• Title/Summary/Keyword: Cytotoxic Effect

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Effects of Phamacopuncture with RUBI FRUCTUS Infusion Solution at $KI_{10}$ on Osteoporotic Rats Induced by Ovariectomy (복분자 음곡 약침이 난소적출 흰쥐의 골다공증에 미치는 영향)

  • Shin, Hee-Woong;Lee, Hyun
    • Journal of Acupuncture Research
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    • v.27 no.4
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    • pp.99-114
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    • 2010
  • Objectives : The purpose of this study is to observe the effects of RUBI FRUCTUS phamacopuncture infusion solution at $KI_{10}$ on osteoporotic Rats Induced by ovariectomy. Methods : The author performed several experimental items to analyze cytotoxic, osteoporosis evaluation, change of ALP, creatinine, Ca, P, osteocalcin, Ca/P ratio and histological change of serum and tibia. Results : 1. Creatinine and phosphorus in serum was decreased significantly in RF-HA than control group. 2. Calcium and phosphorus in tibia was increased significantly in RF-HA than control group. 3. Osteoclast like cell in tibia was increased significantly in control group, decreased significantly in RF-HA. 4. In the histological study in tibia, TBT was significantly increased, GPL was significantly decreased in the RF-HA than control group. Conclusions : This study suggested that RF-HA at KI10 has significant effect on osteoporosis.

Synthesis of Hydroxylactams and Esters Derived from Thalidomide and Their Antitumor Activities

  • Sun, Guanglong;Liu, Xiangchao;Zhou, Heng;Liu, Zenglu;Mao, Zhenmin
    • Bulletin of the Korean Chemical Society
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    • v.35 no.5
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    • pp.1337-1342
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    • 2014
  • A novel and convenient route for the synthesis of a series of thalidomide derivatives is described. Compound 2 was cyclized with different amines under alkaline condition to obtain 4-nitro substituted phthalimidines 3a-d. Hydroxylactams 4a-d were produced via bromination and hydroxylation. Different acyl chlorides were reacted with hydroxylactams to provide the desired esters 5a-d. All compounds were evaluated by MTT assay for their inhibitory activities against HCT-116, MG-63, MCF-7, HUVEC and HMVEC cell lines in vitro. Most of them showed no obvious cytotoxic effect on normal human cells, compounds 4a-d, $5a_2$, $5a_4$, $5a_5$, $5b_2$, $5c_2$ and $5d_2$ exhibited potent antitumor activities, among which compounds $5a_2$ and $5b_2$ were more effective than 5-FU.

Colony Forming Unit(CFU) Assay를 이용한 재조합 단백질 Leukotactin-1(Lkn-1)의 Myelosuppression 및 Myeloprotection 연구

  • Lee, Gyu-Hwa;Lee, Gong-Ju;Lee, Eun-Gyeong;Im, In-Hwan;Jeon, Eun-Yeong;Choe, Mu-Rim;Kim, Dong-Il;Park, Du-Hong;Yun, Yeop
    • 한국생물공학회:학술대회논문집
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    • 2001.11a
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    • pp.775-778
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    • 2001
  • Chemokines are small chemotalic cytokines that have a number of biological functions. Some chemokines regulate the proliferation of hematopoietic stem and progenitor cells(HSPC). Leukotactin-l(Lkn-l) is a CC chemokine and is known to reduce colony forming unit(CFU). The N-terminal truncated Leukotactin-l(rtLkn-l), produced by Pichia pastoris, suppressed CFU from 40 to 60%. The rtLkn-l protected CFU from cytotoxic effect of anticancer drug such as Ara-C, doxorubicin, cyclophosphamide and 5-FU by cell cycle arrest.

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Inhibition of Glutamate-Induced Change in Mitochondrial Membrane Permeability in PC12 cells by 1-Methylated β-carbolines

  • Han, Eun-Sook;Lee, Chung-Soo
    • Biomolecules & Therapeutics
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    • v.11 no.2
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    • pp.112-118
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    • 2003
  • 1-Methylated $\beta$-carbolines (harmaline and harmalol) and antioxidants (N-acetylcysteine and ascorbate) reduced the loss of cell viability in differentiated PC 12 cells treated with 5 mM glutamate. $\beta$-Carbolines prevented the glutamate-induced decrease in mitochondrial membrane potential, cytochrome c release and caspase-3 activation in PC 12 cells. $\beta$-Carbolines reduced the formation of reactive oxygen species and depletion of glutathione due to glutamate in PC12 cells. $\beta$-Carbolines revealed a scavenging action on hydrogen peroxide and reduced the iron and EDTA-mediated degradation of 2-deoxy-D-ribose. The results suggest that I-methylated $\beta$-carbolines attenuate the cytotoxic effect of glutamate on PC12 cells by reducing the alteration of mitochondrial membrane permeability that seems to be mediated by oxidative stress.

Effective Chemopreventive Activity of Genistein against Human Breast Cancer Cells

  • Shon, Yun-Hee;Park, Sun-Dong;Nam, Kyung-Soo
    • BMB Reports
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    • v.39 no.4
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    • pp.448-451
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    • 2006
  • Chemopreventive and cytotoxic effect of genistein against human breast cancer cell lines was investigated. Genistein inhibited cell proliferation in estrogen receptor-positive (MCF-7) and estrogen receptor-negative (MDA-MB-231) human breast carcinoma cell lines. Cytochrome P450 (CYP) 1A1-mediated ethoxyresorufin O-deethylase (EROD) activity was inhibited by genistein in a concentrationdependent manner. Genistein significantly inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cyclooxy-genase-2 activity and protein expression at the concentrations of 10 (p < 0.05), 25 (p < 0.05) and 50 mM (p < 0.01). In addition, ornithine decarboxylase (ODC) activity was reduced to 53.8 % of the control after 6 h treatment with 50 mM genistein in MCF-7 breast cancer cells. These results suggest that genistein could be of therapeutic value in preventing human breast cancer.

Antitumor Activity of 23, 24-dihydrocucurbitacin D Isolated from Bryonia alba L.

  • Sohn, Hyung-Ok;Lee, Young-Gu;Lim, Heung-Bin;Kwon, Nyoun-Soo;Goorgen V. Aprikian;Lee, Dong-Wook
    • Toxicological Research
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    • v.16 no.4
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    • pp.263-267
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    • 2000
  • The cytotoxic and antitumor activity of 23,24-dihydrocucurbitacin D (dhc D) isolated from Bryonia alba L. was examined. Our results showed that dhc D strongly inhibited the viability of the cultured cancer cells, A-549, COLO 205, SK-MEL-2, and L121O. It also exhibited effective antitumor activity in ICR mice, which had been intra peritoneally implanted with sarcoma 180 ascites tumor cells. The dhc D also strongly inhibited the viability of immortalized macrophages RAW 264.7, but not normal peritoneal macrophages. These results indicate that dhc D has antiproliferative effect on cancer cells and it may more sensitive on immortalized cells than normal cells.

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INHIBITION OF NEURITE OUTGROWTH AND TRANSCRIPTION FACTOR ACTIVATION BY OCHRATOXIN A IN CULTURED PC-12 CELLS

  • Hong, Jin-Tae;Oh, Jae-Ho;Jung, Kyoung-Mi;Lee, Eun-Hee;Park, Ki-Sook;Song, Chi-Won;Jung, Hai-Kwan;Lee, Myung-Koo;Yang, Ki-Hwa;Chung, Soo-Youn
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.05a
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    • pp.168-168
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    • 2001
  • The mycotoxin, ochratoxin A (OTA) has been known to induce microcephaly in animals and in vitro whole embryo. Cytotoxic effect and inhibition of cell differentiation were proposed as underlying mechanisms responsible for OTA-induced microcephaly.(omitted)

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Identification of Soil Actinomycetes Producing Anticancer Agent and Its Biological Activities (항암활성물질을 생산하는 토양방선균의 동정 및 함암물질의 생물학적 활성)

  • 박정민;문순옥;오두환
    • Microbiology and Biotechnology Letters
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    • v.22 no.4
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    • pp.347-352
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    • 1994
  • Cytotoxic test was performed by SRB assay on human epidermoid carcinoma HEp-2 cell line for screening the soil microorganism, secreting anticancer agent. One microorganism was selected among two thousand microorganisms for its highest cytotoxicity. And this microorganism was identified with Streptomyces species after performing of diaminopimeric acid and reducing sugar analysis of cell wall and analysing the cultural characteristics and named Streptomyces sp. SM 1119. The effect of anticancer agent in SM 1119 culture extract on the cell cycle was studied by using GG$_{o}$ synchronized NIH 3T3 cells. The extract inhibited the serum stimulation of GG$_{o}$ NIH 3T3 cell only within 1 hour after serum stimulation but not after 6 hours. The extract also reduced the amount of c-myc mRNA in Colo 320 cell. These results suggest that the anticancer agent in the extract inhibits the progression of cell cycle very early stages, probably from G$_{0}$ to G$_{1}$.

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Compound K, Ginseng Saponin Metabolite, Induces Apoptosis in Human Monocytic Leukemia cells

  • Kang, Kyong-Ah;Kim, Dong-Hyun;Hyun, Jin-Won
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.75-75
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    • 2003
  • We report upon the cytotoxic activity of the ginseng saponin metabolite, Compound K (20-O-D-glucopyranosyl-20(S)-protopanaxadiol, IH90l) on various human leukemia cell lines. Compound K had most effect on U937, a human monocytic leukemia cell line, which on treatment showed; a exposure of phosphatidylserine from the inner cell membrane to the outer cell membrane, the formation of apoptotic bodies and DNA fragmentation, - characteristics of apoptosis. Compound K induced apoptosis by up-regulating Bax, disrupting the mitochondria membrane potential, and by activating caspase 9 and caspase 3. Therefore, we suggest that Compound K inhibit U937 cell growth by inducing apoptosis through the up-regulation of Bax and caspase activation.

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The Effect of Ginsenosides on Galactosamine-induced Hepatotoxicity (인삼 사포닌이 간세포 독성에 미치는 영향)

  • kim, Sun-Yeou;Kim, Young-Choong;Byun, Soon-Jung;Kim, Eun
    • Korean Journal of Pharmacognosy
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    • v.22 no.4
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    • pp.219-224
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    • 1991
  • Liver protective effects of ginsenosides as well as fractions of dammarane glycosides of Panax ginseng were studied using galactosamine (GalN)-induced cytotoxicity in primary cultured rat hepatocytes. Preventing effects on GalN-induced hepatotoxicity were found both microscopic observation and determination of GPT level with total dammarane glycosides fraction and $20(S)-ginsenoside-Rb_1$ as well as $20(S)-ginsenoside-Rg_1$ at the concentration of $50{\mu}g/ml$. The syntheses of both protein and RNA were significantly increased by the treatment of $50{\mu}g/ml$ of total dammarane glycoside fraction, $20(S)-ginsenoside-Rb_1$, -Rc, -Re and $-Rg_1$, respectively in both normal and GalN-induced cytotoxic hepatocytes.

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