• The Korean Journal of Physiology and Pharmacology
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• v.13 no.6
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• pp.511-516
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• 2009

A series of substituted 2-arylnaphthyridin-4-one analogues, which were previously synthesized in our laboratory, were evaluated for their in vitro cytotoxic activity against human lung cancer A549 and human renal cancer Caki-2 cells using MTT assay. Some compounds (11, 12, and 13) showed stronger cytotoxicity than colchicine against both tumor cell lines, and compound 13 exhibited the most potent activity with $IC_{50}$ values of 2.3 and $13.4\;{\mu}M$, respectively. Three-dimensional quantitative structure activity relationship (3D-QSAR) studies of comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) were performed. Predictive 3D-QSAR models were obtained with $q^2$ values of 0.869 and 0.872 and $r^2_{ncv}$ values of 0.983 and 0.993 for CoMFA and CoMSIA, respectively. These results demonstrate that CoMFA and CoMSIA models could be reliably used in the design of novel cytotoxic agents.

• Korean Journal of Pharmacognosy
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• v.33 no.3 s.130
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• pp.207-210
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• 2002

The methanol extract from the root of Croton cascarilloides Raeusch. was primarily evaluated for cytotoxic activity in the cultured human lung cancer cell line (A459) and showed cytotoxic potential with $ED_{50}$ value of $5.98\;{\mu}g/ml$. Bioassayguided fractionation of the root extract resulted in 3-acetyl aleuritolic acid, rubiadin-l-methyl ether, and julocrotine. The structures of the compounds were elucidated from the combination of spectroscopic data and references. In addition, the $^{13}C-NMR$ assignments of rubiadin-l-methyl ether were revised.

• Journal of the Korean Society of Food Science and Nutrition
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• v.25 no.3
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• pp.539-549
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• 1996

Large bowel cancer correlates tightly to dietary factors such as dietary fiber and fat. Dietary fiber prevents the large bowel cancer in different modes of action which depend upon physicochemical and fermentable properties. Water-soluble fiber is fermented easily by intestinal microbes producing short chain fatty acids ; in contrast, water-insoluble fiber occurs effectively more rapid transit time due to greater bulk of gut content, though it is unfermentable. Not only short chain fatty acid is utilized in the proximal and distal colon as primary energy source, but also it lowers pH in the colon to normalize cellular differentiation and helps to stimulate peri staltic movement by acting as an osmotic laxative. In particular, butyric acid may also regulate gene expression and cell growth, though it is an important respiratory fuel for the colonocyte. Since dietary fiber and non-digestible oligosaccharides are the major source of butyric acid, this provides a possible link between dietary fiber and oligosaccharide and prevention of large bowel cancer. But, as with many links between dietary fiber and large bowel cancer, a direct casual association has not been established. In addition, RDA of dietary fiber which is 20~25g/day for adult Japanese, appears to be reasonable for the defecation once daily and the prevention of large bowel cancer.

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.2
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• pp.549-552
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• 2003

To investigate the protective effect of Sophorae Radix (SR) on the damage by pulmonary vascular endothelial cells by xanthine oxidase (XO)/hypoxanthine (HX)-induced oxygen tree radical, Neutral Red (NR) and c-fos immunopositive cell assay were used. The results were obtained as follows ; The viability of vascular endothelial cells treated with XO/HX was decreased. And c-fos immunopositive cells represented a maximal increase in group treated with XO/HX for 2 hour in pulmonary vasvular endothelial cells. But pretreated groups with SR extracts were not inhibited the increase of c-fos immunopositive cells by XO/HX in a dose-dependent manner. These results show that XO/HX elicits toxic effects in cultured pulmonary vascular endothelial cells, and suggest that SR extract is very effective in the prevention of XO/HX-induced increase of c-fos immunopositive cells.

• Natural Product Sciences
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• v.20 no.2
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• pp.76-79
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• 2014

In our ongoing search for structurally interesting and biologically active metabolites from Korean wild mushrooms, bioassay-guided fractionation and a chemical investigation of the MeOH extracts of the fruiting bodies of the mushroom Naematoloma fasciculare resulted in the isolation of three ergosterol derivatives, (22E,24R)-ergosta-7,22-diene-$3{\beta}$,$5{\alpha}$,$6{\beta}$,$9{\alpha}$-tetrol (1), (22E,24R)-$5{\alpha}$,$8{\alpha}$-epidioxyergosta-6,22-diene-$3{\beta}$-ol 3-O-${\beta}$-$\small{D}$-glucopyranoside (2), and (22E,24R)-$5{\alpha}$,$8{\alpha}$-epidioxyergosta-6,9,22-triene-$3{\beta}$-ol 3-O-${\beta}$-$\small{D}$-glucopyranoside (3). The structures of 1 - 3 were determined by comparison of their spectroscopic and physical data with reported values. The isolated steroid derivatives 1 and 3 were reported for the first time from this mushroom. Compounds 1 - 3 were tested for their cytotoxic activities against four human cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15).

• Archives of Pharmacal Research
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• v.25 no.5
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• pp.608-612
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• 2002

The twelve-protostane analogues were synthesized from alisol B 23-acetate and assessed for their in vitro antitumor activity against six different human and murine tumor cell lines. Of the compounds synthesized, 23S-acetoxy-24R(25)-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-hy-droxyimine (12) exhibited significant cytotoxic activities against A549, SK-OV3, B16-F10, and HT1080 tumor cells with $ED_{50}/$ values of 10.0, 8.7 ,5.2, and 3.1 ${\mu}g$/ml, respectively. Furthermore, 23S-acetoxy-13(17),24R(25)-diepoxy-11$\beta$-hydroxyprotost-3-one (5), 13(17),24R(25)-diepoxy-11$\beta$, 23S-dihydroxyprotostan-3-one (6), 24R,25-epoxy-11$\beta$,23S-dihydroxyprotost-13(17)-en-3-one (7), and 11$\beta$,23S,24R,25-tetrahydroxyprotost-13(17)-en-3-one (9) showed moderate cytotoxic activities against 816-F10 and HT1080 tumor cells. These results mean that a hydroxyimino group at C-3 position in the protostane-type terpene enhances cytotoxic activity.

• YAKHAK HOEJI
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• v.41 no.6
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• pp.704-708
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• 1997

In our search for bioactive natural products with antitumor activity, we have valuated various extracts of Saururi Herba (Saururaceae), which has been used in traditional medici ne for edema, beriberi, jaundice, turbid urine, carbuncle and furuncle. The hexane extract of the aerial part of this plant was found to show a potent cytotoxicity against several kinds of cultured human solid tumor cell lines (AGS, A549, HCT15, SKOV3, HEP-3B) in vitro. Using cytotoxicity-guided chromatographic separation of the hexane extract, cytotoxic constituent: 10-aminomethyl-3-hydroxy-4-methoxyphenanthrene-carboxylic acid lactam, was isolated and structurally identified by physico-chemical properties and spectroscopic evidences.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.527-531
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• 2001

Two triterpenoids, 24-methylene-3,4-seco-cycloart-4(28)-en-3-oic acid (1) and 3-oxo-$9{\beta}$-lanosta-7,22Z,24-trien-26,23-olive (6) were isolated from Abies koreana, together with $\beta$-sitosterol (2), maltol (3), ${\beta}-sitosterol-O-{$\beta}-D-glucoside$ (4), and hexacosylferulate (5). The structures of the compounds were established based on the spectroscopic data. The cytotoxic activities of triterpenoids have been evaluated using the sulforhodamine B (SRB) method. Compound 1 showed moderate cytotoxicities against human lung carcinoma (A549), ovarian carcinoma (SK-OV-3), malignant melanoma (SK-MEL-2), and colon carcinoma (HCT-15) cell lines.

• Archives of Pharmacal Research
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• v.20 no.6
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• pp.545-549
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• 1997

Effects of swainsonine (SW;8${\alpha}$, ${\beta}$-indolizidine-${\alpha}$, $2{\alpha}$8-triol from Locoweed) on the humoral immune responses of lipopolysaccharide (LPS) wer studied in ICR mice. Mice were divided into 4 groups (10 mice/group), and LPS was given to each mouse 1 hr after i.p. injection with 3.7 mg/kg of swainsonine, by i.p. injection twice a week for 14 days at a dose of 2 mg/kg. Humoral immune responses were evaluated by hemagglutination (HA) titer and splenic plaque forming cells (PFC). The results of this study were summarized as follows: Mice administrated each of LPS and SW showed significant enhancement of the weight ratios of spleen to body, HA titer, 2-mercaptoethanol-resistant HA(MER-HA) titer and PFC compared with those in controls. However, the LPS plus SW treatment decreased HA titer, MER-HA titer and PFC corresponding to humoral immunity, as compared with those in the mice treated with LPS alone. These findings indicated that LPS significantly enhanced humoral immune responses, but their enhancement effects were lowered somewhat by SW.

• Journal of Life Science
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• v.18 no.4
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• pp.542-549
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• 2008

Cisplatin (cis-diamminedichloroplatinum II : CDDP) is the most widely used anticancer drug against a variety of human neoplasms. However, its clinical use is limited by the onset of severe side effects, including ototoxicity and nephrotoxicity. Even though a number of evidences in cytotoxic mechanism of cisplatin have been suggested, the role of pro-inflammatory cytokines in cisplatin cytotoxicity of auditory cells has not yet been demonstrated. Herein our data clearly demonstrated that cisplatin decreased the viability of HEI-OC1 auditory cells, which was inhibited by the addition of neutralizing $anti-TNF-{\alpha}$, $anti-IL-1{\beta}$ and anti-IL-6 antibodies. Consistently, Neutralization with antibodies against pro-inflammatory cytokines ameliorated the cell death and disarrangement of cochlea hair cell layers in the rat primary cochlear explants which were treated with cisplatin. Furthermore, exogeneous supplementation with free radical scavengers, including GSH and NAC, significantly prevented the cytotoxicity of cisplatin in the rat primary cochlea explants. We also observed that $TNF-{\alpha}$ was predominantly expressed in Deiters and Hensen's cells located in hair cell zone of cisplatin-treated cochlear explants. These findings suggest that pro-inflammatory cytokines, including $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6, may play a pivotal role in the pathophysiology of hair cell damages caused by ototoxic drug cisplatin.