RESUMEN
COVID-19 is a disease that has caused a high number of deaths in the world, and despite being controlled, it requires attention and the search for new quick and economical therapeutic strategies. In this sense, vitamin D stands out, an immunomodulator that has shown beneficial effects in decreasing the risk and severity of acute respiratory tract infections, including COVID-19. Therefore, this review presents a number of experimental, observational and clinical studies on the importance of vitamin D against viral infections with an emphasis on COVID-19, highlighting the relationship between vitamin D, Renin-Angiotensin System and cytokine storms with decreased inflammatory lesions in patients with COVID-19. In addition, aspects of pathophysiology, metabolism, risk factors, sources and recommendations of vitamin D are described. We conclude that vitamin D plays a protective role against inflammatory lesions and can decrease the risk of infections and the severity of COVID-19. Therefore, it is essential to maintain adequate levels of vitamin D to avoid complications related to its deficiency.
Asunto(s)
Tratamiento Farmacológico de COVID-19 , Deficiencia de Vitamina D , Adaptación Psicológica , Suplementos Dietéticos , Humanos , SARS-CoV-2 , Vitamina D/uso terapéutico , Deficiencia de Vitamina D/complicaciones , Deficiencia de Vitamina D/tratamiento farmacológico , Vitaminas/uso terapéuticoRESUMEN
Polyacetylene glycosides (PAGs) constitute a relatively small class of secondary metabolites characterized by the presence of a sugar unit anomerically connected to a polyacetylene. These compounds are found in fungi, seaweed, and more often in plants. PAGs exhibit a wide range of biological and pharmacological activities and, as a result, the literature of these compounds has grown exponentially in recent years.
Asunto(s)
Glicósidos , Poliinos , Hongos , Plantas , Polímero PoliacetilénicoRESUMEN
This study describes the synthesis and antioxidant activity of new 1,4-disubstituted 1,2,3-triazoles. These compounds were generated semi-synthetically using the Cu(I)-catalysed azide-alkyne cycloaddition (CuAAC) reaction between ethyl 2-azidoacetate and terminal acetylenes derived from the natural products carvacrol, eugenol, isovanillin, thymol and vanillin. The products were obtained at 50 to 80% yield and characterised through several spectrographic techniques. Antioxidant activity was assayed using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS). The products exhibited moderate antioxidant activity, with ethyl 2-(4-((4-formyl-2-methoxyphenoxy)methyl)-1H-1,2,3-triazol-1-yl) acetate showing the highest antioxidant capacity (EC50 = 75.5 µg/mL) among the generated 1,4-disubstituted 1,2,3-triazoles. In conclusion, the generation of these compounds opens new possibilities for the development of new antioxidant agents.
Asunto(s)
Antioxidantes , Triazoles , Alquinos , Antioxidantes/farmacología , Azidas , Reacción de Cicloadición , Triazoles/farmacologíaRESUMEN
The propargylation of aldehydes promoted by microwave irradiation using allenylboron compounds in a chemo- and regioselective way is described. The corresponding products were obtained in short reaction time, high yield and purity without the need of any solvent when allenylboronic acid pinacol ester was used, or using a minimal amount of acetone when potassium allenyltrifluoroborate was used.
RESUMEN
Enulosides, carbohydrate derivatives containing an α,ß-unsaturated carbonyl unit, were designed and obtained in high yields and isomeric purity. All synthesized compounds exhibited antitumoral activity in micromolar range against four tested tumor cells lines, being the best results observed for HL-60 cells. These compounds open new possibilities to prepare an array of more active, site-specific or selective antitumor agents. 2016 Elsevier Ltd. All rights reserved.
Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Productos Biológicos/farmacología , Carbohidratos/química , Proliferación Celular/efectos de los fármacos , Diseño de Fármacos , Productos Biológicos/química , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Neoplasias/tratamiento farmacológico , Neoplasias/patología , Relación Estructura-Actividad , Células Tumorales CultivadasRESUMEN
An efficient approach for the synthesis of Z-1,3-enynes based on the coupling reaction of Z-vinyl tellurides and alkynes containing a pseudoglycoside moiety is described. The products were obtained in good yields via a stereoselective way. Preliminary screening against three tumor cell lines indicated that the synthesized compounds are promising intermediates for the synthesis of an array of more potent target structures.
Asunto(s)
Alquinos/síntesis química , Alquinos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Telurio/química , Alquinos/química , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Glicósidos/síntesis química , Glicósidos/química , Glicósidos/farmacología , Humanos , Neoplasias/tratamiento farmacológico , Estereoisomerismo , Telurio/farmacología , Compuestos de Vinilo/química , Compuestos de Vinilo/farmacologíaRESUMEN
Lactones are organic cyclic esters that have been described as larvicides against Aedes aegypti and as components of oviposition pheromone of Culex quinquefasciatus. This work describes the effect of six α,ß-unsaturated lactones (5a-5f) on survival of A. aegypti fourth instar larvae (L4). It is also reported the effects of the lactones on L4 gut trypsin activity and oviposition behavior of A. aegypti females. Five lactones were able to kill L4 being the lactones 5a (LC50 of 39.05 ppm), 5e (LC50 of 36.30 ppm) and 5f (LC50 of 40.46 ppm) the most promising larvicides. Only the lactone 5a inhibited L4 gut trypsin activity, with an IC50 of 115.15 µg/mL. Lactones 5a, 5c, 5d and 5e did not exert deterrent or stimulatory effects on oviposition, whereas lactone 5b exhibited a strong deterrent oviposition activity. In conclusion, this work introduces new α,ß-unsaturated lactones as promising alternatives to control A. aegypti dissemination. The larvicidal mechanism of the lactone 5a can involve the disruption of proteolysis at larval gut.
Asunto(s)
Aedes/efectos de los fármacos , Insectos Vectores/efectos de los fármacos , Insecticidas/farmacología , Lactonas/farmacología , Oviposición/efectos de los fármacos , Tripsina/efectos de los fármacos , Aedes/fisiología , Animales , Femenino , Concentración 50 Inhibidora , Insectos Vectores/fisiología , Insecticidas/química , Lactonas/química , Larva/efectos de los fármacos , Tripsina/metabolismo , Inhibidores de Tripsina/farmacologíaRESUMEN
The use of ultrasound irradiation to promote the allylation of aldehydes containing different functionalities with potassium allyltrifluoroborates is described. The method features the use of a minimum amount of acetone as solvent, without any other catalyst or promoter. The products were obtained in high yields, short reaction times, at room temperature and without the need of further purification.
RESUMEN
(-)-Massoialactone, an α,ß-unsaturated δ-lactone isolated from Cryptocarya massoia, and five analogues were synthesized and their antiproliferative and anti-inflammatory activities were evaluated. The lactones were able to mimic the "core" functional group required for the biological activity of their parent natural compounds suggesting that substantially altered analogues may retain their properties.
Asunto(s)
Antiinflamatorios/síntesis química , Antiinflamatorios/farmacología , Antineoplásicos/química , Antineoplásicos/farmacología , Pironas/síntesis química , Pironas/farmacología , Animales , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Resonancia Magnética , Ratones , Ratones Endogámicos BALB CRESUMEN
An efficient method for the allylation of aldehydes containing a broad range of functional groups using potassium allyltrifluoroborate is described. The reaction utilizes a catalytic amount of 18-C-6 in biphasic media under open atmosphere and room temperature to provide the corresponding homoallylic alcohols in high yields and without the necessity of any subsequent purification.
Asunto(s)
Aldehídos/química , Catálisis , Potasio/química , Boratos/química , Éteres Corona/química , Agua/químicaRESUMEN
Complete (1) H, (13) C, and (125) Te NMR spectral data for some vinyl tellurides are described. The (1) H-(125) Te gHMBC experiment was used for the complete chemical shift assignment and structure elucidation of a mixture of regioisomers. The assignment ((125) Te NMR) and coupling constants (J(H,H) ) for all regioisomers are described for the first time.