Enhanced fatty acid oxidation through metformin and baicalin as therapy for COVID-19 and associated inflammatory states in lung and kidney

Redox Biol. 2023 Dec:68:102957. doi: 10.1016/j.redox.2023.102957. Epub 2023 Nov 3.

Abstract

Progressive respiratory failure is the primary cause of death in the coronavirus disease 2019 (COVID-19) pandemic. It is the final outcome of the acute respiratory distress syndrome (ARDS), characterized by an initial exacerbated inflammatory response, metabolic derangement and ultimate tissue scarring. A positive balance of cellular energy may result crucial for the recovery of clinical COVID-19. Hence, we asked if two key pathways involved in cellular energy generation, AMP-activated protein kinase (AMPK)/acetyl-CoA carboxylase (ACC) signaling and fatty acid oxidation (FAO) could be beneficial. We tested the drugs metformin (AMPK activator) and baicalin (CPT1A activator) in different experimental models mimicking COVID-19 associated inflammation in lung and kidney. We also studied two different cohorts of COVID-19 patients that had been previously treated with metformin. These drugs ameliorated lung damage in an ARDS animal model, while activation of AMPK/ACC signaling increased mitochondrial function and decreased TGF-β-induced fibrosis, apoptosis and inflammation markers in lung epithelial cells. Similar results were observed with two indole derivatives, IND6 and IND8 with AMPK activating capacity. Consistently, a reduced time of hospitalization and need of intensive care was observed in COVID-19 patients previously exposed to metformin. Baicalin also mitigated the activation of pro-inflammatory bone marrow-derived macrophages (BMDMs) and reduced kidney fibrosis in two animal models of kidney injury, another key target of COVID-19. In human epithelial lung and kidney cells, both drugs improved mitochondrial function and prevented TGF-β-induced renal epithelial cell dedifferentiation. Our results support that favoring cellular energy production through enhanced FAO may prove useful in the prevention of COVID-19-induced lung and renal damage.

Keywords: COVID-19; Fibrosis; Inflammation; Metabolism; Mitochondria.

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Animals
  • COVID-19*
  • Fatty Acids
  • Fibrosis
  • Humans
  • Inflammation / drug therapy
  • Kidney / metabolism
  • Lung / metabolism
  • Metformin* / pharmacology
  • Metformin* / therapeutic use
  • Respiratory Distress Syndrome*
  • Transforming Growth Factor beta

Substances

  • Metformin
  • AMP-Activated Protein Kinases
  • baicalin
  • Transforming Growth Factor beta
  • Fatty Acids