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Cheaper and most effective anti-malaria drug yet coming soon

Washington, Wed, 18 Jan 2012 ANI

Washington, Jan 18 (ANI): The most effective anti-malaria drug will soon be available in plenty and at an affordable price to provide medication for more than 225 million malaria patients worldwide, especially in the developing world.


Researchers have developed a very simple process for the synthesis of the best anti-malaria drug, artemisinin, more economically and in sufficient volumes.


Peter H. Seeberger, Director at the Max Planck Institute of Colloids and Interfaces in Potsdam and Professor of Chemistry at the Freie Universitat Berlin and his colleague Francois Levesque have discovered a very simple way of synthesising the artemisinin molecule, which is known as an anti-malaria drug from traditional Chinese medicine and has an extremely complex chemical structure.


"The production of the drug is therefore no longer dependent on obtaining the active ingredient from plants," said Seeberger.


As a starting point, the chemists use artemisinic acid - a substance produced as a hitherto unused by-product from the isolation of artemisinin from sweet wormwood, which is produced in volumes ten times greater than the active ingredient itself.


Moreover, artemisinic acid can easily be produced in genetically modified yeast as it has a much simpler structure.


"We convert the artemisinic acid into artemisinin in a single step," stated Seeberger.


"And we have developed a simple apparatus for this process, which enables the production of large volumes of the substance under very controlled conditions," he noted.


The effect of the molecule, which not only targets malaria but possibly also other infections and even breast cancer, is due to, among other things, a very reactive chemical group formed by two neighbouring oxygen atoms - which chemists refer to as an endoperoxide.


Seeberger and Levesque use photochemistry to incorporate this structural element into the artemisinic acid. Ultraviolet light converts oxygen into a form that can react with molecules to form peroxides.


"Photochemistry is a simple and cost-effective method. However, the pharmaceutical industry has not used it to date because it was so difficult to control and implement on a large scale," explained Peter Seeberger.


In the large reaction vessels with which industrial manufacturers work, flashes of light do not penetrate deeply enough from outside and the reactive form of oxygen is not produced in sufficient volumes.


The Potsdam-based scientists have succeeded in resolving this problem using an ingenious trick: They channel the reaction mixture containing all of the required ingredients through a thin tube that they have wrapped around a UV lamp.


In this structure, the light penetrates the entire reaction medium and triggers the chemical conversion process with optimum efficiency.


"The fact that we do not carry out the synthesis as a one-pot reaction in a single vessel, but in a continuous-flow reactor enables us to define the reaction conditions down to the last detail," said Seeberger.


After just four and a half minutes a solution flows out of the tube, in which 40 percent of the artemisinic acid has become artemisinin.


"We assume that 800 of our simple photoreactors would suffice to cover the global requirement for artemisinin," added Seeberger.


Seeberger estimates that the innovative synthesis process could be ready for technical use in a matter of six months. (ANI)


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