BIOLOGICAL ACTIVITY AND PROBABLE MECHANISMS OF ACTION OF DERIVATIVES OF TRYPTANTHRIN AND MOSTOTRIN ALKALOIDS

A. M. Popov; Попов А. М.; L. G. Degenkova; Деженкова Л. Г.; T. V. Moskovkina; Московкина Т. В.; N. E. Grammatikova; Грамматикова Н. Э.; A. S. Kuzmich; Кузьмич А. С.; O. V. Chernikov; Черников О. В.; A. E. Schekotichin; Щекотихин А. Е.; Academician of the RAS V. A. Stonik; Стоник В. А.

doi:10.31857/S2686738922600807

BIOLOGICAL ACTIVITY AND PROBABLE MECHANISMS OF ACTION OF DERIVATIVES OF TRYPTANTHRIN AND MOSTOTRIN ALKALOIDS

Authors: Popov A.M.¹, Degenkova L.G.², Moskovkina T.V.³, Grammatikova N.E.², Kuzmich A.S.¹, Chernikov .V.¹, Schekotichin A.E.², Stonik A.o.¹
Affiliations:
1. G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science
2. Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences
3. Institute of High Technologies and Advanced Materials, Far East Federal University
Issue: Vol 508, No 1 (2023)
Pages: 53-57
Section: Articles
URL: https://journals.rcsi.science/2686-7389/article/view/135677
DOI: https://doi.org/10.31857/S2686738922600807
EDN: https://elibrary.ru/MTHALD
ID: 135677

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Abstract
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Abstract

The alkaloid tryptanthrin and its water-soluble derivative mostotrin exhibit high antimicrobial and antitumor activity. To develop more active and less toxic preparations, syntheses and testing of the biological activities of a number of new and/or little-studied analogs were performed. Some of them have been shown to have higher cytotoxicity against tumor and antimicrobial cells than tryptanthrin and mostotrin. Thus, 8-fluorotryptanthrin effectively inhibits the proliferation of various tumor cell lines, namely: K-562/4, HCT-116 and HCT-116p53ko at lower concentrations than tryptanthrin, and 2,8-difluorostotrin exhibits a stronger antimicrobial effect against pathogenic bacteria S. aureus ATCC 29213 than mostotrin. It has been established that the antiproliferative properties of 8-fluorotryptanthrin and 8-fluormostotrin are associated with their ability in nanomolar concentrations to inhibit the cell cycle of tumor cells at the stage of transition from the G1 phase to the S phase. The data obtained indicate the prospects for further in-depth studies of their antitumor properties.

Keywords

quinazoline alkaloids derivatives, tumor cells, antimicrobial activity, cell cycle blocking

References

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