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Palacký University
08-05-2015, 12:44, Age: 8 y.

U.S. Patent Confirms Significance of Anti-Cancer Substances

By: Martina Šaradínová

The United States patent for new substances with anticancer effects. Reproduction: Žurnál

After Olomoucine, Roskovitine, and Topoline, scientists from the Centre of the Haná Region for Biotechnical Agricultural Research (CRH) have discovered another group of substances derived from cytokinins, plant hormones with a distinct antitumour effect. The significance of their discovery has been confirmed by a recently granted United States patent, which is an important step for commencing the long journey for approval of a newly developed drug.

Olomouc scientists have managed not only to discover this new group of substances in plants, but also synthesise them. “The U.S. patent protects the structure of the substances as well as the method of their preparation and their biological activity. The substances are called cytokinin nucleotides and they show a broad spectrum of anticancer effects,” said one of the co-authors of the patent, Karel Doležal from the Centre.

Hundreds of experiments

The antitumour effects were verified in vitro, in the artificial laboratory environment. “We happened to discover the anticancer activity of these substances quite incidentally, when we studied them as growth plant stimulators. We had to synthesise a large quantity of cytokinin nucleotides. The most difficult part was perhaps the preparation or precursors of these molecules, needed for binding biologically active amines. We managed to perform this task in sufficient quantity and quality. And the subsequent reactions resulted in the production of target molecules that had to be cleansed by chromatography,” explained Marek Zatloukal, who made a major contribution to the synthesis of the substances. According to him, this achievement was preceded by hundreds of experiments performed by the scientists during a period of approximately five years.

Long journey from effective substances to drugs

Long is the path from the discovery of effective substances to approval of development of a drug that helps patients. The U.S. patent is also crucial in negotiations with potential investors who would like to work further with the substances and reach the stage of clinical testing, for instance.

“Being granted a U.S. patent is a big achievement. The whole procedure took five years, was very demanding financially, and we had to submit a number of proofs and refute many opposing opinions,” explained Lucie Plíhalová from the Centre. She further added that the U.S. patent is also a guarantee for foreign scientists that the discovery has been verified and may be considered new and unique. Experts appreciate it similarly, as proves the publication of an article in the prestigious journal Nature.

Cytokinins are plant hormones that regulate the cell cycle in plants. They are used in agriculture and plant biotechnologies, but they have a number of applications in medicine too. The Centre of the Haná Region, which is a joint facility of the Faculty of Science at Palacký University, the Institute of Experimental Botany at the Academy of Sciences of the Czech Republic, and the Crop Research Institute, has already gained several U.S. patents in the past. Most of them, however, involved plants.

Some of the cytokinin derivatives with anticancer activity, discovered by Olomouc scientists in the past, have reached the stage of clinical testing. The new substances promise to be even more effective in the treatment of tumour diseases than Roskovitine, successfully tested at present. “In addition to that, they combine more effects in one molecule, for example anticancer effects are complemented with immunostimulative ones,” explained another member of the research team, Miroslav Strnad.

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Last update: 19. 09. 2012, Vladimír Kubák