• Archives of Pharmacal Research
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• 제29권7호
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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.

• Preventive Nutrition and Food Science
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• 제7권4호
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• pp.447-450
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• 2002

Previously, a methanol extract from seeds of Paeonia lactiflora was shown to have a potent inhibitory activities against tyrosinase and soybean lipoxygenase (SLO). Seven stilbenes, trans-resveratrol-4-Ο-$\beta$-D-glucoside, trans resveratrol, trans-$\varepsilon$-viniferin, cis-$\varepsilon$-viniferin, gnetin H, suffruticosol A and B were isolated from the seeds as active principles for inhibition of the enzymatic activity. Among them, the resveratrol trimer, gnetin H exhibited the most potent inhibitory activities against tyrosinase and SLO, respectively. Additionally, the resveratrol dimers, trans-$\varepsilon$-viniferin and cis-$\varepsilon$-viniferin exhibited significant inhibitory activity against the two oxidative enzymes. Meanwhile, three other stilbene derivatives, such as trans-resveratrol, suffruticosol A and suffruticosol B had also weak inhibition activity. The least inhibitory activity was observed in transresveratrol-4-Ο-$\beta$-D-glucoside. These results suggest that resveratrol dimers and trimer in the seeds of Paeonia lactiflora are potentially useful therapeutic agents against pathological disorders such as hyperpigmentation and inflammation.

• 약학회지
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• 제10권4호
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• pp.7-20
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• 1966

1. Of the 32 extracts from Genus of lishenes broth tested for antimicrobial activity, 28 inhibited at least one of the 3 test microorganisms used. 2. Twenty seven lichnes broth from 32 species tested were active against at least one of the Gram-positive bacteria M. pyogenes var, aureus 203 p, and twenty four lichenes broth from 32 Species tested were active against at least one of the Gram-positive bacteria Bacillus subtilis ATCC 6633. 3 Twenty five lichenes broth from 32 species tested were active against at least one of the Gram-negative bacteria Escherichia coli 0.126. 4. The antibiotic substances in lichenes were readily extracted by organic solvents.

• Bulletin of the Korean Chemical Society
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• 제30권2호
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• pp.435-440
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• 2009

19 Aromatic ring and L-amino acid ester contained rupestonic acid amide derivatives 2a~2l, 3a~3g were synthesized and preliminarily evaluated in vitro against influenza virus $A_3$,B and herpes simplex virus type 1 (HSV-1), 2(HSV-2) by the national center for drug screening of China. The rusults showed that 2i possessed the highest inhibition against both influenza virus $A_3\;(TC_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;19.2\;{\mu}$mol/L, SI = 6.3) and B (T$C_{50}\;=\;120.6\;{\mu}mol/L,\;IC_{50}=\;29.9\;{\mu}$mol/L, SI = 4.0); 2g was more active against influenza $A_3$ virus at very low cytotoxicity ($TC_{50}\;>\;2092.1\;{\mu}mol/L,\;IC_{50}=\;143.7\;{\mu}mol/L,$ SI > 14.6) than the parent compound; Compounds 2b, 2c, 2f showed higher activities both against HSV-1 and HSV-2 than that of the parent compound, and 2f was the most potent inhibitor of HSV-1 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;11.3\;{\mu}mol$/L, SI = 17.7 ) and HSV-2 ($TC_{50}\;=\;200.0\;{\mu}mol/L,\;IC_{50}\;=\;20.7\;{\mu}mol$/L , SI = 9.7).

• 대한한방부인과학회지
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• 제26권1호
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• pp.41-58
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• 2013

Objectives: The object of this study was to observe the in vitro anti-bacterial and anti-inflammatory effects of three single aqueous herbal extracts(Trichosanthes Semen, Gardeniae Fructus, and Angelicae Dahuricae Radix), traditionally used for treating various gynecological diseases including mastitis in Korea, against Staphylococcus aureus and lipopolysaccharide(LPS)-activated Raw 264.7 cells. Methods: Anti-bacterial activities of three single aqueous herbal extracts against S. aureus were detected using standard agar microdilution methods. In addition, the effects on the cell viability, $PGE_2$, NO, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 productions of LPS activated Raw 264.7 cells. The anti-bacterial and anti-inflammatory effects were compared with lincomycin and piroxicam, respectively in the present study. Results: MIC of three single aqueous herbal extracts against S. aureus were detected as over 25, $4.063{\pm}2.096$ and $1.641{\pm}0.972$ mg/ml, respectively. MIC of lincomycin was detected as $0.469{\pm}0.297{\mu}g/ml$ at same conditions. In addition, $ED_{50}$ against LPS-induced cell viabilities and cytokine releases of three single aqueous herbal extracts were as follows - cell viability: 7.635, 13.761, 6.986 mg/ml, NO production : 4.808, 22.015, 2.949 mg/ml, $PGE_2$ production : 3.040, 4.312, 0.821 mg/ml, TNF-${\alpha}$ production : 9.563, 54.931, 1.240 mg/ml, IL-$1{\beta}$ production : 1.362, 1.801, 0.534 mg/ml, IL-6 production : 0.371, 0.797, 0.202 mg/ml, respectively. $ED_{50}$ of piroxicam against LPS-induced cell viabilities, NO, $PGE_2$, TNF-${\alpha}$, IL-$1{\beta}$ and IL-6 were detected as 35.179, 6.552, 1.162, 7.273, 7.101 and 5.044 ${\mu}g/ml$, respectively at same conditions. Conclusions: The results of the study showed anti-bacterial effects against S. aureus in the order of Gardeniae Fructus and Angelicae Dahuricae Radix aqueous extracts, except for Trichosanthes Semen. They also showed anti-inflammatory effects against LPS-activated Raw 264.7 cells in the order of Angelicae Dahuricae Radix, Trichosanthes Semen, and Gardeniae Fructus aqueous extracts. These three herbs are expected to be great substitutes to reduce side-effect of lincomycin and piroxicam, if the amount of those three single aqueous herbal extracts is adjusted appropriately.

• Archives of Pharmacal Research
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• 제28권7호
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• pp.765-769
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• 2005

The essential oil fraction of Ostericum koreanum was analyzed by GC-MS. Inhibiting activities of this oil and its main components were tested by the broth dilution assay and disk diffusion test against one antibiotic-susceptible and two resistant strains of Salmonella enteritidis and S. typhimurium, respectively. The GC-MS analysis revealed thirty-four compounds; the main components were $\alpha$-pinene (41.12%), $\rho$-cresol (17.99%) and 4-methylacetophenone (7.90%). The essential oil of O. koreanum and its main components were significantly effective against the tested antibiotic-susceptible strains as well as against the resistant strains of the two Salmonella species, with MICs (minimum inhibitory concentrations) ranging from 2 mg/mL to 16 mg/mL. The anti-Salmonella effects of the oils were dose-dependent on $M\"{u}ller-Hinton$ agar plates in this experiment. Additionally, checkerboard titer test results demonstrated significant combined effects of streptomycin and O. koreanum oil or cresol, one of the main components of this oil, against the two streptomycin resistant strains of S. typhimurium, with FICIs ranging from 0.12 to 0.37.

• 약학회지
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• 제36권4호
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• pp.334-340
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• 1992

Ethanol, total saponin and petroleum ether extract of Panax ginseng C.A. Meyer were tested for their anticlastogenic effects against induction of micronuclei by cyclophosphamide and benzo(a)pyrene in mice. Ginseng petroleum ether extract (GPEE) showed the highest suppressive effect among three extracts. GPEE was also tested to compare their anticlastogenic effect against several well-known carcinogens: such as mitomycin C, 7, 12-dimethyl benzo(a)anthracene, ethyl methane sulfonate, dimethylnitrosamine and busulfan. GPEE showed the anticlastogenic effect against most of carcinogens, although there were no significant effects against 7, 12-dimethyl benzo(a) anthracene, dimethyl nitrosoamine and busulfan-induced micronuclei.

• 한국미생물·생명공학회지
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• 제29권3호
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• pp.127-133
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• 2001

냉각탑수 중의 Legionella 속 균을 저감시킬 수있는 방법개발의 일환으로 L. pneumophila에 강한 항균성물질을 생산하는P. seruginosa KLP-2 균주를 냉각탑수로부터 분리 동정하였다 P.aeruginosa KLP-2 균주를 냉각탑수로부터 분리 동정하였다. P. aeruginosa KLP-2 균주의 배양여액은 L. pneumophila의 Vibro cholerae non-Ol Bacillus cereus, Bacillus subtilis 및 Staphylococcus aureus에 대해서도 항균성을 나타내었다. P. seruginosa KLP-2 균주 배양여액의 항균활성을 증가시키기 위한 최적조건은 0.1%의 $K_2$$HPO_4$와 0.05%의 $MgSO_4$$7H_2$O로 조성되 무기염배지에 탄소원으로써 1%의 glycerol, 질소원으로써, 0.6%의 proteose peptone이 첨가된 pH 7.0의 배지 조건에서 가장 높은 항균 활성을 나타내었으며 $35^{\circ}C$에서 20시간 진탕배양(50 rpm)한 후 4일간 정치 배양하였을 때 최대의 항균활성을 나타내었다.

• 대한화학회지
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• 제58권4호
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• pp.381-387
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• 2014

A series of new $N^7$-tetrazolo[5,1-f ]-1,2,4-triazin-8-(7H)-one derivatives 4-16 were designed and synthesized from 3 with different reagents. The newly prepared compounds were characterized by spectral data and screened for their antimicrobial activities against various bacteria and fungi strains.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.586-589
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• 1997

Antifungal activities of 6-[(N-4-bromophenyl)amino]-7-chloro-5,8-quinolinedione (RCK7) were tested. The MIC values of RCK7 were determined for antifungal suceptibility, in vitro against Aspergillus niger, Cryptococcus neoformans and Trichophyton mentagrophyte by standard agar streak method. In vitro, RCK7 showed more potent antifungal activity than fluconazole and ketoconazole. Also, RCK7 was tested for in vivo antifungal activity in the treatment of systemic infection with Candida albicans in normal mice. The therapeutic potential of RCK7 had been assessed by evaluating their survival rate against systemic infections compared with that of ketoconazole. $ED_{50}$ of intraperitoneally administered RCK7 ws $2.05{\pm}0.30mg/kg$ but that of ketoconazole was $8.00{\pm}0.73 mg/kg$, respectively. When RCK7 was administered intravenously at the $ED_{50}$(2.05 mg/kg). the colony counts of Candida albicans in the liver after 7 days and 14 days were reduced as likely as ketoconazole at the $ED_{50}(8.00 mg/kg)$, and the better survival rates than ketoconazole's were achieved after 14 days. The results suggest that RCK7 may be a potent antifungal agent.