�Duke University chemists have got patented an efficient technique for synthesizing a marine algae extract in sufficient quantities to now test its ability to inhibit the development of cancerous cells piece leaving normal cells unaffected.
The researchers likewise deduced that this molecule -- called largazole -- acts on cells through the like chemical mechanics as other anti-cancer compounds on the market or in clinical trials. "It's a very exciting molecule," said Jiyong Hong, a Duke helper chemistry professor.
Hong's graduate bookman, Yongcheng Ying, described the work in a speak in Philadelphia during the 236th national meeting of the American Chemical Society. It has also been described in a report in the Journal of the American Chemical Society (JACS).
Hendrik Luesch, a born product chemist at the University of Florida wHO led the group that discovered largazole, was a corresponding author of the JACS composition along with Hong. Luesch's team low gear extracted and identified largazole from a marine teal algae gathered at Key Largo, Fla.
Guided by grounds of therapeutical benefits from extracts of a related algae, the Florida mathematical group demonstrated that largazole could impede white meat cancer cell growth better than the anti-tumor dose Taxol without causing Taxol-like side personal effects on normal breast tissue.
But Luesch's group "isolated just one mg, a very tiny measure, from natural sources that were identical difficult to grow," Hong said. "We needed to develop a concise and efficient synthetical route to make sufficiency largazole for animal studies."
Winning a race with several other groups, the Duke team devised a method to bring forth gram-sized quantities -- well-nigh 1,000 times more -- by identifying threesome key construction blocks in largazole's annulated molecular architecture.
The scientists were then able to habit commercially useable chemicals to make largazole in eight steps, netting what Hong called a "very, very efficient" 20 percent yield.
"My lab's following task was finding the origin of lagarzole's biological activity," Hong said. The molecule appeared to initiate some signal cascades that could affect inappropriately proliferating cells just not normal ones.
In the process of sleuthing this question, Hong said his group accidentally discovered that largazole was structurally like to some other molecule called FK228. FK228 is known to inhibit histone deacytelases (HDACs), enzymes regulating genetic activity that can foment cancerous electric cell growth.
The Duke team confirmed that, like FK228, largazole also suppressed HDACs. Another HDAC suppresser, marketed as Zolinza, has now been approved for the treatment of T-cell lymphoma, Hong said. Others, including FK228, are undergoing clinical trials as antitumor drugs.
Hong's group is today doing follow-up research aimed at ever-changing largazole's structure to increase its effects on cell growth. "It could be a selfsame good dose candidate for the handling of diverse cancers," he said.
The work on synthesizing largazole was supported by the National Oceanographic and Atmospheric Administration's Sea Grant Program, the University of Florida College of Pharmacy and Duke University.
Source: Monte Basgall
Duke University
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Monday 8 September 2008
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