Merulinic acid C overcomes gentamicin resistance in Enterococcus faecium

Rodrigues-Costa, Fernanda; Slivinski, Juliano; Ióca, Laura P.; Bertonha, Ariane F.; Felício, Rafael de; Cunha, Marcos Guilherme da; Madeira, Paulo Vinicius da Mata; Cauz, Ana Carolina Guimarães; Trindade, Daniel Maragno; Freire, Vítor F.; Röpke, Cristina Dislich; Gales, Ana Cristina; Brocchi, Marcelo; Ferreira, Antônio G.; Gueiros‐Filho, Frederico J.; Trivella, Daniela Barretto Barbosa; Berlinck, Roberto G. S.; Dessen, Andréa

doi:10.1016/j.bioorg.2020.103921

Cited by 3 publications

(2 citation statements)

References 47 publications

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“…Terpenoids as merulinic acid and a ursolic acid glycoside, among others, damaged the bacterial cell wall [34, 35]. Berberine can be considered a drug lead for efflux pump inhibition, such as berberine, zeylenol and bulgecin A, see Table 4 and references therein.…”

Section: Resultsmentioning

confidence: 99%

“…Among the reported mechanisms of action that renders synergistic effects of NPs and CAAs are the interaction of NPs with bacteria virulent factors. Which included inhibition of toxin production, biofilm formation, interference with quorum sensing molecules, inhibition of penicillin binding proteins, pump efflux inhibitors and pore forming compounds [148, 149, 150, 151, 49, 152, 50, 34, 35].…”

Section: Resultsmentioning

confidence: 99%

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Perspectives on the enhancement of commercially available antibiotics by natural products

Nitsch-Velasquez

Segura²,

Barrios

et al. 2022

Preprint

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Background: Opportunistic resistant bacteria are health and economically relevant in the health care systems and in industries worldwide, especially in the so-called resistant bacteria era (RBE). Enhancing the activity of commercially available antibiotics (CAAs) with di erent types of natural products (NPs) is a successful antimicrobial strategy, for instance the amoxicillin and clavulanate mixture. Objective: To nd research trends in this eld during 2015-2020 and to detect potential drug hits with potential to diversify formulations and materials design that can be useful to manage the RBE. Systematic review results: It yielded 190 reports of synergistic e ects of CAAs and NPs. The analyzed variables were: a) natural products origin: plant family, genera, secondary metabolite type; b) strains: +/- Gram, genera, most frequent species, application eld; and c) CAAs: family, most frequent CAAs. The families with potential to have more bioactive species were Apocynaceae, Rubiaceae, Euphorbiaceae (Isbio factor). Lonicera had the highest reports amount. Polyphenols and avonoids were the majority of pure NPs tested. Several potential drug hits for antibiotic activity enhancement at synergistic level were identi ed together with potential mechanisms of action: berberine (drug e ux inhibitor{DEI, bio lm inhibitor{BI), curcumin (BI), essential oils (BI), 3-o-metyl-butylgallato (inhibition of fatty acid saturation), among others. About the half of the tested strains were gram positive, being Methicillin Resistant Staphylococcus aureus (MRSA) the most frequently tested. Escherichia coli was the gram negative strain most frequently reported, including enterotoxigenic and extended spectrum beta-lactamases producers. The growth of other foodborne genera strains, such as Listeria and Salmonella, were also inhibited. Aminoglycosides were the family most reported, with gentamicin as the most commonly studied. Conclusions: NPs as either as plant extracts from a variety of families, or as puri ed compounds specially avonoids and polyphenols, have shown e ective results to enhance the antibiotic activity of CAAs against gram positive and negative strains relevant to HC and FI. Their mechanisms of action are starting to be determined, as the case EPIs and BIs. Further research is needed to achieve co-formulations and materials design useful for those elds, that can certainly be positively impacted by pursuing this strategy.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Perspectives on the enhancement of commercially available antibiotics by natural products

Nitsch-Velasquez

Segura²,

Barrios

et al. 2022

Preprint

View full text Add to dashboard Cite

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Recent progress in the evaluation of secondary metabolites from Basidiomycota

Sum,

Ebada,

Clement Matasyoh

et al. 2023

Current Research in Biotechnology

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Chemical Elicitors Induce Rare Bioactive Secondary Metabolites in Deep-Sea Bacteria under Laboratory Conditions

et al. 2021

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Bacterial genome sequencing has revealed a vast number of novel biosynthetic gene clusters (BGC) with potential to produce bioactive natural products. However, the biosynthesis of secondary metabolites by bacteria is often silenced under laboratory conditions, limiting the controlled expression of natural products. Here we describe an integrated methodology for the construction and screening of an elicited and pre-fractionated library of marine bacteria. In this pilot study, chemical elicitors were evaluated to mimic the natural environment and to induce the expression of cryptic BGCs in deep-sea bacteria. By integrating high-resolution untargeted metabolomics with cheminformatics analyses, it was possible to visualize, mine, identify and map the chemical and biological space of the elicited bacterial metabolites. The results show that elicited bacterial metabolites correspond to ~45% of the compounds produced under laboratory conditions. In addition, the elicited chemical space is novel (~70% of the elicited compounds) or concentrated in the chemical space of drugs. Fractionation of the crude extracts further evidenced minor compounds (~90% of the collection) and the detection of biological activity. This pilot work pinpoints strategies for constructing and evaluating chemically diverse bacterial natural product libraries towards the identification of novel bacterial metabolites in natural product-based drug discovery pipelines.

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Merulinic acid C overcomes gentamicin resistance in Enterococcus faecium

Cited by 3 publications

References 47 publications

Perspectives on the enhancement of commercially available antibiotics by natural products

Perspectives on the enhancement of commercially available antibiotics by natural products

Recent progress in the evaluation of secondary metabolites from Basidiomycota

Chemical Elicitors Induce Rare Bioactive Secondary Metabolites in Deep-Sea Bacteria under Laboratory Conditions

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