Resveratrol exerts dose-dependent anti-fibrotic or pro-fibrotic effects in kidneys: A potential risk to individuals with impaired kidney function

Phytomedicine. 2019 Apr:57:223-235. doi: 10.1016/j.phymed.2018.12.024. Epub 2018 Dec 17.

Abstract

Background: Renal fibrosis is the pathological feature of chronic kidney disease (CKD) which leads to end-stage renal disease (ESRD) and renal failure. Resveratrol [3,5,4'-trihydroxy-trans-stilbene (RSV)] has shown benefits for metabolic diseases and anti-cancer therapy, but its potential risk on renal health has not been fully evaluated.

Purpose: To investigate the global effects of RSV on renal fibrosis in human tubular epithelial cell (TEC) line HK-2, and in mice with unilateral ureteral obstruction (UUO).

Methods: A TGF-β-induced in vitro model of epithelial-mesenchymal transition (EMT) in TEC was established. The effects of RSV on cell viability, pro-fibrotic factors, oxidative stress, mitochondria function, and underlying pathway proteins were analyzed. In vivo, the effects of RSV on renal function and fibrosis were assayed in UUO mice.

Results: Our results showed that low concentrations of RSV (5-20 μM) decreased TGF-β-induced EMT via Sirt1-dependent deacetylation of Smad3/Smad4 mechanism. By contrast, long-term (72 h) exposure to high concentrations of RSV (≥ 40 μM) promoted EMT in HK-2 cells via mitochondrial oxidative stress and ROCK1-mediated disordered cytoskeleton remodeling. In vivo, low-dose treatment of RSV (≤ 25 mg/kg) partly improved renal function, whereas high-dose treatment of RSV (≥ 50 mg/kg) lost its anti-fibrotic role and even aggravated renal fibrosis. However, mice with UUO were more susceptible to high RSV-induced renal injury than normal mice.

Conclusion: Dependent on dose, RSV activated either anti-fibrotic or pro-fibrotic effects in kidneys. The risk of RSV consumption in individuals with impaired kidney function should be carefully considered.

Keywords: Dose response; Epithelial-mesenchymal transition; Renal fibrosis; Resveratrol; Tubular epithelial cells.

MeSH terms

  • Animals
  • Cell Line
  • Dose-Response Relationship, Drug
  • Epithelial-Mesenchymal Transition / drug effects*
  • Fibrosis / drug therapy*
  • Fibrosis / pathology
  • Humans
  • Kidney / drug effects*
  • Kidney / pathology
  • Kidney / physiopathology
  • Kidney Tubules, Proximal / cytology
  • Kidney Tubules, Proximal / drug effects
  • Male
  • Mice, Inbred C57BL
  • Mitochondria / drug effects
  • Mitochondria / pathology
  • Resveratrol / administration & dosage*
  • Resveratrol / pharmacology*
  • Sirtuin 1 / metabolism
  • Smad3 Protein / metabolism
  • Transforming Growth Factor beta / toxicity
  • Ureteral Obstruction / drug therapy
  • Ureteral Obstruction / pathology

Substances

  • SMAD3 protein, human
  • Smad3 Protein
  • Transforming Growth Factor beta
  • SIRT1 protein, human
  • Sirtuin 1
  • Resveratrol