Multitarget Action of Xanthones from Garcinia mangostana against α-Amylase, α-Glucosidase and Pancreatic Lipase.

Digestive enzymes such α-amylase (AA), α-glucosidase (AG) and pancreatic lipase (PL), play an important role in the metabolism of carbohydrates and lipids, being attractive therapeutic targets for the treatment of type 2 diabetes and obesity. Garcinia mangostana is an interesting species because there have been identified xanthones with the potential to inhibit these enzymes. In this study, the multitarget inhibitory potential of xanthones from G. mangostana against AA, AG and PL was assessed. The methodology included the isolation and identification of bioactive xanthones, the synthesis of some derivatives and a molecular docking study. The chemical study allowed the isolation of five xanthones (1-5). Six derivatives (6-11) were synthesized from the major compound, highlighting the proposal of a new solvent-free methodology with microwave irradiation for obtaining aromatic compounds with tetrahydropyran cycle. Compounds with multitarget activity correspond to 2, 4, 5, 6 and 9, highlighting 6 with IC50 values of 33.3 µM on AA, 69.2 µM on AG and 164.4 µM on PL. Enzymatic kinetics and molecular docking studies showed that the bioactive xanthones are mainly competitive inhibitors on AA, mixed inhibitors on AG and non-competitive inhibitors on PL. The molecular coupling study established that the presence of methoxy, hydroxyl and carbonyl groups are important in the activity and interaction of polyfunctional xanthones, highlighting their importance depending on the mode of inhibition.

In Vitro and In Silico Study of the α-Glucosidase and Lipase Inhibitory Activities of Chemical Constituents from Piper cumanense (Piperaceae) and Synthetic Analogs.

Digestive enzymes are currently considered important therapeutic targets for the treatment of obesity and some associated metabolic diseases, such as type 2 diabetes. Piper cumanense is a species characterized by the presence of bioactive constituents, particularly prenylated benzoic acid derivatives. In this study, the inhibitory potential of chemical constituents from P. cumanense and some synthesized compounds was determined on digestive enzymes (pancreatic lipase (PL) and α-glucosidase (AG)). The methodology included isolating and identifying secondary metabolites from P. cumanense, synthesizing some analogs, and a molecular docking study. The chemical study allowed the isolation of four prenylated benzoic acid derivatives (1-4). Four analogs (5-8) were synthesized. Seven compounds were found to significantly inhibit the catalytic activity of PL with IC50 values between 28.32 and 55.8 µM. On the other hand, only two compounds (6 and 7) were active as inhibitors of AG with IC50 values lower than 155 µM, standing out as the potential multitarget of these chromane compounds. Enzyme kinetics and molecular docking studies showed that the bioactive compounds mainly interact with amino acids other than those of the catalytic site in both PL and AG. This work constitutes the first report on the antidiabetic and antiobesity potential of substances derived from P. cumanense.

Fitorremediación con Brassicaceae y Apiaceae en suelos contaminados con metales pesados

Introducción: La cuenca media del río Bogotá viene sufriendo contaminación por metales pesados debido a los vertidos industriales. Esta fuente de agua ha sido utilizada para el riego de cultivos de ciclo corto, lo que ha provocado la contaminación por metales pesados de los suelos productivos. Objetivo: Evaluar un proceso de fitorremediación con las especies de Brócoli (Brassica oleracea var. italica Plenck) y Cilantro (Coriandrum sativum L.) en suelos contaminados con metales pesados en Mosquera, Colombia. Métodos: El muestreo se realizó con un diseño factorial al azar: a) proporciones de cilantro/brócoli (30 cilantro/70 brócoli, 50/50, 70 cilantro/30 brócoli y dos controles de tipo monocultivo de cada especie) y b) tiempo de fitorremediación (3, 6 y 9 meses), cada tratamiento con cuatro parcelas experimentales. El suelo y el tejido vegetal se analizó mediante espectrofotometría de absorción atómica para determinar la concentración de los metales pesados. Resultados: Las concentraciones de metales pesados en las muestras de tejido vegetal para brócoli y cilantro mostraron valores de Cd, Pb y Cr más altos que Hg y As, respecto al control. Las concentraciones de Cd, Pb y Cr presentaron valores significativamente más altos (P < 0.05) en suelos con cilantro y brócoli mezclados, respecto al sitio de control donde la concentración de Cd registró niveles significativamente más bajos que en los otros suelos. Las concentraciones de Cd, Pb y Cr fueron más altas en tejidos de cilantro y en suelos con cilantro en comparación con el control. Conclusiones: La fitorremediación por medio de las especies Brassica oleracea var. itálica Plenck y Coriandrum sativum L. en proporciones 70/30 o 30/70 a suelos con pH entre 5.5 y 6.0 permiten una buena recuperación de suelos con contenidos de metales pesados en términos de concentraciones altas a cortos plazos, iniciando la biorremediación a los tres meses y finalizando cargas de disponibilidad variable a los nueve meses.

Introduction: The middle basin of the Bogotá River has been suffering from heavy metal contamination due to industrial discharges. This water source has been used to irrigate short-cycle crops, which has resulted in heavy metal contamination of productive soils. Objective: To evaluate a phytoremediation process with the plant species Broccoli (Brassica oleracea var. Italica plenck) and Cilantro (Coriandrum sativum L.) in soils contaminated with heavy metals in Mosquera, Colombia. Methods: Sampling was performed with a randomized factorial design: a) cilantro/broccoli proportions (30 cilantro/70 broccoli, 50/50, 70 cilantro/30 broccoli and two monoculture type controls of each species) and b) phytoremediation time (3, 6 and 9 months), each treatment with four experimental plots. Soil and plant tissue were analyzed in the laboratory by atomic absorption spectrophotometry to determine the concentration of heavy metals. Results: The concentrations of heavy metals in plant tissue samples for broccoli and cilantro showed higher values of Cd, Pb and Cr than Hg and As, with respect to the control. The concentrations of Cd, Pb and Cr presented significantly higher values (P < 0.05) in soil where there was a mixed presence of cilantro and broccoli, with respect to the control site where the concentration of Cd registered significantly lower levels than in the other soils. Finally, Cd, Pb and Cr concentrations were higher in cilantro tissues and in soils with cilantro compared to the control. Conclusions: Phytoremediation by means of Brassica oleracea var. italica Plenck and Coriandrum sativum L. in 70/30 or 30/70 proportions in soils with pH between 5.5 and 6.0 allows a good recovery of soils with heavy metal contents in terms of high concentrations in short terms, starting bioremediation after three months and ending loads of variable availability after nine months.