• Bulletin of the Korean Chemical Society
• /
• v.33 no.12
• /
• pp.4074-4078
• /
• 2012

The first step in the common pathway for the biosynthesis of branched chain amino acids is catalyzed by acetohydroxyacid synthase (AHAS). The AHAS is found in plants, fungi and bacteria. With an aim to identify new anti-tuberculosis drugs that inhibit branched chain amino acid biosynthesis, we screened a chemical library against Mycobacterium tuberculosis AHAS. The screening identified four compounds, AVS 2087, AVS 2093, AVS 2236, and AVS 2387 with $IC_{50}$ values of 0.28, 0.21, 3.88, and $0.25{\mu}M$, respectively. Moreover, these four compounds also showed strong inhibition against reconstituted AHAS with $IC_{50}$ values of 0.37, 0.26, 1.0, and $1.18{\mu}M$, respectively. The basic scaffold of the AVS group consists of 1-pyrimidin-2-yl-1H-[1,2,4]-triazole-3-sulfonamide. The most active compound, AVS 2387, showed the lowest total interaction energy -8.75 Kcal/mol and illustrates its binding mode by hydrogen bonding with $H_{\varepsilon}$ of Gln517 with the distance of $2.24{\AA}$.

• Korean Journal of Plant Resources
• /
• v.22 no.6
• /
• pp.552-557
• /
• 2009

Allicin, a garlic componente, is believed to provide protection against various diseases including inflammation. Since interactions of the cell adhesion molecules are known to play important roles in mediating inflammation, inhibiting adhesion protein upregulation is a possible therapeutic target. In this study, we demonstrate that TNF-${\alpha}$- and catalase-induced expression of ICAM-1 on human lung epithelial cells (A549) in a dose-dependent manner and catalase expression and activity were also increased in TNF-${\alpha}$-treated cells. Treatment of the TNF-${\alpha}$-treated cells with catalase inhibitor 3-amino-1,2,4-triazole resulted in a significant decreased the level of ICAM-1. These data suggest that induction of ICAM-1 expression by TNF-${\alpha}$ is associated with catalase. In addition, allicin was found to inhibit the TNF-${\alpha}$ induced expression of ICAM-1 on the A549 cells. This compound also inhibited the production of catalase induced by TNF-${\alpha}$, which suggests that the inhibition of ICAM-1 expression by allicin may be due to the modulated production of catalase.

• Journal of Microbiology
• /
• v.33 no.3
• /
• pp.239-243
• /
• 1995

Deinococcus radiophilus, an UV resistant bacterium seemed to contain three issoenzymes of catalase. Among them, the samllest and most abundant species in cell-free extract, catalase-3 which also exhibited peroxidase activity was purified to electrophoretic homogeneity (145-fold purification) by chromatographic procedures. Its molecular weight was 155 kDa composed of four 38 kDa subunits. The $K_{m}$ value of catalase-3 for H$\_$2/O$\_$2/ was approximately 0.5 mM. This enzyme showed a typical ferric heme spectrum with maximum absorption at 405 nm. Upon binding to cyanide, the 405 nm peak shifted to 420 nm. Catalase-3 was very sensitive to inhibitors of heme proteins, such as cyanide, azide and hydroxylamine. A ratio of A$\_$405/A$\_$28O/ was 0.5 Catalase-3 was active over a wide range of pH, between pH 7 and 10. The enzyme was rather heat-labile and partially sensitive to edthanol-chloroform treatment, but resistant to 3-amino-1, 2, 4-triazole. Catalase-3 of D. radiophilus, which is a bifunction catalatic peroxidatic enzyme seemed to share certain molecular properties with the typical catalase and the catalase-[roxidase along with its own unique features.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.12
• /
• pp.3943-3949
• /
• 2012

A series of aromatic hydrazides 3a-j were prepared by refluxing esters 2a-j with hydrazine hydrate in methanol, which were prepared by the esterification of 1a-j. Acetohydrazides 3a-j upon treatment with carbon disulfide and methanolic potassium hydroxide yielded potassium dithiocarbazate salts 4a-j, which on refluxing with hydrazine hydrate yielded substituted 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-j. The target compounds 6a-j were synthesized by condensing furan-3-carboxylic acid in the presence of polyphosphoric acid under reflux. The structures of newly synthesized compounds were characterized by IR, $^1H$ NMR, $^{13}C$ NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their urease, acetylcholine esterase inhibition, antioxidant and alkaline phosphatase inhibition activity. Almost all of the compounds 6a-j showed good to excellent activities against urease and acetylcholine esterase more than the reference drugs. Compounds 6f and 6g were more potent scavenger of free radicals than the reference n-propyl gallate. Compound 6b and 6h showed excellent activities of alkaline phosphatase as compare to the reference $KH_2PO_4$.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.12
• /
• pp.4180-4184
• /
• 2012

The target compounds 6-11a-e were synthesized by condensing 4-amino-5-aryl-3H-1,2,4-triazole-3-thiones 5a-f with various aromatic carboxylic acids in the presence of phosphorous oxychloride. The structures of newly synthesized compounds were characterized by IR, $^1H$ NMR, $^{13}C$ NMR, elemental analysis and mass spectrometric studies. All the synthesized compounds were screened for their antibacterial activity. Almost all the tested compounds were potent against four different strains of bacteria when compared with that of reference drug ciprofloxacin. Compounds 6c, 6e, 8d, 9b, 9e, 11a and 11b showed nearly equal or lower MIC values than standard drug, against all four tested bacterial strains but rest of the compounds showed excellent antibacterial activities.

• Journal of Korean Society for Atmospheric Environment
• /
• v.8 no.1
• /
• pp.13-19
• /
• 1992

This study was conducted to determine the efficacy of using uniconazole,[(E)-1-(4-chlorophenyl)-4,4-dimethyl-2-(1,2,4-triazole-1-yl)-1-penten-3-ol)] as a phytoprotectant against $SO_2$ injury in snap been (Phaseolus vulgaris L. 'Strike'). Thirteen days prior to $SO_2$ fumigation, plants were given a 100 ml soil drench of uniconazole solution at concentrations of 0.02, 0.10, 0.25 and 0.50 mg/pot. All four uniconazole concentrations were significantly effective in providing protection against $SO_2$ exposure(3 h at 1.5 ppm), but uniconazole treatment above 0.02 mg/pot severely reduced stem elongation, leaf enlargement, flowering date and pod number and weight. Uniconazole treatment had little or no effect on stomatal conductance but reduced transpiration rate on a whole plant basis by nearly 40%. This may reflect an alteration in canopy structure by reducing stem elongation and leaf enlargement. Although uniconazole did not increase the activities of superoxide dismutase(SOD) and peroxidase(POD) in non-$SO_2$-fumigated plants, it significantly increased those enzyme activities in $SO_2$-fumigated plants. Chlorophyll concentration on the basis of unit area was increased 50-60% by uniconazole. However, the difference was not detected on the basis of dry weight. $SO_2$ increased variable chlorophyll fluorescence (Fv) 48% after 1.5 h of exposure in non-uniconazole treated plants but decreased Fv in the plants after 3 h of exposure. By appliing uniconazole, it was possible to maintain high Fv values in the latter group of plants. These results suggest that the phytoprotective effects of uniconazole are related to its growth-retarding properties as an anti-gibberellin as well as the increase of activites of free radical scavengers such as SOD and POD.

• Bulletin of the Korean Chemical Society
• /
• v.35 no.5
• /
• pp.1356-1364
• /
• 2014

A new conjugated copolymer, poly{4,8-bis(triisopropylsilylethynyl)benzo[1,2-b:4,5-b']dithiophene-alt-4,7- bis(5-thiophen-2-yl)-5,6-difluoro-2-(heptadecan-9-yl)-2H-benzo[d][1,2,3]triazole} (PTIPSBDT-DFDTBTz), is synthesized by Stille coupling polycondensation. The synthesized polymer has a band gap energy of 1.9 eV, and it absorbs light in the range 300-610 nm. The hole mobility of a solution-processed organic thin-film transistor fabricated using PTIPSBDT-DFDTBTz is $3.8{\times}10^{-3}cm^2V^{-1}s^{-1}$. Bulk heterojunction photovoltaic cells are fabricated, with a conventional device structure of ITO/PEDOT:PSS/polymer:$PC_{71}BM$/Ca/Al ($PC_{71}BM$ = [6,6]-phenyl-$C_{71}$-butyric acid methyl ester); the device shows a power conversion efficiency (PCE) of 2.86% with an open-circuit voltage ($V_{oc}$) of 0.85 V, a short-circuit current density ($J_{sc}$) of 7.60 mA $cm^{-2}$, and a fill factor (FF) of 0.44. Inverted photovoltaic cells with the structure ITO/ethoxylated polyethlyenimine/ polymer:$PC_{71}BM/MoO_3$/Ag are also fabricated; the device exhibits a maximum PCE of 2.92%, with a $V_{oc}$ of 0.89 V, a $J_{sc}$ of 6.81 mA $cm^{-2}$, and an FF of 0.48.

• Radiation Oncology Journal
• /
• v.23 no.4
• /
• pp.211-216
• /
• 2005

Purpose: It has been reported that all-trans retinoic acid (ATRA) can inhibit glioma growing in vitro. However, clinical trials with ATRA alone in gliomas revealed modest results. ATRA has been shown to increase radiosensitivity in other tumor types, so combining radiation and ATRA would be one of alternatives to increase therapeutic efficacy in malignant gliomas. Thus, we intended to know the role of catalase, which is induced by ATRA, for radiosensitivity if radiation-reduced reactive oxygen species (ROS) is removed by catalase, the effect of radiation will be reduced. Materials and Methods: A rat glioma cell line (36B10) was used for this study. The change of catalase activity and radiosensitivity by ATRA, with or without 3-amino-1, 2, 4-triazole (ATZ), a chemical inhibitor of catalase were measured. Catalase activity was measured by the decomposition of $H_2O_2$ spectrophotometrically Radiosensitivity was measured with clonogenic assay. Also ROS was measured using a 2, 7-dichlorofluorescein diacetate spectrophotometrically. Results: When 36B10 cells were exposed to 10, 25 and $50{\mu}M$ of ATRA for 48 h, the expression of catalase activity were increased with increasing concentration and incubation time of ATRA. Catalase activity was decreased with increasing the concentration of AT (1, $10{\mu}M$) dose-dependently. ROS was increased with ATRA and it was augmented with the combination of ATRA and radiation. ATZ decreased ROS production and increased cell survival in combination of ATRA and radiation despite the reduction of catalase. Conclusion: The increase of ROS is one of the reasons for the increased radiosensitivity in combination with ATRA. The catalase that is induced by ATRA doesn't decrease ROS production and radiosensitivity.

• Journal of Chest Surgery
• /
• v.46 no.1
• /
• pp.14-21
• /
• 2013

Background: Reactive oxygen species (ROS) are known to be related to cardiovascular diseases. Many studies have demonstrated that angiotensin-converting enzyme inhibitors have beneficial effects against ROS. We investigated the antioxidant effect of captopril and enalapril in nitric oxide mediated vascular endothelium-dependent relaxations. Materials and Methods: Isolated rabbit abdominal aorta ring segments were exposed to ROS by electrolysis of the organ bath medium (Krebs-Henseleit solution) after pretreatment with various concentrations (range, $10^{-5}$ to $3{\times}10^{-4}$ M) of captopril and enalapril. Before and after electrolysis, the endothelial function was measured by preconstricting the vessels with norepinephrine ($10^{-6}$ M) followed by the cumulative addition of acetylcholine (range, $3{\times}10^{-8}$ to $10^{-6}$ M). The relevance of the superoxide anion and hydrogen peroxide scavenging effect of captopril and enalapril was investigated using additional pretreatments of diethyldithiocarbamate (DETCA, 0.5 mM), an inhibitor of Cu/Zn superoxide dismutase, and 3-amino-1,2,4-triazole (3AT, 50 mM), an inhibitor of catalase. Results: Both captopril and enalapril preserved vascular endothelium-dependent relaxation after exposure to ROS in a dose-dependent manner (p<0.0001). Pretreatment with DETCA attenuated the antioxidant effect of captopril and enalapril (p<0.0001), but pretreatment with 3AT did not have an effect. Conclusion: Both captopril and enalapril protect endothelium against ROS in a dose-dependent fashion in isolated rabbit abdominal aortas. This protective effect is related to superoxide anion scavenging.

• Journal of Korean Society of Environmental Engineers
• /
• v.27 no.6
• /
• pp.606-613
• /
• 2005

The badge-type diffusive sampler for the measurement of formaldehyde in indoor air using three types of colorimetric methods such as chromotrophic acid(CTA), 3-methyl-2-benzothiazolinone hydrazone(MBTH), and 4-amino-3-hydrazino-5-mercapto-1,2,4-triazole(AHMT) method. The washing of the collection filter with several cleaning solution was effected with satisfactory results, regardless of the types of cleaning solutions. The concentrations of absorbance solution in each colorimetric method were experimentally determined by considering the sampling rates. The variation blank values in each colorimetric method was below 15%. As compared with CTA and AHMT methods, the reproducibility of MBTH method was excellent and was below 10% relative standard deviation. The collected formaldehyde mass and time-weighted concentration had a good correlation (correlation coefficient > 0.93). The limit of detection and limit of quantitation, and minimum sampling time were closely correlated to the sampling rates for the measurement of formaldehyde in each method.