Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome

Staphylococcus aureus (S. aureus) is one of the most serious human pathogens. α-Hemolysin (Hla) secreted by S. aureus is a key toxin for various infections. We herein report that Honokiol, a natural plant polyphenol, inhibits the secretion and hemolytic activity of staphylococcal Hla with concomitan...

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Main Authors: Na Guo, Zuojia Liu, Zhiqiang Yan, Zonghui Liu, Kun Hao, Chuanbo Liu, Jin Wang
Format: Article
Language:English
Published: Taylor & Francis Group 2019-01-01
Series:Emerging Microbes and Infections
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Online Access:https://www.tandfonline.com/doi/10.1080/22221751.2019.1617643
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author Na Guo
Zuojia Liu
Zhiqiang Yan
Zonghui Liu
Kun Hao
Chuanbo Liu
Jin Wang
author_facet Na Guo
Zuojia Liu
Zhiqiang Yan
Zonghui Liu
Kun Hao
Chuanbo Liu
Jin Wang
author_sort Na Guo
collection DOAJ
description Staphylococcus aureus (S. aureus) is one of the most serious human pathogens. α-Hemolysin (Hla) secreted by S. aureus is a key toxin for various infections. We herein report that Honokiol, a natural plant polyphenol, inhibits the secretion and hemolytic activity of staphylococcal Hla with concomitant growth inhibition of S. aureus and protection of S. aureus-mediated cell injury within subinhibitory concentrations. In parallel, Honokiol attenuates the staphylococcal Hla-induced inflammatory response by inhibiting NLRP3 inflammasome activation in vitro and in vivo. Consequently, the biologically active forms of the inflammatory cytokines IL-1β and IL-18 are reduced significantly in response to Honokiol in mice infected with S. aureus. Experimentally, we confirm that Honokiol binds to monomeric Hla with a modest affinity without impairing its oligomerization. Based on molecular docking analyses in silico, we make a theoretical discovery that Honokiol is located outside of the triangular region of monomeric Hla. The binding model restricts the function of the residues related to membrane channel formation, which leads to the functional disruption of the assembled membrane channel. This research creates a new paradigm for developing therapeutic agents against staphylococcal Hla-mediated infections.
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publisher Taylor & Francis Group
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spelling doaj-art-9421b2b7b97a49b08de6a01c5e9fc58a2025-08-20T02:08:12ZengTaylor & Francis GroupEmerging Microbes and Infections2222-17512019-01-018170771610.1080/22221751.2019.1617643Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasomeNa Guo0Zuojia Liu1Zhiqiang Yan2Zonghui Liu3Kun Hao4Chuanbo Liu5Jin Wang6State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, People’s Republic of ChinaState Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, People’s Republic of ChinaState Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, People’s Republic of ChinaDepartment of Food Quality and Safety, College of Food Science and Engineering, Jilin University, Changchun, People’s Republic of ChinaDepartment of Food Quality and Safety, College of Food Science and Engineering, Jilin University, Changchun, People’s Republic of ChinaState Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, People’s Republic of ChinaState Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, People’s Republic of ChinaStaphylococcus aureus (S. aureus) is one of the most serious human pathogens. α-Hemolysin (Hla) secreted by S. aureus is a key toxin for various infections. We herein report that Honokiol, a natural plant polyphenol, inhibits the secretion and hemolytic activity of staphylococcal Hla with concomitant growth inhibition of S. aureus and protection of S. aureus-mediated cell injury within subinhibitory concentrations. In parallel, Honokiol attenuates the staphylococcal Hla-induced inflammatory response by inhibiting NLRP3 inflammasome activation in vitro and in vivo. Consequently, the biologically active forms of the inflammatory cytokines IL-1β and IL-18 are reduced significantly in response to Honokiol in mice infected with S. aureus. Experimentally, we confirm that Honokiol binds to monomeric Hla with a modest affinity without impairing its oligomerization. Based on molecular docking analyses in silico, we make a theoretical discovery that Honokiol is located outside of the triangular region of monomeric Hla. The binding model restricts the function of the residues related to membrane channel formation, which leads to the functional disruption of the assembled membrane channel. This research creates a new paradigm for developing therapeutic agents against staphylococcal Hla-mediated infections.https://www.tandfonline.com/doi/10.1080/22221751.2019.1617643Staphylococcus aureusα-HemolysinHonokiolinflammasomebinding interactionmolecular docking
spellingShingle Na Guo
Zuojia Liu
Zhiqiang Yan
Zonghui Liu
Kun Hao
Chuanbo Liu
Jin Wang
Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome
Emerging Microbes and Infections
Staphylococcus aureus
α-Hemolysin
Honokiol
inflammasome
binding interaction
molecular docking
title Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome
title_full Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome
title_fullStr Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome
title_full_unstemmed Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome
title_short Subinhibitory concentrations of Honokiol reduce α-Hemolysin (Hla) secretion by Staphylococcus aureus and the Hla-induced inflammatory response by inactivating the NLRP3 inflammasome
title_sort subinhibitory concentrations of honokiol reduce α hemolysin hla secretion by staphylococcus aureus and the hla induced inflammatory response by inactivating the nlrp3 inflammasome
topic Staphylococcus aureus
α-Hemolysin
Honokiol
inflammasome
binding interaction
molecular docking
url https://www.tandfonline.com/doi/10.1080/22221751.2019.1617643
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