• 대한핵의학회:학술대회논문집
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• 1997.05a
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• pp.172-172
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• 1997

• Korean Journal of Pharmacognosy
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• v.25 no.4 s.99
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• pp.311-318
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• 1994

From the root of Angelica decursiva-albiflora Yook, which has been used as a folk medicine for a sedative, analgesic and expectorant, four free coumarins, e.g., decursidin(I), decursin(II), umbelliferone(III) and nodakenetin(IV), and two coumarin glycosides, e.g., nodakenin(V) and decuroside I(VI) were isolate. The cytotoxicity of nodakenin(V) against L-1210 leukemia cells was less effective than cisplatin, but in the nephrotoxicity against rabbit kidney proximal tubular cell nodakenin(V) showed remarkably less nephrotoxicant than cisplatin.

• Archives of Pharmacal Research
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• v.22 no.5
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• pp.507-514
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• 1999

6-(1-azidoalkyl)-DMNQ derivatives compared to 2-(1-azidoalkyl)-DMNQ isomers, exhibited higher cytotoxic activity against L1210 mouse leukemia cells and stronger inhibition of DNA topoisomerase-I (TOPO-I), suggesting involvement of steric hindrance. However, similar antitumor activity against mice bearing S-180 cell was shown by 2-an 6-(1-azidoalkyl)-DMNQ derivatives.

• YAKHAK HOEJI
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• v.27 no.4
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• pp.309-314
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• 1983

Six hydantoin derivatives, 3-(2-chloroethyl) hydantoin (6a), 3-(2-chloroethyl)-5-isopropylhydantoin (6b), 3-(2-chloroethyl)-5-isobutylhydantoin (6c), 3-(2-chloroetbyl)5-(2-butyl) hydantoin (6d), 3-(2-chloroethyl)-5-benzylhydantoin (6e), 3-(2-chloroethyl)-5-(indolyl-3-methyl) hydantoin (6f), were prepared by the treatment of the corresponding salt of amino acids with 2-chloroethyl isocyanate in cold water, followed by refluxing in concentrated HCl solution. Anticancer activity of the synthesized hydantoin derivatives were examined on murine leukemia L1210 cells growing in Fischer medium. Among them, 3-(2-chloroethy)-5-isobutyl-hydantoin (6c) showed substantially low $ED_{50}$ value of $9.6{\mu}g/ml$.

• Molecules and Cells
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• v.38 no.11
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• pp.966-974
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• 2015

Despite the presence of toll like receptor (TLR) expression in conventional $TCR{\alpha}{\beta}$ T cells, the direct role of TLR signaling via myeloid differentiation factor 88 (MyD88) within T lymphocytes on graft-versus-host disease (GVHD) and graft-versus-leukemia (GVL) effect after allogeneic stem cell transplantation (allo-SCT) remains unknown. In the allo-SCT model of C57BL/6 ($H-2^b$) ${\rightarrow}$ B6D2F1 ($H-2^{b/d}$), recipients received transplants of wild type (WT) T-cell-depleted (TCD) bone marrow (BM) and splenic T cells from either WT or MyD88 deficient (MyD88KO) donors. Host-type ($H-2^d$) P815 mastocytoma or L1210 leukemia cells were injected either subcutaneously or intravenously to generate a GVHD/GVL model. Allogeneic recipients of MyD88KO T cells demonstrated a greater tumor growth without attenuation of GVHD severity. Moreover, GVHD-induced GVL effect, caused by increasing the conditioning intensity was also not observed in the recipients of MyD88KO T cells. In vitro, the absence of MyD88 in T cells resulted in defective cytolytic activity to tumor targets with reduced ability to produce IFN-${\gamma}$ or granzyme B, which are known to critical for the GVL effect. However, donor T cell expansion with effector and memory T-cell differentiation were more enhanced in GVHD hosts of MyD88KO T cells. Recipients of MyD88KO T cells experienced greater expansion of Foxp3- and IL4-expressing T cells with reduced INF-${\gamma}$ producing T cells in the spleen and tumor-draining lymph nodes early after transplantation. Taken together, these results highlight a differential role for MyD88 deficiency on donor T-cells, with decreased GVL effect without attenuation of the GVHD severity after experimental allo-SCT.

• Applied Biological Chemistry
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• v.38 no.4
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• pp.364-369
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• 1995

Anticarcinogenic activity of Moutan radix for mouse ascites cancer induced by mouse Sarcoma 180 (S-180) cells was investigated. Methanol extract of Moutan radix including other folk medicinal plants (Taxus cuspidata, Curcuma longa, Artemisia capillaris, Ligrstri fructus, and Liriope platyphylla) used to remedy or cure many chronic human diseases like cancer was fractionated into hexane, chloroform ($CHCl_3$), ethylacetate (EtOAc), and butanol (BuOH) fractions. Anticarcinogenic activity of the fractions, exhibited a strong cytotoxicity for L1210 and S-180 cells, was examined for mouse ascites cancer induced by S-180 cells. Male ICR mice (7 mice/treatment, $5{\sim}6$ weeks of age, $23{\pm}1\;g$ were injected i.p. with S-180 cells ($1{\times}10^{7}\;cell/1\;ml$ PBS). One day later, each mouse was given 0.1 ml of 10% DMSO containing sample ($30\;{\mu}g/g$ body weight) every day for 10 consecutive days. Control mice were only given 0.1ml S-180 cells and 0.1 ml 10% DMSO. Mice treated with EtOAc fraction of Moutan radix showed 28.7 days of life, which is 167% of control mice's life. Based on the dose-dependant experiment mice treated with $30\;{\mu}g$ showed longer life relative to mice treated with ootherr doses (5, 15, $60\;{\mu}g$), and mice treated with $60\;{\mu}g$ exhibited toxic symptoms. Body weight of mice treated with Moutan radix was significantly reduced relative to that of control mice (p<0.05). GC-MS analysis in conjunction with silica-gel column chromatography revealed that the EtOAc fraction contained 2-methoxylphenol, benzoic acid, 1-(4-hydroxy-3-methoxyphenyl)ethanone, 8-methyl-2,4(1H,3H)pteridinedione and 2,5-furan-dicarboxylic dimethyl ester as regards to the anticarcinogenic property of the EtOAc fraction. These results suggest that Moutan radix might be included as an anticarcinogenic medicinal plant for treatment of ascites cancer.

• YAKHAK HOEJI
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• v.34 no.6
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• pp.395-400
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• 1990

The FU-fat conjugates(4a-e) as a prodrug have been synthesized by condensing various fatty acids(1a-e) via isocyanates(2a-e) as carbamoyl group at $N^1-position$ of 5-fluorouracil and their structures characterized. Preliminary testing for their antitumor effect was carried out on leukemia L1210 cells in culture. Most of them(4a-d) like the parent FU exhibited less than 50% inhibition on grouth of the cultrued cells at the concentration of $1\;{\times\;10^{-7}M$. Only a dicarboxylic acid derivative, 4e, showed over 50% inhibition at the same level.

• Toxicological Research
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• v.17
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• pp.105-108
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• 2001

Several marine toxins with macrolide structure have been found to act on actin. One of these toxins is mycalolide B isolated from the genus Mycale. This compound belongs to macrolide antibiotics and consists of tris-oxazole with strong cytotoxic activity ($IC_{50}$: 10-50 nM for growth of L1210 murine leukemia cells). This compound was found to be an actin-depolymerizing agent with the mode of action distinct from that of the known actin inhibitor, cytochalasin D. Tolytoxin, a macrolide isolated from cyano-bacteria with similar chemical structure to mycalolide B, seems to have similar effect. Another macrolide compound, aplyronine A, showed the effects similar to those of mycalolide B. Although bistheonellide A, a dimeric macrolide, did not show a severing effect, it de polymerized F-actin and sequestered G-actin by forming 1 : 2 complex with G-actins. Swinholide A has a structure and effects similar to those of bistheonel-lide A. In conclusion, mycalolide B, tolytoxin, aplyronine A, bistheonellide A and swinholide A are the members of "actin de polymerizing macrolide" the mechanism of which is different from that of cytochalasin D.halasin D.

• Bulletin of the Korean Chemical Society
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• v.15 no.5
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• pp.364-368
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• 1994

Growth inhibition potency of the anthraquinones, anthraquinone-1,5-disulfonic acid and carminic acid, for Sarcoma 180 and L1210 leukemia cells in vivo and in vitro, was induced by the divalent transition metal ion, $Cu^{2+}$. On the other hand spectroscopic titration data show that the anthraquinone drugs form $Cu2^+$ chelate complexes (carminic acid : $Cu^{2+}$ = 1 : 6; anthraquinone-1,5-disulfonic acid : $Cu^{2+}$ = 1 : 3). Furthermore the $Cu^{2+}$-drug complexes associate with DNA to form the $Cu^{2+}$-anthraquinone-DNA ternary complexes. The formation of the complexes was further supported by the $H_2O_2-dependent$ DNA degradation, which can be inhibited by ethidium bromide, caused by the $Cu^{2+}$-drug complexes. It is likely that the $Cu^{2+}$-mediated cytotoxicity of the anthraquinone drugs is related with the $Cu^{2+}-mediated$ binding of the anthraquinone drugs to DNA and DNA degradation.

• Journal of Microbiology and Biotechnology
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• v.21 no.3
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• pp.256-262
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• 2011

A 20.9-kDa metalloprotease was isolated from dried fruiting bodies of the wild basidiomycete mushroom Lepista nuda. The N-terminal amino acid sequence of the protease was seen to be ATFVLTAATNTLFTA, thus displaying no similarity with the sequences of previously reported metalloproteases. The protease was purified using a procedure that entailed ion-exchange chromatography on CM-Cellulose, Q-Sepharose, and Mono S, and FPLC-gel filtration on Superdex 75. The protease functioned at an optimum pH of 7.0 and an optimum temperature of $50^{\circ}C$. It was also noted that the protease demonstrated a proteolytic activity of 1,756 U/mg toward casein. The $K_m$ of the purified protease toward casein was 6.36 mg/ml at a pH of 7.0 and with a temperature of $37^{\circ}C$, whereas the $V_{max}$ was 9.11 ${\mu}g\;ml^{-1}\;min^{-1}$. The activity of the protease was adversely affected by EDTA-2Na, suggesting that it is a metalloprotease. PMSF, EGTA, aprotinin, and leupeptin exerted no striking inhibitory effect. The activity of the protease was enhanced by $Fe^{2+}$, but was curtailed by $Cd^{2+}$, $Cu^{2+}$, $Hg^{2+}$, $Pb^{2+}$, $Zn^{2+}$, and $Fe^{2+}$ ions. The protease also exhibited inhibitory activity against HIV-1 reverse transcriptase with an $IC_{50}$ value of 4.00 ${\mu}M$. The $IC_{50}$ values toward hepatoma Hep G2 and leukemia L1210 cells in vitro were 4.99 ${\mu}M$ and 3.67 ${\mu}M$, respectively.