Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant <i>Escherichia coli</i>

Sun, Hang; Huang, Shiyu; Jeyakkumar, Ponmani; Cai, Gui‐Xin; Fang, Bo; Zhou, Cheng‐He

doi:10.1021/acs.jmedchem.1c01592

Cited by 66 publications

(38 citation statements)

References 61 publications

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“…The cellular constituents such as DNA, RNA, and proteins will be leaked once the bacterial cell membrane was irreversibly damaged. 53,54 The leaked nucleotides could be detected by UV absorptions at 260 nm. As stated in Figure 13, the absorption intensity at 260 nm rapidly increased in both MRSA (exposed to 5g and 5i) and P. aeruginosa ATCC 27853 (exposed to 23b−c) cells with the concentration increase of compounds.…”

Section: ■ Results and Discussionmentioning

confidence: 99%

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

et al. 2022

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Novel carbazole-oxadiazoles were developed as new potential antibacterial agents to combat dreadful resistance. Some target compounds displayed predominant inhibitory effects on the tested Gram-positive and -negative bacteria, and carbazole-oxadiazoles 5g, 5i–k, 16a–c, and tetrazole analogues 23b–c were found to be efficient in impeding the growth of MRSA and Pseudomonas aeruginosa ATCC 27853 (MICs = 0.25–4 μg/mL). Furthermore, compounds 5g and 23b–c not only possessed rapid bactericidal ability and low tendency to develop resistance but also exhibited low cytotoxic effects toward Hek 293T, HeLa, and red blood cells (RBCs), especially molecule 5g also showed low toxicity in vivo, which showed the therapeutic potential of these compounds. Further exploration indicated that compounds 5g, 5i, and 23b–c could disintegrate the integrity of bacterial cell membranes to leak the cytoplasmic contents, thus exerting excellent antibacterial effects. These facts mean that carbazole-based antibacterial agents might have bright prospects in confronting bacterial infections.

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Section: ■ Results and Discussionmentioning

confidence: 99%

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

et al. 2022

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“…Figure 8 D shows a protein leakage assay that was performed to determine the leakage of cellular proteins. Once the bacterial cell membrane has been irreversibly disrupted, cellular contents, such as DNA, RNA, and proteins, will leak [ 30 , 31 ]. An increase in protein concentration with increasing MIC doses, in comparison to negative controls, untreated and DMSO treated samples, were observed, indicating the possibility of cell membrane damage and protein leakage.…”

Section: Resultsmentioning

confidence: 99%

“…These observations agreed with the MBC values (Table 2) of the compounds and the positive control, vancomycin. Since bactericidal activity was determined from bacteria exposed to compounds for 20 h, it cannot be completely ruled out that low colony counts could have arisen from a failure of a subpopulation to recover from a viable non-culturable state brought on by antibiotic exposure [31]. performed the time kill assay at 4× MIC concentration to determine the erties of our hit compounds.…”

Section: Bactericidal Properties and Time-kill Assaymentioning

confidence: 99%

Development of 4-[4-(Anilinomethyl)-3-phenyl-pyrazol-1-yl] Benzoic Acid Derivatives as Potent Anti-Staphylococci and Anti-Enterococci Agents

Gilmore

Alam

2022

Antibiotics

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From a library of compounds, 11 hit antibacterial agents have been identified as potent anti-Gram-positive bacterial agents. These pyrazole derivatives are active against two groups of pathogens, staphylococci and enterococci, with minimum inhibitory concentration (MIC) values as low as 0.78 μg/mL. These potent compounds showed bactericidal action, and some were effective at inhibiting and eradicating Staphylococcus aureus and Enterococcus faecalis biofilms. Real-time biofilm inhibition by the potent compounds was studied, by using Bioscreen C. These lead compounds were also very potent against S. aureus persisters as compared to controls, gentamycin and vancomycin. In multiple passage studies, bacteria developed little resistance to these compounds (no more than 2 × MIC). The plausible mode of action of the lead compounds is the permeabilization of the cell membrane determined by flow cytometry and protein leakage assays. With the detailed antimicrobial studies, both in planktonic and biofilm contexts, some of these potent compounds have the potential for further antimicrobial drug development.

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“…Secondly, 4′, 6-diamino-2-phenylindole (DAPI) and propidium iodide (PI) as staining agents to further analyze the antibacterial mechanism of compound Ru-3 . DAPI can enter both living and dead cells and produce blue fluorescence, while PI can only enter cells with damaged membrane and combine with nucleic acid to produce red fluorescence ( Sun et al, 2021 ). As shown in Figure 11 , only blue fluorescence was observed in the negative control group, suggesting intact cell membranes of Staphylococcus aureus .…”

Section: Resultsmentioning

confidence: 99%

Ruthenium polypyridine complexes with triphenylamine groups as antibacterial agents against Staphylococcus aureus with membrane-disruptive mechanism

Jiang

Xiong

et al. 2022

Front. Chem.

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Due to the emergence and wide spread of methicillin-resistant Staphylococcus aureus, the treatment of this kind of infection becomes more and more difficult. To solve the problem of drug resistance, it is urgent to develop new antibiotics to avoid the most serious situation of no drug available. Three new Ru complexes [Ru (dmob)2PMA] (PF6)2 (Ru-1) [Ru (bpy)2PMA] (PF6)2 (Ru-2) and [Ru (dmb)2PMA] (PF6)2 (Ru-3) (dmob = 4,4′-dimethoxy-2,2′-bipyridine, bpy = 2,2′-bipyridine, dmb = 4,4′-dimethyl-2,2′-bipyridine and PMA = N-(4-(1H-imidazo [4,5-f] [1,10] phenanthrolin-2-yl) -4-methyl-N-(p-tolyl) aniline) were synthesized and characterized by 1H NMR, 13C NMR and HRMS. The detailed molecular structure of Ru-3 was determined by single crystal X-ray diffraction. Their antibacterial activities against Staphylococcus aureus (Staphylococcus aureus) were obvious and Ru-3 showed the best antibacterial effect with the minimum inhibitory concentration value of 4 μg ml−1. Therefore, further study on its biological activity showed that Ru-3 can effectively inhibit the formation of biofilm and destroy cell membrane. In vitro hemolysis test showed that Ru-3 has almost negligible cytotoxicity to mammalian red blood cells. In the toxicity test of wax moth insect model, Ru-3 exhibited low toxicity in vivo. These results, combined with histopathological studies, strongly suggest that Ru-3 was almost non-toxic. In addition, the synergistic effect of Ru-3 with common antibiotics such as ampicillin, chloramphenicol, tetracycline, kanamycin and gentamicin on Staphylococcus aureus was detected by chessboard method. Finally, in vivo results revealed that Ru-3 could obviously promote the wound healing of Staphylococcus aureus infected mice.

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Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant Escherichia coli

Cited by 66 publications

References 61 publications

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

Development of 4-[4-(Anilinomethyl)-3-phenyl-pyrazol-1-yl] Benzoic Acid Derivatives as Potent Anti-Staphylococci and Anti-Enterococci Agents

Ruthenium polypyridine complexes with triphenylamine groups as antibacterial agents against Staphylococcus aureus with membrane-disruptive mechanism

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