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Abstract: PO0367

Cilastatin Inhibits Renal Myoglobin Endocytosis and AKI Following Rhabdomyolysis

Session Information

Category: Acute Kidney Injury

  • 103 AKI: Mechanisms

Authors

  • Hebert, Jessica Faith, Oregon Health & Science University, Portland, Oregon, United States
  • Burfeind, Kevin G., Oregon Health & Science University, Portland, Oregon, United States
  • Nickerson, Megan N., Oregon Health & Science University, Portland, Oregon, United States
  • Funahashi, Yoshio, Oregon Health & Science University, Portland, Oregon, United States
  • Eiwaz, Mahaba B., Oregon Health & Science University, Portland, Oregon, United States
  • Groat, Tahnee, Oregon Health & Science University, Portland, Oregon, United States
  • Hutchens, Michael, Oregon Health & Science University, Portland, Oregon, United States
Background

Muscle-derived myoglobin, a renal toxin, causes rhabdomyolysis-induced acute kidney injury (AKI) via megalin-mediated endocytosis into proximal tubule cells (PTs). Endocytosis kinetics and inhibition are poorly understood. We characterized myoglobin uptake in vivo, hypothesizing cilastatin, a putative megalin inhibitor, would prevent endocytosis akin to megalin knockouts.

Methods

Procedures in wild-type (WT) male C57BL/6 mice and inducible, PT-specific megalin-deleted mice (iMegKO) were approved by OHSU or PVAMC IACUC. FITC-myoglobin (FMb) and cilastatin (200 mg/kg) were injected retroorbitally. Experimental rhabdomyolysis (ER) was induced via intramuscular injection of 50% glycerol (8 mL/kg). Glomerular filtration rate (GFR) was measured 24h later, and immunofluorescence and single-cell RNASeq were performed on renal tissue.

Results

FMb was observed in PTs 15 min post-injection in control mice; in iMegKO mice, FMb puncta were nearly absent (p<0.0001). FMb puncta were reduced in cilastatin-treated WTs without ER vs vehicle controls (p=0.0012). iMegKO prevented AKI following ER, with 24h GFR 5x control (p<0.001). Cilastatin injection did not affect GFR in iMegKO (p=0.89), but had a significant effect on ER-induced AKI in wild-type mice: GFR was 8x vehicle (p=0.03) while PT uptake of endogenous myoglobin decreased (p<0.05). A composite score of endocytosis related genes (endoscore) showed significant alterations (Figure 1).

Conclusion

Megalin interference prevents ER-induced AKI by reducing myoglobin endocytosis; cilastatin recapitulates the effect in a megalin-inhibitory fashion. Alteration of endocytosis-related genes confirms this process is critical in rhabdomyolysis, and may suggest additional therapeutic targets. Future studies will also include cilastatin delivery timing, dosage, and formulation.

Funding

  • NIDDK Support