New Oral Drug Triggers Insulin Release, Treats Diabetes
Diabetes is associated with insufficient insulin release by the beta cells of the pancreas in response to blood glucose levels. The release of insulin entails many intricate biochemical processes.
One such process involves protein structures called GLP1R present in the cells. In one such process, a hormonal molecule, called GLP1, released after the ingestion of a meal, binds to proteins, called GLP1R. This triggers the release of insulin.
Current drugs used for the treatment of diabetes, such as exenatide and liraglutide, mimic GLP1 and bind to GLP1R to trigger insulin release. However, these drugs are administered as injections, and they are costly and unstable after administration.
“We seek to find simpler drugs that are stable, cheap, and effective against both Type 1 and Type 2 diabetes,” the release quoted study author Dr. Prosenjit Mondal, Associate Professor, School of Basic Sciences, as saying.
The researchers found that PK2 was rapidly absorbed by the gastrointestinal tract, which means that it can be used as an oral medication rather than an injection.
After two hours of administration, PK2 was found distributed in the liver, kidney, and pancreas of the mice, but there were no traces of it in the heart, lungs, and spleen.
There was a small amount present in the brain, which shows that the molecule may be able to cross the blood-brain barrier. It was cleared from circulation in about 10 hours, the release said.
“Beyond increasing insulin release, PK2 was also able to prevent and even reverse beta cell loss, a cell essential for insulin production, making it effective for both Type 1 and Type 2 diabetes,” Dr. Mondal said.
To test the biological effects of PK2, the researchers administered it orally to experimental mice developing diabetes and measured glucose levels and insulin secretion. There was a six-fold increase in serum insulin levels in PK2-treated mice over the control group.