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

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Resumo

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.

Sobre autores

A. Popov

G.B. Elyakov Pacific Institute Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science

Autor responsável pela correspondência
Email: popovam@piboc.dvo.ru
Russian Federation, Vladivostok

L. Degenkova

Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences

Email: popovam@piboc.dvo.ru
Russian Federation, Moscow

T. 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. Grammatikova

Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences

Email: popovam@piboc.dvo.ru
Russian Federation, Moscow

A. 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. 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. Schekotichin

Gauze Research Institute for The Search for New Antibiotics, Russian Academy of Sciences

Email: popovam@piboc.dvo.ru
Russian Federation, Moscow

Academician 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

Bibliografia

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Declaração de direitos autorais © А.М. Попов, Л.Г. Деженкова, Т.В. Московкина, Н.Э. Грамматикова, А.С. Кузьмич, О.В. Черников, А.Е. Щекотихин, В.А. Стоник, 2023

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