MOSCOW, December 20. Lobachevsky University scientists have developed a new antitumor conjugate based on colchicine, and also confirmed its performance using laboratory tests. According to the authors, the new substance has reduced toxicity and can have a controlled, stepwise effect on the tumor. The results were published in the scientific journal Journal of Liposome Research.
Colchicine is a tropolone alkaloid isolated from plants of the genera Colchicum, Merendera and Gloriosa of the Colchicum family (Colchicaceae). This is a relatively inexpensive drug that has a strong anti-inflammatory effect and is widely used in the treatment of gout and other diseases.
Scientists from the National Research Nizhny Novgorod State University (NNSU) named after. N.I. Lobachevsky set themselves the task of selecting a nano-sized system for delivering antitumor drugs to the site of the disease and making the drug work in a targeted manner (i.e., released from a nanocontainer in or near the tumor, and not in any other place in the body). This would reduce the unwanted toxic effect of the drug on the patient’s body and improve its tolerability.
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“The system of targeted delivery of the colchicine drug that we have selected does provide a stepwise controlled release of the active substance; we have confirmed its effectiveness through experiments on mice. Previously, such developments have not been carried out, since for each new drug the delivery system is either modified or selected and created from scratch,” said Associate Professor of the Department of Organic Chemistry of the Faculty of Chemistry of UNN. N.I. Lobachevsky Ekaterina Shchegravina.
According to her, the resulting delivery system significantly increases the bioavailability of the drug. This means that a lot of active substance penetrates into the cells and is absorbed by them. In this case, the drug enters the body in an inactive form (in the form of a prodrug), its disintegration occurs near the tumor, and the active agent is released. This significantly reduces the toxicity of the drug and the side effects it causes.
“Our development reduces the rate of tumor growth by approximately 4-6 times compared to the control group of animals, and survival in the therapeutic group increases significantly (up to 10 times in mice),” noted Shchegravina.
Universal techniques developed by scientists will make it possible to design delivery systems not only for drugs based on colchicine, but also for different classes of anticancer drugs.
“We want to expand the new technology and adapt it to other types of drugs, including other socially significant diseases. We plan to study the reaction of the body's immune system to the particles we have developed in order to reduce the risk of possible side effects,” the speaker noted.
The work was carried out with the support of the Russian Science Foundation.
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