this study, we report the synthesis of acridone derivatives and their potential as photosystem II (PSII) inhibitors, as well as their preand post-emergence herbicidal activities through chlorophyll a fluorescence and germination assays. Among the compounds tested for PSII activity, acridin-9(10H)-one showed the most promising results, reducing the performance index on an absorption basis and decreasing the quantum yield for electron transport compared to the control. These findings suggest an inhibitory effect on PSII within the electron transport chain. Additionally, 2-chloroacridin-9(10H)-one and 9(10H)-acridone-4-carboxylic acid exhibited post-emergence herbicidal activity against Amaranthus lividus and Amaranthus viridis weeds, respectively, leading to a reduction in radicle and hypocotyl lengths. Furthermore, we applied a molecular docking approach with the D1 protein and 4-hydroxyphenylpyruvate dioxygenase to investigate the structure-activity relationships among the acridone derivatives with these enzymes. The analysis highlighted the importance of the carbonyl group and aromatic substituents on the acridone scaffold facilitating ligand interactions, especially through hydrogen bonding. Consequently, our research group aims to optimize these molecular features to develop new, potent bioactive molecular scaffolds.

The spread of antibiotic-resistant pathogens had motivated the search for plant-derived antimicrobial agents, such as essential oils. This work investigated the antibacterial, antifungal and antibiofilm properties of the essential oil from the inflorescence of Etlingera elatior and its major compounds. Dodecanal (42.46%) and 1-dodecanol (25.84%) were the major compounds. The oil, dodecanal and 1-dodecanol were active against Staphylococcus aureus, with minimum bactericidal concentrations of 124, 31 and 62 µg mL-1, respectively. For Pseudomonas aeruginosa, the essential oil had an inhibitory effect against a multidrug resistant isolate (minimum inhibitory concentration (MIC): 4,000 µg mL-1). Dodecanal had an MIC of 60,000 µg mL-1 for all Candida species, but fungicidal activity was only detected for Candida albicans (minimum fungicidal concentration: 60,000 µg mL-1). 1-Dodecanol (60,000 µg mL-1) exhibited fungistatic activity for C. albicans. Biofilm inhibition linked to an anti-adhesive effect of the oil and dodecanal was only detected for the standard S. aureus isolate and C. albicans, respectively. In conclusion, the essential oil from the inflorescence of E. elatior and its major components were more active against nonresistant strains S. aureus. Essential oil, dodecanol and dodecanal showed excellent activity against S. aureus, however, these same materials showed low activity against P. aeruginosa.

In this study, we aimed to investigate the anticancer activity of the extract, fractions, and isolated compounds of the flowers of Fridericia platyphylla, and to characterize the bioactive compounds. The chemical diversity of the extracts and fractions was investigated using liquid chromatography coupled with high resolution mass spectrometry (LC-HRMS). We were able to annotate 26 compounds from the classes of flavones, flavonols, flavanones, isoflavones, and cinnamic acid and its derivatives. The dichloromethane fraction showed greater cytotoxicity at a concentration of 100 µg mL−1. In addition, the inhibitory concentrations of the dichloromethane fraction were 22.14 and 30.9 µg mL−1 for MCF-7 and MDA-MB-231 cell lines, respectively, and were capable of inhibiting tumor cell migration. Brachydins A and C were isolated from the dichloromethane fraction and showed the greatest cytotoxicity. The results obtained from this study show the potential biological effect of F. platyphylla flowers as a possible antitumor pharmacological agent. extract LCHRMS. LCHRMS LC HRMS . (LC-HRMS) 2 flavones flavonols flavanones isoflavones derivatives 10 mL1 mL 1 addition 2214 22 14 22.1 309 30 9 30. mL− MCF7 MCF 7 MCF- MDAMB231 MDAMB MDA MB 231 MDA-MB-23 lines respectively migration F agent (LC-HRMS 221 22. 3 MDAMB23 23 MDA-MB-2 MDAMB2 MDA-MB- MDA-MB

RESUMO: Em geral, alelopatia pode ser definido como o processo biológico no qual um organismo produz metabolitos que alteram a germinação, o crescimento, a sobrevivência e a reprodução de outros organismos, influenciando a estabilidade de agroecossistemas. O colesterol, o mais abundante esterol isolado da alga vermelha marinha Plocamium brasiliense, foi estudado quanto ao seu potencial efeito inibitório na germinação de sementes, alongamento das radículas e desenvolvimento do hipocótilo das ervas daninhas Mimosa pudica (malicia) e Senna obtusifolia (mata-pasto). Colesterol foi isolado do extrato em Hexano por métodos cromatográficos. Durante 15 dias, os bioensaios de germinação foram realizados a 25 ºC e fotoperíodo de 12 horas, enquanto os bioensaio de alongamento da radícula e do hipocótilo foram realizados a 25 ºC e fotoperíodo de 24 horas. Posteriormente, placas de Petri de 9,0 cm de diâmetro foram revestidas de papelfiltro, e 25 sementes foram mantidas em câmaras de germinação, enquanto seis sementes pré-germinadas foram postas em placas de Petri por 2-3 dias. Após dez dias, a extensão da radícula e do hipocótilo foi medida. O potencial inibitório do colesterol foi avaliado a 5, 10, 15 e 20 ppm. Em ambas as ervas M. pudica e S. obtusifolia, foram afetadas significativamente pela ação do cholesterol alcançando maiores percentuais de inibição na germinação das sementes (50% e 33%, respectivamente), alongamento da radícula (68% e 60%, respectivamente) e desenvolvimento do hipocótilo (66% e 55%, respectivamente). Os efeitos inibitórios foram dose-dependentes em todos os experimentos, tendo efeitos alelopaticos mais acentuados a 20 ppm. RESUMO geral crescimento organismos agroecossistemas brasiliense malicia (malicia matapasto. matapasto mata pasto . (mata-pasto) cromatográficos 1 dias 2 horas Posteriormente 90 9 0 9, papelfiltro prégerminadas pré germinadas 23 3 2- medida 5 10 ppm M S 50% 50 (50 33 33% respectivamente, respectivamente , 68% 68 (68 60 60% 66% 66 (66 55 55% respectivamente. dosedependentes dose dependentes experimentos (mata-pasto (5 6 (6 (

ABSTRACT: In general, allelopathy can be defined as a biological process by which an organism produces one or more metabolites that can change the germination, growth, survival, and reproduction of other organisms, and thus influencing the stability of agroecosystems. Cholesterol is a very abundant sterol isolated from the marine red alga Plocamium brasiliense that has been studied regarding its potential inhibitory effects on seed germination, radicle elongation, and hypocotyl development of the weeds Mimosa pudica (malicia) and Senna obtusifolia (mata-pasto). Cholesterol was isolated from a hexane extract by chromatographic methods. Over a 15-day period, germination bioassays were performed at 25 ºC with a 12-h photoperiod. Radicle elongation and hypocotyl development were assayed at 25 ºC with a 24-h photoperiod. Later, Petri dishes 9.0 cm in diameter were coated with filter paper, and 25 seeds were placed in a germination chamber. Six pre-germinated seeds were placed in the Petri dish for 2-3 days. After 10 days, radicle and hypocotyl extensions were measured, and the inhibitory potential of cholesterol was assessed at 5, 10, 15, and 20 ppm. In both herbs, M. pudica and S. obtusifolia, they were significantly affected by the action of cholesterol, achieving higher percentages of inhibition in seed germination (50% and 33%, respectively), radical germination (68% and 60%, respectively), and hypocotyl development (66% and 55%, respectively). The inhibition effects were dose-dependent in all experiments, having more pronounced allelopathic effects at 20ppm. ABSTRACT general growth survival organisms agroecosystems malicia (malicia matapasto. matapasto mata pasto . (mata-pasto) methods 15day day 15 period 2 12h h 12 photoperiod 24h 24 Later 90 9 0 9. paper chamber pregerminated pre germinated 23 3 2- days 1 measured 5 ppm herbs M S 50% 50 (50 33 33% respectively, respectively , respectively) 68% 68 (68 60 60% 66% 66 (66 55 55% respectively. dosedependent dose dependent experiments 20ppm (mata-pasto (5 6 (6 (

Paratuberculosis (Johne's disease) has devastating outcomes on ruminant health and impacts on national and international trade. The current work assessed the diagnostic value of the VersaTREK automated liquid culture system in isolating Mycobacterium avium subspecies paratuberculosis (MAP) from faecal and intestinal tissue samples from ovine under South African conditions and compared it with the current method of choice, histopathological examination. Intestinal tissue and faecal samples from 111 sheep (including complete set from 104 slaughter sheep from flocks with a history of MAP infection as well as incomplete sample sets from 7 sheep) were analysed using the liquid culture method. One set of tissues was subjected to histopathological examination. Deoxyribonucleic acid (DNA) extracted from culture isolates was subjected to polymerase chain reaction (PCR) amplification using primers that target the IS900 regions of the MAP for species verification. Overall, the VersaTREK automated liquid culture in combination with IS900 PCR showed a comparable level of detection in tissues (12.6%) as histopathology (13.5%), but the detection rate for faecal samples was lower than for tissues (10.8%). A combination of histopathology and faecal culture increased the detection rate from 13.5% (n = 14/104) and 9.6% (n = 10/104), respectively, to 15.4% (n = 16/104). CONTRIBUTION: Our findings highlight the diagnostic utility of the VersaTREK automated liquid culture system in detecting MAP in ovine samples collected both ante and postmortem. However, an inhibitory effect on the MAP isolation rate observed when the antibiotic cocktail was added to the culture medium warrants further investigation. The outcome of the study is beneficial in guiding the strategic planning of the nationwide control programme.

Resumen (Objetivo) El objetivo de este estudio fue evaluar la eficiencia antimicrobiana del aceite esencial de diversos quimiotipos de Lippia graveolens contra la cepa Aeromonas hydrophila resistente a la oxitetraciclina, la cual afecta principalmente a la acuicultura de tilapia (O. niloticus) en Guatemala. (Metodología) L. graveolens se colectó en tres departamentos de Guatemala, los aceites esenciales (AE) se obtuvieron mediante hidrodestilación y se caracterizaron mediante cromatografía de gases y espectrometría de masas (GC/MS). Posteriormente, se realizó un ensayo antimicrobiano utilizando pruebas de susceptibilidad en disco y dilución, y se evaluaron las interacciones sinérgicas entre los diferentes quimiotipos. Cada prueba se repitió res veces. (Resultados) El análisis evidenció la presencia de veintisiete compuestos en los AE obtenidos de los quimiotipos, siendo los monoterpenos la clase principal. Los principales constituyentes identificados fueron cis-dihidro-β-terpineol (8.84 %) en el quimiotipo I, carvacrol (51.82 %) en el quimiotipo II y timol (79.62 %) en el quimiotipo III. Todos los AE de los diferentes quimiotipos de L. graveolens demostraron capacidad para inhibir el crecimiento de A. hydrophila. En particular, el quimiotipo timol obtuvo el efecto inhibitorio más fuerte contra el crecimiento bacteriano, con una concentración mínima inhibitoria (CMI) de 92.4 µg/mL y una concentración mínima bactericida (B) de 184.8 µg/mL. Los resultados sugieren que no existe un efecto sinérgico o aditivo al combinar los diferentes quimiotipos de L. graveolens. (Conclusiones) Este estudio constituye el primer reporte sobre la actividad antimicrobiana de los diferentes quimiotipos de L. graveolens contra A. hydrophila resistente a la oxitetraciclina. Los hallazgos sugieren que el quimiotipo timol podría ser un tratamiento potencial para las infecciones en la acuicultura de tilapia en Guatemala.

Resumo (Objetivo) O objetivo deste estudo foi avaliar a eficiência antimicrobiana do óleo essencial de vários quimiotipos de Lippia graveolens contra a cepa Aeromonas hydrophila resistente à oxitetraciclina, que afeta principalmente a aquicultura de tilápia (O. niloticus) na Guatemala. (Metodologia) A L. graveolens foi coletada em três setores da Guatemala, os óleos essenciais (OE) foram obtidos por hidrodestilação e caracterizados por cromatografia a gás acoplada à espectrometria de massas (GC/MS). Posteriormente, foi realizado um ensaio antimicrobianos por meio de testes de suscetibilidade de disco e diluição, e foram avaliadas as interações sinérgicas entre os diferentes quimiotipos. Cada teste foi repetido três vezes. (Resultados) A análise revelou a presença de vinte e sete compostos nos OEs obtidos dos quimiotipos, sendo os monoterpenos a classe principal. Os principais constituintes identificados foram cis-di-hidro-β- terpineol (8,84%) no quimiotipo I, carvacrol (51,82%) no quimiotipo II e timol (79,62%) no quimiotipo III. Todos os OEs dos diferentes quimiotipos de L. graveolens mostraram a capacidade de inibir o crescimento de A. hydrophila. Em particular, o quimiotipo timol obteve o efeito inibitório mais forte contra o crescimento bacteriano, com uma concentração inibitória mínima (CIM) de 92,4 μg/mL e uma concentração bactericida mínima (CBM) de 184,8 μg/mL. Os resultados sugerem que não há efeito sinérgico ou aditivo ao combinar os diferentes quimiotipos de L. graveolens. (Conclusões) Este estudo é o primeiro relatório sobre a atividade antimicrobiana dos diferentes quimiotipos de L. graveolens contra A. hydrophila resistente à oxitetraciclina. Os resultados sugerem que o quimiotipo timol pode ser um tratamento em potencial para infecções na aquicultura de tilápia na Guatemala.

Abstract (Objective) This study aimed to evaluate the antimicrobial efficacy of essential oil (EO) from diverse chemotypes of Lippia graveolens against oxytetracycline-resistant Aeromonas hydrophila, which primarily affects the tilapia aquaculture (O. niloticus) in Guatemala. (Methodology) L. graveolens were collected in three departments in Guatemala. The EO was obtained by hydrodistillation and characterized using gas chromatography and mass spectrometry (GC/MS). Subsequently, an antimicrobial assay was conducted using disk and dilution susceptibility tests and evaluation of synergistic interactions among the chemotypes. Each test was performed in triplicate. (Results) The analysis revealed the presence of twenty-seven compounds in the EO obtained from the chemotypes, with the main class being monoterpenes. The major constituents identified were cis-Dihydro-β-terpineol (8.84%) in chemotype I, carvacrol (51.82%) in chemotype II, and thymol (79.62%) in chemotype III. All EO chemotypes of L. graveolens demonstrated the ability to inhibit the A. hydrophila growth. Thymol chemotype exhibited the strongest inhibitory effect against bacterial growth, with a minimum inhibitory concentration (MIC) of 92.4 µg/mL and a minimum bactericidal concentration (MBC) of 184.8 µg/mL. Furthermore, the results suggest that there is no synergistic or additive effect when combining different chemotypes of L. graveolens. (Conclusions) This is the first report of L. graveolens chemotypes exhibiting antimicrobial activity against oxytetracycline-resistant A. hydrophila. The findings suggest that the chemotype thymol could be a potential treatment for infections in the tilapia aquaculture in Guatemala.

SUMMARY: Caloric restriction (CR) alongside its ability to increase longevity, exerts inhibitory effects against various tumors. The purpose of this current research was to investigate the conceivable implications of CR, either independently or in conjunction with a cyclooxygenase 2 inhibitor (Celecoxib), on the pathophysiology of induced hepatocellular carcinoma (HCC). Forty adult male Wistar rats were allocated into four groups: Control, HCC; induced by injecting diethylnitrosamine intraperitoneally, then subsequently given a weekly subcutaneous injection of carbon tetrachloride (CCl4) once a week for 6 consecutive weeks, CR group, and CR-Celecoxib group. The results revealed enhanced serum insulin growth factor-I (IGF-I) and- II (IGF-II) levels, along with a significant increase in COX-2 and IL-6 gene expression as well as acceleration of pathological changes, glycogen depletion, enhanced fibrosis, and decreased caspase 3 expression in the liver. However, both IGF-I, II, and alpha-fetoprotein (AFP) were significantly decreased in the CR group co-treated with Celecoxib which was positively reflected on the liver architecture. We concluded that combined CR and COX-2 inhibition interferes with the pathogenesis of HCC.

RESUMEN: La restricción calórica (RC), junto con su capacidad para aumentar la longevidad, ejerce efectos inhibidores contra varios tumores. El propósito de esta investigación actual fue investigar las posibles implicaciones de la RC, ya sea de forma independiente o junto con un inhibidor de la ciclooxigenasa 2 (Celecoxib), en la fisiopatología del carcinoma hepatocelular inducido (CHC). Cuarenta ratas Wistar macho adultas se dividieron en cuatro grupos: Control, CHC; inducido mediante inyección intraperitoneal de dietilnitrosamina, luego se le administró una inyección subcutánea semanal de tetracloruro de carbono (CCl4) una vez por semana durante 6 semanas consecutivas, grupo CR y grupo CR-Celecoxib. Los resultados revelaron niveles mejorados de factor de crecimiento insulínico sérico I (IGF-I) y II (IGF-II), junto con un aumento significativo en la expresión de los genes COX-2 e IL-6, así como aceleración de cambios patológicos, depleción de glucógeno, fibrosis mejorada y disminución de la expresión de caspasa 3 en el hígado. Sin embargo, tanto IGF-I, II como alfa-fetoproteína (AFP) disminuyeron significativamente en el grupo CR co-tratado con Celecoxib, lo que se reflejó positivamente en la arquitectura hepática. Concluimos que la inhibición combinada de CR y COX- 2 interfiere con la patogénesis del CHC.

Resumen Antecedentes: Las especies arbóreas pioneras que comúnmente dominan la sucesión secundaria temprana del bosque tropical caducifolio pueden afectar las posibles rutas sucesionales. Mimosa acantholoba var. eurycarpa es una especie muy dominante en el bosque tropical caducifolio de México. Hipótesis: Mimosa acantholoba var. eurycarpa ejerce un efecto inhibitorio sobre la germinación, establecimiento, supervivencia y crecimiento inicial de especies pioneras intolerantes a la sombra, pero facilita estos procesos para especies de bosque maduro tolerantes a la sombra. Especies de estudio: Lonchocarpus torresiorum, Lysiloma divaricatum, Mimosa acantholoba var. eurycarpa y Vachellia farnesiana Sitio y años de estudio: Nizanda, Oaxaca, México, 2020-2021. Métodos: En 12 parcelas de sucesión secundaria temprana, aplicamos tres niveles de remoción de copa de M. acantholoba. Las cuatro especies de estudio se sembraron y registramos su germinación, establecimiento, supervivencia y crecimiento inicial durante dos meses. Resultados: El tratamiento de remoción de la copa no afectó significativamente la germinación. Lysiloma divaricatum tuvo la mayor probabilidad de germinación, la germinación más rápida y la mayor probabilidad de establecimiento, independientemente del tratamiento. Lonchocarpus torresiorum tuvo la mayor probabilidad de establecimiento en las parcelas sin cobertura de copa de M. acantholoba. La probabilidad de supervivencia de ambas especies fue más alta donde M. acantholoba fue removida por completo. Conclusiones: La germinación de las especies tolerantes a la sombra fue exitosa pero su supervivencia se inhibió por el denso dosel de M. acantholoba. La reducción de las copas de M. acantholoba puede estimular la recuperación de áreas forestales.

Abstract Background: Individual pioneer tree species often dominate early tropical dry forest succession and thereby affect possible successional pathways. Mimosa acantholoba var. eurycarpa is a highly dominant species in the tropical dry forest in Mexico. Hypothesis: Mimosa acantholoba var. eurycarpa exerts an inhibitory effect on the germination, establishment, survival, and early growth of light-demanding pioneers, while facilitating these processes for shade-tolerant old-growth forests species. Studied species: Lonchocarpus torresiorum, Lysiloma divaricatum, Mimosa acantholoba var. eurycarpa and Vachellia farnesiana. Study site and dates: Nizanda, Oaxaca, Mexico, 2020-2021. Methods: In 12 early successional plots, we applied three levels of crown cover removal (100, 50, and 0 %) of established trees of the dominant pioneer legume (M. acantholoba var. eurycarpa). We sowed seeds of the four study species in each experimental plot and recorded their germination, establishment, survival, and early growth over a 2-mo period. Results: The removal of crown cover of established M. acantholoba var. eurycarpa trees did not significantly affect germination. Lysiloma divaricatum had the highest germination probability, the fastest germination, and the highest establishment probability regardless of treatment. Lonchocarpus torresiorum had the highest establishment probability in plots where the crown cover of established M. acantholoba var. eurycarpa trees was removed. The survival probability of both shade-tolerant species was highest in the 100 % removal treatment. Conclusions: Despite successful germination of shade-tolerant species, their survival is inhibited under the dense canopy of the dominant legume. Therefore, interventions to reduce the crown cover area of this dominant legume may stimulate forest recovery.

RESUMEN Las saponinas son ampliamente conocidas por sus propiedades biológicas, lo que ha llevado al desarrollo de diversas investigaciones aplicadas al sector agrícola. En ese sentido, el objetivo de este estudio fue evaluar el efecto antifúngico in vitro e in vivo de saponinas extraídas de la cascarilla de quinoa, utilizando el extracto crudo e incorporándolo en una formulación contra Botrytis cinerea en fresa. Se estudió la extracción de saponinas por el método de maceración, donde se evaluó el efecto de la temperatura, el tiempo y la concentración de etanol; el proceso se optimizó mediante un diseño central compuesto (DCC). El efecto antifúngico in vitro del extracto crudo de saponinas se evaluó mediante la concentración mínima inhibitoria (CMI), por su parte, el efecto antifúngico in vitro e in vivo de la formulación se determinó a través del porcentaje de inhibición micelial y el porcentaje de control, respectivamente. El punto óptimo de extracción de saponinas se obtuvo a 49,8 °C, 0,367 h y 47,4% de etanol. Por otro lado, la actividad antifúngica contra Botrytis cinerea fue dependiente de la concentración de saponinas; en la evaluación in vitro la CMI del extracto crudo fue de 8,25 mg mL-1 de saponinas y el porcentaje de inhibición micelial de la formulación fue superior al 90%. En la evaluación in vivo de la formulación el porcentaje de control osciló entre el 63,03 y el 76,14%, frente al 61,5% de control exhibido por el fungicida químico Carbendazim.

ABSTRACT Saponins are widely recognized for their biological properties, which has led to the development of several research projects applicable to the agricultural sector. In this sense, the aim of this study was to evaluate the in vitro and in vivo antifungal effect of saponins extracted from quinoa husks, using the crude extract, and incorporated in a formulation against Botrytis cinerea in strawberries. The extraction of saponins by the maceration method was studied, where the effect of temperature, time, and ethanol concentration on the extraction of saponins was evaluated; the process was optimized using a central composite design (CCD). The in vitro antifungal effect of the crude extract of saponins was evaluated by the minimum inhibitory concentration (MIC), while the in vitro and in vivo antifungal effect of the formulation was determined by the mycelial inhibition percentage and control percentage, respectively. The optimum extraction point of saponins was obtained at 49.8 °C, 0.367 h, and 47.4% ethanol. On the other hand, the antifungal activity against Botrytis cinerea was dependent on the concentration of saponins; in the in vitro evaluation the MIC of the crude extract was 8.25 mg mL-1 of saponins and the mycelial inhibition percentage of the formulation was higher than 90%. In the in vivo evaluation of the formulation, the percentage of control ranged from 63.03 to 76.14%, compared to 61.5% control exhibited by the chemical fungicide Carbendazim.

SUMMARY: Marein is a flavonoid compound that reduces blood glucose and lipids and has a protective effect in diabetes. However, the effect and mechanism(s) of marein on renal endothelial-mesenchymal transition in diabetic kidney disease (DKD) have not been elucidated. In this study, single-cell sequencing data on DKD were analyzed using a bioinformation method, and the data underwent reduced dimension clustering. It was found that endothelial cells could be divided into five subclusters. The developmental sequence of the subclusters was 0, 1, 4, 2, and 3, of which subcluster 3 had the most interstitial phenotype.The expression of mesenchymal marker protein:Vimentin(VIM), Fibronectin(FN1), and fibroblast growth factor receptor 1 (FGFR1) increased with the conversion of subclusters. In db/db mice aged 13-14 weeks, which develop DKD complications after 8-12 weeks of age, marein reduced blood levels of glucose, creatinine, and urea nitrogen, improved structural damage in kidney tissue, and reduced collagen deposition and the expression of FN1 and VIM. Marein also up-regulated autophagy marker:Light chain 3II/I(LC3II/I) and decreased FGFR1 expression in renal tissue. In an endothelial-mesenchymal transition model, a high glucose level induced a phenotypic change in human umbilical vein endothelial cells. Marein decreased endothelial cell migration, improved endothelial cell morphology, and decreased the expression of VIM and FN1. The use of the FGFR1 inhibitor, AZD4547, and autophagy inhibitor, 3-Methyladenine(3-MA), further demonstrated the inhibitory effect of marein on high glucose-induced endothelial-mesenchymal transition by reducing FGFR1 expression and up-regulating the autophagy marker protein, LC3II/I. In conclusion, this study suggests that marein has a protective effect on renal endothelial- mesenchymal transition in DKD, which may be mediated by inducing autophagy and down-regulating FGFR1 expression.

RESUMEN: La mareína es un compuesto flavonoide que reduce la glucosa y los lípidos en sangre y tiene un efecto protector en la diabetes. Sin embargo, no se han dilucidado el efecto y los mecanismos de la mareína sobre la transición endotelial- mesenquimatosa renal en la enfermedad renal diabética (ERD). En este estudio, los datos de secuenciación unicelular sobre DKD se analizaron utilizando un método de bioinformación y los datos se sometieron a una agrupación de dimensiones reducidas. Se descubrió que las células endoteliales podían dividirse en cinco subgrupos. La secuencia de desarrollo de los subgrupos fue 0, 1, 4, 2 y 3, de los cuales el subgrupo 3 tenía el fenotipo más intersticial. La expresión de la proteína marcadora mesenquimatosa: vimentina (VIM), fibronectina (FN1) y receptor del factor de crecimiento de fibroblastos. 1 (FGFR1) aumentó con la conversión de subgrupos. En ratones db/db de 13 a 14 semanas de edad, que desarrollan complicaciones de DKD después de las 8 a 12 semanas de edad, la mareína redujo los niveles sanguíneos de glucosa, creatinina y nitrógeno ureico, mejoró el daño estructural en el tejido renal y redujo la deposición y expresión de colágeno de FN1 y VIM. Marein también aumentó el marcador de autofagia: Cadena ligera 3II/I (LC3II/I) y disminuyó la expresión de FGFR1 en el tejido renal. En un modelo de transición endotelial-mesenquimal, un nivel alto de glucosa indujo un cambio fenotípico en las células endoteliales de la vena umbilical humana. Marein disminuyó la migración de células endoteliales, mejoró la morfología de las células endoteliales y disminuyó la expresión de VIM y FN1. El uso del inhibidor de FGFR1, AZD4547, y del inhibidor de la autofagia, 3-metiladenina (3-MA), demostró aún más el efecto inhibidor de la mareína en la transición endotelial-mesenquimal inducida por niveles altos de glucosa al reducir la expresión de FGFR1 y regular positivamente la proteína marcadora de autofagia. , LC3II/I. En conclusión, este estudio sugiere que la mareína tiene un efecto protector sobre la transición endotelial-mesenquimatosa renal en la ERC, que puede estar mediada por la inducción de autofagia y la regulación negativa de la expresión de FGFR1.

Resumen: Las nanopartículas de plata (NPs-Ag) son de gran interés debido a las aplicaciones potenciales en diferentes áreas. En busca de metodologías que no presenten riesgos a la salud y sean amigables con el ambiente, la biosíntesis de nanopartículas ha sido una opción viable. Se sabe que diversas biomoléculas presentes en los microrganismos pueden tener las funciones de agente oxidante, reductor y estabilizador, favoreciendo la formación de nanopartículas. En el presente trabajo se tuvo como objetivo la biosíntesis, caracterización y evaluación de la actividad antibacteriana de NPs-Ag. La biosíntesis se realizó a partir de sobrenadante de un cultivo de Pseudomonas aeruginosa, las nanopartículas se caracterizaron mediante espectroscopía UV-VIS, microscopía electrónica de barrido y difracción de rayos X, y la actividad antibacteriana se evaluó con ensayos de dilución en caldo Mueller Hinton, se determinó la concentración mínima inhibitoria (CMI) y concentración mínima bactericida (CMB) sobre bacterias Gram positivas y negativas. Se encontró que la mejor síntesis fue con una mezcla de 20% de sobrenadante conteniendo 3 mM de AgNO3, observando nanoestructuras con morfologías mixtas. Presentaron actividad contra bacterias Gram positivas y negativas con CMI de 1 a 2 µg/ml y CMB de 2 a 4 µg/ml. En conclusión, el sobrenadante de cultivos de P. aeruginosa es una alternativa viable para la síntesis de NPs-Ag con actividad antibacteriana.

Abstract: Silver nanoparticles (NPs-Ag) are of great interest due to the potential applications in different areas. In order to find methodologies that not represent human health risk and also an ecofriendly one, biosynthesis of these nanoparticles has been a viable option. It is known that diverse biomolecules present in microorganisms can function as an oxidative, reductor and/or stabilizer agents, thanks to that silver nanoparticles synthesis could be favored. In this work the main objectives were the biosynthesis, characterization, and evaluation of antibacterial activity of NPs-Ag. Biosynthesis was made using the culture supernatant of Pseudomonas aeruginosa. The NPs-Ag were characterized using UV-Vis spectroscopy, scanning electron microscopy, X‑ray diffraction and the antimicrobial effect was evaluated by dilution assays in Muller Hinton broth and the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined against Gram-positive and Gram-negative bacteria. A mixture containing 20% of supernatant and 3 mM AgNO3 was the best way to obtain silver nanoparticles. Nanoparticles with mixed morphology were observed. The NPs-Ag showed antibacterial activity over Gram-positive and Gram-negative bacteria with MIC of 1 to 2 µg/ml and MBC of 2 to 4 µg/ml. In conclusion, culture supernatant of P. aeruginosa is a viable pathway for the synthesis of NPs-Ag with antibacterial activity.

Abstract Introduction: glucocorticoids (GC) have been widely used in the treatment of ocular pathologies due to their anti-inflammatory and anti-angiogenic effects. It has been suggested that the anti-angiogenic mechanism of GC may be related to the enzyme phosphatidylinositol-3-kinase (PI3K), which plays a crucial role in angiogenesis mediated by the alpha 7 nicotinic acetylcholine receptor (α7-nAChR). PI3K is a heterodimeric lipoprotein enzyme composed of regulatory (p85) and catalytic (p110) subunits. Objective: this review examines the evidence of how the GC modulate the PI3K signaling pathway activated by α7-nAChR in the process of in vitro angiogenesis. Methodology: a literature search was conducted using the PubMed and Web of Science search engines, relating the concepts of "endothelial cell," "α7-nAChR," "PI3K," and "glucocorticoid." Results: thirty-two articles were selected that reported on the expression of α7-nAChR and PI3K in human endothelial cells. Furthermore, the effect of dexamethasone on PI3K and Akt (protein kinase B) subunits was documented in human, murine, and porcine models. Based on these findings, a mechanism was proposed whereby GC exert their anti-angiogenic effect through modulation of the expression of the inhibitory p85 subunit of PI3K activated by α7-nAChR in human endothelial cells. Conclusion: background evidence suggests that dexamethasone exerts its anti-angiogenic mechanism of action by increasing the expression of the α7-nAChR-activated PI3K inhibitory subunit p85

Resumen Introducción: los glucocorticoides (GC) han sido ampliamente utilizados en el tratamiento de patologías oculares debido a sus efectos antiinflamatorios y anti-angiogénicos. Se ha sugerido que el mecanismo de acción anti-angiogénico de los GC puede estar relacionado con la enzima fosfatidilinositol-3-cinasa (PI3K), la cual desempeña un papel crucial en la angiogénesis mediada por el receptor de acetilcolina nicotínico alfa 7 (α7-nAChR). La PI3K es una enzima lipoproteica heterodimérica compuesta por las subunidades; reguladora (p85) y catalítica (p110). Objetivo: esta revisión examina la evidencia de cómo los GC modulan la vía de señalización de PI3K activada por α7-nAChR en el proceso de angiogénesis in vitro. Metodología: se realizó una revisión bibliográfica utilizando los motores de búsqueda PubMed y Web of Science, relacionando los conceptos “endothelial cell”, “α7-nAChR”, “PI3K” y “glucocorticoid”. Resultados: se seleccionaron 30 artículos que informaron sobre la expresión de α7-nAChR y PI3K en células endoteliales humanas. Además, del efecto de dexametasona sobre las subunidades de PI3K y Akt (proteína cinasa B) en modelos humano, murino y porcino. A partir de estos hallazgos, se propuso un mecanismo mediante el cual los GC ejercen su efecto anti-angiogénico a través de la modulación en la expresión de la subunidad inhibitoria p85 de PI3K activada por α7-nAChR en células endoteliales humanas. Conclusión: los antecedentes evidencian que dexametasona, ejerce su mecanismo de acción anti-angiogénico mediante el incremento de la expresión de la subunidad inhibitoria p85 de PI3K activada por α7-nAChR.

In this study, the typical azo dye methyl orange (MO) was degraded by pyrite (FeS2) activated by hydrogen peroxide (H2O2). When [MO] = 0.1 mM, [FeSJ = 2.0 g/L and [H2O2] = 22 mM, 96.4% MO was removed in 120 min and the TOC removal rate was higher than 50%. HO* was the primary radical responsible for MO degradation, in addition, the acid condition promoted the degradation of MO in the FeS2/H2O2 system. MO in tap water and river water was not effectively degraded, whereas acidification could weaken the inhibitory effect on the FeS2/ H2O2 system to enable the degradation of MO in tap and river water. The OD600 indicated that the solution was environmentally friendly after the reaction, and three degradation pathways of MO were discussed. In summary, Fe(ll) could be dissolved from FeS2, which activated H2O2 to generate Fe(lll) and HO*. FeS2 could reduce Fe(lll) into Fe(ll), thus realizing the Fe(lll)/(ll) cycle and efficiently activating H2O2 to degrade MO.

Resumen Antecedentes: La Moringa peregrina Forssk es una planta muy conocida en etnomedicina debido a sus usos generalizados en diversas enfermedades como la tos, la cicatrización de heridas, la rinitis, la fiebre y la desintoxicación. Las semillas de la planta contienen compuestos citotóxicos para muchas células cancerosas. Durante el uso terapéutico de las plantas por vía oral, algunos compuestos presentes en ellas pueden ser citotóxicos para las líneas celulares normales y los glóbulos rojos. Objetivo: Este estudio fue el primer informe de investigación del perfil citotóxico sobre el cáncer oral, CAL 27, línea celular, y las actividades hemolíticas en eritrocitos humanos del extracto etanólico de semillas de Moringa peregrina (MPSE). Métodos: Se examinó el efecto citotóxico del MPSE contra la línea celular de cáncer oral CAL 27 mediante el ensayo con bromuro de 3-(4, 5-dimetiltiazol-2-il)-2, 5,-difeniltetrazolio (MTT). La toxicidad del MPSE sobre los eritrocitos humanos se determinó mediante un ensayo hemolítico in vitro. Resultados: MPSE mostró una actividad antiproliferativa significativa contra el cáncer oral, línea celular CAL 27 a concentraciones más bajas con un valor de concentración inhibitoria media máxima (IC50) de 21,03 μg/mL. A 1.000 µg/ml de MPSE, la hemólisis máxima fue del 14,3%, lo que está dentro del límite de seguridad. Conclusiones: Este estudio reveló un potencial anticancerígeno oral de MPSE y proporcionó una base para su uso potencial en el tratamiento del cáncer oral con un efecto hemolítico mínimo en los glóbulos rojos humanos.

Abstract Background : Moringa peregrina Forssk is a well-known plant in ethnomedicine due to its widespread uses in various diseases like cough, wound healing, rhinitis, fever, and detoxification. The plant seeds contain compounds that are cytotoxic to many cancer cells. During the therapeutic use of plants via the oral route, some compounds present in the plants may be cytotoxic to normal cell lines and red blood cells. Objective : This study was the first report of investigation of the cytotoxic profile on oral cancer, CAL 27, cell line, and hemolytic activities on human erythrocytes of Moringa peregrina seeds ethanolic extract (MPSE). Methods: MPSE was screened for its cytotoxic effect against oral cancer, CAL 27, cell line using 3-(4, 5-dimethylthiazol-2-yl)-2, 5,-diphenyltetrazolium bromide (MTT) assay. The toxicity of MPSE on human erythrocytes was determined by in vitro hemolytic assay. Results: MPSE showed significant anti-proliferative activity against oral cancer, CAL 27 cell line at lower concentrations with half maximal inhibitory concentration (IC50) value of 21.03 μg/mL. At 1,000 µg/ml of MPSE, the maximum hemolysis was found to be 14.3% which is within safer limit. Conclusions: This study revealed a potential anti-oral cancer of MPSE and provided a baseline for its potential use in oral cancer treatment with minimum hemolytic effect on human RBCs.

Resumen Antecedentes: La Moringa peregrina se utiliza ampliamente en la medicina tradicional de la Península Arábiga para tratar diversas dolencias, ya que posee numerosos componentes farmacológicamente activos con varios efectos terapéuticos. Objetivo: Este estudio tenía como objetivo investigar el efecto inhibidor del extracto etanólico de semillas de Moringa peregrina (MPSE) frente a enzimas clave implicadas en patologías humanas, como la angiogénesis (timidina fosforilasa), la diabetes (α-glucosidasa) y la hipertensión intracraneal idiopática (anhidrasa carbónica). Además, se comprobaron las propiedades anticancerígenas frente al SH-SY5Y (neuroblastoma humano). Resultados: El extracto de MPSE inhibió significativamente la α-glucosidasa, la timidina fosforilasa y la anhidrasa carbónica con concentraciones inhibitorias semimáximas (IC50) de 303,1 ± 1,3, 471,30 ± 0,3 y 271,30 ± 5,1 µg/mL, respectivamente. Además, se observó el efecto antiproliferativo del MPSE en la línea celular del cáncer SH-SY5Y con valores de IC50 de 55,1 µg/mL. Conclusiones: MPSE posee interesantes capacidades inhibitorias frente a enzimas clave y línea celular de neuroblastoma canceroso humano.

Abstract Background: Moringa peregrina is widely used in the traditional medicine of the Arabian Peninsula to treat various ailments, because it has many pharmacologically active components with several therapeutic effects. Objective: This study aimed to investigate the inhibitory effect of Moringa peregrina seed ethanolic extract (MPSE) against key enzymes involved in human pathologies, such as angiogenesis (thymidine phosphorylase), diabetes (α-glucosidase), and idiopathic intracranial hypertension (carbonic anhydrase). In addition, the anticancer properties were tested against the SH-SY5Y (human neuroblastoma). Results: MPSE extract significantly inhibited α-glucosidase, thymidine phosphorylase, and carbonic anhydrase with half-maximal inhibitory concentrations (IC50) values of 303.1 ± 1.3, 471.30 ± 0.3, and 271.30 ± 5.1 µg/mL, respectively. Furthermore, the antiproliferative effect of the MPSE was observed on the SH-SY5Y cancer cell line with IC50 values of 55.1 µg/mL. Conclusions: MPSE has interesting inhibitory capacities against key enzymes and human neuroblastoma cancer cell line.