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Chemists Synthesize Promising Anti-cancer Marine Algae Extract

by Rajashri on August 23, 2008 at 3:26 PM
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 Chemists Synthesize Promising Anti-cancer Marine Algae Extract

A way to synthesize a marine algae extract called largazole in sufficient quantities has been devised by Duke University chemists. This will help them to study its efficacy in inhibiting the progression of cancer cells without affecting the normal ones.

The research team has also discovered that this molecule acts on cells through the same chemical mechanism as other anti-cancer compounds.

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"It's a very exciting molecule," said Jiyong Hong, a Duke assistant chemistry professor.

Earlier, a team led by University of Florida researcher Hendrik Luesch, who discovered Largazole, had shown that it could impede breast cancer cell growth better than the anti-tumour drug Taxol without causing Taxol-like side effects on normal breast tissue.
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Highlighting the fact that Luesch's group had isolated just one milligram of the molecule from natural sources that were very difficult to grow, Hong insisted: "We needed to develop a concise and efficient synthetic route to make enough largazole for animal studies."

The researcher revealed that his team had devised an efficient technique to produce gram-sized quantities by identifying three key building blocks in largazole's ring-shaped molecular architecture.

A research article describing the patented technique, published in the Journal of the American Chemical Society, said that the scientists uses commercially available chemicals to make largazole in eight steps, netting what Hong called a "very, very efficient" 20 per cent yield.

"My lab's next task was finding the origin of lagarzole's biological activity," Hong said.

The molecule appeared to initiate some signalling cascades that could affect inappropriately proliferating cells but not normal ones, he added.

Hong revealed that his group accidentally discovered that largazole was structurally similar to another molecule called FK228 that inhibits histone deacytelases (HDACs), enzymes regulating genetic activity that can foment cancerous cell growth.

The team confirmed that, like FK228, largazole also suppressed HDACs.

Hong and his colleagues are currently carrying out follow-up research aimed at changing largazole's structure to increase its effects on cell growth.

"It could be a very good drug candidate for the treatment of various cancers," he said.

Source: ANI
RAS/M
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