Lithocholic acid and derivatives: Antibacterial activity

Nascimento, Patrícia Georgina Garcia do; Lemos, Telma L. G.; Almeida, Macia C. S. de; Souza, Juliana Maria Oliveira; Bizerra, Ayla Márcia Cordeiro; Santiago, Gilvandete Maria Pinheiro; Costa, José Galberto Martins da; Coutinho, Henrique Douglas Melo

doi:10.1016/j.steroids.2015.07.007

Cited by 31 publications

(27 citation statements)

References 37 publications

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“…It binds to VDR[131], has antibacterial activity[132], produces antiproliferative and pro-apoptotic effect on human cancer cell lines[133,134], inhibits proteasome[135], acts as a membrane pore[136] and has anti-aging properties[137]. It is worldwide recognized that 1,25(OH) 2 D 3 is the main stimulator of the intestinal Ca 2+ absorption, and both LCA and 1,25(OH) 2 D 3 are VDR ligands, although they have different VDR binding affinity[138].…”

Section: Antioxidants and Their Molecular Mechanisms For The Preservamentioning

confidence: 99%

Oxidative stress, antioxidants and intestinal calcium absorption

Barboza¹,

Guizzardi²,

Moine³

et al. 2017

WJG

109

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The disequilibrium between the production of reactive oxygen (ROS) and nitrogen (RNS) species and their elimination by protective mechanisms leads to oxidative stress. Mitochondria are the main source of ROS as by-products of electron transport chain. Most of the time the intestine responds adequately against the oxidative stress, but with aging or under conditions that exacerbate the ROS and/or RNS production, the defenses are not enough and contribute to developing intestinal pathologies. The endogenous antioxidant defense system in gut includes glutathione (GSH) and GSH-dependent enzymes as major components. When the ROS and/or RNS production is exacerbated, oxidative stress occurs and the intestinal Ca2+ absorption is inhibited. GSH depleting drugs such as DL-buthionine-S,R-sulfoximine, menadione and sodium deoxycholate inhibit the Ca2+ transport from lumen to blood by alteration in the protein expression and/or activity of molecules involved in the Ca2+ transcellular and paracellular pathways through mechanisms of oxidative stress, apoptosis and/or autophagy. Quercetin, melatonin, lithocholic and ursodeoxycholic acids block the effect of those drugs in experimental animals by their antioxidant, anti-apoptotic and/or anti-autophagic properties. Therefore, they may become drugs of choice for treatment of deteriorated intestinal Ca2+ absorption under oxidant conditions such as aging, diabetes, gut inflammation and other intestinal disorders.

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Section: Antioxidants and Their Molecular Mechanisms For The Preservamentioning

confidence: 99%

Oxidative stress, antioxidants and intestinal calcium absorption

Barboza¹,

Guizzardi²,

Moine³

et al. 2017

WJG

109

View full text Add to dashboard Cite

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“…They typically stay conjugated with taurine or glycine in the liver forming bile salts that serve as surfactants to solubilize dietary lipids and fats by the formation of micelles allowing digestion of food. Bile acids have been utilized in many areas including gene delivery [ 19 , 20 ], drug delivery [ 21 ], sensing [ 22 ], polymeric gels [ 23 ], antimicrobial agents [ [24] , [25] , [26] ] and other biological applications [ 27 ].…”

Section: Introductionmentioning

confidence: 99%

Facially amphiphilic polyionene biocidal polymers derived from lithocholic acid

Ganewatta

Rahman

Mercado

et al. 2018

Bioactive Materials

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Bacterial infections have become a global issue that requires urgent attention, particularly regarding to emergence of multidrug resistant bacteria. We developed quaternary amine-containing antimicrobial poly(bile acid)s that contain a hydrophobic core of lithocholic acid in the main-chain. Interestingly, by choosing appropriate monomers, these cationic polymers can form core-shell micelles. These polymers exhibited biocidal activity against both Gram-positive and Gram-negative bacterial species. It is demonstrated that the micelles can deliver hydrophobic antibiotics that functionally have dual antimicrobial activities. Cytotoxicity assays against HeLa cells showed dosage-dependent toxicity for polymers with longer linkers.

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“…Notably, this bile acid increased the bactericidal potency of clarithromycin up to 32 times against the H. pylori clarithromycin-resistant strain ATCC 700684. Previous studies have demonstrated synergistic action of LCA and its derivatives on the activities of other conventional antibiotics such as aminoglycosides [53].…”

Section: Discussionmentioning

confidence: 98%

Small Molecule Inhibitors of the Response Regulator ArsR Exhibit Bactericidal Activity against Helicobacter pylori

et al. 2020

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Helicobacter pylori is considered the most prevalent bacterial pathogen in humans. The increasing antibiotic resistance evolved by this microorganism has raised alarm bells worldwide due to the significant reduction in the eradication rates of traditional standard therapies. A major challenge in this antibiotic resistance crisis is the identification of novel microbial targets whose inhibitors can overcome the currently circulating resistome. In the present study, we have validated the use of the essential response regulator ArsR as a novel and promising therapeutic target against H. pylori infections. A high-throughput screening of a repurposing chemical library using a fluorescence-based thermal shift assay identified several ArsR binders. At least four of these low-molecular weight compounds noticeably inhibited the DNA binding activity of ArsR and showed bactericidal effects against antibiotic-resistant strains of H. pylori. Among the ArsR inhibitors, a human secondary bile acid, lithocholic acid, quickly destroyed H. pylori cells and exhibited partial synergistic action in combination with clarithromycin or levofloxacin, while the antimicrobial effect of this compound against representative members of the normal human microbiota such as Escherichia coli and Staphylococcus epidermidis appeared irrelevant. Our results enhance the battery of novel therapeutic tools against refractory infections caused by multidrug-resistant H. pylori strains.

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Lithocholic acid and derivatives: Antibacterial activity

Cited by 31 publications

References 37 publications

Oxidative stress, antioxidants and intestinal calcium absorption

Oxidative stress, antioxidants and intestinal calcium absorption

Facially amphiphilic polyionene biocidal polymers derived from lithocholic acid

Small Molecule Inhibitors of the Response Regulator ArsR Exhibit Bactericidal Activity against Helicobacter pylori

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