• Bulletin of the Korean Chemical Society
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• v.32 no.5
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• pp.1650-1656
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• 2011

A series of potent tricyclic derivatives with a non-aromatic amide as potent PARP-1 inhibitors were successfully synthesized and their PARP-1 inhibitory activity was evaluated. Among the derivatives, 2-(1-propylpiperidin-4-yloxy)-7,8,9,10-tetrahydrophenanthridin-6(5H)-one 23c displayed potent activity in a PARP-1 enzymatic assay and cell-based assay ($IC_{50}$ = 0.142 ${\mu}M$, $ED_{50}$ = 0.90 ${\mu}M$) with good water solubility. Further, molecular modeling studies confirmed the obtained biological results.

• Bulletin of the Korean Chemical Society
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• v.25 no.2
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• pp.195-197
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• 2004

Methyl-4-[[(2E)-3,7-dimethyl-2,6-octadienyl]oxy]-3-hydroxybenzoate (5) has been identified from the New Zealand liverwort Trichocolea hatcheri (T. hatcheri) on the basis of spectroscopic evidence. This compound was tested for its growth inhibitory effects against tumor cell lines, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. It showed growth inhibition activity against Staphylococcus epidermidis (MIC, 1,000 ${\mu}$g/mL). These results suggest that compound 5 possesses antitumoral , antimicrobial and antioxidative activities.

• Environmental Mutagens and Carcinogens
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• v.22 no.3
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• pp.149-156
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• 2002

The detection of many synthetic chemicals used in industry that may pose a genetic hazard in our environment is of great concern at present. Since these substances are not limited to the original products, and enter the environment, they have become widespread environmental pollutants, thus leading to a variety of chemicals that possibly threaten the public health. In this respect, to regulate and to evaluate the chemical hazard will be important to environment and human health. The clastogenicity of 18 synthetic chemicals was evaluated in Chinese hamster lung fibroblast cells in vitro. 4-Chloro-3,5-dimethyl phenol (CAS No. 88-04-0) induced chromosomal aberrations with significance at the concentration of 15.7 $\mu\textrm{g}$/$m\ell$ both in the presence and absence of metabolic activation system. Phenoxybenzene (CAS No. 101-84-8) which is one of the most cytotoxic chemical among 18 chemicals tested revealed no clastogenicity in the range of 0.11-0.43 $\mu\textrm{g}$/$m\ell$ both in the presence and absence of metabolic activation system. From the results of chromosomal aberration assay with 18 synthetic chemicals in Chinese hamster lung cells in vitro, 4-chloro-3,5-dimethyl phenol (CAS No. 88-04-0) revealed weak positive clastogenic results in this study.

• Journal of the Korean Chemical Society
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• v.46 no.6
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• pp.535-540
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• 2002

It is very difficult to analyze the microcystins, cyanobacterial toxins quantitatively since it exists in a trace level in lakes. In this paper, two different analytical methods were tried to analyze the microcystins, cyanobacterial toxins quantitatively in water samples collected in Soyang lake. The first method was solid phase extraction method fol-lowed by High Performance Liquid Chromatography(HPLC), and the second method was Enzyme-Linked Immu-nosorbent Assay(ELISA) using the monoclonal antibody of microcystin.

• BMB Reports
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• v.48 no.2
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• pp.121-126
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• 2015

Here we report a new chemical inhibitor against HIV-1 with a novel structure and mode of action. The inhibitor, designated as A1836, inhibited HIV-1 replication and virus production with a 50% inhibitory concentration ($IC_{50}$) of $2.0{\mu}M$ in an MT-4 cell-based and cytopathic protection antiviral assay, while its 50% cytotoxic concentration ($CC_{50}$) was much higher than $50{\mu}M$. Examination of the effect of A1836 on in vitro HIV-1 reverse transcriptase (RT) and integrase showed that neither were molecular targets of A1836. The characterization and re-infection assay of the HIV-1 virions generated in the presence of A1836 showed that the synthesis of early RT products in the cells infected with the virions was inhibited dose-dependently, due in part to abnormal protein formation within the virions, thus resulting in an impaired infectivity. These results suggest that A1836 might be a novel candidate for the development of a new type of HIV-1 inhibitor.

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.24 no.2
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• pp.160-168
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• 2014

Objectives: Chemical hazard evaluations are important for workers' health and working environments. Allyl chloride (CAS No. 107-05-1) is used in many industries, leading to concerns about the possibility of threats to the health of workers. Since only insufficient or controversial information is available about potential related hazards, an in vitro mammalian chromosomal aberration (CA) assay was conducted in order to gain additional information concerning any such hazards. Moreover, toxicological information from this study could be applied for workers' rights to know, and to prepare or update the Materials Safety Data Sheet (MSDS) for a number of industries. Methods and Results: The assay was performed using the Chinese hamster lung fibroblast cell (ATCC, CRL-1935), by the direct method (-S9) and by the metabolic activated method (+S9 mix). Using the direct method, the seven dosages in the 48-hour treatment group did not show that the frequency of CA is proportionate to the dosage. The frequency of CA is not proportionate to the dosage addition for a six-hour treatment using the metabolic activated method. Conclusions: From these findings, it was decided that this chemical does not induce chromosomal aberrations under the tested conditions.

• Asian-Australasian Journal of Animal Sciences
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• v.17 no.6
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• pp.863-868
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• 2004

Lectin activities and chemical characteristics of Escherichia coli, Lactobacillus spp. and Bifidobacterium spp. originating from the porcine cecal mucosal layer were studied based on hemagglutination assay (HA) and hemagglutination inhibition assay (HIA). Although all the bacterial strains were able to agglutinate erythrocytes of porcine or rabbit origin, much higher HA titers were consistently observed for Lactobacillus spp. than for E. coli or for Bifidobacterium spp. A remarkable reduction in HA titers occurred by the treatment of E. coli and Lactobacillus spp. with protease or trypsin and of Bifidobacterium spp. with protease, trypsin or periodate. There were no significant effects on the HA titers of the three groups of bacteria after the treatment with lipase. Hemagglutination of E. coli was strongly inhibited by D (+)-mannose and D (+)-galactose; Lactobacillus spp. by $\alpha$-L-rhamnose and methyl-$\beta$-galactopyranoside; Bifidobacterium spp. by D (+)-alactose, $\alpha$-L-rhamnose, $\alpha$-L-fucose, L (+)-arabinose, D (+)-mannose, D (-)-fructose at a relatively low concentration (1.43 to 3.75 mg/ml). These results, combined with the enhanced HA activities of the three bacterial strains by modification of rabbit erythrocytes with neuraminidase and abolished HA activity of E. coli after treatment with $\beta$-galactosidase, indicate that it might be the glycoproteinous substances surrounding the surface of the bacterial cells that are responsible for the adhesions of these microorganisms by recognizing the specific receptors on the red blood cell.

• Journal of the Korean Chemical Society
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• v.19 no.4
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• pp.246-251
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• 1975

A spectrophotometric assay technique is descriead for the measurement of free SH-groups in the enzyme reaction mixture. The method utilizes a new substrate, S-hippuryl-thioglycolyl-glycine(S-Hip-thioglycol-Gly) which is the basis for a convenient assay of angiotensin-converting enzyme and other dipeptidyl carboxypeptidases. This substrate contains an appropriately located thioester linkage that is hydrolyzed by the converting enzyme and other dipeptidyl carboxypeptidases. One of the products, thioglycolyl glycine, is readily measured by reaction with Ellman's reagent, 5,5'-dithio-bis-(2-nitrobenzoic acid), DTNB, to produce 5-thio-2-nitrobenzoic acid which has a strong absorption band at 410 nm. The method is sensitive (${\varepsilon}M = 1.36{\times}10^4$ at 412 nm) and can be applied as a continuous recording with DTNB present in the enzymatic reaction mixture.

• Bulletin of the Korean Chemical Society
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• v.34 no.3
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• pp.922-926
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• 2013

3,3',4,4'-Tetrachlorobiphenyl (IUPAC PCB77) is one of seven indicative polychlorinated biphenyls (PCBs) in the surface sediments. The current study presents a novel polyclonal antibody for the determination of the PCB77 using indirect competitive enzyme-linked immunosorbent assay. Under optimum conditions, PCB77 was determined within the concentration range of 0.01-100 ${\mu}g\;L^{-1}$, with a detection limit of 0.057 ${\mu}g\;L^{-1}$. The assays were tested for their cross-reactivity profiles using 3 selected congeners and 4 Aroclor products. The assays were highly specific for coplanar PCB congeners, but less specific for Aroclor1248. The spiked recoveries from five sediment samples were 86%-114% for PCB77 from ELISA, which were satisfactory. The current study demonstrated that the developed antiserum and immunoassay procedure can be used to detect PCB77 in environmental samples. The results of the sediment analysis were confirmed by conventional GC/ECD.

• Molecular & Cellular Toxicology
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• v.2 no.2
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• pp.89-96
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• 2006

The detection of many synthetic chemicals used in industry that may pose a genetic hazard in our environment is of great concern at present. Since these substances are not limited to the original products, and enter the environment, they have become widespread environmental pollutants, thus leading to a variety of chemicals that possibly threaten the public health. In this respect, to regulate and to evaluate the chemical hazard will be important to environment and human health. The clastogenicity of 11 synthetic chemicals was evaluated in Chinese hamster lung fibroblast cells in vitro. 1-Chloro-3-bromopropane CAS No. 109-70-6) induced chromosomal aberrations with significance at the concentration of $185.0\;{\mu}g/mL\;and\;1,600\;{\mu}g/mL$ both in the presence and absence of metabolic activation system, respectively. Triphenyl phosphite (CAS No. 101-02-0), which is one of the most cytotoxic chemical among 11 chemicals tested revealed no clastogenicity in the range of $95.0-4.9\;{\mu}g/mL$ both in the presence and absence of metabolic activation system. From the results of chromosomal aberration assay with 11 synthetic chemicals in Chinese hamster lung cells in vitro, 1-chloro-3-bromopropane revealed a positive clastogenic result in this study.