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Hydrophobic Rose Bengal Derivatives Exhibit Submicromolar-to-Subnanomolar Activity against Enveloped Virusesстатья
Статья опубликована в высокорейтинговом журнале
Статья опубликована в журнале из списка Web of Science и/или Scopus- Авторы: Rubekina Anna A., Kamzeeva Polina N., Alferova Vera A., Shustova Elena Yu, Kolpakova Ekaterina S., Yakovchuk Elizaveta V., Karpova Evgenia V., Borodulina Maria O., Belyaev Evgeny S., Khrulev Alexei A., Korshun Vladimir A., Shirshin Evgeny A., Kozlovskaya Liubov I., Aralov Andrey V.
- Журнал: Biomolecules
- Том: 12
- Номер: 11
- Год издания: 2022
- Издательство: MDPI
- Местоположение издательства: Basel, Switzerland
- DOI: 10.3390/biom12111609
- Аннотация: Rose Bengal (RB) is an anionic xanthene dye with multiple useful biological features,including photosensitization properties. RB was studied extensively as a photosensitizer, mostly for antibacterial and antitumor photodynamic therapy (PDT). The application of RB to virus inactivationis rather understudied, and no RB derivatives have been developed as antivirals. In this work, we used a synthetic approach based on a successful design of photosensitizing antivirals to produce RB derivatives for virus photoinactivation. A series of n-alkyl-substituted RB derivatives was synthesized and evaluated as antiviral photosensitizers. The compounds exhibited similar 1O2 generation rate and efficiency, but drastically different activities against SARS-CoV-2, CHIKV, and HIV; with comparable cytotoxicity for different cell lines. Submicromolar-to-subnanomolar activities and high selectivity indices were detected for compounds with C4-6 alkyl (SARS-CoV-2) and C6-8 alkyl (CHIKV) chains. Spectrophotometric assessment demonstrates low aqueous solubility for C8-10 congeners and a significant aggregation tendency for the C12 derivative, possibly influencing its antiviral efficacy. Initial evaluation of the synthesized compounds makes them promising for further study as viral inactivators for vaccine preparations.
- Добавил в систему: Рубекина Анна Александровна