作者: Fleming, Heather E ; Walesky, Chad ; Evans, Helen ; Shan, Jing ; Schepers, Arnout G ; Goessling, Wolfram ; Huang, Ada ; Bhatia, Sangeeta N ; Cox, Andrew G

The utility of in vitro human disease models is mainly dependent on the availability and functional maturity of tissue-specific cell types. We have previously screened for and identified small molecules that can enhance hepatocyte function in vitro. Here, we characterize the functional effects of one of the hits, FH1, on primary human hepatocytes in vitro, and also in vivo on primary hepatocytes in a zebrafish model. Furthermore, we conducted an analogue screen to establish the structure-activity relationship of FH1. We performed affinity-purification proteomics that identified NQO2 to be a potential binding target for this small molecule, revealing a possible link between inflammatory signaling and hepatocellular function in zebrafish and human hepatocyte model systems.

2020-09-01·Bulletin of Environmental Contamination and Toxicology4区 · 环境科学与生态学

Biodegradation of Atrazine by Mixed Bacteria of Klebsiella variicola Strain FH-1 and Arthrobacter sp. NJ-1

4区 · 环境科学与生态学

Article

作者: Zhang, Jinpeng ; Zhao, Xiaofeng ; Gao, Ning ; Zhang, Hao ; Ma, Xiulan ; Pan, Zequn

The purpose of this study is to enhance the biodegradability of atrazine with FH-1 and NJ-1 alone by selecting the mixing ratio, optimizing the culture medium and conditions. The results showed that FH-1 and NJ-1 have the best biodegradation effect on atrazine being mixed in a volume ratio of 3:2. In a single factor experiment, sucrose and NH₄Cl provided carbon and nitrogen sources for the mixed bacteria. Subsequently, composition of fermentation medium was further optimized using Box-Behnken design of response surface methodology. Based on the results, growth of mixed bacteria and biodegradation of atrazine performed best effects with a biodegradation rate of 85.6% when sucrose and NH₄Cl amounts were 35.30 g/L and 10.28 g/L. The optimal medium condition was 10% inoculum of mixed bacteria, with initial atrazine concentration of 50 mg/L, neutral or weakly alkaline pH value, 30°C. The biodegradation rate reached 97.4%, 11.8% higher than the unoptimized condition.

1988-01-01·Chemical and Pharmaceutical Bulletin4区 · 医学

Estimation of the rates of available fraction for some 4-substituted acetophenone derivatives in the rat: Reversible drug-metabolite pharmacokinetics.

4区 · 医学

Article

作者: ASADA, SHOZO ; OTAWA, TOMOKO ; NAKAE, HIROKO ; NAGAMINE, SACHIKO

4-Acetamidoacetophenone, 4-acetylbenzenesulfonamide, and acetohexamide and the resp. reduced compounds, 4-substituted α-hydroxyethylphenyl derivatives, are in a reversible drug-metabolite relationship in rats.The pharmacokinetic profiles of these agents were studied after intraportal (pv) administration in comparison with those after i.v. administration using an interconversion model.Fundamental clearances, CL₁₀, CL₁₂, CL₂₀ and CL₂₁, were calculated using four AUC (area under the plasma concentration-time curve) values obtained after i.v. administration of the drug and preformed metabolite.The hepatic available fraction of parent drug, F_H1 and sequential hepatic available fraction of its metabolite, F_H2, also were estimated

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适应症	最高研发状态	国家/地区	公司	日期
HIV感染	临床前	日本	Kumamoto University	2022-10-12
HIV感染	临床前	日本	Science Farm Co. Ltd.	2022-10-12
HIV感染	临床前	土耳其	KOC University	2022-10-12