Scientists have developed new composites based on betulin dipropionate. Unlike the original substance betulin, they are soluble in water, being several times more effective at destroying cancer cells. The researchers suggest that these substances can become a promising tool for pharmacology. The results of the study are published in the journal Biointerface Research in Applied Chemistry.

Betulin dipropionate is a natural compound, an ester of betulin and propionic acid, which is a promising drug for the treatment of a wide range of diseases, including cancer. To obtain it, scientists have developed a simplified one-step synthesis directly from birch bark. It differs from other methods of obtaining betulin esters in that it does not require an additional stage of betulin isolation. However, the poor solubility and low bioavailability of this compound in water limit its application in medicine.

Scientists from the Krasnoyarsk Science Center of SB RAS and Institute of Solid State Chemistry and Mechanochemistry of SB RAS (Novosibirsk) have created new water-soluble composite materials based on betulin dipropionate, which have antitumor activity, and revealed the possibility of their use in cancer treatment. Betulin dipropinate and its mechanically altered variants cause the destruction of cancer cells better than the original substance.

To improve the characteristics of betulin dipropionate, the researchers decided to supplement it with arabinogalactan. The polysaccharide arabinogalactan from larch wood is water-soluble and has antioxidant and immunomodulatory activities. To increase the dissolution rate, composites were created in the form of powder and thin films. The authors of the study note that both ground and film materials showed high solubility in water.

The scientists evaluated the anticancer activity by the ability of the material to activate the death of A549 lung cancer cells in cell culture. The antitumor effect of all the obtained composites was several times higher than that of pure betulin. At the same time, the material in the form of water-soluble films had the highest antitumor ability, although the content of the active substance in it was 4-5 times lower than in other composites.

“Betulin ester derivatives selectively cause the destruction and stop the division of cancer cells, while they exhibit antioxidant activity in healthy cells. The results of our work show that betulin esters, in particular, composites of betulin dipropionate with arabinogalactan, can be obtained without using complex synthetic methods, and moreover, they are water-soluble and have a strong antitumor activity as compared to the original betulin. Possessing various pharmaceutically valuable properties, these substances can become promising materials in pharmacology. The study of their pharmacological activity is a task for future research,” said Yuri Malyar, Candidate of Chemical Sciences.