• Journal of Ginseng Research
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• v.44 no.2
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• pp.215-221
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• 2020

Background: Panax ginseng has been used for a variety of medical purposes in eastern countries for more than two thousand years. From the extensive experiences accumulated in its long medication use history and the substantial strong evidence in modern research studies, we know that ginseng has various pharmacological activities, such as antitumor, antidiabetic, antioxidant, and cardiovascular system-protective effects. The active chemical constituents of ginseng, ginsenosides, are rich in structural diversity and exhibit a wide range of biological activities. Methods: Ginsenoside constituents from P. ginseng flower buds were isolated and purified by various chromatographic methods, and their structures were identified by spectroscopic analysis and comparison with the reported data. The 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H- tetrazolium bromide method was used to test their cytotoxic effects on three human cancer cell lines. Results: Six ginsenosides, namely 6'-malonyl formyl ginsenoside F₁ (1), 3β-acetoxyl ginsenoside F₁ (2), ginsenoside Rh₂₄ (6), ginsenoside Rh₂₅ (7), 7β-hydroxyl ginsenoside Rd (8) and ginsenoside Rh₂₆ (10) were isolated and elucidated as new compounds, together with four known compounds (3-5 and 9). In addition, the cytotoxicity of these isolated compounds was shown as half inhibitory concentration values, a tentative structure-activity relationship was also discussed based on the results of our bioassay. Conclusion: The study of chemical constituents was useful for the quality control of P. ginseng flower buds. The study on antitumor activities showed that new Compound 1 exhibited moderate cytotoxic activities against HL-60, MGC80-3 and Hep-G2 with half inhibitory concentration values of 16.74, 29.51 and 20.48 μM, respectively.

• Archives of Pharmacal Research
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• v.29 no.12
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• pp.1091-1095
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• 2006

For the development of novel antitumor agents, we designed and synthesized terpyridines, and their biological activities were evaluated. Although most of the newly prepared terpyridines showed strong cytotoxicity against several human cancer cell lines, [2,2';6',2"]-terpyridine displayed the most significant cytotoxicity.

• Bulletin of the Korean Chemical Society
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• v.35 no.1
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• pp.129-134
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• 2014

Two series of SAHA-liked hydroxamate analogues were designed, synthesized and evaluated for their biological activities against nuclear HDACs. Compounds of Series I were found to be very effective inhibitors of cancer cell growth in the PC-3, Hut78, K562 and Jurkat E6-1 cancer cell lines with mean $IC_{50}$ values from $0.54{\mu}M$ (Ic, Jurkat E6-1) to $7.73{\mu}M$ (Ib, K562), indicating that they are cell permeable and the benzimidazolyl-based ligands are flexible enough to occupy the binding site of HDAC.

• Bulletin of the Korean Chemical Society
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• v.32 no.1
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• pp.65-70
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• 2011

Coumarins are ubiquitous in plant kingdom and have been used as antitumor, antifungals, anticoagulants, insecticides. Chalcones are also widespread in plant kingdom and have been known to possess diverse biological activities; antibacterial, antifungal, antitumor and anti-inflammatory, etc. As they are considered as important natural products, numerous synthetic approaches have been reported up to the present. We devise a new selective method of preparing dihydrocoumarins and chalcones from aryl cinnamates by the selection of reagents. Dihydrocoumarin derivatives were prepared selectively by using intramolecular cyclization catalyzed by p-toluene sulfonic acid. Also, chalcones were prepared by Fries-rearrangement catalyzed by $TiCl_4$. This method can be used for preparing various coumarin & chalcone compounds.

• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.3
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• pp.691-697
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• 1999

The pharmacological effects of hydrocooked(110oC, 5 hours) extracts of Bastard halibut have been investigated. All of the hydrocooked extracts showed the measurable contractile effect on the isolated rat duodenum and decreased the normal blood pressure in anesthetized rat. The hydrocooked extracts also exhibited a dose dependent relaxation on the isolated rat aorta precontracted with phenylephrine. Only RM 60 fraction of these extracts had the cytotoxic effect against MCF7 cell(human breast adenocarcinoma cell line), but the other fractions showed neither antibacterial activity nor antitumor activity. Although fish extracts fed group of rat maintained their original body weight, there were no notable changes in the hematological parameters, except that the levels of high density lipoprotein was significantly increased. These results suggest that the hydrocooked extracts of bastard halibut may contain a variety of bioactive materials.

• Korean Journal of Veterinary Service
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• v.25 no.3
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• pp.309-314
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• 2002

Recombinant interleukin-2(IL-2) has demonstrated as an antineoplastic agent in mice and human, but the relatively low response rates observed in clinical trials. Therefore, the present study was undertaken in order to evaluate therapeutic activities of IL-2 for the establishment of therapeutic applications. At the onset of the experiment, normal C3H/HeN mice were injected with 5$\times$10$\^$6/ RD-995 tumor cells, murine ultraviolet radiation-induced fibrosarcoma, intraperitoneally. Beginning on day 6, experimental groups were treated with a 5-day course of IL-2(subcutaneous injection of 30,000 IU every 12 hours for 5 days). The result of this experiment revealed that body weight gradually decreased from 20th day in control mice. Subcutaneous IL-2 therapy prevented partially decrease body weight, and prolonged survival of mice compared with control group.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.354.2-354.2
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• 2002

Fifty of 3.4-diaryl-2(5H)-furanone derivatives were synthesized and evaluated for their cytotoxicity in a small panel of cancer cell lines. Eleven compounds in this series, were found to have significant cytotoxic activities with ED$_{50}$ values of less than 1 4{\mu}$M in most of the cell lines tested. Compound RTMSI, 3-(3.4, 5-trimethoxyphenyl)-4-(3-amino-4-methylamino)-2(5H)-furanone exhibited the most potent cytotoxic activity with ED$_{50}$ value of 0.003 4{\mu}$M and antitumor activity on BDF1 mice bearing Lewis lung carcinoma cells with inhibition ratio of 72 %.%.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.129.2-129.2
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• 2003

Antitumor and immunomodulatory activities of an aqueous extract (GF100) of Acanthopanax senticosus was examined. In experimental lung metastasis of colon26-M3.l carcinoma cells, intravenous (i.v.) administration of GF100 2 days before tumor inoculation significantly inhibited lung metastasis in a dose-dependant manner. The i.v. administration of GF100 also exhibited the therapeutic effect on tumor metastasis of colon26-M3.1 cells, when it was injected 1 day after tumor inoculation. In an in vitro cytotoxicity analysis, GF100 enhanced the responsiveness to a mitogen, concanavalin A (ConA), of splenocytes in a dose-dependent manner. (omitted)

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.347.3-347.3
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• 2002

Recent study indicated that terpyridine and its derivatives displayed highly active antitumor properties. In this presentation. derivatives of terpyridines having three pyridine moieties at 2',4',6'-position of central pyridine skeleton were prepared, and evaluated their cytotoxicity against several human cancer cell lines and topoisomerase I inhibitory activities. Most of the prepared compounds showed strong cytotoxicity compared to doxorubicln. In addition. several compounds displayed better cytotoxicity than that of doxorubicin. In addition, several compounds displayed better cytotoxicity than that of doxorubicin. Structure-activity relationship study was perfomed to be indicated that [2.2':6',2']terpyidine skeleton is important to show strong xytotoxicity. Significant topoxicity. Significant topoisomerase I inhibitory activity was not observed for prepared compounds.

• Journal of the Korean Society of Food Science and Nutrition
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• v.33 no.3
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• pp.475-479
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• 2004

The proteinpolysaccharides (PPS) from Polyporus umbellatus (P. umbellatus) screlotium is composed by 78.2% of saccharide, 16.8% of protein, and 4.0% of ash. PPS from P. umbellatus showed antitumor activities against 180 solid tumor in ICR mice at the concentration of 20-160 mg/kg/day. PPS from P. umbellatus inhibited cell viability to 47.4% and 45.0% in leukemia cell lines, L-1210 and K-562 cells at 50-400 $\mu\textrm{g}$/mL concentration, respectively. But the hall mark of cell apoptosis, DNA fragmentation was not observed at those concentration. 2.5-10.0% of PPS from P. umbellatus inhibited mutagenecity evoked by 2-nitrofluorene and sodium azide in Salmonella typhimurium TA 98 and TA 100. From these results, it is suggested that the PPS of P. umbellatus has antitumor and antimutagenic effect, and its cytotoxic effect may not be ascribed to the apoptosis.