RESUMEN
Heat stress (HS) has a great influence on the etiology of male infertility. Coenzyme Q10 (CoQ10), known to have powerful antioxidant effects, has been reported to have such actions that are effective to treat infertility caused by HS. The aim of the present study was to investigate the antioxidative effect of CoQ10 on sperm quality, testicular antioxidant activities, and male fertility under HS. For this purpose, 18 mature male rabbits (aged 22 wk) of the Sinai Gabali breed were equally divided into 3 groups and placed at temperature-humidity index of 29 for 8 wk at a farm. The supplementation of CoQ10 at 0, 10, and 20 mg/kg of body weight was done in the first, second, and third groups, respectively. The results showed that the supplementation of CoQ10 had significant (P < 0.05) effect on semen quality factor (SQF) and testicular antioxidant activities by the supplementation of CoQ10. Moreover, a significant improvement in the concentration of testosterone, integrity of testicular DNA, and the expression of melatonin receptors was also observed, which were consistent with a significant improvement in buck fertility. The prolificacy was significantly increased (P < 0.05) in females when inseminated from bucks that were treated with CoQ10. Our results suggest that CoQ10 tends to decrease oxidative stress by enhancing testicular antioxidant activities, which are considered the most important factors for a buck's fertility. Hence, CoQ10 could be a suitable feed supplement to increase fertility, through enhancing the semen quality, in male rabbits and reducing the harmful effects of HS.
Asunto(s)
Estrés Oxidativo , Receptor de Melatonina MT1/metabolismo , Análisis de Semen/veterinaria , Testículo/fisiología , Termotolerancia , Ubiquinona/análogos & derivados , Alimentación Animal/análisis , Fenómenos Fisiológicos Nutricionales de los Animales , Animales , Dieta/veterinaria , Regulación de la Expresión Génica , Calor , Humedad , Masculino , Modelos Moleculares , Conformación Proteica , Conejos , Receptor de Melatonina MT1/genética , Ubiquinona/administración & dosificación , Ubiquinona/farmacologíaRESUMEN
3 series of novel fused heterocyclic systems, viz. triazolo[4,3-a]quinazolin-7-ones (3), 1 2 4 5-tetrazino[4,3-a]-quinazolin-8-ones (5) and Schiff's bases of isatin derivatives with 2-hydrazinoquinazolin-4-ones (7) have been synthesized. Several of them showed variable and promising in vitro antiproliferative activity against the MCF-7 cells. Compounds 3a-3c, 6, 7a-7 f showed promising activity (IC50=12.45-15.79 µM). Compound 7 f possessed notable cell cycle disrupting and apoptotic activities with enhanced selectivity against cancer cells, suggesting the potential for the development of new selective cell cycle inhibitors. In silico docking study of the compound 7 f with EGFR enzyme postulated that the designed compound might act on the same enzyme target where DJK_3021_A x-ray structure acted.
Asunto(s)
Antineoplásicos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Leucemia Mielógena Crónica BCR-ABL Positiva/tratamiento farmacológico , Quinazolinas/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Neoplasias de la Mama/patología , Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Receptores ErbB/antagonistas & inhibidores , Femenino , Humanos , Concentración 50 Inhibidora , Isatina/síntesis química , Isatina/química , Isatina/farmacología , Células K562 , Leucemia Mielógena Crónica BCR-ABL Positiva/patología , Simulación del Acoplamiento Molecular , Quinazolinas/síntesis química , Quinazolinas/química , Relación Estructura-ActividadRESUMEN
A potentiometric lipoate-selective sensor based on mercuric lipoate ion-pair as a membrane carrier is reported. The electrode was prepared by coating the membrane solution containing PVC, plasticizer, and carrier on the surface of graphite electrode. Influences of the membrane composition, pH, and possible interfering anions were investigated on the response properties of the electrode. The sensor exhibits significantly enhanced response toward lipoate ions over the concentration range 1 x 10(-7) molL(-1) to 1 x 10(-2) molL(-1) with a lower detection limit of (LDL) of 9 x 10(-8) molL(-1) and a slope of -29.4 m V decade(-1), with S.D. of the slope is 0.214 mV. Fast and stable response, good reproducibility, long-term stability, applicability over a pH range of 8.0-9.5 is demonstrated. The sensor has a response time of
Asunto(s)
Electrodos de Iones Selectos/normas , Preparaciones Farmacéuticas/análisis , Ácido Tióctico/análisis , Análisis de Inyección de Flujo , Concentración de Iones de Hidrógeno , Membranas Artificiales , Compuestos de Mercurio , Preparaciones Farmacéuticas/química , Cloruro de Polivinilo , Reproducibilidad de los Resultados , Ácido Tióctico/orinaRESUMEN
The success or failure of 3D QSAR, particularly CoMFA, is most strongly dependent, especially for flexible compounds, on the conformation of the molecule used in the analysis, and on the orientation of the molecule relative to the other molecules in 3D space (i.e., alignment). The present study suggests a rational procedure for the estimation of binding conformation that uses the transferred nuclear Overhauser effect (TRNOE) experiment in combination with conformational analysis using CAMDAS (Conformational Analyzer with Molecular Dynamics And Sampling) program that is developed in our laboratory. In the next step the TRNOE-obtained conformation can be used as a reference template in order to obtain alignment of other ligands, that have a common binding site. In this step we used the SUPERPOSE program created in our laboratory, in order to estimate the binding conformation of other compounds, and to simultaneously obtain the alignment of compounds for CoMFA. The resulting CoMFA models could be expected to closely reproduce the interaction mode with protein represented by the reported X-ray results. In order to confirm the validity of our procedure described above, we show its application in obtaining CoMFA models of thermolysin inhibitors. We obtained twenty CoMFA models, and that with the highest q2 value (q2 = 0.701) was found to provide an interaction mode very similar to that represented by the X-ray results.
Asunto(s)
Relación Estructura-Actividad Cuantitativa , Termolisina/antagonistas & inhibidores , Conformación MolecularRESUMEN
FeSO4 . 7 H2O, PbSO4, CuSO4 . 5 H2O, MnSO4 . 4 H2O, ZnSO4 . 7 H2O, CoCl2 . 6 H2O, and (NH4)6Mo7O24 . 4 H2O were added to the fermentation medium to investigate their potentialities on citric acid production by Candida lipolytica (Y 1095). FeSO4 . 7 H2O and MnSO4 . 4 H2O were more suitable than the other micronutrients for citric acid production. Addition of certain amino acids to the fermentation medium completely inhibited biosynthesis of citric acid by Candida lipolytica (Y 1095). When the fermentation medium was supplied with certain vitamins, yield of citric acid was increased in the presence of thiamine, nicotinic acid, and nicotinamide. The optimum concentration of thiamine which favoured yield of citric acid was 6 mg/l.