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Canagliflozin reduces cisplatin uptake and activates Akt to protect against cisplatin-induced nephrotoxicity

Am J Physiol Renal Physiol. 2020 Apr 1;318(4):F1041-F1052. doi: 10.1152/ajprenal.00512.2019. Epub 2020 Mar 9.

Abstract

Cisplatin is a widely used chemotherapy drug with notorious nephrotoxicity. Na+-glucose cotransporter 2 inhibitors are a class of novel antidiabetic agents that may have other effects in the kidneys besides blood glucose control. In the present study, we demonstrated that canagliflozin significantly attenuates cisplatin-induced nephropathy in C57BL/6 mice and suppresses cisplatin induced renal proximal tubular cell apoptosis in vitro. The protective effect of canagliflozin was associated with inhibition of p53, p38 and JNK activation. Mechanistically, canagliflozin partially reduced cisplatin uptake by kidney tissues in mice and renal tubular cells in culture. In addition, canagliflozin enhanced the activation of Akt and inhibited the mitochondrial pathway of apoptosis during cisplatin treatment. The protective effect of canagliflozin was diminished by the phosphatidylinositol 3-kinase/Akt inhibitor LY294002. Notably, canagliflozin did not affect the chemotherapeutic efficacy of cisplatin in A549 and HCT116 cancer cell lines. These results suggest a new application of canagliflozin for renoprotection in cisplatin chemotherapy. Canagliflozin may protect kidneys by reducing cisplatin uptake and activating cell survival pathways.

Keywords: Akt; acute kidney injury; canagliflozin; cisplatin; nephrotoxicity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Apoptosis / drug effects*
  • Canagliflozin / pharmacology*
  • Cells, Cultured
  • Cisplatin*
  • Cytochromes c / metabolism
  • Cytoprotection
  • Disease Models, Animal
  • Enzyme Activation
  • JNK Mitogen-Activated Protein Kinases / metabolism
  • Kidney / drug effects*
  • Kidney / enzymology
  • Kidney / pathology
  • Kidney Diseases / chemically induced
  • Kidney Diseases / enzymology
  • Kidney Diseases / pathology
  • Kidney Diseases / prevention & control*
  • Male
  • Mice, Inbred C57BL
  • Phosphorylation
  • Proto-Oncogene Proteins c-akt / metabolism*
  • Rats
  • Signal Transduction
  • Tumor Suppressor Protein p53 / metabolism
  • bcl-2-Associated X Protein / metabolism
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • Bax protein, rat
  • Tp53 protein, rat
  • Trp53 protein, mouse
  • Tumor Suppressor Protein p53
  • bcl-2-Associated X Protein
  • Canagliflozin
  • Cytochromes c
  • Proto-Oncogene Proteins c-akt
  • JNK Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases
  • Cisplatin