Inflammation intervention

Botanisol wins NIH grant for anti-inflammatory compound that could bypass side effects of NSAIDs

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SCOTTSDALE, Ariz.—The global anti-inflammatory drug market currently exceeds $60 billion, with non-steroidal anti-inflammatory drugs (NSAIDs)—among them ibuprofen, naproxen and celecoxib—standing as one of the most common treatments for moderate to acute inflammatory pain. In fact, NSAIDs account for some $12 billion in sales globally each year, but their usefulness comes with a cost—NSAID usage has been linked to bleeding ulcers, kidney problems, stroke and heart attacks in a number of studies and reports, with recent data highlighting greatly increased risk for cardiovascular complications for individuals over the age of 65. As a result, NSAID usage leads to 100,000 hospitalizations, 17,000 deaths and roughly $2 billion in healthcare costs each year in the United States alone.
Despite those side effects, NSAIDs remain a standard of care for their effectiveness, but Arizona-based Botanisol recently received a grant for the development of a potential new option—TAI-LCx—for treating inflammation without the health risks of NSAIDs. The company was informed on August 9 that it would receive a competitive grant award from the National Institutes of Health (NIH) and National Center for Complementary and Integrative Medicine (NCCIM). According to Botanisol CEO P. Scott Waterhouse, the grant is worth just under $225,000 and is the full amount they requested. Government funding issues being what they are, he says they were “a bit surprised by that, but obviously overjoyed.” The funding will support three parts of TAI-LCx’s development.
The cause for NSAIDs’ dangerous side effects is their very method of action. As noted by the American College of Rheumatology on the organization’s website, NSAIDs work by blocking enzymes that produce prostaglandins, “a group of naturally occurring fatty acids that play a role in pain and inflammation. Older NSAIDs like ibuprofen block two of these enzymes, COX-1 and COX-2.”
Waterhouse explains that “It’s the mediation of the COX2 enzyme, cyclooxygenase 2 enzyme, that causes the cardiovascular side effects of the NSAIDs,” while COX1 “is the enzyme that protects the stomach lining and kidneys, and as a result, the NSAIDs that mediate COX1 are the ones that have the gastrointestinal side effects and cause the kidney problems and the adverse effects of NSAIDs.”
Botanisol’s new compound, however, could offer a way to avoid the issue of COX inhibition. The compound in question is called TAI-LCx, short for turmeric anti-inflammatory lipophilic compound. TAI-LCx, says Waterhouse, is an extraction from the turmeric root, but from the essential oils of the root, not from the more popular curcamin. The compound was originally discovered at the University of Arizona via a multiyear NIH-supported research program, and Botanisol is the exclusive licensee of the patented technologies.
The most promising feature of TAI-LCx is its method of action; rather than impacting COX1 or COX2, Waterhouse says the compound directly affects TNFα (tumor necrosis factor alpha), PEG2 and one or two of the interleukins. In rat models of rheumatoid arthritis, he says TAI-LCx “was shown to be as effective or more effective than indomethacin, but with a much better safety profile than indomethacin, so there’s a lot of early information that is really quite positive with the initial compound TAI-LCx.” With this recent NIH/NCCIM grant, Botanisol will be able to further explore the nature and method of action of TAI-LCx.
“The original discovery was based upon three different methods of extraction at laboratory-scale. Each of these three have some shortcomings, not to mention that they’re difficult ones to scale up for manufacturing,” Waterhouse tells DDNews. “So the first piece of our next stage that we now have funded is a commercially scalable extraction process to separate the very specific compound in very high quality and very high purity. Part two is additional studies of the structure of the compound. We’re looking for the exact chemical structure and molecular weight, etc., of the compound, along with researching the existing compound to look for variants that will have different and more specific anti-inflammatory activity, either on the inflammatory processes in the body or even specific tissues.
“Then the third piece of this is additional studies of the biologic activity so that we can expand our knowledge. The original research only researched, I think, five or six of the inflammatory pathways, and we’re going to expand that to a whole suite of inflammatory pathways and hopefully have a very thorough map of exactly how the compound is working.”
Dr. David Gang, chief science officer of Botanisol, will direct the new research at rented laboratories at Washington State University. Gang commented in a press release that, “What we know about TAI-LCx is very encouraging. Through the grant, we will learn a great deal more about its structure and effect on other inflammatory pathways. The expertise, support and facilities at WSU, especially the TIPL lab, are ideal for us.”
Botanisol is a translational biopharmaceuticals company focused on applying modern science to known bioactive constituents of plants with the goal of getting safer, more affordable drugs and healthcare products into the pipelines of pharmaceutical and healthcare companies.
“What we have found is there’s really a very large inventory of plant sources in research that have determined the biologic activity of different constituents of plants, but these have never been researched using modern science and new techniques to discover, find and develop their drug properties … There are reports that even the existing modern Western medicines have as much as 25 percent plant material in them to begin with. We’re just kind of stepping back in time and saying it’s now time to find out what Mother Nature knew about medicines and use that knowledge to develop better medicines that are probably safer and more affordable,” Waterhouse remarks.

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