Related Experiment Video
Updated: Jul 20, 2025
Cardiac Spheroids as in vitro Bioengineered Heart Tissues to Study Human Heart Pathophysiology
Published on: January 23, 2021
Sex-specific cytotoxicity of ostarine in cardiomyocytes
Natalia Leciejewska1, Ewa Pruszyńska-Oszmałek1, Leszek Nogowski1
1Department of Animal Physiology, Biochemistry and Biostructure, Poznan University of Life Sciences, 60-637, Poznan, Poland.
Abstract:
Ostarine is the most popular compound in the selective androgen receptor modulator group (SARMs). Ostarine is used as a physical performance-enhancing agent. The abuse of this agent in higher doses may lead to severe side effects. Here, we evaluate the effects of ostarine on the heart. We utilized a cardiomyocyte H9C2 cell line, isolated primary female and male cardiac fibroblast cells, as well as hearts obtained from rats. Ostarine increased the accumulation of two fibrosis protein markers, αSMA and fibronectin (p < 00.1) in male, but not in female fibroblast cells. Ostarine increased the expression of the cardiomyopathy marker βMhc in the H9C2 cell line (p < 0.05) and in the heart in rats (p < 0.01). The unfavorable changes were observed at high ostarine doses. Moreover, a decrease in viability and an increase in cytotoxicity marker LDH were observed already at lowest dose (1 nmoL/l). Taken together, our results suggest that ostarine is cardiotoxic which may be more relevant in males than in females.
Insights
This study reveals that Ostarine, a popular selective androgen receptor modulator (SARM), can be cardiotoxic. Unfavorable cardiac changes and reduced cell viability were observed, particularly in male subjects.
Area of Science:
- Pharmacology
- Cardiovascular Research
- Toxicology
Background:
- Selective androgen receptor modulators (SARMs) like Ostarine are widely used for physical enhancement.
- High-dose SARM use is associated with potential severe adverse effects.
- The cardiac impact of Ostarine requires thorough investigation.
Purpose of the Study:
- To investigate the cardiotoxic effects of Ostarine.
- To evaluate Ostarine's impact on cardiac cells and tissues.
- To determine potential sex-based differences in Ostarine's cardiac toxicity.
Main Methods:
- Utilized H9C2 cardiomyocyte cell line.
- Isolated primary male and female cardiac fibroblast cells.
- Examined rat hearts and cardiac cells exposed to Ostarine.
Main Results:
- Ostarine increased fibrosis markers (αSMA, fibronectin) in male but not female fibroblasts.
- Ostarine elevated the cardiomyopathy marker βMhc in H9C2 cells and rat hearts.
- Reduced cell viability and increased cytotoxicity (LDH) were noted even at low Ostarine doses.
Conclusions:
- Ostarine demonstrates cardiotoxicity.
- Observed cardiac effects suggest potential sex-specific differences, with males being more susceptible.
- Ostarine's use, especially at high doses, poses risks to cardiovascular health.
