ANTITUMOR AND RADIATION-SENSITIZING EFFECTS OF К-26

Abstract

The new colchicine derivative ‘K-26’ manifested both high cytotoxic activity in vitro at the National Cancer Institute of the USA (NCI) and high antitumor activity in a number of transplanted animal tumors. The high antitumor activity of the K-26, as well as its further study as a radiation sensitizer, suggests the study of the alkylating action (effect on DNA and RNA synthesis, on internucleosomal degradation and DNA fragmentation), impact on topoisomerase II activity and drug resistance as well as mitotic activity and induction of CFU. The study showed that K-26 inhibits DNA synthesis, the activity of topoisomerases and MDR2. It stimulates p53, which explains its high antitumor and mitotic effect, leading to the synchronization of cell division and radiation-sensitizing activity. Stimulation of CFEC, which ensures the formation of hematopoietic and immune cells, can protect the body from its intense cytotoxic effect.