Literature DB >> 21116565

{2-[1-(3-Methoxycarbonylmethyl-1H-indol-2-yl)-1-methyl-ethyl]-1H-indol-3-yl}-acetic acid methyl ester (MIAM): its anti-cancer efficacy and intercalation mechanism identified via multi-model systems.

Wenjing Wang1, Ming Zhao, Yuji Wang, Jiawang Liu, Jianhui Wu, Guifeng Kang, Shiqi Peng.   

Abstract

{2-[1-(3-Methoxycarbonylmethyl-1H-indol-2-yl)-1-methyl-ethyl]-1H-indol-3-yl}-acetic acid methyl ester (MIAM) was provided as a DNA-intercalator. For the comprehensive evaluation of this new intercalator, an assay system consisting of cell, S180 mouse, healthy mouse, spectrum, non-spectrum, and gel electrophoresis models was constructed. On the cell (S180, K562, MCF-7, HeLa and HepG2) models, MIAM selectively inhibited the viability of HeLa. On the S180 mouse model, 0.89, 8.9, 89 and 890 μmol kg(-1) of MIAM dose-dependently inhibited the tumor growth. Even at a dose of 890 μmol kg(-1), MIAM did not damage the treated S180 mice. The safety of MIAM was supported by a high spleen index and an obvious increase of body weight of the treated S180 mice. On the healthy mouse model the LD(50) value of MIAM is higher than 890 μmol kg(-1). The ultraviolet (UV), fluorescence, circular dichroism (CD), relative viscosity, melting curve, and gel electrophoresis assays of DNA with or without MIAM consistently supported an intercalation mechanism for MIAM.

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Year:  2010        PMID: 21116565     DOI: 10.1039/c0mb00049c

Source DB:  PubMed          Journal:  Mol Biosyst        ISSN: 1742-2051


  4 in total

1.  Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and the mammalian target of rapamycin complex 1 activity.

Authors:  Yuji Wang; Pingxin Li; Shu Wang; Jing Hu; Xiangyun Amy Chen; Jianhui Wu; Megan Fisher; Kira Oshaben; Na Zhao; Ying Gu; Dong Wang; Gong Chen; Yanming Wang
Journal:  J Biol Chem       Date:  2012-05-17       Impact factor: 5.157

2.  {2-[1-(3-Methoxycarbonylmethyl-1H-indol-2-yl)-1-methyl-ethyl]-1H-indol-3-yl}-acetic Acid Methyl Ester Inhibited Hepatocellular Carcinoma Growth in Bel-7402 Cells and Its Resistant Variants by Activation of NOX4 and SIRT3.

Authors:  Ye Li; Wenjing Wang; Xiaoxue Xu; Shiyue Sun; Xiaoyu Xu; Xian-jun Qu
Journal:  Biomed Res Int       Date:  2015-04-15       Impact factor: 3.411

3.  5-(Bis(3-(2-hydroxyethyl)-1H-indol-2-yl)methyl)-2-hydroxybenzoic acid (BHIMHA): showing a strategy of designing drug to block lung metastasis of tumors.

Authors:  Taiping Gan; Yuji Wang; Ming Zhao; Jianhui Wu; Jian Yang; Shiqi Peng
Journal:  Drug Des Devel Ther       Date:  2016-02-16       Impact factor: 4.162

4.  Discovery of DEBIC to correlate P-selectin inhibition and DNA intercalation in cancer therapy and complicated thrombosis.

Authors:  Haiyan Chen; Wenjing Wang; Xiaoyi Zhang; Shan Liu; Yaonan Wang; Haimei Zhu; Jianhui Wu; Yuji Wang; Ming Zhao; Shiqi Peng
Journal:  Oncotarget       Date:  2017-12-08
  4 in total

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