CPF-C1 analog with effective antimicrobial and antibiofilm activities against Staphylococcus aureus including MRSA

Xie, Junqiu; Li, Yao; Guo, Xiaomin; Rao, Jing; Yan, Tiantian; Mou, Lingyun; Wu, Xiaohong; Xie, Xinxin; Yang, Wenle; Zhang, Bangzhi

doi:10.1016/j.biochi.2020.06.003

Cited by 6 publications

(9 citation statements)

References 46 publications

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“…The MICs of the Feleucin-K3 analogs were 4-8 µg/mL, which were much lower than the MICs of AML against MRSA (up to 128 µg/mL) [16]. It was also found in previous studies that the MICs of imipenem against multidrug-resistant A. baumannii were as high as 64 µg/mL, indicating that the antimicrobial activity was significantly weaker than that of the designed Feleucin-K3 analogs [16]. Notably, these Feleucin-K3 analogs had more powerful antimicrobial activities than Magainin 2, which has been studied in greater detail.…”

Section: Antimicrobial Activity In Vitromentioning

confidence: 76%

“…Moreover, for MRSA and A. baumannii isolated from the clinic, the antimicrobial activity of these peptides was significant in comparison with the antibiotics tested (Tables 3 and 4). The MICs of the Feleucin-K3 analogs were 4-8 µg/mL, which were much lower than the MICs of AML against MRSA (up to 128 µg/mL) [16]. It was also found in previous studies that the MICs of imipenem against multidrug-resistant A. baumannii were as high as 64 µg/mL, indicating that the antimicrobial activity was significantly weaker than that of the designed Feleucin-K3 analogs [16].…”

Section: Antimicrobial Activity In Vitromentioning

confidence: 76%

“…In brief, MRSA ATCC 33591 (5 × 10 5 CFU/mL) and an equal volume of peptides (final concentration 4 µg/mL or 8 µg/mL) were incubated in culture dishes. Propidium iodide (PI) at the concentration of 6 µg/mL and the same concentration of SYTO9 were premixed and added to the dish [16]. After incubation for 30 min, CLSM (Zeiss LSM 710 Meta; Karl, Germany) was used to visually observe the results.…”

Section: Confocal Laser Scanning Fluorescence Microscopy (Clsm)mentioning

confidence: 99%

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Potent Antimicrobial and Antibiofilm Activities of Feleucin-K3 Analogs Modified by α-(4-Pentenyl)-Ala against Multidrug-Resistant Bacteria

et al. 2021

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The dramatic increase in antimicrobial resistance (AMR) highlights an urgent need to develop new antimicrobial therapies. Thus, antimicrobial peptides (AMPs) have emerged as promising novel antibiotic alternatives. Feleucin-K3 is an amphiphilic α-helical nonapeptide that has powerful antimicrobial activity. In our previous study, it was found that the fourth residue of Feleucin-K3 is important for antimicrobial activity. After α-(4-pentenyl)-Ala was introduced into this position, both the antimicrobial activity and stability were greatly improved. Herein, to improve the limitations of Feleucin-K3, this unnatural amino acid was further introduced into different positions of Feleucin-K3. Among these synthetic Feleucin-K3 analogs, the N-terminal-substituted analog Feleucin-K65 (K65) and C-terminal-substituted analog Feleucin-K70 (K70) had preferable antimicrobial activity. In particular, their antimicrobial activities against multidrug-resistant bacteria were more potent than that of antibiotics. The stabilities of these peptides in salt and serum environments were improved compared with those of Feleucin-K3. In addition, these analogs had low hemolytic activity and AMR. More importantly, they effectively inhibited biofilm formation and exhibited considerable efficacy compared with traditional antibiotics against biofilm infection caused by methicillin-resistant Staphylococcus aureus (MRSA). In antimicrobial mechanism studies, K65 and K70 mainly permeated the outer membrane and depolarized the cytoplasmic membrane, resulting in cellular component leakage and cell death. In summary, analogs K65 and K70 are potential antimicrobial alternatives to solve the antibiotic crisis.

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Section: Antimicrobial Activity In Vitromentioning

confidence: 76%

Section: Antimicrobial Activity In Vitromentioning

confidence: 76%

Section: Confocal Laser Scanning Fluorescence Microscopy (Clsm)mentioning

confidence: 99%

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Potent Antimicrobial and Antibiofilm Activities of Feleucin-K3 Analogs Modified by α-(4-Pentenyl)-Ala against Multidrug-Resistant Bacteria

et al. 2021

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“…AMPs, such as Temporin-l, CPF-2, and Kassinatuerin-3, were also found to destroy the biofilm. However, the specific mechanism needs further investigation [ 120 , 139 , 140 ].…”

Section: Other Mechanismsmentioning

confidence: 99%

Mechanism of Antimicrobial Peptides: Antimicrobial, Anti-Inflammatory and Antibiofilm Activities

Luo

Song

2021

IJMS

208

114

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Antimicrobial peptides (AMPs) are regarded as a new generation of antibiotics. Besides antimicrobial activity, AMPs also have antibiofilm, immune-regulatory, and other activities. Exploring the mechanism of action of AMPs may help in the modification and development of AMPs. Many studies were conducted on the mechanism of AMPs. The present review mainly summarizes the research status on the antimicrobial, anti-inflammatory, and antibiofilm properties of AMPs. This study not only describes the mechanism of cell wall action and membrane-targeting action but also includes the transmembrane mechanism of intracellular action and intracellular action targets. It also discusses the dual mechanism of action reported by a large number of investigations. Antibiofilm and anti-inflammatory mechanisms were described based on the formation of biofilms and inflammation. This study aims to provide a comprehensive review of the multiple activities and coordination of AMPs in vivo, and to fully understand AMPs to realize their therapeutic prospect.

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“…99 Another simpler in vivo catheter model involves inserting catheters subcutaneously on the backs of mice. 100 Once implanted, MRSA can be injected in the vicinity of the sterile catheters and treated with HDPs, twice per day for three days, to demonstrate biolm inhibition. The synthetic D-peptide CPF-C2 was shown both to inhibit and eradicate biolm formation on subcutaneous urinary catheters.…”

Section: In Vivo Catheter and Device Modelsmentioning

confidence: 99%

Antibiofilm peptides: overcoming biofilm-related treatment failure

2021

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CPF-C1 analog with effective antimicrobial and antibiofilm activities against Staphylococcus aureus including MRSA

Cited by 6 publications

References 46 publications

Potent Antimicrobial and Antibiofilm Activities of Feleucin-K3 Analogs Modified by α-(4-Pentenyl)-Ala against Multidrug-Resistant Bacteria

Potent Antimicrobial and Antibiofilm Activities of Feleucin-K3 Analogs Modified by α-(4-Pentenyl)-Ala against Multidrug-Resistant Bacteria

Mechanism of Antimicrobial Peptides: Antimicrobial, Anti-Inflammatory and Antibiofilm Activities

Antibiofilm peptides: overcoming biofilm-related treatment failure

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