Metabolism and Excretion Study of Daphnoretin in Rats after Oral Administration

The metabolism and excretion profile in rats were investigated after a single dose of daphnoretin. Metabolites of daphnoretin in rats were characterized by HPLC-MS n analysis. A HPLC-UV method was developed to determine the concentration of daphnoretin in rat urine, feces and bile. Daphnoretin was biotransformed via conjunctive and oxidative pathways to three detected metabolites. The structures of these metabolites were tentatively identified. The cumulative excretion percentage of daphnoretin in urine, feces and bile of rats was 0.13, 52.7, and 0.018 %, respectively. All the metabolites and excretion data are reported for the first time.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Metabolism and Excretion Study of Daphnoretin in Rats after Oral Administration

The metabolism and excretion profile in rats were investigated after a single dose of daphnoretin. Metabolites of daphnoretin in rats were characterized by HPLC-MS n analysis. A HPLC-UV method was developed to determine the concentration of daphnoretin in rat urine, feces and bile. Daphnoretin was biotransformed via conjunctive and oxidative pathways to three detected metabolites. The structures of these metabolites were tentatively identified. The cumulative excretion percentage of daphnoretin in urine, feces and bile of rats was 0.13, 52.7, and 0.018 %, respectively. All the metabolites and excretion data are reported for the first time.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Evaluation and optimization of a novel cascade refrigeration system driven by waste heat

Direct discharge of waste heat from internal combustion engines (ICEs) is unfavorable for the efficient and clean fuel utilization. Here, a novel combined absorption-compression cascade refrigeration cycle is proposed to efficiently capture low-grade waste heat and supply cooling capacity for food freezing in vessels or refrigerated trucks. The intention of this work lies in: i) Comprehensively evaluating the performances of the proposed system; ii) Gaining the optimal operating conditions of the system. Aimed that, analysis models of energy, exergy, economy, and environment are set up to evaluate the sweeping performances. Further, multi-objective optimization is introduced to obtain the optimal operating parameters including evaporation and condensation temperature of the low-temperature stage, generation temperature and condensation temperature of the high-temperature stage, and cascade temperature differences. By applying multi-objective optimization, the coefficient of performance and exergy efficiency of the system are elevated from 1.283 to 1.547, and 0.222 to 0.246, respectively, the discharge amount of carbon dioxide are reduced from 71.40 to 59.57 tons year−1, and annual total cost are decreased from 16,028 to 15,055 $ year−1 compared to initial operating conditions

Implementation of a semantic web site for a computer engineering department

Ontologies -- Technology of semantic web -- Toward a system of SW -- Evaluation of SWSAS

Synthesis, Crystal Structure, Absolute Configuration and Antitumor Activity of the Enantiomers of 5-Bromo-2-chloro-N-(1-phenylethyl)pyridine-3-sulfonamide

Pyridinesulfonamide is an important fragment which has a wide range of applications in novel drugs. R- and S-isomers of 5-bromo-2-chloro-N-(1-phenylethyl)pyridine-3-sulfonamide have been synthesized, and the stereostructures have been researched. Single crystals of both compounds were obtained for X-ray analysis, and the absolute configurations (ACs) have been further confirmed by electronic circular dichroism (ECD), optical rotation (OR) and quantum chemical calculations. The crystal structures and calculated geometries were extremely similar, which permitted a comparison of the relative reliabilities of ACs obtained by ECD analyses and theoretical simulation. In addition, the effect of stereochemistry on the PI3Kα kinase and anticancer activity were investigated. Compounds 10a and 10b inhibit the activity of PI3Kα kinase with IC50 values of 1.08 and 2.69 μM, respectively. Furthermore, molecular docking was performed to analyze the binding modes of R- and S-isomers

Comprehensive Analysis of FASN in Tumor Immune Infiltration and Prognostic Value for Immunotherapy and Promoter DNA Methylation

Fatty acid synthase (FASN) promotes tumor progression in multiple cancers. In this study, we comprehensively examined the expression, prognostic significance, and promoter methylation of FASN, and its correlation with immune cell infiltration in pan-cancer. Our results demonstrated that elevated FASN expression was significantly associated with an unfavorable prognosis in many cancer types. Furthermore, FASN promoter DNA methylation can be used as a tumor prognosis marker. Importantly, high levels of FASN were significantly negatively correlated with tumor immune infiltration in 35 different cancers. Additionally, FASN was significantly associated with tumor mutational burden (TMB) and microsatellite instability (MSI) in multiple malignancies, suggesting that it may be essential for tumor immunity. We also investigated the effects of FASN expression on immunotherapy efficacy and prognosis. In up to 15 tumors, it was significantly negatively correlated with immunotherapy-related genes, such as PD-1, PD-L1, and CTLA-4. Moreover, we found that tumors with high FASN expression may be more sensitive to immunotherapy and have a good prognosis with PD-L1 treatment. Finally, we confirmed the tumor-suppressive effect of mir-195-5p through FASN. Altogether, our results suggested that FASN may serve as a novel prognostic indicator and immunotherapeutic target in various malignancies

Cynomolgus-rhesus hybrid macaques serve as a platform for imprinting studies

Genomic imprinting can lead to allele-specific expression (ASE), where one allele is preferentially expressed more than the other. Perturbations in genomic imprinting or ASE genes have been widely observed across various neurological disorders, notably autism spectrum disorder (ASD). In this study, we crossed rhesus cynomolgus monkeys to produce hybrid monkeys and established a framework to evaluate their allele-specific gene expression patterns using the parental genomes as a reference. Our proof-of-concept analysis of the hybrid monkeys identified 353 genes with allele-biased expression in the brain, enabling us to determine the chromosomal locations of ASE clusters. Importantly, we confirmed a significant enrichment of ASE genes associated with neuropsychiatric disorders, including ASD, highlighting the potential of hybrid monkey models in advancing our understanding of genomic imprinting