• YAKHAK HOEJI
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• v.40 no.5
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• pp.608-615
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• 1996

6-[(N-3,4-Difluorophenyl)amino]-7-chloro-5,8-quinolinedione(RCK4) was tested for antifungal activities, against systemic infections with Candida albicans in normal mice. The therapeutic potential of RCK4 had been assessed in comparison with ketoconazole and fluconazole. RCK4 had $ED_{50},\;0.30{\pm}0.14$ but ketoconazole and fluconazole had $ED_{50},\;8.00{\pm}0.73,\;10.00{\pm} 0.43mg/kg$ respectively. Intraperitoneally administered RCK3 at the $ED_{50}$ for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver as well as ketoconazole and fluconazole at these $ED_{50}$. And administered RCK4 at the $ED_{50}$ for 14 days improved survival rates as well as ketoconazole. Acute oral toxicity studies of RCK4 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK4 were low and $LD_{50}$ values were over 2,850mg/kg in ICR mice. The genotoxicities of RCK4 had been evaluated. RCK4 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK4 with in vivo mouse micronucleus assay. RCK4 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK4 has no genotoxic potential under these experimental conditions.

• Natural Product Sciences
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• v.4 no.2
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• pp.105-114
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• 1998

The antimutagenic activity of a methanol extract of Ecklonia stolonifera (Laminariaceae) against aflatoxin $B_1\;(AFB_1)$ was demonstrated with the Salmonella typhimurium assay. The numbers of revertants per plate decreased significantly when this extract was added to the assay system using S. Salmonella typhimurium TA100. The methanol extract also exhibited significant inhibitory effects on the micronuclei formation in mouse peripheral blood reticulocytes and the DNA damage in mouse spleen lymphocytes induced by N-methyl-N-nitrosourea (MMU) and benzo(a)pyrene (B(a)P). The MeOH extract was then sequentially partitioned with $CH_2Cl_2,\;CH_2Cl_2$ insoluble intermediate, EtOAc, n-BuOH, and $H_2O$. All fractions possessed antimutagenic activity but the $H_2O$ fraction was inactive. Among active fractions, the EtOAc and $CH_2Cl_2$ insoluble intermediate fractions showed the highest activity. Column chromatography using $SiO_2$ and Sephadex LH-20 yielded phloroglucinol from the EtOAc fraction. Phloroglucinol also demonstrated significant antimutagenic activity, and inhibitory effects on the micronuclei formation in mouse peripheral blood reticulocytes and DNA damage in mouse spleen lymphocytes induced by MMU and B(a)P.

• YAKHAK HOEJI
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• v.42 no.5
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• pp.527-533
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• 1998

6-(3,4-Dichlorophenyl)amino-7-chloro-5,8-quinolinedione (RCK50) was tested for antifungal activities in mice systemically infected with Candida albicans. The therapeutic potential of RCK50 was also assessed in comparison with ketoconazole. CK50 had $ED_{50}$ 0.22${\pm}$0.01mg/kg. Ketoconazole as a positive control had $ED_{50}$ 6.00${\pm}$1.70mg/kg. Intraperitoneally administered RCK50 at the $ED_{50}$ for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver. And administered RCK50 at the $ED_{50}$ for 14 days improved survival rates. The genotoxicities of RCK50 had been evaluated. RCK50 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. RCK50 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK50 has no genotoxic potential under these experimental conditions. Acute oral toxicity studies of RCK50 were carried out in ICR mice of both sexes. RCK50 did not show acute oral toxicities and $LD_{50}$ values were over 2,850mg/kg in ICR mice.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.414-421
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• 1998

In order to compare the suppressive effect of quercetin and its glycosides, such as quercitrin (quercetin-3-rhamnoside), isoquercitrin (quercetin-3-glucoside), hyperin (querceti n-3-galactoside)and rutin (quercetin-3-rhamnosyl glucoside), on the genotocicity by benzo(a)pyrene(B(a)P), in vitro sister chromatid exchange(SCE) test using mouse spleen lymphocytes and in vivo micronucleus test using mouse peripheral blood were performed. B(a)P-induced SCEs in vitro were slightly decreased by the simultaneous treatment of quercetin and its glycosides, although there was no significant decrease. On the other hand, MNU induced micronucleated reticulocytes(MNRL7s) in vivo were significantly decreased with a dose-dependent manner in all compounds tested. However, there were no differences between quercetin aglycone and glycosides in the suppressive effects under experimental condition of this study. To elucidate, the action mechanism of quercetin aglycone and its glycosides against B(a)P-induced genotoxicity, the assay of DNA binding with B(a)P was studied. Quercetin aglycone and its glycosides inhibited B(a)P metabolism in the presence of S-9 mix and decreased the B(a)P/DNA binding in the calf thymus DNA with S-9 mix. These results suggest that antigenotoxicity of quercetin antiglycosides on B(a)P-induced genotoxicity is due to decrease of DNA binding with B(a)P through the inhibition of metabolism with B(a)P in the calf thymus DNA. Therefore, quercetin and its glycosides may act as an antigenotoxicity agent and may be useful as a chemopreventive agent of polycyclic aromaic hydrocarbons like B(a)P.

• Journal of Korean Medicine Rehabilitation
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• v.31 no.1
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• pp.59-79
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• 2021

Objectives This study was performed to observe the genotoxic effect of the ChondroT. Methods To evaluate the genotoxicity of ChondroT, an experiment of bacterial reverse mutation test, in vitro mammalian chromosomal aberration test and mammalian erythrocyte micronucleus test in mouse was conducted. Results TA98, TA100 and TA1537 strains in the absence of metabolic activation system (S9 mix), the number of revertant colonies being greater than 2-fold of the respective negative control value. Both in -S9 mix and +S9 mix, the frequencies of aberration cells with structural aberration and numerical aberrations of chromosome were less than 5%. There was no increase of polychromatic erythrocyte with one or more micronuclei at any dose of test substance compared to the negative control group (p<0.05). Conclusions In TA98, TA100 and TA1537 strains in the absence of metabolic activation system (S9 mix), the number of revertant colonies was greater than 2-fold of the respective negative control value, showing positive results. ChondroT was considered to be non-clastogenic to Chinese hamster lung (CHL/IU) cells under the present experimental condition. and ChondroT was determined not to induce an increased frequency of micronuclei in the bone marrow cells of male ICR mice under the present experimental condition.

• The korean journal of orthodontics
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• v.44 no.3
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• pp.128-135
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• 2014

Objective: This study evaluated the cytotoxicity and genotoxicity of fixed orthodontic treatment with three different light-cured orthodontic bonding composites by analyzing micronucleus (MN) formation in the buccal mucosa during a 6-month period. Methods: Thirty healthy volunteers were selected from consecutive patients referred for orthodontic treatment. Equilibrium 2 brackets and molar tubes (Dentaurum) were bonded with three different lightcured orthodontic bonding composites-Transbond XT (3M Unitek), Kurasper F (Kuraray Europe), or GrenGloo (Ormco Corporation)- to all teeth in both arches. Exfoliated buccal epithelial cells were scraped from the middle part of the inner cheeks with sterile cement spatulas before treatment and at 1, 3, and 6 months after treatment. MNs and nuclear alterations, such as karyorrhexis (KR), karyolysis (KL), and binucleated cells (BNs), were scored under a light microscope. Repeated measure ANOVA was used to calculate statistical differences in degenerative nuclear abnormalities. Results: MN rates did not significantly differ among different time points within the same cell type (p > 0.05). In contrast, the number of BNs in buccal epithelial cells significantly increased in all composite groups (p < 0.01, Transbond XT; p < 0.001, Kurasper F and GrenGloo). KL frequency significantly increased between the beginning and end of the study in the Kurasfer F ($0.80{\pm}0.79$ to $1.90{\pm}1.10$; p < 0.05) and GrenGloo ($1.30{\pm}1.06$ to $2.40{\pm}1.08$; p < 0.05) groups. Conclusions: After 6 months of fixed orthodontic treatment with different light-cured composites, morphological signs of cytotoxicity were observed but genotoxic effects were absent.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2021.04a
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• pp.67-67
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• 2021

The genus Glycyrrhiza (Licorice) has been used as an oriental herbal medicine for a long time in Asian countries. Wongam (WG), which is Glycyrrhiza new variety, have been developed to improve limitation of licorice including low productivity, environmental restriction and insufficient components by Korea Rural Development Administration. To using WG as a herbal medicine, it is important to reveal the adverse effects in health. In this study, we evaluated the genotoxicity test of WG extract through in vitro bacterial reverse mutation (AMES) assay, in vitro chromosomal aberration assay and in vivo mouse bone marrow micronucleus assay. When compared with the control, WG extract with or without the S9 mix showed no genotoxicity in the AMES assay up to 5000 ㎍/plate and in the chromosomal aberration assay up to 1100 ㎍/ml. In micronucleus assay, no significant increase in the number of micronucleated polychromatic erythrocytes or in the mean ratio of polychromatic to total erythrocytes up to 5000 mg/kg/day for 2 days. The present study demonstrated that WG extract is safe and reliable herbal medicine since no detectable genotoxic effects at least under the conditions of this study.

• Toxicological Research
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• v.23 no.3
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• pp.245-251
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• 2007

Water extract of Cordyceps militaris grown upon Protuetja dreujtarsis (CMPD) was examined for the genetic toxicity-bacterial mutagenicity, chromosome aberration, and micronucleus formation. For mutagenicity assay, bacterial reversion test with Salmonella typhimurium TA98, TA100, TA1535, TA 1537, and E. coli WP2uvrA were performed. The extract at the concentrations of $50{\sim}5,000{\mu}g/plate$ did not induce mutagenicity at all. Chromosome aberration test was performed by using Chinese lung (CHL) cells. There was no significant chromosome aberration in CHL cells with S-9 mixture at the concentrations of $312.5{\sim}1,250{\mu}g/ml$ of the extract and without S-9 mixture at the concentrations of $1.2{\sim}19.5{\mu}g/ml$ of the extract. For micronucleus test, ICR mice were treated with the extract at the dose of 0.5, 1, and 2g/Kg. The frequencies of the micronucleated polychromatic erythrocytes (MNPCE) in bone marrow preparations of the extract-treated group were not increased compared to the untreated control group. Taken together, our results show that water extract of CMPD did not induce any harmful genotoxicity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.27 no.4
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• pp.745-750
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• 1998

The antimutagenic and antigenotoxic effects of ethanol, methanol, water and non-heating ethanol extract of Ligularia fischeri were investigated using Ames test and micronucleus test. Four solvent extracts by themseleves did not induce mutagenesis. The four extract of 200㎍/plate showed approximately 84.7%, 77.1%, 72.5% and 71% inhibitory effect on the mutagenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) and 67.9%, 66.8%, 64.6% and 56% inhibition on the mutagenesis by 4-nitroquinoline-1-oxide(4NQO) against TA100 strain, whereas 70.2%, 60.9%, 61.9% and 52.8% inhibitions were observed on the mutagenesis induced by 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indol(Trp-P-1) in the presence of 200㎍/plate. TA100 strain was more sensitive than TA98 strain by four kinds of extracts on antimutagenesis. The effects of Ligularia fischeri extracts on the frequencies of micronucleated poly chromatic erythrocytes(MNPECs) induced by MNNG were investigated in the bone marrow. Ten, 20, 40 and 80mg g/kg of each extract were administered to animals immediately after injection of MNNG and the exposure time was 36 hours. Inhibitory effects of Ligularia fischeri ethanol extracts were 12%, 35.3%, 58.8%, and 57%, in the presence of 20, 40, 60 and 80mg/kg, respectively whereas methanol extracts showed 15.5%, 32.7%, 50.8%, and 57.9% inhibitory effects, respectively. Both extracts showed enhanced antimutagenic and antigenotoxic effects. These results showed a good correlation between antimutagenic effects in in vitro and in in vitro assay.

• YAKHAK HOEJI
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• v.37 no.3
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• pp.278-285
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• 1993

The anticlastogenic effect of N-acetylcysteine was tested in vivo in mouse bone-marrow micronucleus assay. The frequencies of micronuclei induced by adriamycin (5 mg/kg i.p.) in bonemarrow cells were decreased by the oral administration of N-acetylcysteine at 12 h before adriamycin injection. The observed suppressing effect was not a reflection of a delay in the formation of micronuclei by the cytotoxic effect of N-acetylcysteine. The anticlastogenic effects of SH compound including N-acetylcysteine, cysteine, cystine, S-carboxy methylcysteine and glutathione were also investigated by the multiple pretreatment. Each SH compound was administered orally every day for 5 days and adriamycin (5 mg/kg i.p.) was injected at 24h after the last dose of test compound. N-acetylcysteine and glutathione showed significantly the suppressive effect at dose of 10 and 25 mg/kg for N-acetylcysteine and at the dose of 25 mg/kg for glutathione. Our study suggests that N-acetylcysteine is capable of protecting the chromosomal damages in the normal cells during cancer chemotherapy by adriamycin, and may act as an anticlastogen against induction of micronuclei by superoxide generating agent such as adriamycin.