Электронный архив

Unraveling the molecular mechanism of selective antimicrobial activity of 2(5H)-furanone derivative against Staphylococcus aureus

Показать сокращенную информацию

dc.contributor.author Sharafutdinov I.
dc.contributor.author Pavlova A.
dc.contributor.author Akhatova F.
dc.contributor.author Khabibrakhmanova A.
dc.contributor.author Rozhina E.
dc.contributor.author Romanova Y.
dc.contributor.author Fakhrullin R.
dc.contributor.author Lodochnikova O.
dc.contributor.author Kurbangalieva A.
dc.contributor.author Bogachev M.
dc.contributor.author Kayumov A.
dc.date.accessioned 2020-01-15T21:48:15Z
dc.date.available 2020-01-15T21:48:15Z
dc.date.issued 2019
dc.identifier.issn 1661-6596
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/156071
dc.description.abstract © 2019 by the authors. Licensee MDPI, Basel, Switzerland. Staphylococcus aureus causes various infectious diseases, from skin impetigo to life-threatening bacteremia and sepsis, thus appearing an important target for antimicrobial therapeutics. In turn, the rapid development of antibiotic resistance and biofilm formation makes it extremely robust against treatment. Here, we unravel the molecular mechanism of the antimicrobial activity of the recently unveiled F105 consisting of three pharmacophores: chlorinated 2(5H)-furanone, sulfone, and l-menthol moieties. F105 demonstrates highly selective activity against Gram-positive bacteria and biofilm-embedded S. aureus and exhibits low risk of resistance development. We show explicitly that the fluorescent analogue of F105 rapidly penetrates into Gram-positive bacteria independently of their cell integrity and viability and accumulates there. By contrast, Gram-negative bacteria remain impermeable and, therefore, insusceptible to F105. Apparently, in bacterial cells, F105 induces reactive oxygen species (ROS) formation and nonspecifically interacts with a number of proteins, including ROS-utilizing ones. Using native and 2D PAGE, we confirm that F105 changes the charge of some proteins by either oxidation or direct interaction with them. Therefore, it seems justified to conclude that being simultaneously a ROS inducer and damaging proteins responsible for ROS utilization, F105 impairs the cellular anti-ROS defense representing a prospective ROS-inducing antibacterial agent.
dc.relation.ispartofseries International Journal of Molecular Sciences
dc.subject 2(5H)-furanones
dc.subject Biofilms
dc.subject Drug discovery
dc.subject ROS
dc.subject Staphylococci
dc.title Unraveling the molecular mechanism of selective antimicrobial activity of 2(5H)-furanone derivative against Staphylococcus aureus
dc.type Article
dc.relation.ispartofseries-issue 3
dc.relation.ispartofseries-volume 20
dc.collection Публикации сотрудников КФУ
dc.source.id SCOPUS16616596-2019-20-3-SID85061256975


Файлы в этом документе

Данный элемент включен в следующие коллекции

  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

Показать сокращенную информацию

Поиск в электронном архиве


Расширенный поиск

Просмотр

Моя учетная запись

Статистика