Natural products as inspiration for the development of bacterial antibiofilm agents

Melander, Roberta J.; Basak, Abhishek

doi:10.1039/d0np00022a

Cited by 107 publications

(77 citation statements)

References 207 publications

(232 reference statements)

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“…Natural compounds offer a large and largely untapped resource of novel drug candidates [ 36 ]. Our results demonstrate that chicory is a source of valuable bioactive compounds with antimicrobial properties, and the isolation of chicory extracts and compounds from industrial waste streams has the potential to create added value that can be exploited to benefit human health.…”

Section: Discussionmentioning

confidence: 99%

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

et al. 2021

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Chicory (Cichorium intybus L.) is an important industrial crop cultivated mainly to extract the dietary fiber inulin. However, chicory also contains bioactive compounds such as sesquiterpene lactones and certain polyphenols, which are currently discarded as waste. Plants are an important source of active pharmaceutical ingredients, including novel antimicrobials that are urgently needed due to the global spread of drug-resistant bacteria and fungi. Here, we tested different extracts of chicory for a range of bioactivities, including antimicrobial, antifungal and cytotoxicity assays. Antibacterial and antifungal activities were generally more potent in ethyl acetate extracts compared to water extracts, whereas supercritical fluid extracts showed the broadest range of bioactivities in our assays. Remarkably, the chicory supercritical fluid extract and a purified fraction thereof inhibited both methicillin-resistant Staphylococcus aureus (MRSA) and ampicillin-resistant Pseudomonas aeruginosa IBRS P001. Chicory extracts also showed higher antibiofilm activity against the yeast Candida albicans than standard sesquiterpene lactone compounds. The cytotoxicity of the extracts was generally low. Our results may thus lead to the development of novel antibacterial and antifungal preparations that are both effective and safe for human use.

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Section: Discussionmentioning

confidence: 99%

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

et al. 2021

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“…Many natural products with antibiofilm activity have been identified from plants, microbes and marine life and they include various compounds classes, such as alkaloids, fatty acids, organosulfurs, cyclic compounds, phenolics, steroids, terpenoids and other aliphatic compounds. These compounds include: elligic acid glycosides, hamamelitannin, carolacton, skyllamycins, promysalin, phenazines, bromoageliferin, flustramine C, meridianin D and brominated furanones [ 18 , 45 , 46 , 47 , 48 , 49 , 50 ]. The most significant groups of plant-derived QS inhibitors belong to terpenes, terpenoids, phenylpropanoids, acid derivatives, diarylheptanoids, coumarins, flavonoids and tannins [ 46 , 51 , 52 ].…”

Section: Discussionmentioning

confidence: 99%

Natural and Enantiopure Alkylglycerols as Antibiofilms Against Clinical Bacterial Isolates and Quorum Sensing Inhibitors of Chromobacterium violaceum ATCC 12472

et al. 2021

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Resistance mechanisms occur in almost all clinical bacterial isolates and represent one of the most worrisome health problems worldwide. Bacteria can form biofilms and communicate through quorum sensing (QS), which allow them to develop resistance against conventional antibiotics. Thus, new therapeutic candidates are sought. We focus on alkylglycerols (AKGs) because of their recently discovered quorum sensing inhibition (QSI) ability and antibiofilm potential. Fifteen natural enantiopure AKGs were tested to determine their effect on the biofilm formation of other clinical bacterial isolates, two reference strains and their QSI was determined using Chromobacterium violaceum ATCC 12472. The highest biofilm inhibition rates (%) and minimum QS inhibitory concentration were determined by a microtiter plate assay and ciprofloxacin was used as the standard antibiotic. At subinhibitory concentrations, each AKG reduced biofilm formation in a concentration-dependent manner against seven bacterial isolates, with values up to 97.2%. Each AKG displayed QSI at different levels of ability without affecting the growth of C. violaceum. AKG (2S)-3-O-(cis-13’-docosenyl)-1,2-propanediol was the best QS inhibitor (20 μM), while (2S)-3-O-(cis-9’-hexadecenyl)-1,2-propanediol was the least effective (795 μM). The results showed for the first time the QSI activity of this natural AKG series and suggest that AKGs could be promising candidates for further studies on preventing antimicrobial resistance.

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“…Although natural products and their derivatives have antimicrobial potential, they are still limited as anti-biofilm agents. 56 To find effective agents to prevent and control biofilm, researchers have started to evaluate small molecules of secondary metabolites that are produced by organisms as a protective response to the external environment. 57 , 58 For microorganisms, the secretion of secondary metabolites is a means to compete with other species for resources in the living environments.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Anti-Biofilm Capability of Cordycepin Against Candida albicans

Wang¹,

Pei²,

Lou³

et al. 2021

IDR

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Introduction The opportunistic pathogen Candida albicans can form biofilms, resulting in drug resistance with great risk to medical treatment. Methodology We investigated the ability of C. albicans to form biofilms on different materials, as well as the inhibitory and eradicating effects of cordycepin on biofilm. The action mechanism of cordycepin against biofilm was studied by crystal violet staining, XTT [2, 3-bis (2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] reduction method, phenol-sulfuric acid method, cellular superficial hydrophobicity (CSH) assay, and confocal laser scanning microscope observation. We also evaluated the acute toxicity of cordycepin in vivo. Results The results showed facile formation of biofilms by C. albicans on polypropylene. The 50% minimum inhibitory concentration (MIC 50 ) of cordycepin was 0.062 mg/mL. A concentration of 0.125 mg/mL significantly decreased biofilm formation, metabolic activity, secretion of extracellular polysaccharides, and relative CSH. Cordycepin could inhibit biofilm formation at low concentration without affecting fungal growth. In addition, cordycepin effectively eradicated 59.14% of mature biofilms of C. albicans at a concentration of 0.5 mg/mL. For acute toxicity, the LD 50 (50% of lethal dose) of cordycepin was determined as higher than 500 mg/kg for mice. Conclusion The results of this study show that cordycepin significantly inhibited and eradicated biofilms by decreasing metabolic activity, the ratio of living cells, the hydrophobicity, and damaging the extracellular polysaccharides of biofilm. These findings should facilitate more effective application of cordycepin and suggest a new direction for the treatment of fungal infections.

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Natural products as inspiration for the development of bacterial antibiofilm agents

Abstract:
Synthetic and medicinal chemistry are important tools in the development of more potent, more accessible, or more pharmacologically favorable derivatives of anti-biofilm natural products, in addition to facilitating structure confirmation and understanding of mechanistic pathways.

Cited by 107 publications

References 207 publications

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

Natural and Enantiopure Alkylglycerols as Antibiofilms Against Clinical Bacterial Isolates and Quorum Sensing Inhibitors of Chromobacterium violaceum ATCC 12472

Evaluation of Anti-Biofilm Capability of Cordycepin Against Candida albicans

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Natural products as inspiration for the development of bacterial antibiofilm agents

Abstract: Synthetic and medicinal chemistry are important tools in the development of more potent, more accessible, or more pharmacologically favorable derivatives of anti-biofilm natural products, in addition to facilitating structure confirmation and understanding of mechanistic pathways.

Cited by 107 publications

References 207 publications

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

Chicory Extracts and Sesquiterpene Lactones Show Potent Activity against Bacterial and Fungal Pathogens

Natural and Enantiopure Alkylglycerols as Antibiofilms Against Clinical Bacterial Isolates and Quorum Sensing Inhibitors of Chromobacterium violaceum ATCC 12472

Evaluation of Anti-Biofilm Capability of Cordycepin Against Candida albicans

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Product

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Abstract:
Synthetic and medicinal chemistry are important tools in the development of more potent, more accessible, or more pharmacologically favorable derivatives of anti-biofilm natural products, in addition to facilitating structure confirmation and understanding of mechanistic pathways.