V. Klück (1), L. Mies (1), R. Bakker (2), T. O. Crișan (3), L. Joosten (1,3)
Affiliation(s):
1. Department of Internal Medicine, Radboudumc, Nijmegen, The Netherlands 
2. Departement of Rheumatology, Radboudumc, Nijmegen, The Netherlands 
3. Department of Medical Genetics, Luliu Hatieganu University of Medicine and Pharmacy, Cluj Napoca, Romania.
 Introduction: Hyperuricemia, elevated serum urate levels, is  the main risk factor for gout, but is also associated with higher  incidence of comorbidities such as cardiovascular disease, type 2  diabetes, metabolic syndrome and chronic kidney disease [1].  Crisan et al. showed that urate leads to increased production of  interleukin (IL)-1β, a pro-inflammatory cytokine, and downregulation of  IL-1 receptor antagonist (IL-1Ra), the natural inhibitor of IL-1, in  human monocytes [2].  This imbalance between IL-1β and IL-1Ra is mediated by epigenetic  reprogramming of innate immune cells [2]. RNA sequencing in  urate-treated monocytes demonstrated that the TGF-β signalling pathway  was differentially expressed [3].  The objective of this study is to further explore the role of TGF-β in  urate induced priming of human monocytes.
Methods: Human peripheral blood mononuclear cells (PBMCs) were  isolated from healthy volunteers, adhered to a flat bottom plate, and  treated for 24h with a dosing range of urate after which mRNA was  isolated.  For validation experiments, PBMCs from 9 gout patients and 7 healthy  controls were isolated and adhered to a flat bottom plate for 4h after  which cells were stored for RNA isolation.  qPCR primers designed for TGF-β, TGF-β receptor I and II, MMP9, SMAD7  and ITGAV were used to assess expression levels of the TGF-β pathway in  these adherent monocytes.  For priming experiments, adherent monocytes were primed for 24h with  urate and/or recombinant TGF-β1 (R&D systems) with or without a  TGF-β receptor II antibody (R&D systems), cells were washed and  restimulated with LPS for 24h.  Cytokine levels in supernatant were determined by ELISA for IL-1β, IL-6  and IL-1Ra.
Findings: mRNA expression of TGF-β and its downstream targets  were upregulated in urate treated monocytes and in gout patients  compared to healthy controls. Moreover, urate levels significantly  correlated to TGF-β in individuals with gout. Both urate and TGF-β  priming increased the release of IL-1β and IL-6 after LPS stimulation in  human monocytes.  We did not observe a synergistic effect between the two and therefore  hypothesized that urate induced inflammation is mediated via TGF-β.  Blocking the TGF-β receptor II partly reversed the urate induced  phenotype: lowered IL-1β and IL-6 production and restored levels of  IL-1Ra. Further validation experiments are ongoing.
Significance of the project: This study contributes to the  understanding of the pathways involved in urate induced inflammatory  status and might in the future provide a mechanistic explanation for the  occurrence of some comorbidities in patients with gout.  Additionally, as TGF-β is a major player in the pathogenesis of systemic  sclerosis, this study might give a rationale for treatment of  hyperuricemia in this population.
References:  1. Bardin, T. and P. Richette, Impact of comorbidities on gout and  hyperuricaemia: an update on prevalence and treatment options. BMC Med,  2017. 15(1): p. 123. 2. Crisan, T.O., et al., Soluble uric acid primes TLR-induced  proinflammatory cytokine production by human primary cells via  inhibition of IL-1Ra. Ann Rheum Dis, 2016. 75(4): p. 755-62. 3. Crisan, T.O., et al., Uric acid priming in human monocytes is driven  by the AKT-PRAS40 autophagy pathway. Proc Natl Acad Sci U S A, 2017.  114(21): p. 5485-5490.