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Cytotoxic Activities of some Geranylated Flavones against L1210 Cell (L1210세포에 대한 제라닐화 후라본의 세포독성)

  • Baik, Kyeong-Up;Ahn, Byung-Zun
    • YAKHAK HOEJI
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    • v.32 no.2
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    • pp.125-128
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    • 1988
  • Geranylation of some synthetic and natural flavones have yielded cytotoxic products against L1210 coll; 5,2´-dihydroxy-6,7,8-trimethoxy-6´-geranyloxyflavone 4$(8.5{\mu}g/ml)$, 5,6-dihydroxy-7-gerenyloxyflavone 9$(2.3{\mu}g/ml)$. 2 has showed the same range of cytotoxicity as the starting material, 5,2´-dihydroxy-6,7,8-trimethoxy-6´-benzyloxyflavone$(17.0{\mu}g/ml)$. The cytotoxicity of 4 was lower than its starting substance, 5,2´,6´-trihydroxy-6,7,8-trimethoxyflavone $(4.5{\mu}g/ml)$. On geranylating 5,6,7-trihydroxyflavone(baicalein, $15.0{\mu}g/ml$) the cytotoxic activity has been strongly potentiated($2.3{\mu}g/ml$ of 9). The presence of at least a free hydroxy group in B-ring of Skullkapflavone II-type flavones. was essential for a high activity. A larger RD-group than methoxy in the B-ring has weakened the activity. The cytotoxicities of baicalein series could not be correlated to their structures.

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Synthesis and evaluation of antifungal activities of 5-arylamino-6-chloro-4. 7 -dioxoindazoles

  • You, Hea-Jung;Shim, Ju-Yeon;Shon, Eun-Ha;Choi, Ko-Un;Choi, Ik-Hwa;Chae, Mi-Jin;Ryu, Chung-Kyu
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.353.2-353.2
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    • 2002
  • 5-Arylamino-6-chloro-4.7-dioxoindazoles (DZs) were newly synthesized for the evaluation of antifungal activities. The compounds DZs were prepared by regioselective nucleophilic substitution of 5.6-dichloro-4.7-dioxoindazoles with appropriate arylamines in high yield. DZs were tested for their growth inhibitory activities against Candida species and Aspergillus niger. The MIC values were determined by the two-fold dilution method. In general. DZs showed in vitro antifungal activities. Among the tested compounds, DZ1, 3, 6, 7 and 12 showed potent antifungal activities against Candida species and Aspergillus niger. DZ7 was the most effective in preventing the growth of Candida species.

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Effects of epitope sequence tandem repeat and proline incorporation on polyclonal antibody production against cytochrome 1A2 and 3A4

  • Ahn, Tae-Ho;Yun, Chul-Ho
    • BMB Reports
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    • v.42 no.7
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    • pp.418-420
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    • 2009
  • We describe a method for producing polyclonal antibodies against peptide antigen cytochrome P450 1A2 and 3A4 using a tandem repeat of the epitope region and incorporation of proline residue between the repeated sequences. An ELISA assay revealed more efficient generation of polyclonal antibodies to tandem repeat peptide antigens than mono-epitope peptides. The incorporation of proline residues further stimulated antibody production.

Solvatochromic Effects and Hydrogen Bonding Interactions of 4-(4-Nitrophenylazo)-1-naphthol Derivatives

  • 신동명;권오악
    • Bulletin of the Korean Chemical Society
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    • v.16 no.7
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    • pp.574-577
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    • 1995
  • Solvatochromic effect and hydrogen bonding interaction of NPNOH, NPNO- and NPNOR were investigated. Electronic transition energies of the dyes were plotted against empirical solvent polarity parameters, Taft's π* and Reichardt's ET(30). Good correlations were observed when the excitation energies were plotted against the energy calculated by multiple linear regression method which was developed by Taft. There is an intrinsic difference between betaine for ET(30) polarity scale and the azoderivative, which is derived from the specific hydrogen bond incurred with probe molecules and solvents. The hydrogen bonding plays a very important role for stabilization of an excited state molecule by solvents especially when a solute possesses a negative charge as with NPNO-.

Facile Synthesis and Biological Evaluation of Heterocyclic Compounds Containing Diazepam

  • Berghot, M.A.
    • Archives of Pharmacal Research
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    • v.24 no.4
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    • pp.263-269
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    • 2001
  • Diazepamoxadiazoles 4,5,6,12,14 and 22 were prepared with the binary form system. Diazepamthiadiazoles 15,20 and Diazepamtriazoles 7,8,9,17,18,19 and 21 were also shapely synthesized. Some of these compounds were screened to test their antibacterial activity against E. coli and B. subtilis compounds 15 and 20 show potent activity against these bacteria.

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Verification of Antibacterial Activities of Oriental Herbal Medicine Extracts (한약재 추출물의 항균활성 검증)

  • Lee, Chang-Eun;Jo, Jung-Kwon;Kim, Jae-Deok;Lee, Dong-Geun;Kim, Won-Seok;Lee, Sang-Hyeon
    • Journal of Life Science
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    • v.27 no.6
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    • pp.611-616
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    • 2017
  • The antibacterial activities of nine oriental herbal medicine extracts were measured against seven kinds of bacteria known to cause food poisoning and disease. The extracts were prepared with distilled water using an autoclave ($121^{\circ}C$ for 30 min). The extraction yields of nine oriental herbal medicines were in the rage of 0.5%-33.4%. The antibacterial activities were evaluated using the paper-disc method. Extracts of Hwangryeon, Jiyu, and Ohbaeja showed antibacterial activities while the others did not. Extracts of Coptis japonica, Hwangryeon, and Sanguisorba officinalis, Jiyu showed antibacterial activities only against Clostridium perfringens and Listeria monocytogenes. Extracts of Rhus javanica, Ohbaeja showed the strongest antibacterial activities against all the bacteria tested. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of R. javanica extracts were in the range of 2.4~20 mg/ml for the bacteria tested. In conclusion, the extract of R. javanica showed superior antibacterial activities against the seven bacterial strains tested. The MIC and MBC values for each bacterium were represented as strain names (MIC, MBC), which were Bacillus cereus (11.2, 20), Clostridium perfringens (2.4, 4.7), Escherichia coli (9.1, 9.1), Listeria monocytogenes (11.1, 20), Salmonella typhi (4.7, 9.1), Staphylococcus aureus (2.4, 4.7), and Vibrio parahaemolyticus (2.4, 5.3). Further purification and study of this antibacterial material would be helpful for developing antibiotics or promoting synergistic effects with known antibiotics, producing antibacterial material for lengthening the shelf-life of food, and so on.

Antimutagenic and Cytotoxicity Effects of Phellinus linteus Extracts (상황버섯(Phellinus linteus) 추출물의 항돌연변이원성 및 세포독성 효과)

  • 함승시;지정환;김미남;정차권
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.29 no.2
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    • pp.322-328
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    • 2000
  • This study was performed to determine the antimutagenic and cytotoxic effect of the Phellinus linteus methanol extract on Salmonella typhimurium TA98, TA100 and human cancer cell lines. In the Ames test, methanol extract of P. linteus alone did not exhibit any mutagenicity but showed substantial inhibitory effects against mutation induced by N-methyl-N'-nitro-N-nitrosoguanidine(MNNG), 4-nitroquinoline-nitroquinoline-1-oxide(4NQO), 3-amino-1,4-dimethyl-5H-pyrdo[4,3-blindol(Trp-P-1) and benzo(α)pyrene(B(α)P). The methanol extracts of P. linteus(200㎍/plate) showed approximately 78.3%, 78.7% and 88.1% inhibitory effect on the mutagenesis induced by 4NQO, Trp-P-1 and B(α)P. The anticancer effects of P. linteus extract against human breast adenocarcinoma(MCF7), human lung carcinoma (A549), human fibrosarcoma (HT1080), human hepatocelular carcinoma (Hep3B) and human epitheloid carcinoma (HeLa) were investigated. The treatment of 1mg/mL P. linteus extracts had the highest cytotoxicity against MCF7 (92.0%), followed by Hep3B (84.9%), A549 (84.2%) and HT1080 (82.9%). In contrast 1mg/mL treatment of P. linteus extracts had only 10∼40% cytotoxicity on normal human liver cell (WRL68).

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Antibacterial Activity of Streptomyces Strains Isolated from Different Regions of Jordan

  • Hala Khyami-Horani;Amal Al-Aboudi;Musa Abu Zarga;Monther Sadder;Halima Othman
    • Microbiology and Biotechnology Letters
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    • v.51 no.4
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    • pp.474-483
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    • 2023
  • Members of the genus Streptomyces produce more than 70% of antibiotics. The rise in antibiotic resistance globally enhanced the search for novel species with the ability to produce new bioactive compounds. This study was initiated to investigate different regions in Jordan for previously uncultured and rare Streptomyces species capable of producing novel antimicrobial compounds especially active against bacteria resistant to antibiotics. A total of 191 Streptomyces strains were isolated from 26 soil samples collected from different geographic regions in Jordan. Isolates were characterized based on colony and cellular morphology as well as using 16S rRNA gene sequencing. These isolates were screened for their ability to produce antibiotics by the perpendicular-cross streak method, and then tested by well diffusion method against tested pathogens. Fifty-four isolates showed potential to produce antimicrobial products especially active against resistant bacteria, 20.1% of the isolates showed inhibitory effect against Staphylococcus aureus, 16.9% against clinical MSSA strains, and 18.0% against MRSA: whereas only 4.2% against Esherichia coli, 3.2% against Klebsiella pneumonia, 2.7% against Pseudomonas aeruginosa, and 10.0% against clinical Candida albicans. Three isolates were selected for further identification due to their antibacterial activity against S. aureus, MRSA, and MSSA. These isolates were identified as follows; Streptomyces aburaviensis DSa3, Streptomyces alboniger SAb7 and Streptomyces misionensis ZAb2, based on cultural, biochemical characteristics and molecular analysis of the 16S rRNA.

Antioxidant Activity of Theaflavin and Thearubigin Separated from Korean Microbially Fermented Tea

  • Shon, Mi-Yae;Park, Seok-Kyu;Nam, Sang-Hae
    • Preventive Nutrition and Food Science
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    • v.12 no.1
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    • pp.7-10
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    • 2007
  • Theaflavins (TF) and thearubigins (TR) were separated from Korean microbially fermented tea leaves. Contents of TF (74.4 $\mu$M/g) and TR (37.2%) were higher than reported for black tea fermented by oxidase. Antioxidant activities of TF, TR and EGCG were analyzed and protective effects of COS-7 cells against copper and cadmium-induced toxicity were investigated. TF and TR exhibited good inhibition rates of about 85$\sim$90% for antioxidant and scavenging activities of free radicals and protected COS-7 cells against apoptosis or damage caused by stress, such as cadmium and copper-oxidative injury, free radicals etc. These results indicate that TF, TR and EGCG have antioxidant and scavenging activities against free radicals and protect COS-7 cells from Cu, Cd induced injury.

Cytotoxic and COX-2 Inhibitory Constituents from the Aerial Parts of Aralia cordata

  • Lee, Ik-Soo;Jin, Wen-Yi;Zhang, Xin-Feng;Hung, Tran-Manh;Song, Kyung-Sik;Seong, Yeon-Hee;Bae, Ki-Hwan
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.548-555
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    • 2006
  • Three diterpenes (1, 8, and 9), three triterpenes (3, 4, and 7), one saponin (11), four sterols (2, 5, 6, and 12), and one cerebroside (10) were isolated from the EtOH extract of the aerial parts of Aralia cordata by repeated silica gel column chromatography. Their chemical structures were identified by comparing their physicochemical and spectral data with those published in literatures. All isolated compounds were evaluated for their cytotoxicity against L1210, K562, and LLC tumor cell lines using MTT assay. Of which, $3{\beta},5{\alpha}-dihydroxy-6{\beta}-methoxyergosta-7,22-diene$ (6) showed a potent cytotoxicity against all cell lines with $IC_{50}$ values of 11.7, 11.9, and $15.1\;{\mu}M$, respectively, while compounds 1, 5, and 11 showed a moderate or weak cytotoxicity. These isolates were also examined for their inhibitory activity against COX-1 and COX-2. Although most compounds, except for 2, 10, and 12, showed a strong inhibitory activity against COX-1, they exhibited a moderate or weak inhibitory activity against COX-2.