• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.3
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• pp.710-715
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• 2005

This research was to investigate inhibitory activity of Sasang medicines on Obesity. 56 kind of herb medicines to powder, abstract add 100 times methanol. Examine inhibitory effect against lipase activity in vitro. It was compared Xenical(Orlistat) with 56 kind of herb medicines. Inhibitory effect against lipase activity of Xenical as a standard was 93.3%. It is Inhibitory effect against lipase activity of Taeyangin herb medicine. (Fructus Pruni Tomentosae 77.7% Cortex Acanthopanacis73.5%, Fructus Chaenomelis73.1%, rice bran on a mallet head68.1%, Semen Fagopyri 48.1%, Radix Vitis 31.5%) It is Inhibitory effect against lipase activity of Soyangin herb medicine. (Radix Saposhnikoviae 91.5%, Semen Plantaginis 90.4%, Semen Trichosanthis 89.2%, Herba Schizonepetae 85.7%, Radix Euphorbiae Kansui 76.1%, Rhizoma Anemarrhenae 76.0%, Cortex Phellodendri 75.1%, Herba Menthae 74.8%, Radix Angelicae Pubescentis 61.2%, Rhizoma Alismatis 62.6%, Poria 60.9%, Rhizoma Notopterygii 22.5%, Radix Peucedani 18.2%, Caulis Akebiae 17.7%) It is Inhibitory effect against lipase activity of Taeeumin herb medicine. (Herba Spirodelae 91.4%, Radix Polygalae 88.3%, Arillus Longanae 84.3%, Radix Platycodi 81.7%, Semen Zizyphi Spinosae 80.2%, Spina Gleditsiae 79.7%, Herba Ephedrae 75.3%, Semen Raphani 73.1%, Rhizoma Cimicifugae 73.0%, Rhizoma Acori Graminei 71.8%, Flos Chrysanthemi71.0%, Radix et Rhizoma Rhei 68.4%, Vermiculus Holotrichia 59.9%, Radix Puerariae 55.3%, Fructus Schizandrae 53.4% Semen Coicis 50.6%, Semen Biotae 47.5%, Semen Nelumbinis 46.7%, Radix Angelicae Dahuricae 45.1%, Semen Castaneae 44.4%, Rhizoma Ligustici 34.5%, Tuber Liriopis 16.4%, Radix Scutellariae4.2%) It is Inhibitory effect against lipase activity of Soeumin herb medicine. (Pericarpium Arecae89.9%, Rhizoma Alpiniae Officinarum 89.5%, Radix Polygoni Multiflori81.2%, Rhizoma Cyperi 79.0%, Cortex Magnoliae 72.8%, Radix Aucklandiae 72.0%, Rhizoma Zingiberis 71.9%, Pericarpium Citri Reticulatae Viride 71.3%, Radix Cynanchi Wilfordi 57.7% Rhizoma Pinelliae 36.7%, Fructus Alpiniae Oxyphyllae 35.8% Fructus Aurantii Immaturus 17.5%, Pericarpium Citri 16.1%) Therefore, Radix Saposhnikoviae(91.5) and Herba Spirodelae(91.4%) were the most effective medicice of 56 kind of medicines.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.318-324
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• 2000

9 New cephalosporin derivatives were synthesized and screened for antibacterial activities against various bacteria. (6R,7R) -7$\beta$-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(2-hydroxycarbamoyl)-s-triazolo[1,5-a]-pyrimidin-7-yl]thiomethyl]-3-cephem-4-carboxylic acid sodium salt (compound 3) showed 2 fold enhanced in vitro activity against P. aerurginosa, compared to ceftazidime.

• Archives of Pharmacal Research
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• v.21 no.4
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• pp.440-444
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• 1998

A series of 6-(N-arylamino)-7-methylthio-5,8-quinolinedione derivatives 4a-4l was newly synthesized for the evaluation of antifungal activity. 6-(N-Arylamino)-7-methylthio-5,8-quinolinediones were prepared by regioselective nucleophilic substitution of 6,7-dichloro-5,8-quinolinediones with arylamines in the presence of $Ce^{3+}$, and $Na_2$S/dimethylsulfate. The MIC values of 4a-4l were determined for antifungal susceptibility in vitro against Candida species by agar streak method. The derivatives 4a-4l had generally potent antifungal activities against all human pathogenic fungi. Especially they had the most potent activity against C. krusei at 12.5-0.8 $\mu\textrm{g}$/ml. Compounds 4d, 4g, 4h, 4j and 4k had more potent antifungal activities than fluconazole. Compounds 4g and 4h completely inhibited the fungal growth at 0.8-6.3 $\mu\textrm{g}$/ml against all Candida species, while fluconazole inhibited the growth at 25 $\mu\textrm{g}$/ml. The compounds such as 4g and 4h containing an N-(4-bromo-2-methylphenyl)- or N-(4-bromo-3methylphenyl)amino substituent exhibited the most potent antifungal activities.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.42 no.4
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• pp.335-343
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• 2009

Antimicrobial resistance patterns of Vibrio species isolated from brackish water in Geoje, Tongyeong and Goseong, Gyeongsangnamdo province into which streams, sewage and leachate all flowed. Only 19 strains (10.7%) of 177 V. parahaemolyticus were susceptible to 15 antimicrobials. 146 strains (69.5%) proved resistant against more than one antimicrobial and 12 strains (6.8%) were multi-drug resistant. The resistance rate of 152 strains were 85.9% against AM and 26.6% against RA, 16.4% against AN, 13.6% against Sand 13.0% against TMP. 86 strains of 129 V. cholerae non-O1 (66.7%) were susceptible to antimicrobials and 31 strains (24.0%) were resistant to more than one antimicrobial and 12 strains (9.3%) were multi-drug resistant. The antimicrobial resistance rate of 129 strains against 15 antimicrobials, with the exception of C, CIP, E and GM, i.e. 11 antimicrobials, was 0.7-16.2%, 16.2% of 129 strains proved resistant against RA and 13.9% against AM, 9.3% against TMP, 7.7% against SXT and 6.9% against TE. 19 of 49 strains of V. mimicus (38.8%) were susceptible to antimicrobials and 31 strains (61.2%) were resistant against more than one antimicrobial; none of the strains were multi-drug resistant. 15 strains of V. mimicus were resistant against only RA, AmC and TE. The resistance rate was 59.2% against RA (highest) 4.1% against AmC and 2.0% against TE.

• Journal of Ginseng Research
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• v.8 no.2
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• pp.153-166
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• 1984

The anticancer activities of petroleum ether extract of Panax ginseng root(crude GX) and its partially purified fraction from silicic acid column chromatography (7:3 GX) were studied with Sarcoma 180(S-180) or Walker carcinosarcoma 256 (Walker 256) in vivo and with L1210 leukemic lympocyte in vitro. Potential cytotoxic activities of the crude GX and against L1210 cells were compared with those of 5-Fluorouracil (5-FU) and saponin derivatives (Panax-diol, Panax-triol, Diol saponin, Triol saponin) in vitro. In order to observe the physiological effects of the crude GX and 7:3 GX on the animals with cancer, hemoglobin(Hb), red blood cell(R.B.C) and white blood cell after treatment with each GX in comparison with corresponding control groups, respectively. The anticancer effects of the crude GX and 7:3 GX were estimated by measuring the survival time of S-180 bearing mice after treatment with them. The experimental results obtained are summarized as follows; 1. The one unit of cytotoxic activity against L1210 cells was equivalent to 2.54$\mu\textrm{g}$ and 0.88$\mu\textrm{g}$of the crude GX and 7:3 GX per ml of culture medium, respectively. 2. The cytotoxic activities of Panax-diol, Panax=triol, Diol saponin and triol saponin against L1210 cells were not detected. 3. The anticancer activities of 5-FU against L1210, S-180 and Walker 256 were very effective in vivo and vitro tests. 4. The significantly increased W.B.C values of mice after inoculation with S-180 cells were reduced to normal range by the crude GX treatment. 5. The significantly decreased Hb values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude GX. 6. 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.

• Natural Product Sciences
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• v.25 no.1
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• pp.23-27
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• 2019

From the pericarps of Litsea japonica (Thunb.) Jussieu, eighteen butanolide derivatives (1 - 18) were evaluated for their cytotoxic activity against HeLa, HL-60, and MCF-7 cells. Compounds 1-9 with 2-alkylidene-3-hydroxy-4-methylbutanolides structure exhibited cytotoxic activities against cancer-cell lines. Among them, compound 8 (litsenolide $D_2$) exhibited the most potent cytotoxicity against the tested cell lines, including HeLa, HL-60, and MCF-7, with $IC_{50}$ values of $17.6{\pm}1.3$, $4.2{\pm}0.2$, and $12.8{\pm}0.0{\mu}M$, respectively. Compound 8 induced apoptosis in a dose-dependent manner. Annexin V/Propidium Iodide (PI) double staining confirmed that 8 effectively induced apoptosis in MCF-7 cells. To the best of our knowledge, we have reported cytotoxic activity of butanolides from L. japonica against these cancer-cell lines for the first time.

• 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.

• YAKHAK HOEJI
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• v.37 no.2
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• pp.158-162
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• 1993

6$\beta$-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl)acetamidopenicillanic acid(7a~7c) and 7$\beta$-(trans-3-Aryl-5-oxo-pyrrolidin-2-yl) acetamidocephalosporanic acid(8a~8c) were synthesized and tested in vitro antibacterial activity. Of these new penicillins exhibited good antibacterial activity against Gram-positive bacteria whereas none of the compounds possessed the activity against Gram-negative bacteria at the concentration tested.

• Bulletin of the Korean Chemical Society
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• v.25 no.7
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• pp.991-996
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• 2004

New series of 6-(arylthio)uracils, 6-(4-substituted-1-piperazinyl)uracils, 2,4,5-trioxo-1H,3H-benzothiopyrano[2,3-d]pyrimidine and 5-aryl-2,4-dioxo-1H,3H-pyrimido[5,4-f]benzo[1,4]thiazepines have been prepared and screened for their in vitro activity against herpes simplex-1 virus (HSV-1) and human immunodeficiency virus-1 (HIV-1). The in vitro cytotoxic activity was also evaluated. The results of biological testing revealed that compound 5b showed marginal activity against HSV-1, while compounds 5b and 5f exhibited marginal activity against HIV-1. The rest of the tested compounds were found devoid of antiviral activity against both HSV-1 and HIV-1.

• Archives of Pharmacal Research
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• v.23 no.1
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• pp.42-45
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• 2000

6-Arylamino-7-halo-5,8-quinolinediones (4a-4k, 5a-5b) were tested for in vitro cytotoxicity against human solid tumor cell lines such as A 549 (non-small cell lung). SK-OV-3 (ovarian), SK-MEL-2 (melanoma), HCT-15 (colon) and XF 498 (CNS) by SRB assay. The arylamino-7-chloro-5,8-quinolinediones 4 were also evaluated for cyclin-dependent kinase (CDK2 and CDK4) inhibitory effect. Among them, the 5,8-quinolinediones 4a and 5a with 7-(4-fluorophenyl) amino group were found to be potent cytotoxic against HCT 15, SKOV-3 and XF 498, and the compounds 4f and 4i showed inhibitory activities for the CDK4.