Eugenol and Derivatives Activity Against
            <i>Mycobacterium Tuberculosis</i>
            , Nontuberculous Mycobacteria and Other Bacteria

Almeida, Aryadne Larissa de; Caleffi-Ferracioli, Katiany Rizzieri; Scodro, Regiane Bertin de Lima; Baldin, Vanessa Pietrowski; Montaholi, Débora C; Spricigo, Luiza F; Nakamura-Vasconcelos, Sandra Sayuri; Hegeto, Laíse Adriane; Sampiron, Eloísa G; Costacurta, Giovana Ferreira; Yamazaki, Diego Alberto dos Santos; Gauze, Gisele F.; Siqueira, Vera Ld; Cardoso, Rosilene Fressatti

doi:10.2217/fmb-2018-0333

Cited by 29 publications

(21 citation statements)

References 31 publications

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“…Furthermore, eugenol damages the cell membrane and biofilm production and causes leakage of the cell contents (Yadav et al, 2015). Several studies suggest that eugenol has different ties to maintain its inhibitory activity against pathogens and combine with anti-tuberculosis drugs (de Almeida et al, 2019). Studies of A.…”

Section: Eugenolmentioning

confidence: 99%

From plants to antimicrobials: Natural products against bacterial membranes

Nourbakhsh

Lotfalizadeh

Badpeyma

et al. 2021

Phytotherapy Research

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Bacterial membrane barrier provides a cytoplasmic environment for organelles of bacteria. The membrane is composed of lipid compounds containing phosphatide protein and a minimal amount of sugars, and is responsible for intercellular transfers of chemicals. Several antimicrobials have been found that affect bacterial cytoplasmic membranes. These compounds generally disrupt the organization of the membrane or perforate it. By destroying the membrane, the drugs can permeate and replace the effective macromolecules necessary for cell life. Furthermore, they can disrupt electrical gradients of the cells through impairment of the membrane integrity. In recent years, considering the spread of microbial resistance and the side effects of antibiotics, natural antimicrobial compounds have been studied by researchers extensively.These molecules are the best alternative for controlling bacterial infections and reducing drug resistance due to the lack of severe side effects, low cost of production, and biocompatibility. Better understanding of the natural compounds' mechanisms against bacteria provides improved strategies for antimicrobial therapies. In this review, natural products with antibacterial activities focusing on membrane damaging mechanisms were described. However, further high-quality research studies are needed to confirm the clinical efficacy of these natural products.

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Section: Eugenolmentioning

confidence: 99%

From plants to antimicrobials: Natural products against bacterial membranes

Nourbakhsh

Lotfalizadeh

Badpeyma

et al. 2021

Phytotherapy Research

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“…As a preliminary step to the analysis of the anti-amoebic activity of the synthetic compounds on the intestinal and hepatic tissue slices, their possible cytotoxicity on Vero (ATTC®CCL-81™) cell cultures was evaluated. This cell line is used worldwide to assess the in vitro cytotoxic effect and/or selectivity index of different compounds 70–74 . Additionally Vero cells are endorsed by ISO experts to be suitable to test cytotoxicity of certain compounds and materials of medical devices 75 .The cell line was cultured in Eagle’s Minimum Essential Medium supplemented with 10% fetal bovine serum and 1% (v/v) of a mixture of 100 IU/mL penicillin/50 µg/mL streptomycin.…”

Section: Methodsmentioning

confidence: 99%

Development of a Novel Ex-vivo 3D Model to Screen Amoebicidal Activity on Infected Tissue

Guzmán-Delgado

Carranza-Torres

García-Davis

et al. 2019

Sci Rep

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Amoebiasis is a parasitic disease that causes thousands of deaths every year, its adverse effects and resistance to conventional treatments have led to the search of new treatment options, as well as the development of novel screening methods. In this work, we implemented a 3D model of intestine and liver slices from hamsters that were infected ex vivo with virulent E . histolytica trophozoites. Results show preserved histology in both uninfected tissues as well as ulcerations, destruction of the epithelial cells, and inflammatory reaction in intestine slices and formation of micro abscesses, and the presence of amoebae in the sinusoidal spaces and in the interior of central veins in liver slices. The three chemically synthetized compounds T-001, T-011, and T-016, which act as amoebicides in vitro , were active in both infected tissues, as they decreased the number of trophozoites, and provoked death by disintegration of the amoeba, similar to metronidazole. However, compound T-011 induced signs of cytotoxicity to liver slices. Our results suggest that ex vivo cultures of precision-cut intestinal and liver slices represent a reliable 3D approach to evaluate novel amoebicidal compounds, and to simultaneously detect their toxicity, while reducing the number of experimental animals commonly required by other model systems.

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“…abscessus , potential use as an adjuvant) 87 ; the acetamide bridge‐containing E11 (modest in vitro activity, MICs = 12–25 µM against M. abscessus strains; an MmpL3 inhibitor) 219 ; a salicylanilide carbamate derivative (MIC = 0.2 µM against M. abscessus , but high cytotoxicity) 222 ; the eugenol‐core‐containing compound EUG(3) (MIC < 0.97 µg/mlm against M. abscessus subs. massiliense ) 223 ; and the 3‐amino‐5‐(1 H ‐indol‐6‐yl)‐1 H ‐pyrazole‐based compound AW7 (MIC ~50 µM against M. abscessus subsp. abscessus ) 41 (Figure 11).…”

Section: Interesting Early‐stage Small Molecules Active Against M Abscessus: From Bench To Bedside?mentioning

confidence: 99%

Pipeline of anti‐Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities

Egorova¹,

Jackson

Gavrilyuk³

et al. 2021

Medicinal Research Reviews

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The Mycobacterium abscessus complex is a group of emerging pathogens that are difficult to treat. There are no effective drugs for successful M. abscessus pulmonary infection therapy, and existing drug regimens recommended by the British or the American Thoracic Societies are associated with poor clinical outcomes. Therefore, novel antibacterial drugs are urgently needed to contain this global threat. The current anti‐M. abscessus small‐molecule drug development process can be enhanced by two parallel strategies—discovery of compounds from new chemical classes and commercial drug repurposing. This review focuses on recent advances in the finding of novel small‐molecule agents, and more particularly focuses on the activity, mode of action and structure–activity relationship of promising inhibitors from five different chemical classes—benzimidazoles, indole‐2‐carboxamides, benzothiazoles, 4‐piperidinoles, and oxazolidionones. We further discuss some other interesting small molecules, such as thiacetazone derivatives and benzoboroxoles, that are in the early stages of drug development, and summarize current knowledge about the efficacy of repurposable drugs, such as rifabutin, tedizolid, bedaquiline, and others. We finally review targets of therapeutic interest in M. abscessus that may be worthy of future drug and adjunct therapeutic development.

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Eugenol and Derivatives Activity Against Mycobacterium Tuberculosis , Nontuberculous Mycobacteria and Other Bacteria

Cited by 29 publications

References 31 publications

From plants to antimicrobials: Natural products against bacterial membranes

From plants to antimicrobials: Natural products against bacterial membranes

Development of a Novel Ex-vivo 3D Model to Screen Amoebicidal Activity on Infected Tissue

Pipeline of anti‐Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities

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