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1.
Biomedical and Environmental Sciences ; (12): 181-193, 2022.
Artículo en Inglés | WPRIM | ID: wpr-927652

RESUMEN

Objectives@#It is unclear whether G protein-coupled receptor 61 (GPR61) affecting body weight, plays a role in the association between birth weight and weather. This study aimed to assess the effects of prenatal weather and GPR61 on birth weight.@*Methods@#A total of 567 mother-newborn pairs were recruited in Houzhai Center Hospital during 2011-2012. We detected the maternal and neonatal GPR61 promoter methylation levels, and obtained meteorological and air pollution data.@*Results@#A positive association was observed between maternal and neonatal GPR61 methylation levels, and both of them were affected by precipitation, relative humidity (RH) and daily temperature range (DTR). Birth weight was associated negatively with RH and positively with DTR ( P < 0.05). A significant association was observed between birth weight and neonatal GPR61 methylation. We observed that maternal GPR61 methylation seemed to modify associations between weather and birth weight ( P interaction < 0.10), while neonatal GPR61 methylation mediated the effects of RH and DTR on birth weight ( P < 0.05).@*Conclusions@#Our findings revealed the significant associations among prenatal weather, GPR61 methylation and birth weight. Maternal GPR61 methylation may modify the susceptibility of birth weight to prenatal weather conditions, while neonatal GPR61 methylation may be a bridge of the effects of prenatal RH and DTR on birth weight.


Asunto(s)
Femenino , Humanos , Recién Nacido , Embarazo , Contaminación del Aire/análisis , Peso al Nacer , Proteínas del Tejido Nervioso , Receptores Acoplados a Proteínas G/metabolismo , Temperatura , Tiempo (Meteorología)
2.
Acta Pharmaceutica Sinica ; (12): 191-198, 2015.
Artículo en Chino | WPRIM | ID: wpr-251796

RESUMEN

A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.


Asunto(s)
Animales , Ratones , Inhibidores de la Colinesterasa , Química , Dioxoles , Química , Diseño de Fármacos , Indanos , Concentración 50 Inhibidora , Isoindoles , Química , Trastornos de la Memoria , Quimioterapia , Piperidinas , Escopolamina
3.
Acta Pharmaceutica Sinica ; (12): 1143-1149, 2014.
Artículo en Chino | WPRIM | ID: wpr-299155

RESUMEN

A series of novel 4-substituted-3-nitrobenzamide derivatives were designed and synthesized. The structures of the target compounds were confirmed with 1H NMR, 13C NMR, MS and element analysis. Anti-tumor activities against HCT-116, MDA-MB435 and HL-60 cell lines in vitro were evaluated by SRB assay. The results indicated most of the target compounds exhibited potent anti-tumor activity. Compound 4a showed the most potent inhibitory activities against three cancer cell lines with the GI50 values of 1.904-2.111 micromol x L(-1). Compounds 4g, 41-4n exhibited more potent inhibitory activities against MDA-MB435 and HL-60 cell lines with the GI50 values of 1.008-3.586 micromol x L(-1) and 1.993-3.778 micromol x L(-1), respectively. The structure-activity relationship of these compounds is discussed preliminarily.


Asunto(s)
Humanos , Antineoplásicos , Farmacología , Benzamidas , Farmacología , Línea Celular Tumoral , Proliferación Celular , Diseño de Fármacos , Células HL-60 , Concentración 50 Inhibidora , Relación Estructura-Actividad
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