RESUMO
Metabolic syndrome is a set of risk factors that consist of abdominal obesity, arterial hypertension, alterations in the lipid profile, and hyperglycemia. The current therapeutic strategy includes polypharmacy, using three or more drugs to control each syndrome component. However, this approach has drawbacks that could lead to therapeutic failure. Multitarget drugs are molecules with the ability to act on different targets simultaneously and are an attractive alternative for treating complex diseases such as metabolic syndrome. Previously, we identified a triamide derivative of 5-aminoanthranilic acid that exhibited hypoglycemic, hypolipemic, and antihypertensive activities simultaneously. In the present study, we report the synthesis and in combo evaluation of new derivatives of anthranilic acid, intending to identify the primary structural factors that improve the activity over metabolic syndrome-related parameters. We found that substitution on position 5, incorporation of 3,4-dimethoxyphenyl substituents, and having a free carboxylic acid group lead to the in vitro inhibition of HMG-CoA reductase, and simultaneously the diminution of the serum levels of glucose, triglycerides, and cholesterol in a diet-induced in vivo model.
RESUMO
Sleep disturbances are common in the third trimester of pregnancy and generate changes in the secretion of melatonin in pregnant women who sleep less than eight hours or have sleep disturbances, which promote various physiological changes in the mother that in turn result in low birth weight (LBW) in the fetus. LBW is associated with a phenomenon known as "metabolic programming," in which the fetus is subjected to a stressful situation that results in irreversible metabolic alterations that predispose it to the development of obesity in adulthood.
En el tercer trimestre del embarazo son frecuentes las alteraciones del sueño, las cuales generan cambios en la secreción de melatonina en mujeres gestantes que duermen menos de ocho horas o presentan alteraciones de sueño, promoviendo diversos cambios fisiológicos en la madre, que a su vez derivan en bajo peso al nacimiento (BPN) en el producto. El bajo peso al nacimiento está asociado con un fenómeno conocido como "programación metabólica", en la que el feto es sometido a estrés que tiene como resultado alteraciones metabólicas irreversibles que lo predisponen al desarrollo de obesidad en la edad adulta.
Assuntos
Obesidade/epidemiologia , Complicações na Gravidez/epidemiologia , Transtornos do Sono-Vigília/epidemiologia , Adulto , Feminino , Humanos , Recém-Nascido de Baixo Peso , Recém-Nascido , Obesidade/etiologia , Gravidez , Terceiro Trimestre da GravidezRESUMO
Resumen En el tercer trimestre del embarazo son frecuentes las alteraciones del sueño, las cuales generan cambios en la secreción de melatonina en mujeres gestantes que duermen menos de ocho horas o presentan alteraciones de sueño, promoviendo diversos cambios fisiológicos en la madre, que a su vez derivan en bajo peso al nacimiento (BPN) en el producto. El bajo peso al nacimiento está asociado con un fenómeno conocido como "programación metabólica", en la que el feto es sometido a estrés que tiene como resultado alteraciones metabólicas irreversibles que lo predisponen al desarrollo de obesidad en la edad adulta.
Abstract Sleep disturbances are common in the third trimester of pregnancy and generate changes in the secretion of melatonin in pregnant women who sleep less than eight hours or have sleep disturbances, which promote various physiological changes in the mother that in turn result in low birth weight (LBW) in the fetus. LBW is associated with a phenomenon known as "metabolic programming," in which the fetus is subjected to a stressful situation that results in irreversible metabolic alterations that predispose it to the development of obesity in adulthood.
