Anti-cancer compound once only found in a shrub can now be synthesized in lab (10/4/2007)

The search for anti-cancer compounds in plants often hits a brick wall when only small amounts of the substance can be extracted. Researchers from the University of Melbourne have now developed a technique which can synthesize relatively large amounts of a potent compound, previously only found in a shrub.

The drug has potential for treatment of colon cancer as it shows activity against several human cancer cells lines and has been shown to shrink tumours in tests.

Researchers at the University of Melbourne and collaborators at the Victorian College of Pharmacy and a Melbourne company (formally Cerylid Biosciences) have achieved the chemical synthesis of two potent, but rare naturally occurring molecules named episilvestrol and silvestrol.

These compounds were originally isolated in small quantities from several species of Aglaia which is a small woody shrub that grows in Malaysia and other parts of S.E. Asia.

"We are excited by the prospect that we can produce these complex and potent compounds in the laboratory" said Associate Professor Rizzacasa from the University of Melbourne's Bio21 Institute.

The compounds show potent activity against several human cancer cells lines and have been shown to shrink tumour cells in mice. However, only small amounts of these molecules can be isolated from Nature so chemical synthesis is an option as a source of these compounds for further testing towards a cancer treatment.

"What is even more exciting is that active analogues of these compounds can be made from less expensive starting materials" added Associate Professor Mark A. Rizzacasa

The group used simple starting materials (a simple sugar and a flavone) to synthesize the anti-cancer compounds. In addition, a simplified analogue has also been synthesized which shows potent activity against human colon cancer when assayed by Professor Tony Burgess and his team at the Ludwig Cancer Institute.

The next step will be further testing in vivo. "We are now working to further optimize the synthesis to make it higher yielding and cheaper" states Associate Professor Mark A. Rizzacasa

The paper describing this work has appeared online as an Early View article in the prestigious chemistry journal Angewandte Chemie see: dx.doi.org/10.1002/anie.200702700.

Note: This story has been adapted from a news release issued by the University of Melbourne

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