• Title/Summary/Keyword: anticancer agent

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Genotoxicily Studies of An Anticancer Agent of Camptothecin Series, CKD-602 (Camptothecin계 항암제 CKD-602의 유전독성평가)

  • 하광원;오혜영;허옥순;박장환;손수정;한의식;김종원;강일현;강혁준
    • Environmental Mutagens and Carcinogens
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    • v.18 no.2
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    • pp.129-134
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    • 1998
  • To evaluate the genotoxicity of CKD-602, an anticancer agent the in viかo reverse mutation assay using Salmonella typhimurium, the Chromosome aberration assay using Chinese hamster lung (CHL) cells and the in vivo micronucleus assay using bone marrow cells of ddY mice were performed. In the reverse mutation assay, CKD-602 did not induced mutagenicity in Salmonella typhimurium TA 98, TA 100, TA 1535, and TA 1537 strains with and without metabolic activation. In the chromosome aberration test using CHL cells, there was an increased incidence of structural aberrations induced by CKD-602 without metabolic activation during 24 and 48 hours, but CKD-602 did not induce chromosome aberration with metabolic activation. The in vivo induction of micronuclei was measured in polychromatic erythrocytes of bone marrow of male ddY mice. At 24 hours after treatment with CED-602 by i.p. once, there was an increased incidence of micronucleated polychromatic erythrocytes in bone marrow of ddY male mice.

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ent-Kaurane Diterpenoids from Croton tonkinensis Inhibit LPS-induced Transcription Factor NF-${\kappa}{B}$ Activation and NO Production

  • Giang, Phan-Minh;Jin, Hui-Zi;Lee, Jung-Joon
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.120.1-120.1
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    • 2003
  • Nuclear factor-${\kappa}{B}$ (NF-${\kappa}{B}$) belongs to a group of homodimers and heterodimers of Rel/NF-${\kappa}{B}$ proteins that bind to DNA target sites, where they directly regulate gene transcription. The activation of NF-${\kappa}{B}$ has been shown to mediate inflammation and suppress apoptosis. Activated NF-${\kappa}{B}$ has been found n various inflammatory diseases such as rheumatoid arthritis, Atherosclerosis, asthma, nflammatory bowel disease, and Helicobacter pylori-associated gastritis and associated with cancer, cachexia, diabetes, euthyroid sick syndrome, and AIDS. (omitted)

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A study of the tendency of anti-cancer experimental study using herbal medicines (한약(韓藥)을 이용(利用)한 항암(抗癌) 실험연구(實驗硏究)의 경향(傾向)에 관(關)한 고찰(考察))

  • Kim, Hyung-A;Lim, Sung-Woo;Lee, Won-Chul
    • THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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    • v.4 no.1
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    • pp.211-232
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    • 1998
  • Because there were lots of side effects and tolerances to the existing anticancer therapeutics, the experiment extracting the anticancer effect from medicinal herbs is in progress liviely. Therefore the purpose of this study were to research the tendency and the course of anticancer studies. To research the tendency of anticancer studies, medicinal herbs of fifty three experimental papers were analyzed and to examine the course of studies, anticancer papers in the medical world were used. The obtained results were as follows: Methods of herbal medicinal treatments were elimination the pathogenic factor(祛邪) and supporting healthy energy(扶正) method used. In this study, immediately tumor bearing and immune response were the most important point. The subject of immediately tumor bearing was not in the specific cancer but in the influence on the life span of general cencerous cells. In the experimental study of immune response, the effect on NK cell activity of medicinal herbs most studied. The combined usage of medicinal herbs and anticancer agent mostly intended to know whether it inhibits the tumor cell growth. The serum test and blood cell number test show if medicinal herbs inhibit side effect of anticancer agent. More than 80 percents of used medicinal herbs, there were anticancer activities. However anticancer experimental studies using medicinal herbs two weak points. The one, it was difficult to choose a prescription according to differentiation of symptoms and signs(辨證論) of the Oriental Medicine, because we put to the test not a man but a mouse. The other, as we observed the indirect effect of the whole physiological regulation caused by synergic effects of the complex prescription, we don't understand the detailed mechanism of the herb. Therefore, if the anticancer effect of the herb is proved the experiment, we should research the concrete medical action of medicinal herbs and immunological analysis of herbal medicines to the body.

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Cholesterol-Lowering Effect and Anticancer Activity of Kimchi and Kimchi Ingredients (김치와 김치재료의 콜레스테롤 저하 및 항암효과)

  • 이재준;정영기
    • Journal of Life Science
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    • v.9 no.6
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    • pp.743-752
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    • 1999
  • The purpose of the paper is to explore the current knowledge on the nutritional evaluation, cholesterol-lowering effect and antitumor activity of kimchi and its ingredients(Korean cabbage, garlic, red pepper powder, ginger and onion). Kimchi contains high contents of nutrients such as vitamins(ascorbic acid, $\beta$-carotene and vitamin B complex), minerals(calcium, potassium, iron and phosphorous), essential amino acids and dietary fiber. Kimch also contains high levels of lactic acid bacteria, allicin, capsaicin, organic acid, phenol compounds, flavonoid and sulfur compounds. The dietary fiber and lactic acid bacteria isolated from kimchi are effective in improving intestinal microflora of human. Isoluble dietary fiber shows anticancer activity, but soluble dietary fiber shows hypocholesterolemic effect. Lactic acid bacteria isolated from kimchi acts as a hypocholesterolemic or anticancer agent. A major ingredient of kimchi is mainly cruciferous and allium family vegetables, which were also reported to prevent cancer and atherosclerosis. It is suggested that kimchi is important not only as one of the traditional fermented Korean food but also as therapeutic agent for carcinogenesis and hypercholesterolemic state.

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Preparation and Characterization of Tributyrin Sub-micron Emulsion as Carrier for Paclitaxel

  • Fei, Xiang;Xu, Wenting;Yue, Yuan;Lee, Mi-Kyung
    • Journal of Pharmaceutical Investigation
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    • v.41 no.5
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    • pp.295-300
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    • 2011
  • Paclitaxel is a well known anticancer agent and has been a pharmaceutical challenge because of its extremely poor water-solubility and susceptibility to the p-glycoprotein (p-gp)-mediated efflux in multi-drug resistant (MDR) cancer cells. Tributyrin (TB), a triglyceride with relatively short fatty acid chains, was chosen as solubilizing vehicle for paclitaxel based on the solubility study (26.6 mg/mL). Tributyrin (10%) o/w emulsion containing paclitaxel (5%), egg phosphatidylcholine (5%) and pegylated phospholipid (0.5%) was prepared by high pressure homogenization to obtain submicron-sized emulsion. The mean particle size of the resultant TB emulsion was 395.5 nm. Paclitaxel in TB emulsion showed higher anticancer activity against human breast cancer cell line, MCF-7, than free form delivered in DMSO solution. On the other hand, its anticancer activity was significantly reduced in MCF-7/ADR, a MDR variant cancer cell line of MCF-7, and recovered by the presence of verapamil, suggesting of the susceptibility to the p-gp mediated efflux even though paclitaxel was encapsulated into emulsion. The TB emulsion showed great potential as a promising vehicle for water-insoluble anticancer agent, paclitaxel.

Development of Anticancer Prodrugs and Tumor Specific Adjuvant Prodrugs for Chemotherapy

  • Moon, Ki-Young
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2000.04a
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    • pp.8-9
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    • 2000
  • Despite the advances made in the past few decades in cancer chemotherapy, many conventional anticancer drugs display relatively poor selectivity for cancer cells. The nonselectivity of anticancer drugs and the development of anticancer drug resistance have been recognized as serious limitations in their clinical usefulness. Therefore, a major challenge in cancer chemotherapy is the development of new anticancer agents with improved selectivity for tumor cells as well as the prevention of the host cell resistance, both of which result in the improvement of therapeutic effect against cancer cells. Cyclophosphamide (CP), a widely used anticancer agent, is a prodrug that is activated by hepatic microsomal mixed-function oxidase (MFO) catalyzed C$_4$- hydroxylation. The resulting 4-hydroxycyclophosphamide (4-OH-CP) is converted to the ring-opened tautomer to aldophosphamide (Aldo) which subsequently undergoes a base- catalyzed ${\beta}$-elimination to generate cytotoxic phosphoramide mustard (PDA) and acrolein. The cytotoxic activity of CP is attributed to the aziridinium ion species derived from PDA that cross-links interstrand DNA.

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Facile analysis of protein-protein interactions in living cells by enriched visualization of the p-body

  • Choi, Miri;Baek, Jiyeon;Han, Sang-Bae;Cho, Sungchan
    • BMB Reports
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    • v.51 no.10
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    • pp.526-531
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    • 2018
  • Protein-Protein Interactions (PPIs) play essential roles in diverse biological processes and their misregulations are associated with a wide range of diseases. Especially, the growing attention to PPIs as a new class of therapeutic target is increasing the need for an efficient method of cell-based PPI analysis. Thus, we newly developed a robust PPI assay (SeePPI) based on the co-translocation of interacting proteins to the discrete subcellular compartment 'processing body' (p-body) inside living cells, enabling a facile analysis of PPI by the enriched fluorescent signal. The feasibility and strength of SeePPI (${\underline{S}}ignal$ ${\underline{e}}nhancement$ ${\underline{e}}xclusively$ on ${\underline{P}}-body$ for ${\underline{P}}rotein-protein$ ${\underline{I}}nteraction$) assay was firmly demonstrated with FKBP12/FRB interaction induced by rapamycin within seconds in real-time analysis of living cells, indicating its recapitulation of physiological PPI dynamics. In addition, we applied p53/MDM2 interaction and its dissociation by Nutlin-3 to SeePPI assay and further confirmed that SeePPI was quantitative and well reflected the endogenous PPI. Our SeePPI assay will provide another useful tool to achieve an efficient analysis of PPIs and their modulators in cells.

Anti-Angiogenesis Effects Induced by Octaminomycins A and B against HUVECs

  • Jang, Jun-Pil;Han, Jang Mi;Jung, Hye Jin;Osada, Hiroyuki;Jang, Jae-Hyuk;Ahn, Jong Seog
    • Journal of Microbiology and Biotechnology
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    • v.28 no.8
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    • pp.1332-1338
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    • 2018
  • In the course of studies to discover natural products with anti-angiogenic properties, two cyclic octapeptides, octaminomycins A (1) and B (2), were isolated from the cultures of Streptomyces sp. RK85-270. Octaminomycins suppressed the vascular endothelial growth factor (VEGF)-induced proliferation, adhesion, tube formation, migration, and invasion of HUVECs. Anti-angiogenic activity was futher confirmed in vivo by the chicken chorioallantoic membrane assay. We also identified that 1 and 2 inhibited the phosphorylation of VEGF receptor 2, AKT, and ERK1/2 and the expression and activities of MMP-2 and MMP-9. These results suggest that 1 and 2 may serve as potential scaffolds for the development of therapeutic agents to angiogenesis-dependent diseases.