A5019064611- Chemical Synthesis and Analysis
- Neuropeptides and Animal Physiology
- Protease and Inhibitor Mechanisms
- Blood Coagulation and Thrombosis Mechanisms
- Receptor Mechanisms and Signaling
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Peptidase Inhibition and Analysis
- Enzyme Production and Characterization
- Biochemical and Structural Characterization
- Pharmacological Receptor Mechanisms and Effects
- Synthesis and Biological Evaluation
- Synthesis and Reactions of Organic Compounds
- Pain Mechanisms and Treatments
- Click Chemistry and Applications
- DNA and Nucleic Acid Chemistry
- Tuberculosis Research and Epidemiology
- Computational Drug Discovery Methods
- Neuroendocrine Tumor Research Advances
- Carbohydrate Chemistry and Synthesis
- Cell Adhesion Molecules Research
- Blood properties and coagulation
- Mycobacterium research and diagnosis
- Hemophilia Treatment and Research
- Glycosylation and Glycoproteins Research
- RNA Interference and Gene Delivery
Osaka Prefectural Institute of Public Health
2025
Kobe Gakuin University
2014-2023
Wakayama Medical University
2020-2021
Pharmaceutical Biotechnology (Czechia)
1981-2017
Tokai University
2015
Ebara (Japan)
2014
Hoshi University
2014
Osaka Medical and Pharmaceutical University
2010-2013
Semmelweis University
2008
Kyoto Institute of Technology
2008
Purpose: Ophthalmologic examinations were conducted on atomic bomb (A‐bomb) survivors 55 years after exposure.Materials and methods: A‐bomb who had been exposed before 13 of age at the time bombings in 1945 or examined a previous study between 1978 1980. The examinations, June 2000 September 2002, included slit‐lamp examination, digital photography cataract grading system for three parts lens (nucleus, cortex posterior subcapsule) as an outcome variable. Proportional odds logistic regression...
The structure of gymnemagenin (3β, 16β, 21β, 22α, 23, 28-hexahydroxy-olean-12-ene), the sapogenin antisweet principles Gymnema sylvestre, was established by X-ray analysis 3β, 23;21β, 22α-di-O-isopropylidene derivative. On basis this result, deacylgymnemic acid elucidated as 3-O-β-glucuronide from carbon-13 nuclear magnetic resonance spectra.Five principles, gymnemic acid-III, -IV, -V, -VIII, and -IX, were isolated in pure states hot water extract leaves sylvestre. Of these, three (GA-III,...
Background: The clinical treatment of various types pain relies upon the use opioid analgesics. However most them produce, in addition to analgesic effect, several side effects such as development dependence and addiction well sedation, dysphoria, constipation. One solution these problems are chimeric compounds which pharmacophore is hybridized with another type compound incease antinociceptive effects. Neurotensin-induced antinociception not mediated through system. Therefore, hybridizing...
The zymogen protease plasminogen and its active form plasmin perform key roles in blood clot dissolution, tissue remodeling, cell migration, bacterial pathogenesis. Dysregulation of the plasminogen/plasmin system results life-threatening hemorrhagic disorders or thrombotic vascular occlusion. Accordingly, inhibitors this are clinically important. Currently, tranexamic acid (TXA), a molecule that prevents activation through blocking recruitment to target substrates, is most widely used...
Abstract Regional disparities in the incidence of tuberculosis (TB) pose several challenges to effective TB control. This study aimed investigate such Osaka City, Japan, by analyzing relationship between and residents’ socioeconomic indicators. Using 42 indicators from 2010 population census, city was clustered into 15 social areas through a factor analysis, during 2012–2016 compared across 4,852 cases. Two geographically adjacent (Area D O) exhibited significantly higher rates, each with...
The C terminus of endomorphin-2 (EM-2) analogues (Tyr-Pro-Phe-NH-X) was modified with aromatic, heteroaromatic, or aliphatic groups (X = phenethyl,benzyl, phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, tert-butyl, cyclohexyl, adamantyl; 3-18) to study their effect on opioid activity. Only 9 (1-naphthyl), 11 (5-quinolyl), 16 (cyclohexyl), and 18 (2-adamantyl) exhibited mu-opioid receptor affinity in the nanomolar range (K(i) 2.41-6.59 nM), which, however, 3- 10-fold less than parent...
Six analogues of tyrosine, which contained alkyl groups at positions 2', 3', and 6', either singly or in combination on the tyramine ring, were investigated for their effect opioid activity [Xaa1]endomorphin-2 (EM-2). The displayed following characteristics: (i) high μ-opioid receptor affinity [Ki(μ) = 0.063−2.29 nM] with selectivity [Ki(δ)/Ki(μ)] ranging from 46 to 5347; (ii) potent functional agonism [GPI assay (IC50 0.623−0.924 nM)] a correlation between δ-opioid affinities bioactivity...
Endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH2) and [Dmt1]EM-2 (Dmt = 2',6'-dimethyl-l-tyrosine) analogues, containing alkylated Phe3 derivatives, 2'-monomethyl (2, 2'), 3',5'- 2',6'-dimethyl (3, 3', 4', respectively), 2',4',6'-trimethyl (6, 6'), 2'-ethyl-6'-methyl (7, 7'), 2'-isopropyl-6'-methyl (8, 8') groups or Dmt (5, 5'), had the following characteristics: (i) [Xaa3]EM-2 analogues exhibited improved μ- δ-opioid receptor affinities. The latter, however, were inconsequential (Kiδ 491−3451 nM). (ii)...
To determine the effect of 2,2′‐azobis(2‐amidinopropane) dihydrochloride (AAPH) on ultrasound (US)‐induced cell killing, human monocytic leukemia cells (U937) were incubated at various temperatures (25.0, 37.0 and 40.0°C) for 1 min in air‐saturated phosphate‐buffered solution (PBS) containing 50 m M AAPH before exposure to nonthermal MHz US an intensity 2.0 W/cm 2 . Cell viability was determined by means Trypan blue dye exclusion test immediately after sonication. Apoptosis measured 6‐h...
Novel bioactive opioid mimetic agonists containing 2′,6′-dimethyl-l-tyrosine (Dmt) and a pyrazinone ring interact with μ-and δ-opioid receptors. Compound <b>1</b> [3-(4′ -Dmt-aminobutyl)-6-(3′-Dmt-aminopropyl)-5-methyl-2(1<i>H</i>)pyrazinone] exhibited high μ-opioid receptor affinity selectivity (<i>K</i><sub>i</sub>μ = 0.021 nM <i>K</i><sub>i</sub>δ/<i>K</i><sub>i</sub>μ 1,519, respectively), agonist activity on guinea pig ileum (IC<sub>50</sub> 1.7 nM) weaker δ-bioactivity mouse vas...
The inability of opioid peptides to be transported through epithelial membranes in the gastrointestinal tract and pass blood−brain barrier limits their effectiveness for oral application an antinociceptive treatment regime. To overcome this limitation, we enhanced hydrophobicity while maintaining aqueous solubility properties a class opioid-mimetic substances by inclusion two identical N-termini consisting Dmt (2',6'-dimethyl-l-tyrosine) coupled pyrazinone ring platform means alkyl chains...
Unique opioid mimetic substances containing identical N-terminal aromatic residues separated by an unbranched alkyl chain two to eight methylene groups were developed. Regardless of the length interposing chain, bis-Tyr and bis-Phe compounds inactive; however, replacement a single Dmt (2',6'-dimethyl-l-tyrosine) residue enhanced activity orders magnitude. Moreover, bis-Dmt another 10-fold more potent with optimum intra-aromatic ring distance about four six units. 1,4-Bis(Dmt-NH)butane (7)...
Abstract γ‐Glutamylcyclotransferase (GGCT) depletion inhibits cancer cell proliferation. However, whether the enzymatic activity of GGCT is critical for regulation growth remains unclear. In this study, a novel diester‐type cell‐permeable prodrug, pro‐GA, was developed based on structure N ‐glutaryl‐ l ‐alanine (GA), by optimization using temporary fluorophore‐tagged prodrug candidates. The antiproliferative pro‐GA demonstrated GGCT‐overexpressing NIH‐3T3 cells and human including MCF7,...