First technique to produce effective anti-leukaemia agent developed

Washington, Apr 18: More than a decade after discovering kapakahines- marine-derived natural products with anti-leukaemia potential-scientists have found the first technique to synthesise them in laboratory in large quantities, by using only acetylene gas, a handful of amino acids, and a dozen inventive steps.

Kapakahines were isolated from a South Pacific sponge in trace quantities, but its lack of availability stalled any future studies.

But, thanks to the efforts of researchers at Scripps Research Institute that unlimited production of kapakahine is now possible.

Thus, research on the compound can proceed and may eventually lead to new drug treatments.

Cripbrochalina olemda, a common tube-type sponge like organism, produces a compound called kapakahine B, among other molecules of interest, which has shown potential for fighting leukaemia.

The researchers have said that kapakahine B, which has an unusual structure, uses some never-before-seen mechanism to fight cancer cells.

For a long time, researchers around the world have unsuccessfully tried to devise a method for synthesizing the kapakahines.

Scripps researchers, led by Phil Baran, started on with more basic research, in which they successfully synthesized a simpler related compound, psychotrimine, with no known pharmaceutical potential.

Inspired by this, the researchers created a highly reactive and selective chemical component referred to as a quaternary centre that, because of structural similarities, also drives the essential first step in the kapakahines synthesis.

Later, they set out on a somewhat riskier venture to develop a second stage needed to synthesize kapakahines.

Then, the researchers predicted that using the quaternary centre, they could produce two intermediate isomers, or molecules with the same chemical formula but different structures.

One of the isomers was predicted to be an ideal stepping stone toward the kapakahines, but more difficult to make.

They predicted that the second isomer would be much more reactive, and in theory its concentration would grow sufficiently as it moved toward equilibrium with the first isomer.

And finally, they synthesized two kapakahines for the first time and in gram quantities.

One of the compounds, kapakahine B, has shown potential in fighting leukaemia cells, which could further help in developing potential drug treatment.

The research has been published online by the Journal of the American Chemical Society.

Copyright Asian News International/