1 Ocak 2019 Dergi makalesi Açık Erişim

Delman, Murat; Avci, Sanem Tercan; Akcok, Ismail; Kanbur, Tugce; Erdal, Esra; Cagir, Ali

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  "@context": "https://schema.org/", 
  "@id": 74491, 
  "@type": "ScholarlyArticle", 
  "creator": [
    {
      "@type": "Person", 
      "affiliation": "Izmir Inst Technol, Dept Biotechnol & Bioengn, TR-35430 Izmir, Turkey", 
      "name": "Delman, Murat"
    }, 
    {
      "@type": "Person", 
      "name": "Avci, Sanem Tercan"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Izmir Inst Technol, Fac Sci, Dept Chem, TR-35430 Izmir, Turkey", 
      "name": "Akcok, Ismail"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Izmir Inst Technol, Fac Sci, Dept Chem, TR-35430 Izmir, Turkey", 
      "name": "Kanbur, Tugce"
    }, 
    {
      "@type": "Person", 
      "name": "Erdal, Esra"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Izmir Inst Technol, Fac Sci, Dept Chem, TR-35430 Izmir, Turkey", 
      "name": "Cagir, Ali"
    }
  ], 
  "datePublished": "2019-01-01", 
  "description": "Cytotoxic effects of (R)-4'-methylklavuzon were investigated on hepatocellular carcinoma cells (HuH-7 and HepG2) and HuH-7 EpCAM(+)/CD133(+) cancer stem cells. IC50 of (R)-4'-methylklavuzon was found as 1.25 mu M for HuH-7 parental cells while it was found as 2.50 mu M for HuH-7 EpCAM(+)/CD133(+) cancer stem cells. (R)-4'-methylklavuzon tended to show more efficient in vitro cytotoxicity with its lower IC50 values on hepatocellular carcinoma cell lines compared to its lead molecule, goniothalamin and FDA-approved drugs, sorafenib and regorafenib. Cell-based Sirtuin/HDAC enzyme activity measurements revealed that endogenous Sirtuin/HDAC enzymes were reduced by 40% compared to control. SIRT1 protein levels were upregulated indicating triggered DNA repair mechanism. p53 was overexpressed in HepG2 cells. (R)-4'methylklavuzon inhibited CRM1 protein providing increased retention of p53 and RIOK2 protein in the nucleus. HuH-7 parental and EpCAM(+)/CD133(+) cancer stem cell spheroids lost intact morphology. 3D HepG2 spheroid viabilities were decreased in a correlation with upregulation in p53 protein levels. (C) 2019 Elsevier Masson SAS. All rights reserved.", 
  "headline": "Antiproliferative activity of (R)-4 '-methylklavuzon on hepatocellular carcinoma cells and EpCAM(+)/CD133(+) cancer stem cells via SIRT1 and Exportin-1 (CRM1) inhibition", 
  "identifier": 74491, 
  "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", 
  "license": "http://www.opendefinition.org/licenses/cc-by", 
  "name": "Antiproliferative activity of (R)-4 '-methylklavuzon on hepatocellular carcinoma cells and EpCAM(+)/CD133(+) cancer stem cells via SIRT1 and Exportin-1 (CRM1) inhibition", 
  "url": "https://aperta.ulakbim.gov.tr/record/74491"
}