The Chemistry Department at BYU has developed a compound that can help in imaging and early detection of infections. They have effectively coupled Ceragenin (a synthetically produced molecule that is antibacterial in a broad spectrum) with 99mTc (a medical tracer) to produce a compound that is able to attack the wall membranes of a virus and at the same time identify its location. This results in a new type of technology that can enable doctors and surgeons to identify and image infected and cancer stricken parts of the body. This effective method of detection and imaging can lead to timely treatments and effective treatments.

The Chemistry Department at BYU has developed a compound based on its recently discovered Ceragenin (CSA) molecules that can help doctors and surgeons image infections in the body.

Ceragenins (cationic steroid antimicrobials or CSA’s) are small molecules that are synthetically produced which display a broad spectrum of antibacterial activity. These compounds are derived from a steroid backbone appended with amino groups, amino acids and other chemical groups. They are simple to prepare and are not affected by proteases. In vitro studies show that ceragenins are active against a wide range of viral, fungal, and bacterial targets including those resistant to current therapies. Specific ceragenins can effectively permeate the outer membranes of Gram-negative bacteria, a property of ceragenin that allows it to effectively combat any strain or mutation of a given virus. Ceragenin compounds have a net positive charge that is electro-statically attracted to the negatively charged cell membranes of certain viruses, fungi and bacteria. Ceragenins have a high binding affinity for such membranes (including lipid A) and are able to rapidly disrupt the target membranes leading to rapid cell death. While ceragenins have a mechanism of action that is also seen in antimicrobial peptides, which form part of the body's innate immune system, they avoid many of the difficulties associated with their use as medicines.

BYU’s Chemistry department has developed a simple, rapid and efficient method of labeling ceragenin with 99mTc, a medical tracer that emits safe levels of gamma rays which medical equipments can detect. This new technology uses the special antiviral property of ceragenin and the marking property of 99mTc to produce a compound that can help doctors detect and image infections leading to a timely treatment.

This technology has direct application in infection treatments. The compound may be used for early detection enabling doctors and surgeons to treat the problem while it is still in its early stages. When coupled with 99mTc, ceragenin can attach itself along the walls of an infected cell and emit safe levels of gamma rays giving the location and creating a map image of the infection.

Structure of CSA-13

Ceragenins (CSA’s) are a new class of antimicrobial agents that display broad spectrum antibacterial activity and may find use in the treatment of various infections. A member of this class CSA-13 was labeled with 99mTc using SnCh-2H20 as a reducing agent. The labeling efficiency depended on the ligand / reductant ratio, pH and volume of reaction mixture. Radiochemical purity and stability of 99mTc_CSA was determined by thin layer chromatography. Biodistribution studies of 99mTc_CSA were performed in Sprague Dawley rats, Liver and spleen uptake was quite high. A significantly higher accumulation of 99mTc_CSA was seen at sites of S.aureus infected rats.

To discuss this technology please contact:

Mike Alder
801-422-6266
malder@byu.edu

Dee Anderson
801-422-6266
dee_anderson@byu.edu