• Korean Journal of Pharmacognosy
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• v.28 no.1
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• pp.54-58
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• 1997

The cytotoxic activities of methanolic extract and its fractions of Ailanthi Cortex Radicis and column chromatographic eluates of its dichloromethane fraction (DCM fr.) were investigated. DCM fr. Showed the strongest cytotoxicity against hepatoma cells. Furthermore, the active equates 1-3, 8 and 9 were obtained. Effects on free radical generation and the growth of vascular endothelial cells were tested to elucidate the action mechanism of anticancer activity. Eluates 1-3 stimulated free radical generation, while eluates 8 and 9 showed no changes. Especially, eluates 8 and 9 efffectively inhibited the proliferation of vascular endothelial cells in a dose- dependant manner. It is speculated that the anticancer effects of eluates 1-3, 8 and 9 might be due to free radical generation and inhibition of endothelial cell growth, respectively.

• Journal of Food Hygiene and Safety
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• v.10 no.4
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• pp.219-224
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• 1995

The antimutagenic effects of 46 kinds of medicinal plants that have been used as traditional folk antitumor agents in Korea were studied by using Ames mutagenicity test. Most of the methanolic extracts from the plants which were used in this experiment showed strong antimutagenic activity toward aflatoxin B1(AFB1) in Salmonella typhimrium TA100 and TA98. However, N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) induced mutagenicity was not blocked by adding the methanolic extracts of the plants except persimmon leaves (Diospyros kaki Thunberg)and Elaeagnus umbellata.

• Proceedings of the Korean Society of Fisheries Technology Conference
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• 2001.10a
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• pp.151-152
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• 2001

Chitin, a polymer of N-acetylglucosamine ($\beta$-1,4 linked 2-acetamido-D-glucose), is a cellulose-like biopolymer present richly in the exoskeleton of crustaceans and in cell walls of fungi, insects and yeast. Chitosan is derived from chitin by deacetylation, to different degrees, in the presence of alkali. [l]. Recent studies for chitin and chitosan have been concentrated in bioactivities such as antitumor activity, immuno-enhancing effects, enhancing protective effects against infection with some pathogens in mice, and antimicrobial activeity [2]. (omitted)

• Journal of Marine Bioscience and Biotechnology
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• v.1 no.4
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• pp.225-231
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• 2006

The secondary metabolites from Taiwanese marine soft corals and sponges have attracted much attention because they possess considerable potential biological activities. To explore the origin of bioactivity, many cytotoxic natural products were isolated and characterized in the past few years. For examples, The lipophilic extracts from marine sponges Petrosia elastica and Ircinia formosana were found active against several human tumor cells. The investigation of the gorgonian Junceela has also resulted in the discovery of a series of new juncenolides. Bioassay-directed fractionation of Clavularia viridis yielded seven new prostanoids. These compounds have been tested and evaluated as potential antitumor agents. The soft corals of the genus Cespitularia produced novel secondary metabolites with diverse chemical structures and interesting biological activities. Four new norditerpenoids, designated cespitulactones and cespihypotins were isolated from Cespitularia hypotentaculata. Cespitulactones are novel structures having a bond cleavage between C-10 and C-11. In addition, three novel diterpenes were isolated from C. taeniata and designated cespitulactams A, B and C having a phenylethyl amino side chain.

• Archives of Pharmacal Research
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• v.23 no.4
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• pp.288-301
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• 2000

A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (I6 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

• Archives of Pharmacal Research
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• v.23 no.5
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• pp.450-454
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• 2000

Eight 2-alkylaminosubstituted 5,8-dimethoxy-4-methylquinolines and nine 2-alkylaminosub-stituted or 2,6-disubstituted 4-methylquinoline-5,8-diones were synthesized and evaluated in vitro cytotoxicity against four human cancer cell lines (HOP62, SK-OV-3, HCT15 and SF295).

• Journal of Ginseng Research
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• v.42 no.3
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• pp.255-263
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• 2018

Orally administered ginsengs come in contact with the gut microbiota, and their hydrophilic constituents, such as ginsenosides, are metabolized to hydrophobic compounds by gastric juice and gut microbiota: protopanxadiol-type ginsenosides are mainly transformed into compound K and ginsenoside Rh2; protopanaxatriol-type ginsenosides to ginsenoside Rh1 and protopanaxatriol, and ocotillol-type ginsenosides to ocotillol. Although this metabolizing activity varies between individuals, the metabolism of ginsenosides to compound K by gut microbiota in individuals treated with ginseng is proportional to the area under the blood concentration curve for compound K in their blood samples. These metabolites such as compound K exhibit potent pharmacological effects, such as antitumor, anti-inflammatory, antidiabetic, antiallergic, and neuroprotective effects compared with the parent ginsenosides, such as Rb1, Rb2, and Re. Therefore, to monitor the potent pharmacological effects of ginseng, a novel probiotic fermentation technology has been developed to produce absorbable and bioactive metabolites. Based on these findings, it is concluded that gut microbiota play an important role in the pharmacological action of orally administered ginseng, and probiotics that can replace gut microbiota can be used in the development of beneficial and bioactive ginsengs.

• YAKHAK HOEJI
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• v.52 no.6
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• pp.514-519
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• 2008

We developed a convenient synthetic route to 3-alkylated 2-phenyl-4-quinolone derivatives (4a-h and 5a-c), which were expected to retain antitumor activity. A series of 2,3-dihydro-2-hydroxy-2-phenyl-4-quinolones (3a-h) was synthesized through dehydration, dealcoholation and hydration using acid-catalyzed one-pot reaction from anilines and ethyl benzoylacetates. 3-Methyl (or 3,3-dimethyl)-2-phenyl-4-quinolone derivatives 4 and 5 were synthesized from 3a-h through the methylation using methyl iodide. Formation of quinolone nucleus was undertaken with p-toluenesulfonic acid (p-TSA) at $90{\sim}110^{\circ}C$ in toluene for 3${\sim}$7.5 hr over the Dean-Stark apparatus. The key intermediates in these preparations are ${\beta}$-ketoesters 2a-h, which can be readily obtained from the corresponding anilines 1a-e by reaction with ethyl bezoylacetates.

• YAKHAK HOEJI
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• v.27 no.4
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• pp.309-314
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• 1983

Six hydantoin derivatives, 3-(2-chloroethyl) hydantoin (6a), 3-(2-chloroethyl)-5-isopropylhydantoin (6b), 3-(2-chloroethyl)-5-isobutylhydantoin (6c), 3-(2-chloroetbyl)5-(2-butyl) hydantoin (6d), 3-(2-chloroethyl)-5-benzylhydantoin (6e), 3-(2-chloroethyl)-5-(indolyl-3-methyl) hydantoin (6f), were prepared by the treatment of the corresponding salt of amino acids with 2-chloroethyl isocyanate in cold water, followed by refluxing in concentrated HCl solution. Anticancer activity of the synthesized hydantoin derivatives were examined on murine leukemia L1210 cells growing in Fischer medium. Among them, 3-(2-chloroethy)-5-isobutyl-hydantoin (6c) showed substantially low $ED_{50}$ value of $9.6{\mu}g/ml$.

• Proceedings of the Korean Biophysical Society Conference
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• 1999.06a
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• pp.34-34
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• 1999

TRAIL (also known as Apo-2L) is a newly identified cytokine belonging to the large tumor necrosis factor (TNF) family. TRAIL is a novel molecule in that it induces apoptosis in a wide variety of tumor cells but not in normal cells. In order to help elucidating its biological roles and designing mutants with improved therapeutic potential, we have determined the crystal structure of human TRAIL.(omitted)