• Journal of the Korean Chemical Society
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• v.55 no.4
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• pp.590-593
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• 2011

A novel organotin(IV) complex has been prepared from $Bu_2SnCl_2$ and the N, O and S donor ligand, 5-(p-dimethylaminobenzylidene) rodanine (HL). The ligand is deprotonated in the presence of a base and the complex with the general formula $SnBuCl_2L$ is formed. This complex was fully characterized by IR, $^1H$ NMR and $^{119}Sn$ NMR and elemental analysis. Spectroscopic data indicate the ligand is coordinated through the oxygen atom to the tin and the coordination number of four is supported by $^{119}Sn$ NMR data in solution.

• Biomolecules & Therapeutics
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• v.18 no.1
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• pp.77-82
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• 2010

Peroxisome proliferator-activated receptor $\gamma$ (PPAR${\gamma}$) is a ligand-activated transcription factor that is used as a target for anti-diabetic drug development. In a search for novel PPAR${\gamma}$ agonists, the $\beta$-carboxyethyl-rhodanine derivative SP1818 was identified. We report here the characteristics of SP1818 as a selective PPAR${\gamma}$ agonist. In transactivation assays, SP1818 selectively activated PPAR${\gamma}$, but the degree of PPAR${\gamma}$ stimulation was less than with $1{\mu}M$ rosiglitazone. SP1818 also stimulated glucose uptake in a concentration-dependent manner. The adipocyte differentiation markers adiponectin, scavenger receptor CD36 and aP2 were weakly induced by treatment with SP1818, and TRAP220 subunit was specifically recruited into PPAR${\gamma}$ activated by rosiglitazone but not PPAR${\gamma}$ activated by SP1818.

• Korean Journal of Veterinary Research
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• v.62 no.4
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• pp.31.1-31.5
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• 2022

A 12-year-old intact male Dalmatian dog presented hyporexia and vomiting for 1 week. Blood analysis revealed increased liver enzyme activity. Histopathological examination of the liver confirmed chronic hepatitis with fibrosis and necrosis. Copper staining revealed marked copper accumulation (2,770 ppm; normal range, 200 to 400 ppm), prominent in the centrilobular region, and compatible with copper-associated chronic hepatitis. However, copper metabolism domain containing 1 (COMMD1) mutation predisposing to copper accumulation in the liver tissue was not identified. The dog received medications but died 1 month after first visit. This is the first case of primary copper-associated hepatitis without COMMD1 mutation in a Dalmatian dog in South Korea.

• Bulletin of the Korean Chemical Society
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• v.26 no.2
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• pp.285-291
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• 2005

The nonstructural protein 5B (NS5B) of hepatitis C virus (HCV) is the viral RNA-dependent RNA polymerase (RdRp), which is the essential catalytic enzyme for the viral replication and is an appealing target for the development of new therapeutic agents against HCV infection. A small amount of serum from a single patient with hepatitis C was used to get the genome of a Korean HCV isolate. Sequence analysis of NS5B 1701 nucleotides showed the genotype of a Korean isolate to be subtype 1b. The soluble recombinant HCV NS5B polymerase lacking the C-terminal 24 amino acids was expressed and purified to homogeneity. With the highly purified NS5B protein, we established in vitro systems for RdRp activity to identify potential polymerase inhibitors. The rhodanine family compounds were found to be potent and specific inhibitors of NS5B from high throughput screening (HTS) assay utilizing the scintillation proximity assay (SPA) system. The binding mode of an inhibitor was analyzed by measuring various kinetic parameters. Lineweaver-Burk plots of the inhibitor suggested it binds not to the active site of NS5B polymerase, but to an allosteric site of the enzyme. The activity of NS5B in in vitro polymerase reactions with homopolymeric RNA requires interaction with multiple substrates that include a template/primer and ribonucleotide triphosphate. Steady-state kinetic parameter, such as Km, was determined for the ribonucleotide triphosphate. One of compounds found interacts directly with the viral polymerase and inhibits RNA synthesis in a manner noncompetitively with respect to UTP. Furthermore, we also investigated the ability of the compound to inhibit NS5B-directed viral RNA replication using the Huh7 cell-based HCV replicon system. The investigation is potentially very useful for the utility of such compounds as anti-hepatitic agents.

• Journal of Veterinary Clinics
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• v.28 no.2
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• pp.249-253
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• 2011

A 4-year-old intact female American Cocker Spaniel presented with lack of appetite, shivering, and abdominal distension. It was initially diagnosed with chronic hepatitis with cirrhosis, by serum chemistry, radiography, ultrasonography, and histopathologic examination following liver biopsy. Abundant copper granules were detected in most hepatocytes with rhodanine stain, with hepatic copper concentration at 1460 ppm (reference range: <400 ppm). Based on these findings, copper-associated hepatitis with cirrhosis was diagnosed and successfully managed with long-term D-penicillamine, s-adenosylmethionine, biphenyl-dimethyl-dicarboxylate and supportive care. The spaniel died 35 months after diagnosis.