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Centre Researchers Fight Hypertension
Posted on 13/10/2008SARTANS (selective AT1 receptor antagonists) act to reduce hypertension by controlling the ability of the peptide, Angiotensin II, from binding to its biological receptor.
Several sartans, including eprosartan, losartan and candesartan are already on the market. Interaction with the AT1 receptor can also result in the release of reactive oxygen species that include free radicals, and these reactive molecules can result in inflammation that has further hypertensive consequences. A new class of sartan incorporating selenium has been developed by Centre researchers. Not only have these new molecules proven to be effective at blocking the AT1 receptor, they have the potential to quench free radicals generated during hypertension through recognition that selenium not only has a significant affinity toward free radicals, but selenium-containing molecules also have beneficial properties that are able to reduce other reactive oxygen species and can lead to reduced inflammation.
“We are particularly excited that our selenium-containing sartans are potent AT1 receptor antagonists in in vitro testing”, says Professor Carl Schiesser, the project leader. ”Time will tell whether or not they are equally effective in vivo and more research still needs to be done”.
“These compounds may have significant future impact in the way blood pressure is regulated”, remarked Professor James Angus, Centre Chief Investigator and team member.
The research team is currently synthesising compounds that are even more effective against free radicals, while maintaining sartan activity. “These compounds will provide interesting new lead compounds for structure-activity studies that may result in clinical trials in the not too distant future”, says Dr James Ziogas, Centre Associate Investigator and expert in the pharmacology of hypertension.
The Centre Team are somewhat circumspect in revealing further details. “We need to be particularly prudent in regard to the valuable intellectual property associated with this research, which will be protected through patenting once further key data become available”, says Schiesser, who as Centre Director is responsible for Centre IP, “stay tuned”!