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

Мұқаба

Дәйексөз келтіру

Толық мәтін

Ашық рұқсат Ашық рұқсат
Рұқсат жабық Рұқсат берілді
Рұқсат жабық Тек жазылушылар үшін

Аннотация

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.

Авторлар туралы

A. Popov

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

Хат алмасуға жауапты Автор.
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

Әдебиет тізімі

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© 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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