LED 209 conjugated chitosan as a selective antimicrobial and potential anti-adhesion material

Zhou, Zongbao; Chen, Tao; Mei, Naibin; Li, Bing; Xu, Zunkai; Wang, Lei; Wang, Xiaoying; Tang, Shunqing

doi:10.1016/j.carbpol.2018.11.044

Cited by 12 publications

(5 citation statements)

References 54 publications

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“…Chitosan peptide/amino acid conjugates are usually obtained by direct condensation of the carboxyl groups of the amino acids with amino groups of chitosan to form amide bonds. In the process, 1-ethyl-3-(3dimethylaminopropyl)-carbodiimide (EDC) and N-hydroxysuccinimide (NHS) are often used to activate the carboxyl groups of amino acids in the reaction process (Zhou et al, 2019). To avoid side reactions and reduce reaction steric hindrance, some spacer molecules are often used in the coupling process (Table 3) (Denora et al, 2016;Petrin et al, 2019).…”

Section: Introducing Peptides /Amino Acidsmentioning

confidence: 99%

Cationic chitosan derivatives as potential antifungals: A review of structural optimization and applications

Qin

Guo

2020

Carbohydrate Polymers

118

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The increasing resistance of pathogen fungi poses a global public concern. There are several limitations in current antifungals, including few available fungicides, severe toxicity of some fungicides, and drug resistance. Therefore, there is an urgent need to develop new antifungals with novel targets. Chitosan has been recognized as a potential antifungal substance due to its good biocompatibility, biodegradability, non-toxicity, and availability in abundance, but its applications are hampered by the low charge density results in low solubility at physiological pH. It is believed that enhancing the positive charge density of chitosan may be the most effective approach to improve both its solubility and antifungal activity. Hence, this review mainly focuses on the structural optimization strategy of cationic chitosan and the potential antifungal applications. This review also assesses and comments on the challenges, shortcomings, and prospect of cationic chitosan derivatives as antifungal therapy.

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Section: Introducing Peptides /Amino Acidsmentioning

confidence: 99%

Cationic chitosan derivatives as potential antifungals: A review of structural optimization and applications

Qin

Guo

2020

Carbohydrate Polymers

118

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“…The conjugate not only remained the strong antibacterial activity, but also inhibited virulence gene expression of gram-negative bacteria without inducing resistance development of the pathogens. A subsequently obtained chitosan (CS)-LED209 was also reported to have a higher selectively antimicrobial and anti-adhesion activity against MDR- E. coli as well as the lower cytotoxicity to the mammalian cell than CS ( Zhou et al, 2019 ). An all D-amino acid analogue of Tachyplesin I (TPAD) which belongs to cationic β-hairpin antimicrobial peptides with broad-spectrum antimicrobial activity was reported, but it was found that TPAD tends to induce bacterial resistance by activating the QseC/B TCS.…”

Section: Novel Histidine Kinase-targeted Antimicrobial Agentsmentioning

confidence: 99%

Recent Advances in Histidine Kinase-Targeted Antimicrobial Agents

Chen

et al. 2022

Front. Chem.

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The prevalence of antimicrobial-resistant pathogens significantly limited the number of effective antibiotics available clinically, which urgently requires new drug targets to screen, design, and develop novel antibacterial drugs. Two-component system (TCS), which is comprised of a histidine kinase (HK) and a response regulator (RR), is a common mechanism whereby bacteria can sense a range of stimuli and make an appropriate adaptive response. HKs as the sensor part of the bacterial TCS can regulate various processes such as growth, vitality, antibiotic resistance, and virulence, and have been considered as a promising target for antibacterial drugs. In the current review, we highlighted the structural basis and functional importance of bacterial TCS especially HKs as a target in the discovery of new antimicrobials, and summarize the latest research progress of small-molecule HK-inhibitors as potential novel antimicrobial drugs reported in the past decade.

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“…(2) Solubility. Modification of chitosan often significantly improves its water solubility [25,31,114]. This is because the introduction of bioactive groups reduces the force of intramolecular hydrogen bonding interactions within chitosan.…”

Section: Physiochemical Properties and Antimicrobial Activitiesmentioning

confidence: 99%

“…Further studies have shown that the conjugates can maintain the characteristics of CS and LED 209, and prevent bacterial adhesion. Therefore, these findings provide a feasible strategy for the synthesis of multifunctional antibacterial agents [114]. Mu et al successfully combined chitosan with streptomycin, thereby improving the ability of antibiotics to resist biofilms formed by gram-positive bacteria rather than gram-negative bacteria, and thus providing a new solution to the problem of antibiotic resistance.…”

Section: Potential Applicationsmentioning

confidence: 99%

“…The following points are specifically emphasized: It is generally believed that the higher the DS of the chitosan conjugate is, the stronger its antibacterial activity is [114]. However, due to the structure of the chitosan macromolecule and its potential steric hindrance, the coupling rate of chitosan is not high in many cases [33,57,63], which may bring the problem of the insufficient effective concentration of active ingredients in the body.…”

Section: How Can Chitosan Conjugates Be Properly Designdesigned and Smentioning

confidence: 99%

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Antimicrobial Chitosan Conjugates: Current Synthetic Strategies and Potential Applications

Qin

2020

IJMS

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As a natural polysaccharide, chitosan possesses good biocompatibility, biodegradability and biosafety. Its hydroxyl and amino groups make it an ideal carrier material in the construction of polymer-drug conjugates. In recent years, various synthetic strategies have been used to couple chitosan with active substances to obtain conjugates with diverse structures and unique functions. In particular, chitosan conjugates with antimicrobial activity have shown great application prospects in the fields of medicine, food, and agriculture in recent years. Hence, we will place substantial emphasis on the synthetic approaches for preparing chitosan conjugates and their antimicrobial applications, which are not well summarized. Meanwhile, the challenges, limitations, and prospects of antimicrobial chitosan conjugates are described and discussed.

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LED 209 conjugated chitosan as a selective antimicrobial and potential anti-adhesion material

Cited by 12 publications

References 54 publications

Cationic chitosan derivatives as potential antifungals: A review of structural optimization and applications

Cationic chitosan derivatives as potential antifungals: A review of structural optimization and applications

Recent Advances in Histidine Kinase-Targeted Antimicrobial Agents

Antimicrobial Chitosan Conjugates: Current Synthetic Strategies and Potential Applications

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