16.06.2017 change 16.06.2017

Silesian scientists have developed new compounds with anticancer activity

Researchers from the University of Silesia and the Silesian University of Technology have developed new quinolinic acid compounds that can be used in anticancer drugs. Prior to their potential introduction to the market, in vivo tests are still necessary.

Previous studies conducted in vitro showed that some chinaldicarboxylic acid derivatives exhibited antitumour activity without damaging healthy cells.

According to the information provided by the University of Silesia press office, the combination of these systems with sugar units has contributed to improving the biocompatibility and pharmacokinetic parameters of the new compounds, as well as increasing their activity. The results are quinolinic acid glycoconjugates covered by the patent protection.

A team of scientists from the University of Silesia, under the supervision of Dr. Robert Musioł from the Department of Organic Chemistry, studied quinoline derivatives. These xenobiotics do not occur naturally in the human body - and are not produced by it. Therefore, it was necessary to find a solution to introduce them into the human body so that they would not be rejected.

"Carbohydrates are subject to metabolic processes in the human body, so we decided to combine our compounds with sugar units, thus improving the biocompatibility of the new substances" said Musioł, quoted in the university release. He added that a xenobiotics combined with a sugar derivative and introduced into a patient\'s body, for example in the form of a tablet, remains "unnoticed" by the body, allowing it to reach the affected site.

The researchers emphasised that the quinoleic acid glycoconjugates obtained by combining these organic compounds have a higher antitumor activity than other substances tested by the team; their pharmacokinetic parameters are also better.

Glucoconjugates of quinoline acids have been tested mainly on tumour cells located in the large intestine. "Special protein structures found there absorb glucose from the digestive tract, which is why researchers consider them to be a great space for compounds that contain sugar units. They will be absorbed by the body, and +released+ derivatives of chinaldicarboxylic acids will begin the process of destroying cancer cells" - the researchers explained.

The results of these studies will help researchers to carry out further, deeper analyses performed in vivo. This is yet another stage preceding the potential introduction of compounds into the pharmaceutical market.

In addition, researchers are also planning to study more compounds of this type in the near future in order to increase their antitumour activity, improve their production methods and pharmacokinetic parameters.

According to the University of Silesia, the authors of the invention are: Dr. Gabriela Pastuch-Gawołek from the Faculty of Chemistry of the Silesian University of Technology, as well as scientists associated with the University of Silesia - from the Department of Organic Chemistry: Dr. Maciej Serda, Dr. Wioleta Cieślik, Dr. Robert Musioł and Prof. Jarosław Polański, and from the Department of Solid State Physics: Dr. Anna Mrozek-Wilczkiewicz and Prof. Alicja Ratuszna.

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