Indoles as promising Therapeutics: A review of recent drug discovery efforts

Bioorganic Chemistry, Год журнала: 2024, Номер 154, С. 108092 - 108092

Опубликована: Дек. 25, 2024

Язык: Английский

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A novel function of short cationic peptide FP-CATH9 without antimicrobial activity reverses resistance to minocycline in common multidrug-resistant gram-negative bacteria

Microbiology Spectrum, Год журнала: 2025, Номер unknown

Опубликована: Фев. 25, 2025

ABSTRACT The increase in bacterial resistance to minocycline and other tetracyclines poses a serious threat global public health. Because the development of new antibiotics has proven problematic, antibiotic sensitization therapy is now an effective coping strategy. While antimicrobial peptides generally exhibit broad-spectrum antibacterial activity good biocompatibility, naturally truncated portions (such as snake cathelicidin) often do not activity, their function remains unknown. FP-CATH9 short cationic peptide derived from FP-CATH (snake cathelicidin peptide) with amphiphilic α-helical structure no discernible activity. However, was previously found significantly enhance against gram-negative bacteria. In present paper, clinically relevant minocycline-resistant bacteria ( Escherichia coli , Klebsiella pneumoniae Acinetobacter baumannii Pseudomonas aeruginosa ) were used test for screening. be dose dependent double-dilution assay. synergistic on subsequently determined using checkerboard method. An ethidium bromide efflux revealed that caused accumulation Additionally, exhibited low hemolytic red blood cells cytotoxicity Raw264.7 cells. vivo model infection, combined 80% protective effect Galleria mellonella larvae infected multidrug-resistant K. . summary, adjuvant reverses by increasing intracellular minocycline. This finding broad application potential. IMPORTANCE existence pump system enables expel antibiotics, reduce concentration cells, make unable effectively inhibit or kill bacteria, which one main mechanisms antibiotics. some pumps are substrate specific, while others wide range substrates. this study, can specifically reverse provides way solve problem drug resistance.

Язык: Английский

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Dimeric Acylphloroglucinol Derivatives with Anti-MRSA Activities from Chamelaucium uncinatum

Journal of Natural Products, Год журнала: 2025, Номер unknown

Опубликована: Май 5, 2025

Chamelauciumols A-I (1-9), nine undescribed dimeric acylphloroglucinol derivatives, were isolated from the aerial parts of Chamelaucium uncinatum. Structurally, compound 1 featured a new carbon skeleton characterized by an unprecedented prenyl-substituted methanodibenzo[b,f][1,5]dioxocin core. Compounds 2 and 3 represented scaffolds, consisting two methylated derivatives linked via prenyl units. 4-9 phloroglucinol dimers with various linkage patterns. The structures absolute configurations these compounds elucidated comprehensive spectroscopic data, single-crystal X-ray diffraction analysis, electronic circular dichroism calculation. Besides, antibacterial activities against Gram-positive Gram-negative bacterial strains isolates evaluated. 4 exhibited potent inhibitory effects methicillin-resistant Staphylococcus aureus minimum concentration values ranging 0.5 to μg/mL. A preliminary study on mechanism action revealed that exerted anti-MRSA through disrupting cell membrane integrity. Additionally, also demonstrated remarkable antibiofilm activities.

Язык: Английский

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Oleanolic Acid Derivatives against Drug-resistant Bacteria and Fungi by Multi-targets to Avoid Drug Resistance

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 280, С. 116940 - 116940

Опубликована: Окт. 5, 2024

Язык: Английский

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