Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
In: Bioorganic & medicinal chemistry letters, Jg. 64 (2022-05-15), S. 128695
academicJournal
Zugriff:
The dramatic rise in drug resistance accelerated the desire for new antibacterial agents to safeguard human health. This work constructed a novel type of aloe emodin-hybridized sulfonamide aminophosphates as unique potential antibacterial agents. The biological assay revealed that some target hybrids possessed potent inhibitory activity. Particularly, ethyl aminophosphate-hybridized sulfadiazine aloe emodin 7a (EASA-7a) not only displayed preponderant antibacterial efficiency against drug-resistant E. faecalis at low concentration as 0.25 μg/mL but also possessed strong bacteriostatic capacity and low propensity to develop resistance toward E. faecalis. The weak hemolysis toward human red blood cells and efficient biofilm-disruptive ability further implied the therapeutic potential of EASA-7a. Preliminary studies disclosed that the excellent antibacterial behavior of EASA-7a might be attributed to its capacity to permeate and depolarize the bacterial membrane, as well as promote ROS accumulation and intercalate with DNA. These findings manifested that EASA-7a was worthy of further development to combat life-threatening bacterial infections.
(Copyright © 2022 Elsevier Ltd. All rights reserved.)
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Natural aloe emodin-hybridized sulfonamide aminophosphates as novel potential membrane-perturbing and DNA-intercalating agents against Enterococcus faecalis.
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Autor/in / Beteiligte Person: | Deng, Z ; Sun, H ; Bheemanaboina, RRY ; Luo, Y ; Zhou, CH |
Zeitschrift: | Bioorganic & medicinal chemistry letters, Jg. 64 (2022-05-15), S. 128695 |
Veröffentlichung: | Oxford : Elsevier Science Ltd ; <i>Original Publication</i>: Oxford ; New York : Pergamon Press, c1991-, 2022 |
Medientyp: | academicJournal |
ISSN: | 1464-3405 (electronic) |
DOI: | 10.1016/j.bmcl.2022.128695 |
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