• Bulletin of the Korean Chemical Society
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• 제31권7호
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• pp.2003-2010
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• 2010

A new class of halobenzyloxy or alkoxy 1,2,4-triazoles and their hydrochlorides were synthesized through cyclization starting from commercially available phenylhydrazine. The structures were characterized by MS, IR and $^1H$ NMR spectra as well as elemental analyses. All the synthesized compounds were screened for their antibacterial activities in vitro against Staphylococcus aureus (ATCC29213), methicillin-resistant Staphylococcus aureus (N315), Bacillus subtilis, Escherichia coli (ATCC25922), Pseudomonas aeruginosa, Shigella dysenteriae, Eberthella typhosa, and antifungal activities against Candida albicans (ATCC76615), Aspergillus fumigatus by broth microdilution assay method. The results of preliminary bioassay indicated that 3-(2,4-difluorobenzyloxy)-1-phenyl-1H-1,2,4-triazole hydrochloride exhibited the best inhibitory activity with an MIC value of 56.25 ${\mu}M$ against P. aeruginosa superior to Chloramphenicol, and showed comparable activity with Chloramphenicol against E. coli (ATCC25922).

• 한국미생물·생명공학회지
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• 제23권4호
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• pp.378-383
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• 1995

Antifungal activity of caproic acid against Botrytis cinerea was investigated in this research. In vitro 200 ppm of caproic acid was inhibited on the germination and the mycelium growth of B. cinerea. 250 ppm of caproic acid showed the fungicidal activity against sensitive B. cinerea. To compared the inhibitory effect of treatments against B. cinerea, the field essay was carried out in the grape vineyard. The rot (%) of control, 3000 ppm of caproic acid, 3000 ppm of sodium caproate, and sumisclex were 30.7%, 10.2%, 22.8%, and 3.1%, respectively. The anti-Botrytis efficiency (%) was also evaluated as follows; 3000 ppm of caproic acid 66.8%, 3000 ppm of sodium caproate 25.7%, and sumisclex 89.9%. The efficiency between sumisclex and 3000 ppm of caproic acid was no significant difference at the 1% level by Tukey test. These results suggest that 3000 ppm of caproic acid may be greater than that of sodium caproate.

• Archives of Pharmacal Research
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• 제25권5호
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• pp.608-612
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• 2002

The twelve-protostane analogues were synthesized from alisol B 23-acetate and assessed for their in vitro antitumor activity against six different human and murine tumor cell lines. Of the compounds synthesized, 23S-acetoxy-24R(25)-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-hy-droxyimine (12) exhibited significant cytotoxic activities against A549, SK-OV3, B16-F10, and HT1080 tumor cells with $ED_{50}/$ values of 10.0, 8.7 ,5.2, and 3.1 ${\mu}g$/ml, respectively. Furthermore, 23S-acetoxy-13(17),24R(25)-diepoxy-11$\beta$-hydroxyprotost-3-one (5), 13(17),24R(25)-diepoxy-11$\beta$, 23S-dihydroxyprotostan-3-one (6), 24R,25-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-one (7), and 11$\beta$,23S,24R,25-tetrahydroxyprotost-13(17)-en-3-one (9) showed moderate cytotoxic activities against 816-F10 and HT1080 tumor cells. These results mean that a hydroxyimino group at C-3 position in the protostane-type terpene enhances cytotoxic activity.

• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1987년도 Proceedings of Korea-Japan Panax Ginseng Symposium 1987 Seoul Korea
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• pp.29-37
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• 1987

This study was devised to observe the cytotoxlc activities of petroleum-ether extract of Panax ginseng root(crude Gx) and its partially purified fraction from silicon acid column chromatography(7:3 CX) against sarcoma-180(5-180) and Walker carcinosarcoma 256(Walker 256) in vivo, and murine leukemic lymphocytes(L1210) and human rectal cancer cell(HRT-18) and human colon cancer cells(HT-29 and HCT-48) in vitro . Each cell-line was cultured in medium containing serial concentrations of the crude Gx or 7:3 Gx in vitro. A highly lipid soluble compound in the extract of Panax ginseng root was cytocidal to murine leukemic cells and human colon and rectal cancer cells in vitro In the meantime, ginseng saponin derivatives did not cytotoxic effects at its corresponding concentration. The growth rates of the cancer cells in medium containing ginseng extracts were inhibited gradually to a significant degree roughly in proportion to the increase of the extract concentration. The cytotoxic activity of 7:3 Gx was about 3 times more potent than that of crude Gx, one unit of cytotoxic activity against L121f cells being equivalent to 2.54$\mu\textrm{g}$ and 0.88 $\mu\textrm{g}$ for the crude Gx and 7:3 Gx, respectively. The Rf value of the active compound on silica -gel thin layer chromatography with petroleum-ether/ethyl ether/acetic acid mixture (90:10:1, v/v/v) as a developing solvent was 0.23. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7:3 Gx treatment compared with their control group. The significantly decreased hemoglobin values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude Gx. The synthetic levels of protein, DNA and RNA in human colon and rectal cancer cells were significantly diminished by treatment with the crude Gx, which can explain a part of the origin of its anticancer activity.

• 농약과학회지
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• 제10권2호
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• pp.149-152
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• 2006

벼도열병균에 선택적 활성을 나타내는 3-알킬-2-페닐이미노-1,3-티아졸린 유도체 1의 분자수정을 통하여 2-벤질이미노-1,3-티아졸린 유도체 7의 집중 라이브러리 구축 및 이들의 대표적인 식물병원균 6종에 대한 살균활성(in vivo)을 기술하였다. 조합화학기법에 의하여 54종의 2-벤질이미노-1,3-티아졸린 유도체 7의 집중 라이브러리를 이에 상응하는 $\gamma$-클로로아세토아세트아닐라이드 유도체 6과 N-벤질 티오우레아 5의 반응으로부터 합성하였다. 대표적인 식물병원균 6종에 대한 살균활성시험 결과, 28종의 화합물 7이 $100{\mu}g$ $mL^{-1}$(in vivo)에서 토마토 역병에 대하여 방제가 50% 이상을 나타냈다.

• Natural Product Sciences
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• 제17권3호
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• pp.175-180
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• 2011

Eleven compounds were isolated from fresh leaves of Abies koreana (Pinaceae), and structures of these compounds were determined to be 3-hydroxy-2-methyl-4-pyrone (1), maltol-3-O-${\beta}$-D-glucoside (2), (-)-epicatechin (3), naringenin 7-O-${\beta}$-D-glucopyranoside (4), naringenin-7-O-rhamnoglucoside (5), kaempferol 3-O-${\beta}$-D-glucopyranoside (6), (+)-isolariciresinol (7), secoisolariciresinol (8), rhododendrol (9), ferulic acid (10) and 4-(4-hydroxyphenyl)butan-2-one (rheosmin) (11) by comparing $^1H$-, $^{13}C$-NMR and MS spectroscopic data with reference values. Compounds 3, 5, 7, 8, 9, 10, 11 were isolated for the first time from A. koreana. Among eleven isolates, compounds 1, 7 and 11 showed inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV-2 microglia in a concentration dependent manner.

• 한국수산과학회지
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• 제41권3호
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• pp.188-192
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• 2008

Methyl gallate isolated from bark of the tree Rhus verniciflua Stokes has significant antimicrobial activity against the fish pathogenic bacteria Edwardsiella tarda and Vibrio anguillarum. To evaluate the antimicrobial activity of gallate derivatives, eight alkyl gallates were tested. Ethyl gallate and propyl gallate had the highest activities, with MICs of $15.6-31.3{\mu}g/mL$ against E. tarda. For V. anguillarum, propyl gallate and butyl gallate were highly effective, with MICs of $7.81-31.3{\mu}g/mL$. When used in combination with antibiotics, methyl gallate exhibited synergistic effects with oxytetracycline against E. tarda and with norfloxacin against V. anguillarum. These results suggest that short-chain alkyl gallates can be used as alternatives to antibiotics against the fish pathogenic bacteria.

• 대한수의학회지
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• 제35권3호
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• pp.615-623
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• 1995

Sera from 304 Holsteins or Korean native cattle were collected from slaughterhouse in Kwangju area to study the infection of major virus-borne diseases. Serum antibody titers against infectious bovine rhinotracheitis virus(IBRV), bovine viral diarrhea virus(BVDV), parainfluenza type-3 virus(PI-3V), bovine ephemeral fever virus(BEFV), bovine Ibaraki virus(BIV), bovine Akabane virus(BAKV), bovine rotavirus(BRV), bovine coronavirus(BCV) were measured by serum neutralization tests. Results which obtained were as follows. Sera from 280 cattle(92.1%) contained antibodies against BRV which rate was the highest among the 8 viruses, and serum antibodies against BCV, BVDV, BIV, BAKV, BEFV, IBRV and PI-3V were detected from 266(87.5%), 149(49%), 108(35.5%), 94(30.9%), 80(26.3%), 32(10.5%) and 24(7.9%) cattle, respectively. Prevalence of seropositives to BVDV, BIV, BAKV, BEFV were higher among Holsteins than among the Korean native cattle(P<0.05). Prevalence of antibody titers against BVDV, BIV and BEFV in Korean native cattle were higher among females than males, while more males contained antibodies to BAKV, IBRV and PI-3V than females in their blood(P<0.05). Seropositives to BVDV, BIV, BAKV, BEFV and IBRV in Holsteins were higher among females than males(P<0.05). In Korean native cattle, serum antibody titers against IBRV and PI-3V ranged from 1:2~1:32 and 1:2~1:64, respectively, while serum antibody titers against the rest 6 viruses ranged from $1:2{\sim}1:{\geq}256$. In Holsteins, serum antibody titers against IBRV and PI-3V ranged from 1:2~1:64 and 1:2~1:32, respectively, while serum antibody titers against the rest 6 viruses ranged from $1:2{\sim}1:{\geq}256$.

• Preventive Nutrition and Food Science
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• 제3권4호
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• pp.324-328
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• 1998

We screened the methanol extracts from 133 plant species growing in Korea for antimicrobial activity against enterohemorrhagic Escherichia coli 0157 : H7. Those are selected from three plant grouping ; traditional medicinal herbs, edible plants, and flowers. They were tested by disk diffusion assay. From evaluation of the inhibition zone diameter of microbial growth, we found that the flower extract of Rhododendron Schilpenbachii Max had the most significant antimicrobial activity against this bacteria. Extracts from most of the vegetables and plants did not show antimicrobial activity except for the leaves of Ginkgo biloba L. and seeds of Prunus Dallicina L. did not show antimicrobial activity except for the leaves of Ginkgo biloba L. and the seeds of Prunus sallicina L.

• Biomolecules & Therapeutics
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• 제20권5호
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• pp.477-481
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• 2012

The rhizomes of Acorus gramineus have frequently been used in traditional medicine mainly for sedation as well as enhancing brain function. In this study, the anti-allergic activity of A. gramineus was investigated. The 70% ethanol extract of the rhizomes of A. gramineus was found to inhibit the allergic response against 5-lipoxygenase (5-LOX)-catalyzed leukotriene (LT) production from rat basophilic leukemia (RBL)-1 cells and ${\beta}$-hexosaminidase release from RBL-2H3 cells with $IC_{50}$'s of 48.9 and > $200{\mu}g/ml$, respectively. Among the 9 major constituents isolated, ${\beta}$-asarone, (2R,3R,4S,5S)-2,4-dimethyl-1,3-bis (2',4',5'-trimethoxyphenyl)tetrahydrofuran (AF) and 2,3-dihydro-4,5,7-trimethoxy-1-ethyl-2-methyl-3-(2,4,5-trimethoxyphenyl)indene (AI) strongly inhibited 5-LOX-catalyzed LT production in A23187-treated RBL-1 cells, AI being the most potent ($IC_{50}=6.7{\mu}M$). Against ${\beta}$-hexosaminidase release by antigen-stimulated RBL-2H3 cells, only AI exhibited strong inhibition ($IC_{50}=7.3{\mu}M$) while ${\beta}$-asarone and AF showed 26.0% and 39.9% inhibition at $50{\mu}M$, respectively. In addition, the ethanol extract of A. gramineus showed significant inhibitory action against the hapten-induced delayed hypersensitivity reaction in mice by oral administration at 200 mg/kg. Therefore, it is suggested that A. gramineus possesses anti-allergic activity and the constituents including ${\beta}$-asarone and AI certainly contribute to the anti-allergic activity of the rhizomes of A. gramineus.