• Archives of Pharmacal Research
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• v.22 no.1
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• pp.30-34
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• 1999

When liriodendrin or syringin was incubated for 24 h with human intestinal bacteria, two metabolites, (+)-syringaresinol$\beta$--D-glucopyranoside and (+)-syringaresionl, from liriodendrin and one metabolite, synapyl alcohol, from syringin were produced. The metabolic time course of liriodendrin was as follows: at early time liriodendrin was converted to (+)-syringaresinol-$\beta$-D-glucopyranoside, and then (+)-syringaresinol. The in vitro cytotoxicities of these metabolites, (+)-syringaresinol and synapyl alcohol, were superior to those of liriodendrin and syringin.

• Archives of Pharmacal Research
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• v.18 no.3
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• pp.164-168
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• 1995

In order to elucidate the cytotoxicity-structure correlation of ginseng-derived components, several prosapogenins and sapogenins were prepared from Korean red ginseng (Panax ginseng) saponins by acid hydrolysis or alkaline cleveage, and their chemical structures were identified by a combination of spectral and physical methods. Some of these degradation products showed the cytotoxic activities against various cancer cell lines, A549, SK-OV-3, SK-Mel-2, P388, L1210 and K562. The significant difference in cytotoxicity between stereoisomers was not found and the activity was inversely proportional to the number of sugars linked to sapogenins. Diol-type prosapogenins and sapogenins showed higher cytotoxicity than triol-type ones.

• Archives of Pharmacal Research
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• v.22 no.6
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• pp.638-641
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• 1999

Cytotoxicities of four urushiols, congeners isolated from the sap of Korean lacquer tree (Rhus vernicifera Stokes), to 29 human cancer cell lines originated from 9 organs were evaluated. Their values of 50% growth inhibition were below $4{\mu}g/ml$, and showed cell line specific cytotoxicity. The present results is the first report on the cytotoxicity of urushiols suggesting that they would have an anticancer activity to human cancer cells.

• YAKHAK HOEJI
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• v.47 no.6
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• pp.376-381
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• 2003

2-Arylchromones, also known as flavones, are among the most ubiquitous classes of natural products occurring in the plant kingdom. On the other hand, 2-styrylchromones are relatively scarce in nature and only a few compounds has been isolated from the blue-green algae species. Therefore, new 2-arylethenylchromone derivatives ( 4a∼n, 5a∼f) were synthesized by the aldol condensation of 2-methylchromone ( 3) with several aromatic aldehydes in order to evaluate their cytotoxicities using a MTT assay on three tumor cells. 2-Arylethenylchromone derivative 4a showed the significant cytotoxic activities on KB, HL-60 and P-388 cell lines with $IC_{50}$/ values of 25.2, 63.59 and 49.51 $\mu$M, respectively, indicating that 2-arylethenylchromone skeleton has a potential anti-tumor application.

• Microbiology and Biotechnology Letters
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• v.28 no.4
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• pp.209-213
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• 2000

The cultured mycelia of Ganoderma lucidum were extracted and the extract was separated into six fractions by organic solvent fractionation. The antihepatotoxic activity of all the fractions was evaluated by measuring activities of glutamic pyruvic transaminase (GPT) and glutamic oxaloacetic transaminase (GOT). Among the fractions tested, the high-polarity fractions such as aqueous and n-butanol fractions significantly reduced activities of GPT and GOT in CCl4- and galactosamine-intoxicated rat primary hepatocytes. When intracellular synthetic activities were measured by pulsing the rate primary cultured hepatocytes with [3H]-uridine and [3H]-leucine, activities of DNA, RNA and protein. When direct toxicities of the fractions were measured against human hepatoma(SK-Hep-1), the non-polarity fractions such as n-butanol and ethyl acetate fractions showed potent direct cytotoxicities even at the concentration of 1 $\mu\textrm{g}$/ml. These data showed that Ganoderma lucidum has hepatoprotective and hepatotoxic recovery principles in its mycelia.

• Korean Journal of Pharmacognosy
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• v.28 no.4
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• pp.192-197
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• 1997

As a part of searching for new antitumor agents from natural products, 94 kinds of Chinese plants were extracted with petroleum ether/ether (1:1), ethyl acetate and methanol, successively and their cytotoxicities were evaluated against A549 (human lung carcinoma) cell line. Among them, six kinds of ether extracts, seven kinds of ethyl acetate extracts and one kind of methanol extracts showed significant cytotoxic activities (above 70% inhibition) at a concentration of $50\;{\mu}g/ml$. These results surest that they may be involved in natural sources with possible anticancer activities.

• Bulletin of the Korean Chemical Society
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• v.12 no.1
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• pp.85-87
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• 1991

Poly[(tri-O-acetyl-D-glucal)-alt-(maleic anhydride)] was synthesized by free radical copolymerizations of the relevant comonomers. The alternating sequence of the copolymer was confirmed by $^1$H-NMR, elemental analysis, and titration of anhydride groups incorporated into the copolymer. Hydrolysis of the copolymer under different conditions resulted in poly[(2-acetoxymethyl-3,4-diacetoxytetrahydropyran-5,6-diyl) (1,2-dicarboxyethylene)] and poly[(2-hydroxymethyl-3,4-dihydroxytetrahydropyran-5,6-diyl) (1,2-dicarboxyethylene)]. The cytotoxicities of these polymers measured against normal and tumor cells (3LL, B16) in vitro were found to be higher than that of DIVEMA, a prototype polymer having a high antitumor activity.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.499-502
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• 2001

To evaluate the role of imidazolidinone moiety of potential anticancer 4-phenyl-1-arylsulfonylimidazolidinones 1 for their cytotoxicity conformationally similar 4-phenyl-2-arylsulfonylaminooxazolines 2 were synthesized and compared their cytotoxicities with those of the corresponding 1. Compounds 2 showed much reduced activity compared to N-arylsulfonylimidazolidinones 1. This result might indicate that the imidazolidinone ring of 1 have the other roles for the activity as an essential structural motif in addition to conformational contribution .

• YAKHAK HOEJI
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• v.44 no.2
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• pp.169-174
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• 2000

Pedunculagin is an ellagitannin purified from Alnus hirsuta var. microphylla. Betulaceae. The effects of pedunculagin on immune system have been characterized to induce enhancement of NK (natural killer) cell cytotoxicities against tumor cells. Here, we report the evaluation of the effects of pedunculagin on the growth of murine Bl6-F10 melanoma in vivo. After the intradermal inoculation of Bl6-F10 melanoma, Bl6-F10 tumors grew progressively in immunocompetent syngenic C57BL/6 mice. The mice treated with pedunculagin(10 mg/kg, every 48 hrs) resulted in a significant improvement in survival. Inhibitory effects of pedunculagin on lung metastasis in C57BL/6 mice were also detected. Summarizing treatment with pedunculagin has a significant antitumor effect upon Bl6-F10 murine melanoma.

• Archives of Pharmacal Research
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• v.26 no.9
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• pp.686-696
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• 2003

Ethyl (coumarin-4-oxy)acetate 1 was prepared through the reaction of 4-hydroxycoumarin with ethyl bromoacetate. Compound 1 was allowed to react with hydrazine hydrate to produce coumarin-4-oxyacetic hydrazide 2. The synthesis of N-(arylidene and alkylidene)-coumarin-4-oxyacetic hydrazones 3-20 was performed. The preparation of 2-substituted-3-[(coumarin-4-oxy) acetamido]thiazolidinones 21-26 and 2-[(coumarin-4-oxy )methyl]-4-acetyl-5-substituted-$\Delta^2$-1,3,4-oxadiazolines 27-33 was performed by the reaction of the hydrazones 3, 4, 7, 9, 12, 14 with mercaptoacetic acid and the hydrazones 3, 4, 5, 7, 12, 15, 16 with acetic anhydride, respectively. The antiviral activities, cytotoxicities and structure-activity relationship (SAR) towards different microorganisms of the prepared compounds were studied.