Russian Scientists Develop New Compound for Treating Aggressive Tumours
A team of Russian researchers has synthesised a novel compound for boron neutron capture therapy (BNCT), a treatment for advanced cancer that uses the boron-10 isotope. The compound exhibits low toxicity, excellent water solubility, and eliminates the need for administering large volumes. Most importantly, the active substance reaches the tumour with minimal impact on healthy tissues. The study was published in the International Journal of Molecular Sciences shortly before World Cancer Day, observed annually on February 4.
Boron neutron capture therapy (BNCT) is an advanced cancer treatment that leverages the properties of the boron-10 isotope. The method involves first saturating tumour cells with boron-10, followed by irradiation with thermal neutrons. This triggers a nuclear reaction that selectively destroys cancer cells while sparing healthy tissue. Thus, the treatment success largely depends on the compound's ability to effectively deliver boron-10 to the tumour and maintain the necessary boron concentration.
A team of scientists from the HSE Faculty of Chemistry, the Institute of General and Inorganic Chemistry of the Russian Academy of Sciences, and the N.N. Blokhin National Medical Research Centre of Oncology has developed three compounds that combine the closo-dodecaborate anion with amino acids containing a side-chain amino group. The molecules are structurally similar to natural amino acids, allowing them to 'trick' the body's transport systems into capturing and delivering them to cells, including cancer cells. This makes the substance effective at targeting tumours, where it accumulates.
One of the compounds demonstrated low toxicity, with the half-lethal dose (LD50) for experimental animals ranging from 150 to 300 mg per kilogram of body weight. In experiments, the compound not only demonstrated the ability to accumulate boron in tumour tissues but also confirmed its effectiveness in animals. When administered to laboratory mice, the boron concentration in melanoma tumour cells was six times higher than in healthy tissues after 45 minutes.
The compound can exist in two forms depending on the pH level. The first form is a sodium salt, which is highly soluble in water under conditions close to physiological pH, making it convenient for therapeutic use. The second form occurs upon acidification, when the compound transforms into an insoluble internal salt useful for obtaining a medically pure product during the stages of synthesis, isolation, and purification.
Margarita Ryabchikova
'The aim of the study was to reduce toxicity and simplify the compound purification process, building on data from previous research. As a result, three new compounds were synthesised. One of them exhibited optimal characteristics: it does not cause significant side effects when administered intravenously and dissolves well in water, setting it apart from existing therapeutic drugs,' explains study author Margarita Ryabchikova, a third-year student at the HSE Faculty of Chemistry. 'We aimed not only for high efficacy but also for production convenience. The developed method can be easily scaled to produce the required quantities of the product while remaining economically viable.'
The study demonstrated that the new compound accumulates more effectively in the tissues of certain types of tumours compared to the currently used drug. This is an important step toward developing a safer and more accessible therapy. The research is still in its early stages, but this development has the potential to significantly improve cancer treatment outcomes and broaden the applications of boron neutron capture therapy in the fight against various types of tumours.
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