• Journal of the Korean Society of Food Science and Nutrition
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• v.27 no.3
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• pp.537-542
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• 1998

The present study was performed to elucidate desmutagenic principles from Ecklonia stolonifera extracts against 2-amino-1-methyl-6-phenylimidazo[4,5-b] pyridine(PhIP) and 2-amino-3,8-dime-thylimidazo[4,5-f]duinoxaline(MeIQx) with Salmonella/mammalian-microsome mutagenicity test. Alginate, phenols, chlorophyll and carotenoids from Ecklonia stolonifera were extracted and their desmutagenicities were assayed. Alginate hydroysates showed desmutagenic activities against PhIP and MeIQx at high level dose. Phenol fractions and bromophenol showed desmutagenic activity of about MeIQx at high level dose. Phenol fractions and bromophenol showed desmutagenic activity of about 90% per 0.5mg against PhIP and MeIQx. Chlorophyllin among chlorophyll derivatives exhibited remarkable desmutagenic activities of 92.9% and 82.7% at 20uM against PhIP and MeIQx, respectively. Carotenoids, such as lutein and $\alpha$-cryptoxanthin isolated from Ecklonia stolonifera exerted also high desmutagenic activity. Major desmutagenic substances from Ecklonia stolonifera are considered to be chlorophyllin, phenols, lutein, $\alpha$-cryptoxanthin and low molecular alginates.

• Advances in Traditional Medicine
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• v.1 no.1
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• pp.45-54
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• 2000

Cannabidiol derivatives (1, 2 and 3), and 5-fluorouracil (4, 5-FU) were tested for their growth inhibitory effects against human oral epitheloid carcinoma cell lines (KB) using two different 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and sulforhodamine B protein (SRB) assay. These compounds showed a potent inhibitory activity in vitro in the micromolar range against KB cell lines. In general, the antitumor activity of these compounds (1, 2, 3 and 4) was in a dose-dependent over the micromolar concentration ranges from $1\;{\mu}M\;to\;100\;{\mu}M$. The comparison of $IC_{50}$ values of these compounds in tumor cell lines shows that their susceptibility to these compounds decreases in the following order: CBD > 5-FU > CBDME > CBDDE by the MTT assay and SRB assay. Cannabidiol derivatives (1, 2 and 3), and 5-FU were tested for their cytotoxic effects on NIH 3T3 fibroblasts using two different MTT assay and SRB assay. These compounds exhibited potent cytotoxic activities in vitro in the micromolar range against NIH 3T3 fibroblasts. In general, the cytotoxic activities of these compounds (1, 2, 3 and 4) were in a dose-dependent over the micromolar concentration range $1\;{\mu}M\;to\;100\;{\mu}M$. The comparison of $CD_{50}$ values of these compounds on NIH 3T3 fibroblasts shows that their susceptibility to these compounds decreases in the following order; CBD > 5-FU > CBDDE > CBDME by MTT assay, CBD > 5-FU > CBDME > CBDDE by SRB assay. These results suggest that cannabidiol (1, CBD) retains the most growth-inhibitory activity against KB cell lines.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.125-130
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• 1993

The araC prodrugs (1~5) carrying a special acyl group at 5'-Ο-or $N^4$-position were evaluated for in vitro antiviral activity against various human viruses. When tested against HSV-1 and HSV-2 cultured in the verso cells, the prodrugs exhibited slightly higher $ED_{50}$ values compared with one of the parent araC but showed more increased $CC_{50}$ values in all cases. Consequently the overall selectivity indexes of prodrugs were higher than that of arab. The prodrugs, except compound 5, exhibited very potent activity similar to that of araC ($ED_{50}$ about $0.12{\mu}g/mι$) when evaluated against another human DNA virus, cytomegarovirus. However, theses araC prodrugs were completely inactive against RNA viruses i.e. poliovirus and coxackie B3 virus at the concentration of 4250{\mu}g/mι.$

• Research in Plant Disease
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• v.25 no.4
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• pp.179-187
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• 2019

This study was carried out to test the antimicrobial activities of nano metal hybrid materials produced by plasma technologies (radio frequency-thermal plasma system and direct current sputtering system) against microbes isolated from cucurbit (watermelon, pumpkin, and gourd) seeds. Eight different nano metal hybrid materials and four carriers were tested against five different fungal and ten different bacterial isolates in vitro. Among the tested nano metal hybrid material, Brass/CaCO₃ (1,000 ppm) exhibited 100% antimicrobial effect against all the five tested fungi. However, nano metal hybrid material Brass/CaCO₃ (1,000 ppm) inhibited only four bacterial isolates, Weissella sp., Rhodotorula mucilaginosa, Burkholderia sp., and Enterococcus sp. at 100% level, and did not inhibited other six bacterial isolates. Nano metal hybrid material graphite-nickel (G-Ni) showed 100% inhibition rate against Rhizopus stolonifer and 52.94-71.76% inhibition rate against four different fungal isolates. Nano metal hybrid material G-Ni did not show any inhibition effects against tested ten bacterial isolates. In summary, among the tested eight different nano metal hybrid materials and four carriers, Brass/CaCO₃ showed inhibition effects against five fungal isolates and four bacterial isolates, and G-Ni showed variable inhibition effects (52.94-100%) against five fungal isolates and did not show any inhibition effects against all the bacterial isolates.

• YAKHAK HOEJI
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• v.16 no.4
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• pp.162-175
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• 1972

Fifty six compounds of 4-methylthiosemicarbazone and thiorcarbohydrazone derivatives were prepared and subjected to biological tests. The following five compounds, 2-hydroxybenzaldehyde monothiocarbohydrazone (2),4-methylbenzaldehyde monothiocarbohydrazone (8), 1-(2-hydroxybenzaldehyde)-5(4-hydroxy-3-methoxybenzaldehyde) dithiocarbohydrazone (45), 1-(2-hydroxybenzaldehyde)-5-furfural dithiocarbohydrazone (46) and 1-benzaldehyde-5-cinnamaldehyde dithiocarbohydrazone (49) exhibited marked antimicrobial activity against E. coli, St. aureus and P. chrysogenum. In addition to these compounds, 3-methoxybenzaldehyde monothiocarbohydrazone (12) and 4-methylbenzaldehyde dithiocarbohydrazone (29) showed marked inhibition of HeLa cell growth at the concentration of 10 ${\nu}$g/ml. It was generally observed that most compounds demonstrated significant antifungal activity against P. chrysongenum but only one compound, 3-hydroxy-4-methoxybenzaldehyde dithiocarbohydrazone (39), exerted antituberculosis activity against M. tuberculosis H$_{37}$ RV at the concentration of 10 ${\nu}$g/ml.

• Archives of Pharmacal Research
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• v.23 no.2
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• pp.121-127
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• 2000

Cannabigerol (1, CBG), methyl 4-[(2E)-3,7-dimethyl-2,6-octad ienyl)oxy]-3-methoxybenzoate (2, DTM), 5-fluorouracil (3, FU) as a reference, and cannabidiol (4, CBD) were tested for their growth inhibitory effects against KB(ATCC NO, OCL 17) cell lines using two different assays, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay and the sulforhod-amine B protein (SRB) assay. These compounds showed inhibitory activity in vitro in the micromolar range against KB cell lines. In general, the antitumor activities of these compounds (1, 2, 3 and 4) were dose-dependent over the micromolar concentration range of 1 to 100 M. The comparison of $IC_{50}$ values of these compounds in tumor cell lines showed that their susceptibility to these compounds decreases in the following order: DTM > CBD > 5-FU > CBG by MTT assay and DTM = CBD > 5-FU > CBG by SRB assay. CBG 1, DTM 2, 5-FU 3, and CBD 4 were tested for their cytotoxic effects on NIH 3T3 fibroblasts using two different assays, the MTT assay and SRB assay. These compounds exhibited potent cytotoxic activities in vitro in the micromolar range against NIH 3T3 fibroblasts. In general, the cytotoxic acivities of these compounds (1, 2, 3 and 4) were dose-dependent over the micromolar concentraion range of 1 to 100 M. The comparison of $CD_{50}$ values of these compounds in NIH 3T3 fibroblasts shows that their susceptibility to these compounds in decreases the following order(:) CBD > 5-FU > DTM > CBG by MTT assay, CBD > 5-FU > CBG > DTM by SRB assay. These results suggest that DTM 2 has the most growth-inhibitory activity against KB cell lines.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.483-486
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• 1994

A series of 6-[N-(halophenyl)amino]-7-chloro-5, 8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, aginst pathogenic Candida species such as C. ablbicans, C glabrata, C. krusei, C. parapsilosis and C. tropicalis. The MICs were determined by the standard macrodilution techniques, according to the NCCLS 1992 guidelines. The 6-[N-(halo-standard macrodilution techniques, according to the NCCLS 1992 gidelines. The 6-[N-(halo-phenyl)amino]-7-chloro-5, 8-quinolinedione derivatives showed generally potent antifungal activities against pathogenic Candida species. Among them, derivative 1, 2, 5, and 7 showed more potent antifungal activities than kietoconazole. All derivatives 1-10 had specially potent activities against C. torpicalis. Derivative 1 and 2 containing 9N-3, 4-dihalo-phenyl)amino moiety exhibited the potent antifugal activities. Derivative 2 with (3, 4-dichlorophenyl)amino substitutent was the most effetive in preventing the growth of Candida species at MICs 4.mu.g/ml respectively.

• Restorative Dentistry and Endodontics
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• v.5 no.1
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• pp.25-28
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• 1979

The antibacterial efficacy of a few filling materials were studied in vitro. Zinc oxide eugenol cement. dycal, cavitec, hipol, cervident, clearfill and microfill were tested against Staphylococcus albus and Lactobacillus acidophilus on thioglycolate agar in order to determine whether the materials are effective inhibitors of bacterial growth. 1. Of these materials tested, zinc oxide eugenol cement was the most effective inhibitor of bacterial growth and revealed about 5.5mm in width of inhibition zone against Staphylococus albus and about 5.0mm against Lactobcillus acidophilus. 2. Dycal was moderate inhibitor of the both bact$\={e}$ria showing 2.5mm of the zone in width. 3. Cavitec was the slightest effect against the both bacteria 4. Composite resins tested in this study showed no evidence of inhibiting bacterial growth against the both bacteria.

• Bulletin of the Korean Chemical Society
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• v.34 no.5
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• pp.1349-1354
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• 2013

Twenty two new 5-fluorouracil (5-FU) derivatives, 2-butoxy-4-substituted 5-fluoropyrimidines, were synthesized and characterized by IR, $^1H$ NMR, MS, HRMS. All compounds were preliminarily evaluated by MTT assay on human liver BEL-7402 cancer cell line in vitro. Ten compounds were selected to test their cytotoxic activity against A549, HL-60 and MCF-7 cancer cell lines in vitro. These compounds were more sensitive to BEL-7402 than other cell lines, particularly, cytotoxic activity of compounds 6b, 6d-f, 6p, 6s-u were in sub-micromolar scale. The highest cytotoxic potency against A549, HL-60 and MCF-7 was shown by 2-butoxy-4-chloro-5-fluoropyrimidine (5) with $IC_{50}$ values of 0.10, 1.66 and $0.59{\mu}M$, respectively. Compounds 6d and 6e were effective against MCF-7 with $IC_{50}$ $9.73{\mu}M$ and HL-60 with $IC_{50}$ $8.83{\mu}M$, respectively.

• The Journal of Korean Medicine
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• v.16 no.2 s.30
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• pp.386-413
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• 1995

In order to prove the antitumor effect of Taraxaci Herba experimentally, studies were done. The antitumor effect against hepatic cancers such as Hep G2. Hep 3B & PLC and also the synergstric action was evaluated in the combined treatment with anticancer drugs using chiefly for liver cancer. such as. The results were obtained as follows: 1.$IC_{50}$ against Hep G2. Hep 3B and PLC was $15.5{\mu}g/ml.\;25.4{\mu}g/ml,\;31.25{\mu}g/ml$ in Mitomycin C(MMC), $92.5{mu}g/ml,\;50.2{\mu}g/ml,\;62.5{\mu}g/ml $in cisplatin(CPT) and 125 in 5-flurouracil(5-FU) respectively. 2. In cytotoxic effect against Hep G2 every fractions showed the anti tumor effect as compared with the data of control but EE fraction of Taraxaci Herba was most effective and also hexane fraction was most effective in the combined treatment with anticancer drugs. 3. In cytotoxic effect against Hep 3B every fractions showed the antitumor effect as compared with the data of control but EE fraction of Taraxaci Herba was most effective and also hexane fraction was most effective in the combined treatment with anticancer drugs. 4. In cytotoxic effect against PLC every fractions showed the anti tumor effect in the concentrations of $10^{-5}g/ml$ above as compared with the data of control and also the combined treatment with MMC was most effective. 5. Fractions of Taraxaci Herba showed the most antitumor effect against Hep 3B and also the combined treatment with MMC was most effective. From the above result it was concluded that ethyl ether fraction of Taraxaci Herba was most effective fraction, every fraction showed more antitumor effect against Hep 3B and Hep G2 than PLC.