• Natural Product Sciences
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• v.17 no.1
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• pp.5-9
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• 2011

An alkaloid, 3-methylcanthin-5, 6-dione, was isolated from the stem of Picrasma quassioides (D. Don) Benn. and characterized by comprehensive analyses of its 1D and 2D NMR spectra. It was also evaluated for its cytotoxic activity in vitro against three human cancer cell lines (MDA-MB-231, HT-29 and NCI-N87), using MTT assays. We found that 3-methylcanthin-5, 6-dione exhibited significant anti-inflammatory activity via inhibiting NO production induced in LPS-stimulated murine macrophage RAW264.7 cells. The antioxidant activity of 3-methylcanthin-5, 6-dione was measured by DPPH free radical scavenging assays, hydroxyl radical scavenging assays and reducing power assays. Our results showed that 3-methylcanthin-5, 6-dione has significant biological activities.

• Biomolecules & Therapeutics
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• v.20 no.3
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• pp.313-319
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• 2012

In recent years, inhibition of HDACs has emerged as a potential strategy to reverse aberrant epigenetic changes associated with cancer, and several classes of HDAC inhibitors have been found to have potent and specific anticancer activities in preclinical studies. But their precise mechanism of action has not been elucidated. In this study, a novel synthetic inhibitor of HDAC, 3-(4-dimethylamino phenyl)-N-hydroxy-2-propenamide [IN-2001] was examined for its antitumor activity and the underlying molecular mechanisms of any such activity on human breast cancer cell lines. IN-2001 effectively inhibited cellular HDAC activity ($IC_{50}$ = 0.585 nM) inMDA-MB-231 human breast cancer cells. IN-2001 caused a significant dose-dependent inhibition of cell proliferation in estrogen receptor (ER) negative MDA-MB-231human breast cancer cells. Cell cycle analysis revealed that the growth inhibitory effects of IN-2001 might be attributed to cell cycle arrest at $G_0/G_1$ and/or $G_2$/Mphase and subsequent apoptosis in human breast cancer cells. These events are accompanied by modulating several cell cycle and apoptosis regulatory genes such as CDK inhibitors $p21^{WAF1}$ and $p27^{KIP1}$ cyclin D1, and other tumor suppressor genes such as cyclin D2. Collectively, IN-2001 inhibited cell proliferation and induced apoptosis in human breast cancer cells and these findings may provide new therapeutic approaches, combination of antiestrogen together with a HDAC inhibitor, in the hormonal therapy-resistant ER-negative breast cancers. In summary, our data suggest that this histone deacetylase inhibitor, IN-2001, is a novel promising therapeutic agent with potent antitumor effects against human breast cancers.

• Korean Journal of Food Science and Technology
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• v.41 no.6
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• pp.687-693
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• 2009

This study was conducted to investigate the antioxidant activity, fibrinolytic activity and cytotoxic effect of Korean traditional noble rice wine made using different methods (A-C) and commercial rice wine (D-H) on various tumor cell lines. The antioxidant activity of rice wine was measured by DPPH (2,2-dipicryl-1-picrylhydrazyl), ABTS [2,2'-azinobis(3-ethylbenzthiazoline-6-sulphonic acid)] and NO (nitric oxide) radical scavenging assay. In this study, Samhaeju showed the greatest fibrinolytic activity of 13-17U and exhibited the highest antioxidant activity. Among the different Samhaeju, the sample prepared using method C had the highest antioxidant activity. The cytotoxic effect of rice wine were also examined against the human cancer cell line (A549 cells and HeLa cells) based on the results of a WST-1 assay and morphological changes. Rice wine induced the inhibition of cell proliferation and morphological changes in tumor cell lines in a concentration-dependent manner, with Samhaeju diluted 10 fold having the strongest effect on these factors. These findings suggest that Korean rice wine has antioxidant activity and cytotoxic effect, and that these factors are influenced by the method of preparation.

• Archives of Pharmacal Research
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• v.18 no.2
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• pp.118-120
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• 1995

The cytotoxicity-directed fractionation of MeOH extract of Terminalia chebula fruits led to the isolation of three hydrolyzed tannins and a related compound, gallic acid(1), $1,2,3,4,6-penta-O-galloy-{\beta}-_D/-glucopyranose(II)$,. chebulagic acid (III) and chebulinic acid(IV), as active principles. They were shoen to exhibit moderate cytotoxicity against cultured human tumor cell lines including A-549, SK-OV-3, Sk-MEL-2, XF-498 and HCT-15 in vitro.

• Journal of the Korean Chemical Society
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• v.41 no.7
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• pp.357-361
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• 1997

8-Azaxanthine (1), 3-${\beta}$-D-ribofuranosyl-8-azaxanthine (2), 3-${\beta}$-D-ribofuranosyl-8-azaxanthine-5'-monophosphate (3), and 3-${\beta}$-D-ribofuranosyl-8-azaxanthine-5'-(3-pyridinylcarbonyl)monophosphate (4) were synthesized. The in vitro antitumor activities of the synthesized compounds against P388 mouse leukemia, FM3A mammary carcinoma, and U937 human histiocytic lymphoma cells were determined by MTT assay. 2 with unnatural N-3 and C-1' glycoside bond had activity against three tumor cell lines and $IC_{50}$s of these compounds were 0.05, 0.06, and 0.06 ${\mu}mol/mL$ against three tumor cell lines, respectively. But these compounds had no antibacterial activity. $IC_{50}$s against U937 human histiocytic lymphoma cells were verified with the structural modification: $IC_{50}$s of 1, 2, 3, and 4 were 0.33, 0.06, 0.25, and 0.33 ${\mu}mol/mL$, respectively.

• Fisheries and Aquatic Sciences
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• v.3 no.1
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• pp.52-63
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• 2000

Non-specific reaction has been a problem in doing, especially, research and diagnosis for infectious agents. Avidin-biotin-peroxidase complex (ABC) techniques has widely been used to amplify a reaction. Photobacterium damse1a subsp. piscicdia (formerly Pasteurella piscicida) exhibited a capacity to bind with streptavidin non-specifically. The band, estimated 26 K Da in Western blotted paper, was blocked with biotin but incompletely. In an attempt to explore an involvement of the non-specific substance in attaching piscine cells, cell attachment test performed using anti- Ph. d. subsp piscicida sera raised mouse and rabbit exhibited slightly blocking effects for Mediterranean (1736) and significantly for Japanese (Sp 92144) isolate. Biotin decreased the attachment ability significantly for Sp92144 but it was not effective to 1736. Both isolates showed greatly enhanced attachment ability with poly-L-lysin. The non-specific binding substance was contained in bacterial extracellular products (ECPs). The substance was able to purified with 2-imminobiotin affinity column, the purified substance appeared to have 4 bands in silver staining, and had a carbohydrate branch. This purified substance showed cytotoxic effects selectively between 5 piscine cell lines. Moreover, it stimulated rainbow trout macrophage in terms of reduction of cytochrome cas well as yeast phagocytosis, significantly.

• Journal of Plant Biotechnology
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• v.29 no.2
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• pp.135-138
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• 2002

Cotyledonary explants from immature zygotic embryos of each 85 recombinant inbred lines (RILs) were cultured on medium containing MS salts, B5 vitamins, 40 mg$^{-1}$ 2,4-dichlorophenoxyacetic acid and 30 g$^{-1}$ sucrose. Frequency of somatic embryo formation on cotyledonary explants showed in thirty-six lines(＜10%), in thirty-seven lines (11~49%), in nine lines (50~89%), and in three lines(>90%), respectively, The highest frequency (up to 90%) and number (6.36 per cotyledon) of somatic embryos were obtained from lines of KM1010, KM1032 and KM1064. Primary somatic embryos produced from three lines produced numerous secondary somatic embryos on the surfaces, which were subcultured for over one year. Upon transfer to maturation and conversion medium (Komatsuda, 1992), somatic embryos converted to plantlets at a frequency of approximately 25%.

• Journal of Physiology & Pathology in Korean Medicine
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• v.18 no.6
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• pp.1856-1859
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• 2004

The diterpene acid (1) was tested for its growth inhibitory effects against tumor cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Full assignments of the 1D/2D-NMR data of the compound (1) are reported. These results suggest that the diterpene acid (1) possessed a cytotoxic agent.

• Natural Product Sciences
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• v.15 no.2
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• pp.90-95
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• 2009

Phytochemical investigation of the MeOH extract of the leaves of Nelumbo nucifera resulted in the isolation of five norsesquiterpenes, four flavonoids, two triterpenes and one alkaloid. Their chemical structures were characterized by spectroscopic methods to be (E)-3-hydroxymegastigm-7-en-9-one (1), (3S,5R,6S,7E)- megastigma-7-ene-3,5,6,9-tetrol (2), dendranthemoside B (3), icariside $B_2$ (4), sedumoside $F_1$ (5), luteolin (6), quercetin 3-0-${\beta}$-D-glucuronide (7), quercetin 3-0-${\beta}$-D-glucoside (8), isorhamnetin 3-0-rutinoside (9), alphitolic acid (10), maslinic acid (11), and N-methylasimilobine (12). Norsesquiterpenoids (1-5) and triterpenes (10-11) were isolated for the first time from this plant. Compounds 6 and 10-12 exhibited considerable cytotoxicity against four human cancer cell lines in vitro using a SRB bioassay.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.2
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• pp.441-445
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• 2005

Tripterygium regelii has been used as an oriental medicine, especially antiparasitic, anti-inflammatory and detoxifying agents in East asia. During our research to develop new antitumor agents from natural products, MeOH ext. and CH2Cl2 ext. of Tripterygium regelii showed the potent antitumor activity. In order to purify active compounds from Tripterygium regelii, activity-guided fractionation was carried out. Silica gel and RP-18 column chromatography for the active fraction led to the isolation of two compounds and their antitumor activities were studied. Those two compounds didn't show potent antitumor activity against human tumor cell lines. The structure of two compounds were determined by $^1H-NMR$, $^{13}C-NMR$, DEPT, $^1H-^{13}C$ COSY and IR spectrum. Compound I and Compound II were turned out to be Celastrol, and ${\beta}-sitosteryl-3-o-{\beta}-D-glucopyranoside$ respectively.