• Journal of Pharmaceutical Investigation
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• 제20권4호
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• pp.217-222
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• 1990

New antitumor-active pt(II) complexes of trans-l-diamine cyclohexane containing diphosphines as a leaving group were synthesized. The structures of the pt(II) complexes were determined by analyzing the infrared and $^{31}P-nuclear$ magnetic resonance spectra. Antitumor activities of the pt(II) complexes were tested against murine leukemia $L_{l210}$ according to the protocol of the National Cancer Institute. All the pt(II) complexes Synthesized were antitumor-active. In particular, water-soluble $[pt(trans-l-dach) (DPPP)](NO_3)_2$ exhibited excellent antitumor activity, giving T/C % values of 341 and 356 respectively, each with four cured mice out of six at a dose of 25 mg/kg. These pt(II) complexes are considered to be worthy of further development.

• 생약학회지
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• 제30권4호
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• pp.351-354
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• 1999

This study was carried out to evaluate cytotoxicity of the extracts from Sophora flavescens Ait. against L1210 (lymphocytic leukemia) and $P388D_1$ (lymphoid neoplasms) cells in vitro. We have determined cytotoxicity by MTT {3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazo-liumbromide} assay. The order of cytotoxicity of Sophora flavescens Ait. extracts against L1210 and $P388D_1$ cells in vitro is as follows: AM> EASF > CFSF > MTSF > WSF > HXSF and AM> EASF> CFSF> MTSF> HXSF> WSF. These results suggest that the ethyl acetate soluble extract of Sophora flavescens Ait may be a valuable choice for the development of antitumor agents.

• 약학회지
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• 제38권2호
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• pp.158-165
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• 1994

A protein-polysaccaride fraction Kp(53.9% polysaccharide, 14.2% protein) was separated from the shake-cultured mycelia of a basidiomycetous fungus, Phellinus linteus, and its antitumor activity against sarcoma 180 in ICR mice was investigated. When administered after the tumor implantation, Kp exerted antitumor activity by inhibiting the growth of the sarcoma 180 solid tumor by 71.5% and increasing the life span of the sarcoma 180 ascitic mice by 51.5% at 100 mg/kg. In pretreatment tests, in which Kp was administered once daily for 9 days before the tumor implantation, Kp inhibited the growth of the solid and ascites form of sarcoma 180, respectively, by 35.4% and by 80.3% at 100 mg/kg. However, Kp showed no in vitro cytotoxic activity against a murine leukemia L1210 and a human gastric tumor SNU.1 upto the concentration of $200\;{\mu}g/ml$. From these results, it is clear that the antitumor activity of Kp is exerted through its immunomodulating activity on the host's immune system.

• 한국미생물·생명공학회지
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• 제22권2호
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• pp.182-189
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• 1994

The highest antitumor activity was observed in water soluble AS fraction of the Ganoderma lucidum IY 009. AS fraction did not show any cytotoxicity on sarcoma 180 cell but stimulated antibody production, opsonization of macrophage in ICR mouse and superoxide ion production from isolated macrophage. AS fraction activated complement C3 in human serum, and their antitumor activity was inhibited by EDTA, a chelator of cation related complementary activation. AS fraction exerted om prolong of life span and ingibition of tumor growth in the leukemia P388 or L1210 transplanted inbreed mouse,k BDF1 but krestin did not. AS fraction did not show any serious and lethal effects through oral administration on ICR mouse, and LD$_{50}$ of those was above 2,230 mg/kg.

• 약학회지
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• 제43권3호
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• pp.369-377
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• 1999

A new series of highly water soluble platinum(II) complexes {Pt(II)[1,3-bis(phenylthio) propane](trans- -1,2-diaminocyclohexane) (PC-1) and Pt(II)[1,3-bis-(phenythio)propane] cis-1,2-diaminocyclohexane(PC-2)} were synthesized, and characterized by their elemental analysis and by various spectroscopic techniques[infrared(IR), 13C-nuclear magnetic resonance (NMR)]. In vitro antitumor activity of new Pt(II) complexes was tested against P-388 and L-1210 mouse lymphocytic leukemia cell lines, PC-14 / P, PC-14/ADM and PC-14 / CDDP human pulmonary adenocarcinima, DU-145 human prostate carcinoma, HT-1376 human bladder carcinoma, ZR-75-1 human breast carcinoma, MKN-45/P and MKN-45/CDDP human gastric adenocarcinoma cell lines using colorimetric MTT[3-(4,5-dimethyl thiazol-2-yl)-2.5-diphenyltetrazoliumbromide] assay for cell survival and proliferation. PC-1 showed active against L-1210, P-388 leukemia, human lung, stomach, prostate, bladder and breast cancer cell lines, and the antitumor activity of these compounds were comparable or superior to those of PC-2 and displatin. The nephrotoxicities of PC-1 and PC-2 were found quite less than that of cisplatin using MTT and [3H] thymidine uptake in rabbit proximal tubule cells and human kidney cortical cells. Based on these results, this novel platinum (II) complex compound (PC-1) represents a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.

• 동의생리병리학회지
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• 제17권4호
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• pp.1097-1100
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• 2003

This study was performed to evaluate the immunoregulatory effects of Gungchihwadam-Jeon(궁치화담전, GCHDJ) and Cheongsinhwadam-Jeon(청신화담전, CSHDJ) was administered(p.o.) once a day for 14 days to mice. By the treatment of GCHDJ or CSHDJ was increased the cell viability of cultured mice splenocytes, thymocytes and mesenteric lymph node cells. Administration of GCHDJ or CSHDJ was increased the splenic T lymphocyte, especially the Tc cell subpopulation was increased by the GCHDJ, on the while the TH cell was increased by the CSHDJ. The administration of GCHDJ or CSHDJ was significantly increased the apoptosis of transplanted-L1210 leukemia cells to mice peritoneal cavity. These results suggest that GCHDJ and CSHDJ have an immunoregulatory action

• 한국미생물·생명공학회지
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• 제25권5호
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• pp.477-482
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• 1997

To investigate the cytotoxicity of Korean traditional fermented soybean products using the MTT assay, we extracted soybean, Kanjang, Doenjang, Kochujang, and Chongkukjang with water, methanol, and hexane. Primary testing of cytotoxicity of 14 extracts was done for P388D1(mouse lympoid neoplasm) and L1210(mouse leukemia) cell lines. Doenjang methanol extract, Kochujang hexane extract, Chongkukjang methanol extract, and Chongkukjang hexane extract showed cytotoxicity of 86.1, 94.3, 83. 6, and 81.1%, respectively against P388D1, and showed cytotoxicity of 69.4, 96.9, 51.4, and 95.1%, respectively against L1210. All the other extracts showed less than 50% cytotoxicity. Methanol extracts of Doenjang and Chongkukjang showed dose-dependent cytotoxicity against P388DI, L1210, SNU-16 (human stomach cancer), HepG2(human hepatic cancer), WiDr(human colon cancer) cell lines, and IC$_{50}$ of Doenjang methanol extract was 67.7, 90.4, 1338.0, 706.4, and 371.2 $\mu$g/ml, respectively, and IC$_{50}$ of Chongkukjang methanol extract was 107.1, 228.3, 756.2, 1346.0, and 327.0 $\mu$g/ml, respectively.

• Archives of Pharmacal Research
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• 제21권3호
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• pp.266-272
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• 1998

The present study investigated the antitumor activity of the aqueous-alcoholic extracts from unripe cotton balls of Gossypium indicum. An Exposure of murine B16 melanoma and L1210 lymphoma cells to the extracts resulted in their severe deaths in time- and concentration-dependent manners. Of the extracts, hydrophilic fractions were most efficacious for the antitumor activity and found to contain certain amounts of catechin and its derivatives. The hydrophilic extract fraction C36B2-8 had approximately 10 times more cytotoxic effects on B12 and L1210 cells than on isolated murine thymocytes. High concentrations (>150 $\mu$g/ml) of C 36B3-8 mainly induced necrotic cell death. At low concentrations (<100 $\mu$g/ml), however, C 36B3-8 induced not only necrosis but also apoptosis of the two tumor cell lines, which was proved by the TUNEL staining and DNA fragmentation techniques. The data indicate that certain ingredients of the cotton ball extract of G. indicum have an antitumor activity.

• Archives of Pharmacal Research
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• 제6권2호
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• pp.115-121
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• 1983

Cholesteryl p-[3-(2-chloroethyl_-3-nitrosoureido] phenylthioaccetate (2) was synthesized : an intermediate, p-[3(2-chloroethyl_-3-nitrosoureido] phenylthioacetic acid (1) is a congener of an antitumor chlorambucil which both the -CH$_{2}$CH$_{2}$-linkage and -N(CH$_{2}$CH$_{2}$Cl)$_{2}$ group of chlorambucil molecule is doubly modified into the respective -S-linkage and -NH-CO-NNO-CH$_{2}$CH$_{2}$CL group. The attackment of cholesterol moiety as a carrier group to p-[3-(2-chloroethyl-3nitrosoureido] phenylthioacetic acid was accomplished through the esterification of cholesterol with p-[3-(2-chloroethyl-3-nitrosoureido] phenylthioacetyl chloride which was obtained from the treatment of p-[3-(2-chloroethyl)-3-nitrosourei-do] phenylthioaceticacid with SOCL$_{2}$, p-[3-(2-chloroethyl)ureido]]-phenythioacetic acid was nitrosated with NaNO$_{2}$ IN 98-100% HCOOH to give exclusively p-[3-(2-chloroethyl_-3-nitrosoureido] phenylthioacetic acid. Antitumor evaluation of compounds, 1 and 2 on L 1210 leukemia did show significant activity (ED$_{40}$ : 1.14.mu./ml and 8.4.mu.g/ml, repectively). Further studies were subjected..

• 약학회지
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• 제40권2호
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• pp.117-125
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• 1996

3'-Deamino-3-hydroxy-4'-fluoro- or 3'-deamino-3'-hydroxy-4'-azido-daunorubicin(6,8) and -doxorubicin(7,9) have been synthesized, respectively. Compounds 7,8 and 9 were mo re cytotoxic than daunorubicin(1) and doxorubicin(2) against L1210 murine leukemic cell in vitro. When administered intraperitoneally for 9 days starting 1 day after tumor inoculation, compounds 7(T/C 605%) and 9(T/C 488%) showed significant antitumor activity for ip-inoculuated L1210 murine leukemia at wide range of doses.