High expression of CD44v9 and xCT in chemoresistant hepatocellular carcinoma: Potential targets by sulfasalazine

Cancer Sci. 2018 Sep;109(9):2801-2810. doi: 10.1111/cas.13728. Epub 2018 Aug 16.

Abstract

CD44v9 is expressed in cancer stem cells (CSC) and stabilizes the glutamate-cystine transporter xCT on the cytoplasmic membrane, thereby decreasing intracellular levels of reactive oxygen species (ROS). This mechanism confers ROS resistance to CSC and CD44v9-expressing cancer cells. The aims of the present study were to assess: (i) expression status of CD44v9 and xCT in hepatocellular carcinoma (HCC) tissues, including those derived from patients treated with hepatic arterial infusion chemoembolization (HAIC) therapy with cisplatin (CDDP); and (ii) whether combination of CDDP with sulfasalazine (SASP), an inhibitor of xCT, was more effective on tumor cells than CDDP alone by inducing ROS-mediated apoptosis. Twenty non-pretreated HCC tissues and 7 HCC tissues administered HAIC therapy with CDDP before surgical resection were subjected to immunohistochemistry analysis of CD44v9 and xCT expression. Human HCC cell lines HAK-1A and HAK-1B were used in this study; the latter was also used for xenograft experiments in nude mice to assess in vivo efficacy of combination treatment. CD44v9 positivity was significantly higher in HAIC-treated tissues (5/7) than in non-pretreated tissues (2/30), suggesting the involvement of CD44v9 in the resistance to HAIC. xCT was significantly expressed in poorly differentiated HCC tissues. Combination treatment effectively killed the CD44v9-harboring HAK-1B cells through ROS-mediated apoptosis and significantly decreased xenografted tumor growth. In conclusion, the xCT inhibitor SASP augmented ROS-mediated apoptosis in CDDP-treated HCC cells, in which the CD44v9-xCT system functioned. As CD44v9 is typically expressed in HAIC-resistant HCC cells, combination treatment with SASP with CDDP may overcome such drug resistance.

Keywords: anticancer drug resistance; cancer stem cell; combinational therapy; oxidative stress; sphere formation.

MeSH terms

  • Aged
  • Aged, 80 and over
  • Amino Acid Transport System y+ / analysis
  • Amino Acid Transport System y+ / physiology*
  • Animals
  • Apoptosis / drug effects
  • Carcinoma, Hepatocellular / chemistry
  • Carcinoma, Hepatocellular / drug therapy*
  • Cisplatin / pharmacology
  • Drug Resistance, Neoplasm
  • Female
  • Hep G2 Cells
  • Humans
  • Hyaluronan Receptors / analysis
  • Hyaluronan Receptors / physiology*
  • Liver Neoplasms / chemistry
  • Liver Neoplasms / drug therapy*
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Middle Aged
  • Reactive Oxygen Species / metabolism
  • Sulfasalazine / pharmacology*

Substances

  • Amino Acid Transport System y+
  • CD44S antigen
  • CD44v9 antigen
  • Hyaluronan Receptors
  • Reactive Oxygen Species
  • SLC7A11 protein, human
  • Sulfasalazine
  • Cisplatin