Scientists in Spain have found a new molecule, called EPB-53 could help fight Type 2 diabetes and the non-alcoholic fatty liver disease.
According to the new pre-clinical study, levels of FGF21 in the liver and plasma can increase through oral administration of the EPB-53 molecule.
“This effect is possible because EPB-53 is a molecule that activates HRI, a kinase that can boost a factor of transcription involved in the increase of FGF21, which reduces glucose tolerance and hepatic steatosis in mice which are fed with a fat-rich diet,” explains Manuel Vázquez-Carrera, who led the study from the Faculty of Pharmacy and Food Sciences and the Institute of Biomedicine of the University of Barcelona.
The FGF21 hormone -or the fibroblast growth factor 21- is an endocrine factor with a determining role in the energetic metabolism as an anti-diabetes an anti-obesity agent.
This hormone, which mainly synthetizes the liver, is regarded as a potential therapeutic target to treat Type 2 diabetes and the non-alcoholic fatty liver disease, which usually occur due to obesity and insulin resistance.
However, the FGF21 analog compounds that showed pharmaceutical activity in animal models require subcutaneous injection, and can generate adverse effects, including the loss of bone mass, increase of heart rate and arterial pressure, etc.
The conclusions of the study prove the use of FGF21 inducer compounds could lead to new therapeutic strategies to treat Type 2 diabetes and the non-alcoholic fatty liver disease, similarly to what analog compounds do subcutaneously.
“In addition, we hope to see in future studies that these would not cause adverse effects that have been described in some FGF21 analogs,” notes Vázquez-Carrera. “Therefore, we are working on the development of new HRI activators with better pharmacokinetic characteristics for the treatment of Type 2 diabetes such as non-alcoholic steatohepatitis.”
From left to right, the experts Emma Barroso, Marta Montori, David Aguilar, Xavier Palomer, Lucia Peña, Gaia Botteri, Manuel Vázquez-Carrera, Mohammad Zarei and Javier Pizarro (UB/IBUB/CIBERDEM). Credit: University of Barcelona.
The incidence of Type 2 diabetes has grown among the population over the last years and the available drugs cannot control the progress of the disease in all patients.
Also, the non-alcoholic fatty liver disease affects one out of four people and the worst cases -non-alcoholic steatohepatitis- do not have any specific approved drug.
Finding new drugs for oral administration is, thus, one of the challenges in biomedicine to improve health care for millions of people worldwide, who are affected by these metabolic diseases.
The research was published in the British Journal of Pharmacology.
University of Barcelona.
- A new molecule to fight type 2 diabetes and non-alcoholic fatty liver disease. (2019, April 10). EurekAlert! Retrieved: https://www.eurekalert.org/pub_releases/2019-04/uob-anm041019.php