Bociaga-Jasik 2013 Pharmacol Rep

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Bociąga-Jasik M, Polus A, Góralska J, Czech U, Gruca A, Sliwa A, Garlicki A, Mach T, Dembińska-Kieć A (2013) Metabolic effects of the HIV protease inhibitor – saquinavir in differentiating human preadipocytes. Pharmacol Rep 65:937-50.

» PMID: 24145088 Open Access

Bociaga-Jasik M, Polus A, Goralska J, Czech U, Gruca A, Sliwa A, Garlicki A, Mach T, Dembinska-Kiec A (2013) Pharmacol Rep

Abstract: Background: The iatrogenic, HIV-related lipodystrophy is associated with development of the significant metabolic and cardiovascular complications. The underlying mechanisms of antiretroviral (ARV) drugs are not completely explored.

Methods: The aim of the study was to characterize effects of the protease inhibitor (PI) - saquinavir (SQV) on metabolic functions, and gene expression during differentiation in cells (Chub-S7) culture. Results: SQV in concentrations observed during antiretroviral therapy (ART) significantly decreased mitochondrial membrane potential (MMP), oxygen consumption and ATP generation. The effects were greater in already differentiated cells. This was accompanied by characteristic changes in the expression of the genes involved in endoplasmic reticulum (ER) stress, and differentiation (lipid droplet formation) process such as: WNT10a, C/EBPa, AFT4, CIDEC, ADIPOQ, LPIN1.

Conclusions: The results indicate that SQV affects not only metabolic (mitochondrial) activity of adipocytes, but affects the expression of genes related to differentiation and to a lesser extent to cell apoptosis.

Keywords: HIV-associated lipodystrophy, Protease inhibitors, Adipocyte, Oxidative stress, Mitochondrial toxicity, Apoptosis, Gene Expression

O2k-Network Lab: PL Krakow Dembinska-Kiec A

Labels: MiParea: Respiration, mt-Medicine, Pharmacology;toxicology 

Organism: Human  Tissue;cell: Fat, Other cell lines  Preparation: Intact cells 

Coupling state: ROUTINE 

HRR: Oxygraph-2k