Natural compounds and extracts as novel antimicrobial agents

Guglielmi, Paolo; Pontecorvi, Virginia; Rotondi, Giulia

doi:10.1080/13543776.2020.1853101

Cited by 55 publications

(37 citation statements)

References 41 publications

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“…Among the first cluster of alkyloxy derivatives (2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14), the MIC results demonstrated no or weak efficacy against all the strains as well as their parent compound, despite the presence of branched alkyl chains, unsaturations or specific functional groups (ketone, carboxylic acid, ethyl ester). Only three derivatives (3,9,12) with linear and increasing alkyl chains (Et, n-Pr, n-Bu) presented improved MIC values with respect to thymol against some clinical isolates (MIC/MBC = 16 µg/mL).…”

Section: Anti-helicobacter Pylori Activity and Structure-activity Relmentioning

confidence: 99%

“…The triple therapy based on the administration on proto-pump inhibitor and two antibiotics has been considered the standard therapy for many years, however, the increasing rate of triple-therapy failure was registered in many countries as well as the spreading of H. pylori antibiotic resistance. In this context, novel compounds such as components of essential oils endowed with alternative mechanisms of action and the ability to disaggregate lipidic multilayer structures are strongly suggested [7]. More in detail, thymol derivatives have been proposed as inhibitors of CagA and VacA (cytotoxin-associated gene A and vacuolization cytotoxin) oncoproteins of Helicobacter pylori [8] and, recently, Bkhaitan et al also prepared a thymol-metronidazole ester hybrid and assessed its discrete anti-Helicobacter pylori activity and limited cytotoxicity on normal cell lines [9].…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Evaluation of Thymol-Based Synthetic Derivatives as Dual-Action Inhibitors against Different Strains of H. pylori and AGS Cell Line

Sisto¹,

Carradori²,

Guglielmi³

et al. 2021

Molecules

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Following a similar approach on carvacrol-based derivatives, we investigated the synthesis and the microbiological screening against eight strains of H. pylori, and the cytotoxic activity against human gastric adenocarcinoma (AGS) cells of a new series of ether compounds based on the structure of thymol. Structural analysis comprehended elemental analysis and 1H/13C/19F NMR spectra. The analysis of structure–activity relationships within this molecular library of 38 structurally-related compounds reported that some chemical modifications of the OH group of thymol led to broad-spectrum growth inhibition on all isolates. Preferred substitutions were benzyl groups compared to alkyl chains, and the specific presence of functional groups at para position of the benzyl moiety such as 4-CN and 4-Ph endowed the most anti-H. pylori activity toward all the strains with minimum inhibitory concentration (MIC) values up to 4 µg/mL. Poly-substitution on the benzyl ring was not essential. Moreover, several compounds characterized by the lowest minimum inhibitory concentration/minimum bactericidal concentration (MIC/MBC) values against H. pylori were also tested in order to verify a cytotoxic effect against AGS cells with respect to 5-fluorouracil and carvacrol. Three derivatives can be considered as new lead compounds alternative to current therapy to manage H. pylori infection, preventing the occurrence of severe gastric diseases. The present work confirms the possibility to use natural compounds as templates for the medicinal semi-synthesis.

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Section: Anti-helicobacter Pylori Activity and Structure-activity Relmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of Thymol-Based Synthetic Derivatives as Dual-Action Inhibitors against Different Strains of H. pylori and AGS Cell Line

Sisto¹,

Carradori²,

Guglielmi³

et al. 2021

Molecules

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“…It is demonstrated that numerous antimicrobial phytochemicals have been discovered or better characterized ( 22 , 153 ). Wang et al.…”

Section: The Action Mechanisms Of Phytochemicalsmentioning

confidence: 99%

Pharmacological Applications and Action Mechanisms of Phytochemicals as Alternatives to Antibiotics in Pig Production

Sun

Zhao

et al. 2021

Front. Immunol.

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Antibiotics are widely used for infectious diseases and feed additives for animal health and growth. Antibiotic resistant caused by overuse of antibiotics poses a global health threat. It is urgent to choose safe and environment-friendly alternatives to antibiotics to promote the ecological sustainable development of the pig industry. Phytochemicals are characterized by little residue, no resistance, and minimal side effects and have been reported to improve animal health and growth performance in pigs, which may become a promising additive in pig production. This paper summarizes the biological functions of recent studies of phytochemicals on growth performance, metabolism, antioxidative capacity, gut microbiota, intestinal mucosa barrier, antiviral, antimicrobial, immunomodulatory, detoxification of mycotoxins, as well as their action mechanisms in pig production. The review may provide the theoretical basis for the application of phytochemicals functioning as alternative antibiotic additives in the pig industry.

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“…These limitations include high cytotoxicity, short-term antimicrobial activity, effectiveness against a limited spectrum of bacterial strains, and acquired and/or developed bacterial resistance. Confronted by these obstacles, natural compounds hold promise with their featured properties such as broad-scale structural diversity, antimicrobial mechanisms through non-specific interaction against a large spectrum of pathogens, interference with multiple targets, rarer side-effects, and relatively low costs [ 13 ]. Hence, the bioactivity of natural compound-based coating materials on polymeric surfaces has been widely recognized in recent years, providing vital opportunities in the development of antimicrobial performance.…”

Section: Introductionmentioning

confidence: 99%

Surface Functionalization of Ureteral Stents-Based Polyurethane: Engineering Antibacterial Coatings

et al. 2022

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Bacterial colonization of polyurethane (PU) ureteral stents usually leads to severe and challenging clinical complications. As such, there is an increasing demand for an effective response to this unmet medical challenge. In this study, we offer a strategy based on the functionalization of PU stents with chitosan-fatty acid (CS-FA) derivatives to prevent bacterial colonization. Three different fatty acids (FAs), namely stearic acid (SA), oleic acid (OA), and linoleic acid (LinA), were successfully grafted onto chitosan (CS) polymeric chains. Afterwards, CS-FA derivatives-based solutions were coated on the surface of PU stents. The biological performance of the modified PU stents was evaluated against the L929 cell line, confirming negligible cytotoxicity of the developed coating formulations. The antibacterial potential of coated PU stents was also evaluated against several microorganisms. The obtained data indicate that the base material already presents an adequate performance against Staphylococcus aureus, which slightly improved with the coating. However, the performance of the PU stents against Gram-negative bacteria was markedly increased with the surface functionalization approach herein used. As a result, this study reveals the potential use of CS-FA derivatives for surface functionalization of ureteral PU stents and allows for conjecture on its successful application in other biomedical devices.

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Natural compounds and extracts as novel antimicrobial agents

Cited by 55 publications

References 41 publications

Synthesis and Evaluation of Thymol-Based Synthetic Derivatives as Dual-Action Inhibitors against Different Strains of H. pylori and AGS Cell Line

Synthesis and Evaluation of Thymol-Based Synthetic Derivatives as Dual-Action Inhibitors against Different Strains of H. pylori and AGS Cell Line

Pharmacological Applications and Action Mechanisms of Phytochemicals as Alternatives to Antibiotics in Pig Production

Surface Functionalization of Ureteral Stents-Based Polyurethane: Engineering Antibacterial Coatings

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