a drug to treat cancer and diabetes can protect against heart disease and
drug has been found to melt away the fat in the arteries
study found that the drug also reverses the signs of atherosclerosis
A drug to treat breast cancer and
diabetes has been found to melt away the fat inside arteries that can cause
heart attack and stroke. A single dose of the drug Trodusquemine can reverse
the effects of atherosclerosis. The findings of the study raise the prospect of
new preventative medicines for heart attacks and strokes.
Trodusquemine can Reverse the Effects of Atherosclerosis
A research team from the
University of Aberdeen tested the effect of the drug Trodusquemine on mice with
set-in atherosclerosis. For the study, mice were treated with a single dose of
Trodusquemine after eight weeks of high-fat diet. After six weeks of treatment,
mice treated with Trodusquemine had 20% reduction in body weight with greater
than 50% reduction in fat mass compared to the control group.
The team found that the drug not
only reduced fatty plaques inside the arteries, a single dose had the same
effect as regular doses administered over time.
Trodusquemine works by
blocking an enzyme called protein-tyrosine phosphatase 1B (PTP1B) which is
increased in people with obesity and diabetes.
PTP1B is also increased in
other conditions that involve prolonged inflammation such as sepsis, inflamed
diabetic foot ulcers, and allergic lung inflammation.
The research team also found that
the drug activates a protective enzyme called AMPK ((acetyl-CoA carboxylase)
kinase), which mimics exercise and actively reduces chronic inflammation.
The findings of the study suggest
that the drug can significantly reduce deaths due to heart disease, which is
the number one cause of death globally, claiming lives of 17.7 million people
Professor Mirela Delibegovic from
the University of Aberdeen's Institute of Medical Sciences, who led the study,
said, "Trodusquemine has already been trialed for treatment of diabetes and
breast cancer, but this is the first time it has been used in models of atherosclerosis."
"These have only been tested
at pre-clinical level, in mice, so far but the results were quite impressive
and showed that just a single dose of this drug seemed to completely reverse
the effects of atherosclerosis. The next step is to test the ability of this
drug to improve outcomes in human patients with developed atherosclerosis and
Inflammation plays a crucial role
in atherosclerosis by thinning the connective tissue in plaques and causing
them to rupture. Stopping the build-up of cholesterol plaques in the arteries
can prevent heart attack and stroke. Professor Jeremy Pearson, Associate
Medical Director at the British Heart Foundation, said, "This study shows
Trodusquemine can also limit the build-up of fatty atherosclerotic plaques in
mice. If we see the same effect in patients, the drug may prove even more
useful than currently hoped for."
The research was published in the
journal Clinical Science
is the accumulation of cholesterol
plaques that harden over time and narrow the arteries, leading to heart
attacks, stroke, and peripheral vascular disease. The accumulation of plaque
begins when an artery's inner lining called the endothelium becomes damaged.
The causes of atherosclerosis are elevated levels of triglycerides, high blood
pressure, smoking, high consumption of alcohol, physical inactivity, unhealthy
diet, obesity, and diabetes. Lifestyle change is the main treatment for
Tips to Prevent or Delay Atherosclerosis
Eating - A heart-healthy diet is low in sodium, added sugar and fats. Include whole
grains, fruits and vegetables, seafood, lean meat, fat-free dairy
- Aerobic exercise helps reduce fat mass. Regular exercise helps improve
fitness level and health. Exercising for at least 150 minutes per week can
improve overall cardiovascular health.
Smoking- Smoking can tighten blood vessels and increase the risk of
atherosclerosis. Quitting smoking helps reduce the risk of
- Dawn Thompson, Nicola Morrice, Louise Grant, Samantha Le Sommer, Emma K. Lees, Nimesh Mody, Heather M. Wilson, Mirela Delibegovic. Pharmacological Inhibition of Protein Tyrosine Phosphatase 1B Protects Against Atherosclerotic Plaque Formation in the LDLR Mouse Model of Atherosclerosis. Clinical Science, (2017), 131 (20) 2489-2501; DOI: 10.1042/CS20171066
- How Can Atherosclerosis Be Prevented or Delayed? - (https:www.nhlbi.nih.gov/health/health-topics/topics/atherosclerosis/prevention)