• 제목/요약/키워드: Cytotoxic agents

검색결과 291건 처리시간 0.024초

Endpoint of Cancer Treatment: Targeted Therapies

  • Topcul, Mehmet;Cetin, Idil
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권11호
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    • pp.4395-4403
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    • 2014
  • Nowadays there are several limitations in cancer treatment. One of these is the use of conventional medicines which not only target cancer cells and thus also cause high toxicity precluding effective treatment. Recent elucidation of mechanisms that cause cancer has led to discovery of novel key molecules and pathways which have have become successful targets for the treatments that eliminate only cancer cells. These so-called targeted therapies offer new hope for millions of cancer patients, as briefly reveiwed here focusing on different types of agents, like PARP, CDK, tyrosine kinase, farnysyl transferase and proteasome inhibitors, monoclonal antibodies and antiangiogenic agents.

Antitumor activity of oxaliplatin, 5-FU and paclitaxel given alone and in combination with ZD1839 in human gastric carcinoma cells in vitro.

  • Jang, Ji-Hyun;Lee, Sang-Hak;Kang, Jin-Hyoung;Sun, Hee-Sik;Kuh, Hyo-Jeong
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.227.2-228
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    • 2002
  • ZD1839 is a new anticancer agent which selectively inhibits EGFR tyrosine kinase. Oxaliplatin (LOHP), 5-FU (FU), and paclitaxel (PTX) have shown to be highly active against the gastric carcinomas. and ZD1839 is considered as a good candidate for the treatment of gastric cancers when combined with cytotoxic agents. In this study, we evaluated the antitumor effects of these agents in SNU-l human gastric cancer cells either alone or when given as a doublet. (omitted)

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Myxococcus stipitatus JW150이 생산하는 세포독성 물질의 분리 및 특성 (Isolation and Properties of Cytotoxic Antibiotics Produced by Myxococcus stipitatus JW150)

  • 안종웅;이정옥
    • 약학회지
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    • 제46권2호
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    • pp.108-112
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    • 2002
  • Drug resistance is one of the most significant impediments to successful chemotherapy of cancer. Multidrug-resistance (MDR) is characterized by decreased cellular sensitivity to anticancer agents due to the overexpression of P-glycoprotein. By employing a resistant subline of HCT15 to adriamycin (CL02), we undertook the screening for agents which were effective to multidrug-resistant cancer cells. As a result, a myxobacterial strain JW150 was selected for study since an activity against CL02 cells was discovered in the strain. Cytotoxicity-guided fractionation of the culture broth led to the isolation of cystothiazole A and melithiazole F. The producing organism was identified as Myxococcus stipitatus by taxonomic comparison with type strains of Myxococcus sp. as well as its morphological and physiological characteristics. Cystothiazole A and melithiazole F demonstrated potent cytotoxicity against certain human cancer cells with $IC_{50}$ values ranging from 0.03~ $0.72{\mu}{\textrm{g}}$/ml. Both compounds were interestingly as active against drug-resistant sublines CL02 and CP70 as against the corresponding parental cells.

Cytotoxic and Apoptotic Effects of Echinomycin on Murine Leukemia Cells

  • Kim, Tae-Ue;Yang, Se-Hwan;Kim, Soo-Kie
    • BMB Reports
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    • 제29권6호
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    • pp.489-492
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    • 1996
  • A number of anticancer-chemotherapeutic agents induce cell death through the process of apoptosis. Effects of echinomycin, an anticancer agent on cancer progression, were investigated in P388 murine leukemia cells. First, according to the results of cytotoxicity measurement. $IC_{50}$ of echinomycin was 1.12 nM, a relatively lower value than the other examined anticancer agents, mitomycin-C and etoposide Second, the DNA fragmentation assay for echinomycin-treated cells exhibited that echinomycin was able to induce apoptosis in a shorter period of time and with a lower dose than mitomycin-C or etoposide. The data of DNA fragmentation were quite comparable to those of cytotoxicity measurement. Finally we showed that mitogen-activated protein (MAP) kinase, a key protein in cell mitosis, was translocated into the nucleus from the cytosol after treatment with echinomycin. These findings suggest that a MAP kinase-related process may be involved in apoptosis induced by echinomycin.

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Boronated Porphyrins and Chlorins as Potential Anticancer Drugs

  • Ol'shevskaya, Valentina A.;Zaytsev, Andrey V.;Savchenko, Arina N.;Shtil, Alexander A.;Cheong, Chan-Seong;Kalinin, Valery N.
    • Bulletin of the Korean Chemical Society
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    • 제28권11호
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    • pp.1910-1916
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    • 2007
  • Analyzed are recent advances in design of novel boronared conjugates of synthetic and natural porphyrins and chlorins. These compounds showed high efficacy as cytotoxic agents for tumor cells in culture and as phototoxins in photodynamic therapy of tumor xenografts. Thus, boronated porphyrins and chlorins emerge as promising class of anticancer agents with potentially multiple advantages: the chemotherapeutic drugs alone and photo- and radiosensitizers in binary treatments.

Synthesis and Properties of Soluble and Stable Silyl End-capped Bis-thienylanthracene Oligomers

  • Choi, Jung-Hei;Cho, Dae-Won;Sung, Nam-Kyoung;Jin, Sung-Ho;Yoon, Ung-Chan
    • Bulletin of the Korean Chemical Society
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    • 제28권11호
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    • pp.1931-1938
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    • 2007
  • Analyzed are recent advances in design of novel boronared conjugates of synthetic and natural porphyrins and chlorins. These compounds showed high efficacy as cytotoxic agents for tumor cells in culture and as phototoxins in photodynamic therapy of tumor xenografts. Thus, boronated porphyrins and chlorins emerge as promising class of anticancer agents with potentially multiple advantages: the chemotherapeutic drugs alone and photo- and radiosensitizers in binary treatments.

Development of a new Cox-2 inhibitor as an anticancer agent

  • Park, Jeong-Ran;Hyoung, Kang-Jin;Young, Noh-Ji;Chul, Ryu-Hyung;Park, Sang-Wook;Hwan, Cho-Il;H, Hwang-Daniel;Kim, In-Kyung;Jeog, Kuh-Hyo
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.227.1-227.1
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    • 2002
  • Cyclooxygenase (Cox-2) is involved in tumorigenesis. hence. considered to be a molecular target for chemoprevention and chemomodulation. Selective Cox-2 inhibitors including Celecoxib and Nimesulide have been studied for their anticancer activity when given alone and in combination with radiation or cytotoxic agents. In this study, we synthesized more than 140 analogues of Celecoxib and Nimesulide. and evaluated their inhibitory effects on Cox-l and Cox-2 activity as well as cytotoxicity in order to find promising anticancer agents having selective Cox-2 inhibitory effect. (omitted)

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Fluorouracil의 환경감시 및 제거약제에 관한 연구 (A Study on Environmental Monitoring of Fluorouracil and Decontamination Reagents)

  • 이수길;이내우
    • 한국안전학회지
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    • 제24권4호
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    • pp.47-52
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    • 2009
  • 이 연구는 Fluorouracil(5-FU)가 병원에서 암치료제로 쓰이는 세포독성약제의 한 종류이기 때문에 병원내부에 5-FU의 폭로 정도와 그 관리를 위한 가장 효율적인 세척약제를 조사하기 위한 것이다. 이러한 세포독성 약제실이나 종약학 병동에서 근무하는 실무자들은 세포독성약제로 오염된 표면에 빈번하게 접촉하게 되면 세포유전성이나 DNA손상에 대한 위험이 높게 된다. 따라서 이러한 약제의 세척제실험을 위하여 4가지 약제로서 시행한분해시험에서 0.5%(w/v) NaClO 용액만이 5-FU를 즉시 분해시켰으므로 이 용액은 오염표면의 잔유물을 분해시키는데 사용될 수 있다. 세포독성 약제실의 오염표면에서 확인된 농도범위는 2.0에서 $13.8{\mu}g/m^2$까지이고, 종약학 병동의 오염표면에서 측정한 농도범위는 5.39에서 $11.53{\mu}g/m^2$이었다. 5-FU와 같은 세포독성약제로부터 피부오염을 피하기 위하여 작업장의 노출허용기준과 같은 법적인 조치, 완벽한 표면세척제 및 보호구사용과 같은 엄격한 관리기준이 마련되어야 할 것이다.

Differential Behaviour of Selenium Analogs against Anticancer Drug Induced Apoptosis of Lymphocytes in Human Peripheral Blood

  • Elango, Sonaa;Subbiah, Usha;Jain, Jeong
    • Asian Pacific Journal of Cancer Prevention
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    • 제17권5호
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    • pp.2527-2533
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    • 2016
  • Sensitising cancer cells and at the same time desensitizing normal cells is a double task in cancer management. Agents which can combat the debilitating side effects of cancer therapeutics and simultaneously synergize with anticancer agents in specifically targeting cancer cells are needed. Selenium, a proven anticarcinogen, gains due importance in terms of its efficacy to combat the side effects of cancer therapy. This study is a comparative analysis of the chemoprotective effects of selenium compounds, methyl selenol (generated from organic selenomethionine (5mmol/L ; METase 40U/L)) and sodium selenite (inorganic form)($30{\mu}M$) in peripheral blood human lymphocytes exposed to cisplatin and mitomycin. Biochemical alterations occurring in many cells during apoptosis include loss of plasma membrane phospholipid asymmetry, DNA fragmentation, and activation of caspase-3. The present study demonstrated that the selenium metabolite and selenite are efficient in protecting lymphocytes undergoing DNA damage and exerted their activity by reducing caspase 3 expression. Interestingly organic methylselenol (MeSe) was found to offer more protective effects compared to inorganic selenite (SeL), by reducing the induction of apoptosis by the cytotoxic agents. This suggests that MeSe and to a lesser extent selenite might have potential for assessment in clinical trials and could be considered as strong candidates in pharmacogenomics or in the nutriprotective arena.

A Study on the Tyrosinase Inhibitory and Antioxidant Effect of Microalgae Extracts

  • Ji, Keunho;Kim, Yeeun;Kim, Young Tae
    • 한국미생물·생명공학회지
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    • 제49권2호
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    • pp.167-173
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    • 2021
  • Reactive oxygen species (ROS) disrupt the cellular redox balance, exert cytotoxic effects, and consequently promote the development of various diseases in humans. Previous studies have reported that antioxidants counteract the adverse effects of ROS. Several studies examine the whitening effects of various agents based on their ability to inhibit tyrosinase activity. Tyrosinase is a critical enzyme involved in the synthesis of melanin, which protects the skin against radiation. Various agents exhibiting antioxidant and tyrosinase inhibitory activities have been synthesized. However, these synthetic drugs are associated with toxicity, decreased safety, and poor skin penetration in vivo, which has limited the clinical application of synthetic drugs. This study examined the antioxidant and tyrosinase inhibitory activities of some microalgae. The methanol, dichloromethane, and ethyl acetate extracts of four microalgal species (Tetraselmis tetrathele, Dunaliella tertiolecta, Platymonas sp., and Chaetoceros simplex) were prepared. The physiological and whitening effects of microalgal extracts were investigated by measuring the antioxidant and tyrosinase inhibitory activities. The ethyl acetate extract of D. tertiolecta exhibited the highest antioxidant and tyrosinase inhibitory activities. Future studies must focus on examining the whitening effects of microalgae on cell lines to facilitate the development of microalga-based therapeutics for skin diseases, functional health foods, and whitening agents. Thus, microalgae have potential applications in the pharmaceutical, food, and cosmetic industries.