• Archives of Pharmacal Research
• /
• v.19 no.4
• /
• pp.286-291
• /
• 1996

Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BPO02-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, $9.85\mug/ml$ respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, $4,4^I-di-tert-butylphenyl$, bibenzyl, $2,2^I-dimethylbibenzyl$, cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.

• Korean Journal of Veterinary Research
• /
• v.29 no.2
• /
• pp.83-90
• /
• 1989

The changes in serum total protein and immunoglobulin levels, and BVD, IBR and PI-3 viral neutralizing antibody titers in colostrum-conferred Korean native calves during the first 12 weeks postpartum were studied, and the results obtained were summerized as follows: The Mean concentration of total protein, total immunoglobulin, IgG, IgM and IgA in sera of 9 calves at birth were $3.8{\pm}0.5g/dl$, $0.27{\pm}0.15mg/ml$, $0.06{\pm}0.08mg/ml$, $0.21{\pm}0.11mg/ml$, and extremely low concentration, respectively. Serum total protein level reached a maximum at 20 hours after birth, total immunoglobulin, IgG, and IgM levels at 24 hours, and IgA level at 28 hours, respectively. Serum IgA level reached a minimum at 4 weeks old, IgM level at 5 weeks, total immunoglobulin level at 8 weeks, and IgG level at 10 weeks, respectively. After then those levels had begun to increase, but total protein level was still decreasing at 12 weeks old. The half-lives of IgG, IgM, and IgA were 21.1 days, 4.0 days, and 2.6 days-respectively. In 10 Korean native cows immediately after parturition, serum neutralizing antibody titers specific to BVD, IBR and PI-3 virus were $8.7{\pm}1.5{\log}_2$, $5.7{\pm}1.2{\log}_2$, and $6.8{\pm}1.01{\log}_2$, respectively. And colostral neutralizing antibody titers against BVD, IBR, and PI-3 virus were $10.1{\pm}1.4{\log}_2$, $6.8{\pm}1.3{\log}_2$ and $7.8{\pm}1.7{\log}_2$, respectively. Before suckling the colostrum, SN antibody titers against BVD, IBR, and PI-3 virus were undetectable from all of 9 Korean native calves. Nevertheless SN antibody titer against BVD virus reached a maximum level ($9.2{\pm}0.6{\log}_2$) at 24 hours after birth, that against IBR virus ($6.1{\pm}1.0{\log}_2$) at 20 hours after birth, and that against PI-3 virus ($6.8{\pm}0.9{\log}_2$) at 32 hours after birth, respectively. In 12 weeks old calves, the SN antibodies against BVD and IBR virus were still decreasing, but that against PI-3 virus reached a minimum at 10 weeks, and increased after 12 weeks of age. The half-lives of SN antibodies against BVD, PI-3 and IBR, virus were 16.0 days, 22.6 days, and 25.5 days, respectively.

• Journal of the Korean Chemical Society
• /
• v.56 no.3
• /
• pp.341-347
• /
• 2012

A series of 2-(4-chlorophenylimino)-5-((3-(p-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl) methylene) thiazolidin-4-one ($\mathbf{3a-h}$) compounds were prepared from the 2-(4-chlorophenylimino) thiazolidin-4-one ($\mathbf{1}$) and 1-phenyl-3-(p-substituted phenyl)-1H-pyrazole-4-carbaldehyde ($\mathbf{2a-h}$). All compounds were characterized by elemental (C, H, N) analysis and spectral (FT-IR, $^1H$ NMR and GC-MS) analysis. These newly synthesized compounds were screened for their antibacterial and antifungal activities. Antimicrobial activity was observed and evaluated against the bacterial strains like Eschericha coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442) and against the fungal strains like Candida albicans (MTCC 227), Aspergillus niger (MTCC 282) and Aspergillus clavatus (MTCC 1323). All the synthesized compounds were found to possess moderate to excellent antimicrobial activity against above selected strains.

• Mycobiology
• /
• v.35 no.4
• /
• pp.210-214
• /
• 2007

Antibacterial and antifungal activities of liquid culture filtrate, water and ethanol extract (solid culture) of Stereum ostrea were evaluated against 5 bacteria and 3 plant pathogenic fungi. To determine the minimal inhibitory concentration (MIC), we studied $5{\sim}300\;mg/ml$ concentrations against bacteria and fungi separately. The MIC was 10 mg/ml for Bacillus subtilis and 40 mg/ml for Colletotrichum gloeosporioides and Colletotrichum miyabeanus. Liquid culture filtrate was more effective against Gram positive than Gram negative bacteria, and Staphylococcus aureus was the most inhibited (20.3 mm) bacterium. Water and ethanol extracts were effective against both Gram positive and Gram negative bacteria, and water extract was better than ethanol extract. In water and ethanol extract, inhibition zones were 23.6 and 21.0 mm (S. aureus) and 26.3 and 22.3 mm (Pseudomonas aeruginosa), respectively. For plant pathogenic fungi, the highest and lowest percent inhibition of mycelial growth (PIMG) was found 82.8 and 14.4 against C. miyabeanus and Botrytis cinerea in liquid culture filtrate, respectively. In water extract, the PIMG was found to be the highest 85.2 and lowest 41.7 for C. miyabeanus and C. gloeosporioides, respectively. The inhibitory effect of ethanol extract was better against C. miyabeanus than C. gloeosporioides and B. cinerea. Among 3 samples, water extract was the best against tested pathogenic fungi. This study offers that the extracts isolated from S. ostrea contain potential compounds which inhibit the growth of both bacteria and fungi.

• YAKHAK HOEJI
• /
• v.18 no.4
• /
• pp.249-254
• /
• 1974

Eighteen 2-aryl-3-(5-nitro-2-furyl) acrylamides were synthesized as antimicrobial agent, by the condensation of 2-(p-sulbstituted phenyl)-3-(5-nitro-2-furyl) acryloyl chloride with amino component, such as sulfisozxazole, sulfamethoxypyridazine and sulfadimethoxine. All compounds showed fair bacteriostatic activity against staphylococcus aureus 6538p, Bacillus subtilis, Escherichia coli, and Klebsiella pneumoniae. 2-(p-Hydroxyphenyl)-and 2-(p-acetoxyphenyl) compounds also showed antimicrobial activity against Saccharomyces cerevisiae 396 and Aspergillus oryzae.

• YAKHAK HOEJI
• /
• v.49 no.1
• /
• pp.20-24
• /
• 2005

The synthesis of 4',5'-doubly branched carbocyclic nucleosides was accomplished in this study. The selective methylation in the 5'-position was made by Felkin-Anh controlled Grignard addition. The construction of the required 4'-quaternary carbon was carried out by using a [3,3]-sigmatropic rearrangement. Bis-vinyl 6 was successfully cyclized using a Grubbs' catalyst II. The natural pyrimidine bases (cytosine, uracil, thymine) were efficiently coupled using a Pd(0) catalyst. When the synthesized compounds were examined for their activity against several viruses such as the HIV-1, HSV-1, HSV-2 and HCMV, the cytosine analogue 13 exhibited weak antiviral activity against the HCMV.

• International Journal of Oral Biology
• /
• v.45 no.4
• /
• pp.211-217
• /
• 2020

Molecular mimicry is the most common mechanism that breaches self-tolerance. We previously identified autoantibodies to aquaporin-5 (AQP5) in the sera of patients with Sjögren's syndrome and found that the aquaporin of Prevotella melaninogenica (PmAqp), an oral commensal, is highly homologous to human AQP5. This study aimed to test whether PmAqp can induce anti-AQP5 autoantibodies via molecular mimicry. From the amino acid sequence of PmAqp, an immunizing peptide; i.e., PmE-L, was designed, which contained both the B cell epitope "E" and T cell epitope. C57BL/6 and BALB/c mice were subcutaneously immunized with linear or cyclic forms of PmE-L emulsified in incomplete Freund's adjuvant. The concentrations of the antibodies in sera were measured using enzyme-linked immunosorbent assays. Both linear and cyclic PmE-L induced high levels of antibodies against not only the immunized peptides but also autoantibodies against AQP5E and antibodies against PmE, a Pm homolog of AQP5E. In C57BL/6 mice; however, the cyclic form of PmE-L was more efficient than the linear form in inducing autoantibodies against AQP5E that contained a cyclic epitope. The levels of anti-PmE antibodies and anti-AQP5E autoantibodies showed a strong positive correlation (r = 0.95, p < 0.0005), suggesting molecular mimicry. Collectively, the mice produced anti-AQP5E autoantibodies in response to a PmAqp-derived peptide. This model proved to be useful for studying the mechanisms of autoantibody production by molecular mimicry.

• Korean Journal of Veterinary Service
• /
• v.21 no.4
• /
• pp.439-449
• /
• 1998

From September 1997 to August 1998, Korean indigeous goats infected with internal parasites were examined for efficacy of anthelminthics by fecal egg counts. Efficacy of anthelmintic drugs against gastointestinal Haemonchus contortus in goats were effective with Ivermectin(94.9%), Piperazine(92.8%), Levamisole(88.3%), Albendazole(68.2%), respectively. Albendazole was effective against goats with Haemonchus contortus in 3 herds, but not effective in 1 herds. Efficacy of anthelmintic drugs against gastointestinal Paramphistomim sp in goats were effective with Ivermectin(95.3%), Piperazine(93.3%), Albendazole(92.9%), Levamisole(91.1%), respectively. Efficacy of anthelmintic drugs against Eimeria sp in goats were effective with Toltrazuril(92.6%), Diclazuril(90.4% ), Nicarbazin (87.5%), Amprolium(70.0%), respectively. Amprolium was effective against goats with Eimeria sp in 3 herds, but not effective in 1 herds.

• The Plant Pathology Journal
• /
• v.40 no.2
• /
• pp.192-204
• /
• 2024

In this study, the efficacy of the essential oil of Mentha longifolia, Achillea arabica and Artemisia absinthium plants were evaluated against important soil-borne fungal pathogens as Verticillium dahliae, Rhizoctonia solani, and Fusarium oxysporum. Essential oils were obtained from plants by hydrodistillation method and the chemical components of essential oils were determined by analyzing by gas chromatography-mass spectrometry. The main components found as piperitone oxide (13.61%), piperitenone oxide (15.55%), pulegone (12.47%), 1-menthone (5.75%), and camphor (5.75%) in M. longifolia, á-selinene 13.38%, camphor 13.34%, L-4-terpineneol 8.40%, (-)-á-Elemene 7.01%, 1,8-cineole 4.71%, and (-)-spathulenol 3.84% in A. arabica, and á-thujone (34.64%), 1,8-cineole (19.54%), pulegone (7.86%), camphene (5.31%), sabinene (4.86%), and germacrene-d (3.67%) in A. absinthium. The antifungal activities of the oils were investigated 0.05, 0.1, 0.25, 0.5, 1.00, and 2.00 μl/ml concentrations with the contact effect method. M. longifolia oil (1.00 and 2.00 μl/ml) has displayed remarkable antifungal effect and provided 100% inhibition on mycelial growth of V. dahliae, R. solani and F. oxysporum. The results obtained from this study may contribute to the development of new alternative and safe methods against soil-borne fungal pathogens.

• Journal of Food Hygiene and Safety
• /
• v.24 no.1
• /
• pp.46-49
• /
• 2009

The desmutagenic activity of the water extract of Cassia tara L on the mutagenicity induced by 4-nitroquinoline 1-oxide (4-NQO) and N-methyl-N-nitro-N'-nitrosoguani-dine (MNNG) was studied using the SOS Chromotest with Escherichia coli PQ37. The inhibition rates of water extract of Cassia tara L. at concentration of $100{\mu}g$/assay were 27.5% and 40% against 4-NQO and MNNG. The water extract of Cassia tara L. was separated into methanol soluble and methanol insoluble parts. The methanol soluble part exhibited higher inhibition effects than the methanol insoluble part against the mutagenic activities of 4-NQO and MNNG. Step-wise fractionation of methanol soluble part was done to obtain methanol, ethyl acetate and water fractions. Among these fractions, water fraction had the strongest inhibitory effects of 23.0 and 19.0% against mutagenicities of MNNG and 4NQO, respectively. The results clearly indicated that the water fraction showed much stronger antimutagenicity against MNNG than 4NQO. The inhibition rates of aqueous fraction of methanol-soluble from water extracted Cassia tara L. at concentrations of 1.0, 10, 100 and $250{\mu}g$/assay were 8.0%, 12.0%, 25.5% and 43.0%, respectively. The water fraction showed the inhibitory effects with dose response against the mutagenic activities induced by MNNG.