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October 4, 2012

鶹ý professors awarded new U.S. patent for cancer research

The United States Patent & Trademark Office awarded professors from the University of Louisiana at Monroe’s College of Pharmacy another patent for potentially life-saving anticancer research—(US 8,268,786 B2).

This is the fourth patent awarded to the college.

Dr. Khalid El Sayed, associate professor of pharmacy, and Dr. Paul W. Sylvester, Pfizer endowed professor of pharmacology and director of graduate studies and research at 鶹ý, have been awarded the patent for their cancer research.

Dr. Amal Khalil Kaddoumi, assistant professor in pharmacy, and Dr. Sami Nazzal, associate professor of pharmacy, also collaborated on the research.

The patent is titled “Anti-cancer tocotrienol analogues and associated methods.”

Tocotrienol is a rare, but natural form of Vitamin E. This patent stems from research collaboration between 鶹ý College of Pharmacy faculty and First Tech International Limited in Wanchai, Hong Kong.

Sylvester said the compounds and methods in the patent have the potential to save and/or prolong lives through anticancer treatments.

The compounds and methods described in the patent are useful as potent anti-oxidants, and for the development of additional anticancer compounds and anticancer treatments in animals and humans.

El Sayed is well aware of the impact of this newest accomplishment.

“The patent is the first reward for several years of collaborative research activity,” said El Sayed. “The palm oil research group led by Dr. Sylvester is a perfect example of integrating unique strengths and diverse, distinguished expertise in the 鶹ý College of Pharmacy.” 

The prospective uses of these newly discovered anticancer agents are significant within the field of cancer research.

“The patent is for new and potent anticancer agents that were developed by creating carbamate ester analogues of natural tocotrienols—a natural, but rare form of vitamin E,” said Sylvester.

“Specifically, these compounds show significant potential for use in the treatment of breast cancer.”

According to Sylvester, the anticancer activity of tocotrienols is well established, but this activity is reduced in the body due to poor absorption by the intestine and rapid metabolism in the body. 

“The newly awarded patent discloses the invention of novel tocotrienol derivatives with anti-cancer effects, methods of making such compounds, and methods of cancer treatment and prevention involving those compounds that are useful in the fields of cancer treatment, prevention, and research,” continued Sylvester.

Because of this, studies were conducted to develop derivatives by making subtle changes in the natural molecular structure of the vitamin E compounds, resulting in novel tocotrienol-carbamate derivatives that display increased chemical and metabolic stability, increased water solubility, and increased anticancer potency. 

El Sayed said the team is acting as an effective small company. Sylvester discovered the potent activity of the original natural products and understood their mechanism of action, and Dr. Kaddoumi discovered the mechanism of the compound's absorption in the intestine.

“Our group—as a medicinal chemistry unit—then used this knowledge to design simple derivatives with improved pharmaceutical and biological properties,” said El Sayed

“Dr. Nazzal then formulated these new drugs in the most appropriate pharmaceutical form, to guarantee the best results.”

“I am delighted to be part of this team and greatly appreciate this opportunity,” continued El Sayed.

“I believe consecutive successes achieved by the 鶹ý College of Pharmacy and Basic Pharmaceutical Sciences faculty evidently entitle them to become Louisiana's top drug discovery center.”

The College of Pharmacy—the only state-supported pharmacy program in Louisiana—continues to make advancements in cancer research through an effort to combine the expertise of various faculty, creating greater results.

“Dr. Sylvester's continuing development of tocotrienols as anticancer agents has now been enhanced by his collaboration with Dr. El Sayed,” said Dr. Benny Blaylock, dean of the 鶹ý College of Pharmacy.

“The molecular modifications made to the natural compounds by Dr. El Sayed and his research group make the modified compounds even more active as a potential breast cancer treatment.

"These kinds of collaborations within the College of Pharmacy are producing outstanding results that are being recognized internationally by scientific groups and by the industry. The College of Pharmacy and 鶹ý is very proud to have these and other dedicated scientists and researchers as faculty members and colleagues.”

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