• The Korean Journal of Pesticide Science
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• v.5 no.2
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• pp.13-17
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• 2001

A synthesis of new 2-phenylimino-1,3-thiazolines 2 for the purpose of development of new agrochemical fuugicide was described. Reaction of chlorine with diketene followed by treatment of benzylamine without isolation of intermediate 8a gave ${\gamma}-chloro-{\beta}-keto$ benzylamide 10a. Thioureas 4 obtained from the reaction of methyl isothiocyanate with aniline derivatives were subjected to 10a in acetone solution to afford the corresponding 2-phenylimino-1,3-thiazoline hydrochloric acid salts 2 through unisolable inltermediates 11 and 12. The plausible reaction mechanism including nucleophilic attack of sulfur assisted neighboring nitrogen lone pair electron on phenyl of thiourea 4 was discussed.

• Journal of the Korean Society of Food Science and Nutrition
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• v.33 no.6
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• pp.946-950
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• 2004

Young radishes which were grown in the soil containing sulfur increased quinine reductase (QR) activity in Hepa 1clc cells and isothiocyanate-like compound analyzed by HPLC. QR inducing activity was maximum in young radishes grown with 1,818 g/㎥ sulfur and was decreased when the soil was neutralized with lime mortar in order to improve a recovery. These results have suggested that consumption of young radishes, especially grown in the presence of sulfur, would prevent from cancer incidence through inducing detoxification enzymes and could have therapeutic effects for chemoprevention.

• Journal of the korean academy of Pediatric Dentistry
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• v.36 no.2
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• pp.217-226
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• 2009

Allyl isothiocyanate (AIT), the principle ingredient of antimicrobial ingredients from horseradish root, can be prepared from extracts of horseradish root or synthetic method. It is reported that the horseradish root extract has the antimicrobial effect against various oral microorganisms, while there is no further study about the antimicrobial effect against the oral microorganisms of synthetic AIT derived from synthetic method. The aim of the study is to compare the difference of the antimicrobial effect between horseradish root extracts and synthetic AIT. To evaluate the antimicrobial effect, we measured the minimum inhibitory concentration(MIC) and minimum bactericidal concentration (MBC), and the results are like following. 1. The MIC of horseradish root extract against 7 kinds of oral pathogenic microorganisms is about 117$\sim$1,750 ppm(0.0117$\sim$0.175%), and the MIC of the synthetic AIT is about 344$\sim$3,000 ppm(0.0344$\sim$0.3%), which have the antimicrobial effects against all kinds of microorganisms. 2. The MBC of the horseradish root extracts against the 7 kinds of oral microorganisms is about 625.2$\sim$6,000 ppm(0.06252$\sim$0.6%), and the MBC of the synthetic AIT is about 1,750$\sim$7,000 ppm(0.175$\sim$0.7%), which have the antimicrobial effects against all kinds of microorganisms.

• Journal of Applied Biological Chemistry
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• v.54 no.4
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• pp.279-283
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• 2011

Toll-like receptors (TLRs) play an important role in induction of innate immune responses. The activation of TLRs triggers inflammatory responses that are essential for host defense against invading pathogens. Phenethyl isothiocyanate (PEITC) extracted from cruciferous vegetables has an effect on anti-inflammatory therapy. Dysregulated activation of nuclear factor-${\kappa}$B (NF-${\kappa}$B), inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) has been shown to play important roles in the development of certain inflammatory disease. To evaluate the therapeutic potential of PEITC, NF-${\kappa}$B activation and COX-2 and iNOS expression induced by lipopolysaccharide (LPS, TLR4 agonist), polyinosinic-polycytidylic acid (Poly[I:C], TLR3 agonist), 2 kDa macrophageactivating lipopeptide (MALP-2, TLR2 and TLR6 agonist) or oligodeoxynucleotide 1668 (ODN1668, TLR9 agonist) were examined. PEITC inhibits the activation of NF-${\kappa}$B induced by LPS or Poly[I:C] but not by MALP-2 or ODN1668. PEITC also suppressed the iNOS expression induced by LPS or Poly[I:C]. However, PEITC did not suppress COX-2 expression induced by LPS, Poly[I:C], MALP-2, or ODN1668. These results suggest that PEITC has the specific mechanism for antiinflammatory responses.

• Journal of Life Science
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• v.15 no.3 s.70
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• pp.397-405
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• 2005

Sulforaphane, an isothiocyanate derived from hydrolysis of glucoraphanin in broccoli and other cruciferous vegetables, was shown to induce phase II detoxification enzymes and inhibit chemically induced mammary tumors in rodents. Recently, sulforaphane is known to induce cell cycle arrest and apoptosis in human cancer cells, however its molecular mechanisms are poorly understood. In the present study, we demonstrated that sulforaphane acted to inhibit proliferation and induce morphological changes of human cervical carcinoma HeLa cells. Treatment of HeLa cells with $10{\mu}M\;or\;15{\mu}M$ sulforaphane resulted in significant G2/M cell cycle arrest as determined by flow cytometry. Moreover, $20{\mu}M$ sulforaphane significantly induced the population of sub-G1 cells (9.83 fold of control). This anti-proliferative effect of sulforaphane was accompanied by a marked inhibition of cyclin A and cyclin-dependent kinase (Cdk)4 protein and concomitant induction of Cdc2, Cdk inhibitor p16 and p21. However, sulforaphane did not affect the levels of cyelooxygenases and telomere-regulatory gene products. Although further studies are needed, the present work suggests that sulforaphane may be a potential chemoprevetive/ chemotherapeutic agent for the treatment of human cancer cells.

• Bulletin of the Korean Chemical Society
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• v.23 no.1
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• pp.41-47
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• 2002

The reactions of 3-methyl-1-phenyl-5-oxo-${\Delta}^2$-pyrazoline-4-thiocarbohydrazide towards phenyl isothiocyanate, sodium nitrite, cyclohexanone, aromatic aldehydes, and carbon disulphide has been studied. The Vilsmeier-Haack reaction has been applied on 4-substituted pyrazolone derivatives.

• Bulletin of the Korean Chemical Society
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• v.32 no.5
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• pp.1461-1462
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• 2011

• Archives of Pharmacal Research
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• v.14 no.1
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• pp.78-80
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• 1991

Ten 1,2,4-thiadiazolidines were synthesized and screened for their anti-inflammatory and analgesic activities. Butyl isothiocyanate was used as a starting material. Several compounds showed significant anti-inflammatory and analgesic activities. The unsubstituted and o-methyl, p-acetoxy and o-chloro substituted compounds were found to be more potent anti-inflammatory and analgesic agents than the other compounds.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.381-384
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• 1995

Covalent binding of the reactive metabolites of SC_42867 to microsomal proteins has been examined. In the absence of inhibitor of cytochrome oxydase (.alpha.-naphtyl-isothiocyanate) or a radical scavenger (3-terthiobuty-4-hydroxyanisol), up to 4.0% of total redioactivity used in the assay could irreversibly bind to proteins. In the presence of an inhibitor, the highest percentage of covalent binding observed is 0.7% a significant decrease of the metabolism of SC42876 was observed. These results suggest in a cytochrome P-450 dependent generation of SC_42867 metabolites significantly take part in the covalent binding process.

• Bulletin of the Korean Chemical Society
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• v.33 no.7
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• pp.2385-2388
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• 2012