• 제목/요약/키워드: Cytotoxic drug

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

  • 이규화;이공주;이은경;임인환;전은영;최무림;김동일;박두홍;윤엽
    • 한국생물공학회:학술대회논문집
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    • 한국생물공학회 2001년도 추계학술발표대회
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    • pp.775-778
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    • 2001
  • Pichia pastoris에서 생산된 rtLkn-1 은 농도에 따라 CFU의 colony 형성을 억제하였으며, 마우스와 인간 골수 세포에서 항암제에 의한 stem cell 및 progenitor cell의 사멸을 억제하였고 이것은 항암제가 작용하는 동안 세포 주기를 일시적으로 휴지기로 유도하였기 때문으로 사료된다.

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A novel cis/trans-diaminocyclohexane platinum coordination complexes possessing in vitro and in vivo antitumor activity

  • Jung, Jee-Chang;Chang, Sung-Goo;Lee, Kyung-Tae;Park, Young-Soo;Lee, Joo-Han;Lee, Kyou-Heung;Kim, Sang-Lin
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1997년도 춘계학술대회
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    • pp.111-111
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    • 1997
  • As part of a drug discovery program to develope more effective platinum-based anticancer drugs, a series of platinum complexes trans-diaminocyclohexane platinum bi sdiphenylphosphino - ethane ( KHPC- 002) cis-diaminocyclohexane platinum bi sdiphenylphosphino - ethane ( KHPC- 006) has been evaluated in vitro against 4 human carcinoma cell lines with those of cisplatin using a tetrazolium-based colorimetric assay (MTT assay). The cell lines were two human bladder carcinoma cell lines, HT-1197 and HT-1376, human colon carcinoma cell line, HCT-116, and prostate cancer cell line DU-145. in vitro cytotoxic potential of each platinum complex was expressed as the cytotoxicity index (Cl, %).

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A FRACTIONAL-ORDER TUMOR GROWTH INHIBITION MODEL IN PKPD

  • Byun, Jong Hyuk;Jung, Il Hyo
    • East Asian mathematical journal
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    • 제36권1호
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    • pp.81-90
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    • 2020
  • Many compartment models assume a kinetically homogeneous amount of materials that have well-stirred compartments. However, based on observations from such processes, they have been heuristically fitted by exponential or gamma distributions even though biological media are inhomogeneous in real environments. Fractional differential equations using a specific kernel in Pharmacokinetic/Pharmacodynamic (PKPD) model are recently introduced to account for abnormal drug disposition. We discuss a tumor growth inhibition (TGI) model using fractional-order derivative from it. This represents a tumor growth delay by cytotoxic agents and additionally show variations in the equilibrium points by the change of fractional order. The result indicates that the equilibrium depends on the tumor size as well as a change of the fractional order. We find that the smaller the fractional order, the smaller the equilibrium value. However, a difference of them is the number of concavities and this indicates that TGI over time profile for fitting or prediction should be determined properly either fractional order or tumor sizes according to the number of concavities shown in experimental data.

TRAP1 regulation of mitochondrial life or death decision in cancer cells and mitochondria-targeted TRAP1 inhibitors

  • Kang, Byoung-Heon
    • BMB Reports
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    • 제45권1호
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    • pp.1-6
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    • 2012
  • Hsp90 is one of the most conserved molecular chaperones ubiquitously expressed in normal cells and over-expressed in cancer cells. A pool of Hsp90 was found in cancer mitochondria and the expression of the mitochondrial Hsp90 homolog, TRAP1, was also elevated in many cancers. The mitochondrial pool of chaperones plays important roles in regulating mitochondrial integrity, protecting against oxidative stress, and inhibiting cell death. Pharmacological inactivation of the chaperones induced mitochondrial dysfunction and concomitant cell death selectively in cancer cells, suggesting they can be target proteins for the development of cancer therapeutics. Several drug candidates targeting TRAP1 and Hsp90 in the mitochondria have been developed and have shown strong cytotoxic activity in many cancers, but not in normal cells in vitro and in vivo. In this review, recent developments in the study of mitochondrial chaperones and the mitochondria-targeted chaperone inhibitors are discussed.

Metformin Inhibits Growth of Hepatocellular Carcinoma Cells by Inducing Apoptosis Via Mitochondrion-mediated Pathway

  • Xiong, Yu;Lu, Qing-Jun;Zhao, Jing;Wu, Guo-Yang
    • Asian Pacific Journal of Cancer Prevention
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    • 제13권7호
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    • pp.3275-3279
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    • 2012
  • Recently, population-based studies of type 2 diabetes patients have provided evidence that metformin treatment is associated with a reduced cancer incidence and mortality, but its mode of action remains unclear. Here we report effects of metformin on hepatocellular carcinoma (HCC) Hep-G2 cells and details of molecular mechanisms of metformin activity. Our research indicates that metformin displays anticancer activity against HCC through inhibition of the mTOR translational pathway in an AMPK-independent manner, leading to G1 arrest in the cell-cycle and subsequent cell apoptosis through the mitochondrion-dependent pathway. Furthermore, we showed that metformin strongly attenuated colony formation and dramatically inhibited Hep-G2 tumor growth in vivo. In conclusion, our studies suggested that metformin might have potential as a cytotoxic drug in the prevention and treatment of HCC.

Influence of Pretreatment with Immunosuppressive Drugs on Viral Proliferation

  • Lee, Ga-Eun;Shin, Cha-Gyun
    • Journal of Microbiology and Biotechnology
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    • 제28권10호
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    • pp.1716-1722
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    • 2018
  • Immunosuppressive drugs are used to make the body less likely to reject transplanted organs or to treat autoimmune diseases. In this study, five immunosuppressive drugs including two glucocorticoids (dexamethasone and prednisolone), one calcineurin inhibitor (cyclosporin A), one non-steroid anti-inflammatory drug (aspirin), and one antimetabolite (methotrexate) were tested for their effects on viral proliferation using feline foamy virus (FFV). The five drugs had different cytotoxic effects on the Crandell-Ress feline kidney (CRFK) cells, the natural host cell of FFV. Dexamethasone-pretreated CRFK cells were susceptible to FFV infection, but pretreatment with prednisolone, cyclosporin A, aspirin, and methotrexate showed obvious inhibitory effects on FFV proliferation, by reducing viral production to 29.8-83.8% of that of an untreated control. These results were supported by western blot, which detected viral Gag structural protein in the infected cell lysate. As our results showed a correlation between immunosuppressive drugs and susceptibility to viral infections, it is proposed that immune-compromised individuals who are using immune-suppressive drugs may be especially vulnerable to viral infection originated from pets.

Toxicity and Biomedical Imaging of Fluorescence-Conjugated Nanoparticles in Hematopoietic Progenitor Cells

  • Min, Gye-Sik;Kim, Dong-Ku
    • Reproductive and Developmental Biology
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    • 제35권4호
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    • pp.503-510
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    • 2011
  • Cellular uptake of nanoparticles for stem cell labeling and tracking is a critical technique for biomedical therapeutic applications. However, current techniques suffer from low intracellular labeling efficiency and cytotoxic effects, which has led to great interest in the development of a new labeling strategy. Using silica-coated nanoparticles conjugated with rhodamine B isothiocyanate (RITC) (SR), we tested the cellular uptake efficiency, biocompatibility, proliferation or differentiation ability with murine bone marrow derived hematopoietic stem/progenitor cells. The bone marrow hematopoietic cells showed efficient uptake with SR with dose or time dependent manner and also provided a higher uptake on hematopoietic stem/progenitor cells. Biocompatibility tests revealed that the SR had no deleterious effects on cell cytotoxicity, proliferation, or multi-differentiation capacities in vitro and in vivo. SR nanoparticles are advantageous over traditional labeling techniques as they possess a high level of cellular internalization without limiting the biofunctionality of the cells. Therefore, SR provides a useful alternative for gene or drug delivery into hematopoietic stem/progenitor cells for basic research and clinical applications.

Synthesis and Bioactivity of Quercetin Aspirinates

  • Lu, Chenjuan;Huang, Feng;Li, Zexin;Ma, Jinshuo;Li, Huanhuan;Fang, Lizhen
    • Bulletin of the Korean Chemical Society
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    • 제35권2호
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    • pp.518-520
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    • 2014
  • Hybrids of some natural compounds are promising to obtain new leads with good biological activities for drug discovery. Three quercetin aspirinates were synthesized by esterification of the 3-and 7-hydroxyl groups of quercetin with aspirin. Biological activities of these quercetin aspirinates were initially screened and showed better cytotoxic activities against tumor cell lines HL-60 and HepG2 and less scavenging activity against DPPH than the quercetin respectively.

Ginsenoside Rgi is an Anti-apoptotic Agent

  • Zhang, Jun-Tian;Li, Jun-Qing
    • 고려인삼학회:학술대회논문집
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    • 고려인삼학회 1998년도 Advances in Ginseng Research - Proceedings of the 7th International Symposium on Ginseng -
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    • pp.12-20
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    • 1998
  • Primary neuronal culture was studied for observing effect of ginsenoside Rgl (Rgl) on serum-free medium induced apoptosis. Results showed that Rgl at concentration of 1 umol$.$ L-1 and 10 umol$.$L-1 could inhibit apoptosis, decrease intracellular calcium concentration in cultured cortical neurons, enhance SOD activity in both aged rat cortex and cultured cortical neurons, scavenge cytotoxic oxygen free radicals, decrease NO content and NOS activity in aged rat cortex and cultured cortical neurons, increase bel-2 gene expression in rat brain. These results provided new data for elucidating the anti-aging effect of Rgi. Rgl is considered to be a useful drug for treatment of Alzheimer's disease and brain aging.

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