A5029603403- Effects and risks of endocrine disrupting chemicals
- Toxic Organic Pollutants Impact
- Carcinogens and Genotoxicity Assessment
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and biological activity
- Drug-Induced Hepatotoxicity and Protection
- Synthesis of heterocyclic compounds
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Pesticide Exposure and Toxicity
- Drug Transport and Resistance Mechanisms
- Pharmacogenetics and Drug Metabolism
- Quinazolinone synthesis and applications
- Estrogen and related hormone effects
- Synthesis and Reactivity of Heterocycles
- Synthesis and Reactions of Organic Compounds
- Click Chemistry and Applications
- Alcohol Consumption and Health Effects
- Liver Disease Diagnosis and Treatment
- Chemical Synthesis and Analysis
- Environmental Toxicology and Ecotoxicology
- Multicomponent Synthesis of Heterocycles
- Eicosanoids and Hypertension Pharmacology
- Air Quality and Health Impacts
Saitama Prefectural University
2024-2025
Nihon Pharmaceutical University
2015-2024
Saitama Prefecture
2017-2024
China Medical University
2016
Gifu Pharmaceutical University
2015
Okayama University
2014
Hiroshima International University
2012
Hiroshima University
2008-2012
PhoenixBio (Japan)
2012
An increasing number of studies are reporting the existence polybrominated diphenyl ethers (PBDEs) and their hydroxylated (HO) methoxylated (MeO) metabolites in environment tissues from wildlife humans.Our aim was to characterize compare agonistic antagonistic activities principle PBDE congeners HO MeO against human nuclear hormone receptors.We tested receptor estrogen alpha (ERalpha), ERbeta, androgen (AR), glucocorticoid (GR), thyroid alpha(1) (TRalpha(1)), TRbeta(1) BDEs 15, 28, 47, 85,...
To develop novel nonallergenic pyrazolone analgesics, we synthesized a series of compounds in which position 1 the ring was substituted place original methyl group order to block formation allergenic metabolites via N-dealkylation. These analogues were found show as potent an antipyretic and analgesic effect antipyrine (AT). In examination allergenicity, AT induced typical skin reaction guinea pigs, whereas inactive. When administered (po) rats, norantipyrine (NORA) active metabolite...
Indoor dust is a sink for many kinds of pollutants, including flame retardants (FRs), plasticizers, and their contaminants degradation products. These pollutants can be migrated to indoor from household items such as televisions computers. To reveal high-priority end points contaminant candidates in dust, using CALUX reporter gene assays based on human osteosarcoma (U2OS) cell lines, we evaluated characterized the endocrine-disrupting potencies crude extracts collected Japan (n = 8), United...
The affinity for thyroid hormone receptor (TR) of polybromodiphenyl ethers (PBDEs) and hydroxylated PBDEs was examined. 4-Hydroxy-2,2',3,4',5-pentabromodiphenyl ether (4-OH-BDE-90) 3-hydroxy-2,2',4,4'-tetrabromodiphenyl (3-OH-BDE-47) markedly inhibited the binding triiodothyronine (1×10-10 M) to TR in concentration range 1×10-6-1×10-4 M. 2,3,4,5,6-Pentabromophenol (PBP) also showed an inhibitory effect at 1×10-5-1×10-4 However, 2,2',3,4,4',5'-hexabromodiphenyl (BDE-138), decabromodiphenyl...
The convenient and efficient one‐pot acid catalytic cyclization synthesis of imidazo[4,5‐c]pyrazoles or/and pyrazolo[3,4‐d]pyrimidines were individually developed by the reaction 5‐amino‐4‐nitrosopyrazoles with Vilsmeier reagent (HCONH2/POCl3)under mediated solution. In newly method imidazo[4,5‐c]pyrazoles, used as starting materials transformation process was involved denitrosation, amidination form (HCONH2/POCl3), cyclization, substitution, hydrogen migration five steps. This would be...
1. Hydrolytic metabolism of methyl-, ethyl-, propyl-, butyl-, heptyl- and dodecylparaben by various tissue microsomes plasma rats, as well human liver small-intestinal microsomes, was investigated the structure–metabolic activity relationship examined.2. Rat showed highest toward parabens, followed lung microsomes. Butylparaben most effectively hydrolyzed which relatively low hydrolytic towards parabens with shorter longer alkyl side chains.3. In contrast, exhibited higher longer-side-chain...
Prediction of human drug metabolism is important for development. Recently, the number new candidates metabolized by not only cytochrome P450 (P450) but also non-P450 has been increasing. It necessary to consider species differences in between humans and experimental animals. We examined metabolism, especially rats, ibuprofen (<i>S</i>)-naproxen as nonsteroidal anti-inflammatory drugs, which are UDP-glucuronosyltransferase, sulfotransferase, amino acid <i>N</i>-acyltransferase taurine...
An acetaminophen (APAP) overdose can cause hepatotoxicity and lead to fatal liver damage. The hepatoprotective effects of tormentic acid (TA) on (APAP)-induced damage were investigated in mice. TA was intraperitoneally (i.p.) administered for six days prior APAP administration. Pretreatment with prevented the elevation serum aspartate aminotransferase (AST), alanine (ALT), total bilirubin (T-Bil), cholesterol (TC), triacylglycerol (TG), lipid peroxide levels APAP-treated mice markedly...
The oxidative, reductive, and hydrolytic metabolism of methiocarb the carbaryl by liver microsomes plasma rats or humans were examined. effects on their nuclear receptor activities also When was incubated with rat in presence NADPH, sulfoxide, a novel metabolite, sulfone detected. Methiocarb sulfoxide oxidized to reduced back cytosol. Thus, interconversion between found be new metabolic pathway for microsomes. product hydrolysis, which is methylthio-3,5-xylenol (MX), form oxidations...
Parabens, which are a homologous series of esters p-hydroxybenzoic acid, have been used as preservatives in cosmetics, medicines and foods because their antimicrobial activity. However, parabens cosmetics suspected to cause allergic contact dermatitis. In this study, we examined paraben-induced histamine release from rat peritoneal mast cells skin reaction guinea pigs using 17 with different alcohol side chains, ranging methylparaben dodecylparaben. Octylparaben showed the greatest...
The abnormal lipid metabolism in the liver that occurs after high caloric intake is main cause of nonalcoholic fatty disease (NAFLD). Differences between samples from healthy livers and individuals with NAFLD indicate changes function occur during progression. Here, we examined protein expression a model early stages obesity to identify potential alterations function. proteins expressed tissue pre-obese rats were separated via SDS/PAGE stained Coomassie brilliant blue-G250. Peptide mass...
1. Human chimeric mice (h-PXB mice) having humanized liver, constructed by transplantation of human hepatocytes, were evaluated as an experimental model for predicting drug metabolism. Metabolism zaleplon in h-PXB was compared with that rat (r-PXB hepatocytes.
1. When benzophenone-3 (2-hydroxy-4-methoxybenzophenone; BP-3) was incubated with liver microsomes of untreated rats in the presence NADPH, 5-hydroxylated metabolite, 2,5-dihydroxy-4-methoxybenzophenone (5-OH-BP-3), formed as a major novel metabolite BP-3. The 4-desmethylated 2,4-dihydroxybenzophenone (2,4-diOH-BP), previously reported vivo BP-3, also detected. However, amount 5-OH-BP-3 vitro about same that 2,4-diOH-BP.2. oxidase activity affording inhibited by SKF 525-A and ketoconazole,...