• 제목/요약/키워드: anti-tumor effects

검색결과 1,462건 처리시간 0.037초

Antitumor profiles and cardiac electrophysiological effects of aurora kinase inhibitor ZM447439

  • Lee, Hyang-Ae;Kwon, Miso;Kim, Hyeon-A;Kim, Ki-Suk
    • The Korean Journal of Physiology and Pharmacology
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    • 제23권5호
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    • pp.393-402
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    • 2019
  • Aurora kinases inhibitors, including ZM447439 (ZM), which suppress cell division, have attracted a great deal of attention as potential novel anti-cancer drugs. Several recent studies have confirmed the anti-cancer effects of ZM in various cancer cell lines. However, there have been no studies regarding the cardiac safety of this agent. We performed several cytotoxicity, invasion and migration assays to examine the anti-cancer effects of ZM. To evaluate the potential effects of ZM on cardiac repolarisation, whole-cell patch-clamp experiments were performed with human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) and cells with heterogeneous cardiac ion channel expression. We also conducted a contractility assay with rat ventricular myocytes to determine the effects of ZM on myocardial contraction and/or relaxation. In tests to determine in vitro efficacy, ZM inhibited the proliferation of A549, H1299 (lung cancer), MCF-7 (breast cancer) and HepG2 (hepatoma) cell lines with $IC_{50}$ in the submicromolar range, and attenuated the invasive and metastatic capacity of A549 cells. In cardiac toxicity testing, ZM did not significantly affect $I_{Na}$, $I_{Ks}$ or $I_{K1}$, but decreased $I_{hERG}$ in a dose-dependent manner ($IC_{50}$: $6.53{\mu}M$). In action potential (AP) assay using hiPSC-CMs, ZM did not induce any changes in AP parameters up to $3{\mu}M$, but it at $10{\mu}M$ induced prolongation of AP duration. In summary, ZM showed potent broad-spectrum anti-tumor activity, but relatively low levels of cardiac side effects compared to the effective doses to tumor. Therefore, ZM has a potential to be a candidate as an anti-cancer with low cardiac toxicity.

Effects of Acanthopanax sessiliflorus on Immune Cells such as Thymocytes, Splenocytes and Macrophages in Mice

  • Kim, Hyung-Woo;Kim, Gye-Yeop;Jeon, Byung-Gwan;Choi, Jeong-Sik;Jeong, Hyun-Woo;Cho, Su-In
    • The Journal of Internal Korean Medicine
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    • 제28권2호
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    • pp.377-384
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    • 2007
  • Objective : Immune potentiation including activation of T cells, B cells, macrophages, and dendritic cells is known to play a key role in prevention and treatment of patients with cancer. In this study, we investigated the effects of Acanthopanax sessiliflorus (AR) on the immune system, especially on thymocytes, splenocytes, and macrophages. Methods : We investigated the effects of AR on proliferation of splenocytes in normal mice, and the effects on proliferation of splenocytes and thymocytes in tumor-bearing mice. In addition, the effect of AR on NO production using macrophages was investigated. Results : Treatment with AR accelerated proliferation of splenocytes in vitro. AR also accelerated thymocyte proliferation, but did not affect splenocytes proliferation in normal mice. In contrast, AR accelerated proliferation of splenocytes and thymocytes significantly in tumor bearing mice. In addition, NO production level from macrophages was elevated by treatment with AR. Conclusion : These results demonstrate that AR has anti-cancer activities and related mechanisms are involved in immune potentiation such as acceleration of immune cell proliferation and elevation of NO production level in macrophages. In addition, we also demonstrate the possibilities of AR as complementary and alternative medicine to standard anti-cancer drugs.

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Effects of Gunbibosinhangam-tang and Gunbibosinhangam-tang-gamibang on Solid Tumor and Immune Cells in Mice (건비보현항암탕(健脾補腎抗癌湯) 및 건비보현항암탕가미방(健脾補腎抗癌湯加味方)이 고형암 및 면역세포에 미치는 영향)

  • Lee, Seon-A;Ko, Seok-Jae;Eun, Seon-Hye;Lee, Hyun-Ki;Ahn, Min-Seob;Kwon, Young-Mi;Yoo, Da-Young;Moon, Goo
    • Journal of Physiology & Pathology in Korean Medicine
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    • 제24권4호
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    • pp.602-609
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    • 2010
  • This study was carried out to investigate the anti-cancer effects of Gunbibosinhangam-tang (GBHT I) and Gunbibosinhangam-tang-gamibang (GBHT II, GBHT III) on solid tumor and immune cells. The animals were divided into 4 groups ; Control, no treatment. GBHT I, treatment with GBHT itself. GBHT II, treatment with GBHT increased the quantity of Hedyotis Diffusae twice. GBHT III, treatment with GBHT increased the quantity of Hedyotis Diffusae four times. We investigated the effects of GBHT on proliferation of solid tumor cells (S-180), thymocytes, splenocytes in vitro in order to examine cytotoxicity for S-180 and immuno-stimulating activities. The experiments that is about solid tumor weight and survival rate in tumor bearing mice were performed also. As compared with the control group, treatments with GBHT II and GBHT III suppressed the proliferation of S-180 effectively. Treatments with all experimental groups accelerated the proliferation of thymocytes and splenocytes significantly. In addition, GBHT III was significantly decreased on solid tumor weight and increased on survival rate in tumor bearing mice. Based upon these results, we suggest that GBHT and GBHT-gamibang have both anti-cancer effects for S-180 and immuno-stimulating activities for thymocytes and splenocytes. Therefore, we conclude that GBHT and Hedyotis Diffusae is useful to treat the patients with cancer.

Anti-HER-2×anti-CD3 Bi-specific Antibodies Inhibit Growth of HCT-116 Colorectal Carcinoma Cells in Vitro and in Vivo

  • Ren, Hui;Li, Jun;Liu, Jing-Jing;Guo, Hui-Ling;Jiang, Tao
    • Asian Pacific Journal of Cancer Prevention
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    • 제13권6호
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    • pp.2795-2798
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    • 2012
  • Objective: This study is conducted to evaluate the effects of anti-HER-2${\times}$anti-CD3 bi-specific antibodies(BsAb) on HER-2/neuover-expressing human colorectal carcinoma cells. Methods: Growth was assessed by MTT assays after exposure of HCT-116 cells to Herceptin, anti-CD3 and BsAb antibodies. Immunocytochemistry was applied to test the HER-2 level of HCT-116. In a nude mouse model, HER-2${\times}$CD3 BsAb was combined with effector cells (peripheral blood lymph cells from normal human being) for observations on in Vivo growth of tumors. Results: Compared with the control group, using effector cells combined with anti-CD3 McAb, Herceptin or HER2${\times}$CD3 BsAb, tumor cell growth in vitro and in vivo was significantly inhibited (P<0.05), most remarkably in the HER2${\times}$CD3 BsAb case. The growth of xenografts with HER2${\times}$CD3 BsAb combined with effector cells was also significantly inhibited when compared with the anti-CD3 McAb or Herceptin groups (P<0.05). Conclusion: HER-2/neu might be a useful target for immunotherapy in colorectal carcinoma, anti-HER2${\times}$anti-CD3 BsAb exerting clear anti-tumor effects.

Inhibitory effect of Hwang lyun tang water extract on inflammatory mediators

  • Chae, Hee-Sung;Kang, Ok-Hwa;Kwon, Dong-Yeul
    • Journal of Evidence-Based Herbal Medicine
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    • 제1권1호
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    • pp.7-11
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    • 2008
  • The purpose of this study was to investigate the anti-inflammatory effects of extract from Hwang lyun tang (HLT) on the THP-1 cell and HMC-1 cell. To evaluate of anti-inflammatory of HLT, we examined cytokines production in lipopolysacchride (LPS)-induced THP-1 cell and A23187, PMA-induced HMC-1 cell. Extract of HLT inhibit LPS-induced interleukin (IL)-8 production in human monocyte THP-1 cells. Extract of HLT inhibit A23187, PMA-induced IL-8, tumor necrosis factor-$\alpha$ (INF-$\alpha$) production in HMC-1 cells. HLT down-regulated LPS-induced IL-8 production and A23187, PMA-induced IL-8, TNF-$\alpha$ production, which may be provide a clinical basis for anti-inflammatory properities of HLT.

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Effect of Jak-Yak Tang water extract on expression of cytokin and chemokine

  • Oh, You-Chang;Kang, Ok-Hwa;Kwon, Dong-Yeul
    • Journal of Evidence-Based Herbal Medicine
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    • 제1권1호
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    • pp.1-5
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    • 2008
  • Objectives : The purpose of this study was to investigate the anti-inflammatory effects of extract from Jak-Yak Tang (JYT) on the THP-1 cell and HMC-1 cell. Method : To evaluate of anti-inflammatory of JYT, we examined cytokines production in lipopolysacchride (LPS)-induced THP-1 cell and A23187, PMA-induced HMC-1 cell. Result : Extract of JYT inhibit LPS-induced interleukin (IL)-8 production in human monocyte THP-1 cells. Extract of JYT inhibit A23187, PMA-induced IL-8, tumor necrosis factor-$\alpha$ (INF-$\alpha$) production in HMC-1 cells. Conclusion : NT down-regulated LPS-induced IL-8 production and A23187, PMA-induced IL-8, TNF-$\alpha$ production, which may be provide a clinical basis for anti-inflammatory properities of JYT.

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Anti-microbial Activities Against Oral Microbes and Growth-Inhibitory Effect on Oral Tumor Cell of Extracts of Perilla and Mugwort (들깨잎과 쑥 추출물의 구강병 원인균에 대한 항균 및 KB 세포 증식 억제효과)

  • Jo, Min-Jung;Min, Kyung-Jin
    • Journal of Environmental Health Sciences
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    • 제33권2호
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    • pp.115-122
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    • 2007
  • Methanol extracts of Perilla and Mugwort were stepwise extracted with hexane, chloroform, ethyl acetate, butanol and water. Anti-microbial activities and inhibitory effect on growth of oral tumor cell of each extract were investigated. Each extracts of Perilla and Mugwort were investigated to anti-microbial effects on oral microbes by means of agar diffusion method and MIC. These results suggest that the hexane extracts of Perilla and Mugwort have antimicrobial activities against S. mutans and potent inhibitory Effect to KB cell growth.

Antitumor Effect Of Bismuth-conjugated Anti-IL-2R Monoclonal Antibody(2E4) on a IL-2 Receptor Positive Tumor EL4J3.4

  • Kim, Sung-Hoon;Robert-W. Kozak;Chung, Kyeong-Soo;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • 제17권3호
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    • pp.194-198
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    • 1994
  • The antitumor effects of the 2E4 and anti--Tac, monoclonal antibodies directed to Il-2 receptor (IL-2R) conjugated with .alpha.-particle emitting radionuclide bismuth-212., were compared. The $^{212}Bi-2E4$ demonstratedspecific cytotocicity to EL4J3, 4, a I$L-2R^+$ cell line, than to EL4J, a $IL-2R^-$ cell line in thymidine incorporation assy. TEX>$^{212}Bi-2E4$ exerted the maximal antitumor effect in that % T/C in C57BL/6 mice implanted with EL4J3.4 ascitic tumor was 331% at the concentration of $50{\;}{\mu}Ci$, while that of $^{212}Bi-anti-Tac$ was 258% at $100{\;}{\mu}Ci$.

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