Thanks to UC Riverside research, cancer and diabetes patients may now control their illnesses with tablets rather than needles and injections.
Some medications for these conditions dissolve in water, making it impossible to carry them through the intestines, which receive everything we drink and eat. As a result, some medications cannot be used orally. UCR scientists, on the other hand, have developed a chemical “tag” that can be attached to these medications, allowing them to enter blood circulation via the intestines. The specifics of how they discovered the tag, as well as demonstrations of its usefulness, are disclosed in a recent publication published in the Journal of the American Chemical Society.
The tag is made up of a small peptide, which is similar to a protein fragment. “Because they are relatively small molecules, you can chemically attach them to drugs, or other molecules of interest, and use them to deliver those drugs orally,” said Min Xue, UCR chemistry professor who led the research.
When the researchers saw these peptides finding their way into cells, they were doing a separate experiment in Xue’s laboratory.
“We did not expect to find this peptide making its way into cells. It took us by surprise,” Xue said. “We always wanted to find this kind of chemical tag, and it finally happened serendipitously.”
This finding surprised Xue since the researchers previously assumed that this form of delivery tag required to contain positive charges in order to be received by negatively charged cells. Their study with this neutral peptide tag, known as EPP6, demonstrates that this view was incorrect.
The Xue group collaborated with Kai Chen’s group at the University of Southern California’s Keck School of Medicine to test the peptide’s capacity to pass through the body by feeding it to mice. The scientists watched the peptide collecting in the intestines and documenting its final transport into the animals’ organs via the blood using a PET scan, a method analogous to a whole-body X-ray that is accessible at USC.
After successfully navigating the circulatory systems via oral delivery, the team aims to demonstrate that the tag can do the same when connected to a variety of medications. “Quite compelling preliminary results make us think we can push this further,” Xue said.
Many medications, including insulin, must be administered through injection. The researchers expect that their next series of studies will change that, allowing them to attach this tag to a wide range of medications and chemicals, altering how those molecules flow through the body. “This discovery could lift a burden on people who are already burdened with illness,” Xue said.
