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
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Affiliations:
- G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science
- Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences
- 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
Cite item
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.
About the authors
A. M. Popov
G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science
Author for correspondence.
Email: popovam@piboc.dvo.ru
Russian Federation, Vladivostok
L. G. Degenkova
Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences
Email: popovam@piboc.dvo.ru
Russian Federation, Moscow
T. V. Moskovkina
Institute of High Technologies and Advanced Materials, Far East Federal University
Email: popovam@piboc.dvo.ru
Russian Federation, Vladivostok, Russian Island, Ayaks Bay, 10
N. E. Grammatikova
Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences
Email: popovam@piboc.dvo.ru
Russian Federation, Moscow
A. S. Kuzmich
G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science
Email: popovam@piboc.dvo.ru
Russian Federation, Vladivostok
O. V. Chernikov
G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science
Email: popovam@piboc.dvo.ru
Russian Federation, Vladivostok
A. E. Schekotichin
Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences
Email: popovam@piboc.dvo.ru
Russian Federation, Moscow
Academician of the RAS V. A. Stonik
G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science
Email: popovam@piboc.dvo.ru
Russian Federation, Vladivostok
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