• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.226-235
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• 1993

DA-125, a new anthracycline antitumor antibiotic, was administered to Sprague-Dawley rats intravenously for 4 weeks to investigate the repeated dose toxicity Focal alopecia was noted in three female rats receiving 1.0mg/kg/day. In rats receiving 1.0 mg/kg/day, weight gain decreased in both sexes after first or second week. Hematological examination revealed lower counts of total leukocyte and increased numbers of platelet after second week. At terminal necropsy, atrophy of thymus and spleen was observed. Lymphocytic depletion of thymus and atrophy of white pulp in spleen were observed microscopically. A decrease in the number of hematopoietic cells in the bone marrow and degeneration of germinal epithelia in testes were also observed. These treatment-related effects were mainly confined to rats receiving 1.0 mg/kg/day. And toxic effects with microscopic changes were not observed in rats receiving 0.2 mg/kg/day or 0.04 mg/kg/day.

• Journal of the Korean Society of Food Science and Nutrition
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• v.23 no.6
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• pp.916-921
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• 1994

The inhibitory effects of the juice and boiling water extract of Houttuyina cordata Thunb., which has been known as a traditional folk antitumor agent, on the genotxicity induced by mutagens were investigated . For this purpose, Salmonella typhimurium TA98 and TA100, and the transheterozygous (mwh/+) third larvae of Drosophila melanogaster were used. The juice of fresh H. cordata 9JHC) and boiling H. cordata extract (BHC) showed antimutagenicities toared alfatoxin B₁ in S. typhimurium TA 98 and TA100. The JHC's inhibitory effect increased by 76% to 98% as the adding concentrations increased, and the BHC had a 86-97% inhibitory effect. however, in the case of N-methyl-N'-nitro-N nitrosoguanidine (MNNG), the JHC's inhibitory effect was 52-60% irrespectively of its concentrations and the BHC had a low inhibitory effect. The JHC and BHC slightly reduced the somatic chromosomal mutagenicity by MNNG in the wing hair spot test system (mwh/+) of D. melanogaster, which suggests that they can inhibit gene mutation , deletion and mitotic chromosomal recomgination.

• Toxicological Research
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• v.23 no.1
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• pp.19-24
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• 2007

We demonstrate that paclitaxel, an antitumor agent derived from yew tree, inhibits LPS- and $IFN-{\gamma}$-induced NF-kB/Rel activation in RAW 264.7 cells. Previously, paclitaxel ($>10{\mu}M$) has been known to induce iNOS gene expression in macrophages. However, in the previous report we described that the pretreatment of macrophages with low concentration of paclitaxel ($0.1{\mu}M$) for 8 h inhibited LPS-induced iNOS gene expression. Pretreatment of RAW 264.7 cells with paclitaxel significantly inhibited NF-kB/Rel transcriptional activation. Electrophoretic mobility shift assay further confirmed that pretreatment of macrophages with paclitaxel inhibited NF-kB/Rel DNA binding. Taxotere, a semisynthetic analog of paclitaxel, also inhibited LPS- and $IFN-{\gamma}$-induced iNOS gene expression. Collectively, these series of experiments indicate that paclitaxel inhibits iNOS gene expression by blocking NF-kB/Rel activation.

• Journal of Pharmaceutical Investigation
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• v.31 no.3
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• pp.197-200
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• 2001

Lectin-conjugated ellagitannin (LET), a newly introduced melanoma-specific antitumor agent which has been synthesized by conjugation of wheat germ agglutinin as a lectin with praecoxin A as an ellagitannin, was encapsulated into sterically stabilized liposomes (SSL). Modified Folin phenol method was established for the quantitation of LET contents in liposomal formulations protein employing the standard calibration curve with bovine serum albumin. After removal of phospholipid by organic solvent extraction, which interferes the specific selectivity of the Folin-Ciocalteu reagent with the protein, recovery of LET was $94.5{\pm}2.3%$ and the encapsulation efficiency was revealed as $37.8{\pm}5.9%$ for 2.5 mg/ml LET solution.

• Journal of Microbiology and Biotechnology
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• v.1 no.3
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• pp.163-168
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• 1991

A new angiogenesis inhibitor, FR-118487 was obtained by chemical modification of FR-111142 which was isolated from the fermentation products of Scolecobasidium arenarium F-2015. The antiangiogenic activity of FR-118487 was compared with that of the parent compound, FR-111142. In the endothelial cell proliferation test in vitro and the angiogenesis in the chick embryo chorioal-lantoic membrane assay, FR-118487 had about 5∼10 times stronger antiangiogenic activities than FR-111142. In addition, FR-118487 inhibited the angiogenesis in the rabbit corneal assay and suppressed the solid tumor growth in mice. These findings showed that FR-118487 would be a unique antiangiogenic agent with promising antitumor activity.

• Bulletin of the Korean Chemical Society
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• v.35 no.11
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• pp.3232-3238
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• 2014

Mollugin has been reported to have various biological activities including antineoplastic, antitumor, antiviral against the hepatitis B virus, anti-aging and antimutagenic activities. An effective and concise synthesis of mollugin in two steps including kinetic control from the cheap starting material 1,4-naphthoquinone has been introduced, and mollugin derivatives thus prepared are screened for their inhibition ability against the hepatitis C virus (HCV) and the dihydrobenzochromene structure might be an additional anti-HCV agent as a new leading compound.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.2
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• pp.412-415
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• 2009

Chinensis galla has been used as an multi-functional herb, such as anti-inflammatory, anti-virus, and antitumor agent. This study was performed to antimicrobial and cytotoxicity effect in vitro. The results were summarized as follows : Chinensis galla was antimicrobial effect on Staphylococcus aureus subsp. aureus, Bacillus cereus, Bacillus subtilis, Staphylococcus epidermidis. Chinensis galla was antimicrobial effect on Kocuria rhizophila, Corynebacterium ammoniagenes. The extracts of Chinensis galla exhibited cytotoxicity on human dermal fibroblast at $10\;{\mu}{\ell}$ but not at $5\;{\mu}{\ell}$, and the same results was known under a microscope. Accordingly the results show Chinensis galla could antimicrobial effect but exhibited cytotoxicity on human dermal fibroblast at high concentration and it needs more research.

• YAKHAK HOEJI
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• v.44 no.3
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• pp.251-256
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• 2000

Sterically stabilized liposomes (SSL) composed of distearoylphosphatidylcholine, cholesterol, dicetylphosphate and distearoylphosphatiodylethanolamine-N-poly(ethyleneglycol) 2000 (DSPE-PEG 2000) were made by reverse phase evaporation method to prolong biological half-life and decrease toxic side effect of drug. Streptozocin (572), a water-soluble antitumor agent with short half-life, was selected as a model drug. The size of SSL was controlled by polycarbonate extrusion to 100 nm which is adequate size for long circulation in plasma. The release rate of drugs from SSL in PBS was evaluated. And the stability of STZ-containing liposomes against drug leakage into rat plasma was evaluated in order to investigate the interaction of liposome and plasma protein. Incorporation of DSPE-PEG 2000 into conventional liposomes significantly decreased the drug leakage into rat plasma.

• Proceedings of the Korean Society of Toxicology Conference
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• 2003.05a
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• pp.100-101
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• 2003

It has been known that elevated levels of COX-2 is associated with resistance to apoptosis in cancerous or transformed cells. However, recent studies have shown that up-regulation of COX-2 may be implicated in induction of apoptosis. Previous studies from this laboratory have shown that a novel alkylphospholipid type antitumor agent ET-18-O-$CH_3$ (l-O-octadecyl-2-0-methyl-glycero-3-phosphocholine) induces COX-2 expression in H-ras transformed human breast epithelial cells (MCF10A-ras) while it causes apoptosis in the same concentration range.(omitted)

• Biomolecules & Therapeutics
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• v.6 no.3
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• pp.303-311
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• 1998

The general pharmacological properties of new platinum (II) coordination complexes, SA : [Pt(trans-ι-DACH)(DPPE)] . 2NO$_3$, SB : [Pt(cia-DACH)(DPPP)] 2NO$_3$ and SC : [Pt(cia-DACH)(DPPE)] 2NO$_3$on central nervous, respiratory, cardiovascular and digestive systems were studied in various experimental animals. These platinum (II) anticancer agents had no effects on analgesia, thiopental-induced sleeping time, body temperature, strychnine-induced convulsion, inflammation and local anesthetic action in mice and rats. Intestinal motility, stomach-ulcer induced by serotonin and bile-secretion of rats were not influenced by the dose of 30 mg/kg. However SB and SC induced a mild decrease in heart rate in anesthetized rats. Based on these results, these new platinum (II) complexes may be regarded as a valuable lead compound in the development of new anticancer chemotherapeutic agents with marked antitumor activity and low toxicity.