Antifungal evaluation of cholic acid and its derivatives on Candida albicans by microcalorimetry and chemometrics

Kong, Weijun; Wang, Jiabo; Xing, Xiaoyan; Yan, Zhao; Zang, Qingce; Zhang, Ping; Jin, Cheng; Li, Zulun; Liu, Wei

doi:10.1016/j.aca.2011.01.050

Cited by 19 publications

(4 citation statements)

References 36 publications

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“…Bile salt hydrolases have been associated to bile stress resistance in Lactobacillus and Bifidobacterium (Grill et al, 2000 ; McAuliffe et al, 2005 ; Lin et al, 2014 ) and implicated as a mechanism for host-microbe signaling (Zhou and Hylemon, 2014 ; Song et al, 2015 ; McMillin et al, 2016 ). These enzymes hydrolyze conjugated bile salts generating unconjugated bile acids, which often function as a signaling molecules to host cells and have strong anti-microbial effects (Sytnik et al, 1978 ; Grill et al, 2000 ; Schmidt et al, 2001 ; Kong et al, 2011 ), and an amino acid, which can be utilized by both host and microorganisms for protein synthesis (Ridlon et al, 2006 , 2014 ; Patel et al, 2010 ). Studies have shown that BSHs do not always provide a survival advantage to bacteria exposed to bile (Fang et al, 2009 ), suggesting that BSH activity differs between microorganisms.…”

Section: Discussionmentioning

confidence: 99%

Intra-species Genomic and Physiological Variability Impact Stress Resistance in Strains of Probiotic Potential

Arnold

Simpson²,

Roach

et al. 2018

Front. Microbiol.

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Large-scale microbiome studies have established that most of the diversity contained in the gastrointestinal tract is represented at the strain level; however, exhaustive genomic and physiological characterization of human isolates is still lacking. With increased use of probiotics as interventions for gastrointestinal disorders, genomic and functional characterization of novel microorganisms becomes essential. In this study, we explored the impact of strain-level genomic variability on bacterial physiology of two novel human Lactobacillus rhamnosus strains (AMC143 and AMC010) of probiotic potential in relation to stress resistance. The strains showed differences with known probiotic strains (L. rhamnosus GG, Lc705, and HN001) at the genomic level, including nucleotide polymorphisms, mutations in non-coding regulatory regions, and rearrangements of genomic architecture. Transcriptomics analysis revealed that gene expression profiles differed between strains when exposed to simulated gastrointestinal stresses, suggesting the presence of unique regulatory systems in each strain. In vitro physiological assays to test resistance to conditions mimicking the gut environment (acid, alkali, and bile stress) showed that growth of L. rhamnosus AMC143 was inhibited upon exposure to alkaline pH, while AMC010 and control strain LGG were unaffected. AMC143 also showed a significant survival advantage compared to the other strains upon bile exposure. Reverse transcription qPCR targeting the bile salt hydrolase gene (bsh) revealed that AMC143 expressed bsh poorly (a consequence of a deletion in the bsh promoter and truncation of bsh gene in AMC143), while AMC010 had significantly higher expression levels than AMC143 or LGG. Insertional inactivation of the bsh gene in AMC010 suggested that bsh could be detrimental to bacterial survival during bile stress. Together, these findings show that coupling of classical microbiology with functional genomics methods for the characterization of bacterial strains is critical for the development of novel probiotics, as variability between strains can dramatically alter bacterial physiology and functionality.

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Section: Discussionmentioning

confidence: 99%

Intra-species Genomic and Physiological Variability Impact Stress Resistance in Strains of Probiotic Potential

Arnold

Simpson²,

Roach

et al. 2018

Front. Microbiol.

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“…demonstrated by microcalorimetry. Cholic acid had the strongest effect, followed by glycocholic acid and taurocholic acid [28]. Obviously, this effect does not generally protect against fungal cholangitis or cholecystitis, particularly in patients at high risk.…”

Section: Discussionmentioning

confidence: 95%

Biliary amphotericin B pharmacokinetics and pharmacodynamics in critically ill liver transplant recipients receiving treatment with amphotericin B lipid formulations

Welte¹,

Eschertzhuber²,

Weiler³

et al. 2015

International Journal of Antimicrobial Agents

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Fungal cholangitis is a potentially life-threatening condition. As amphotericin B (AmB) has a broad antimycotic spectrum, in this study its biliary penetration and activity was determined in two patients treated with liposomal AmB (L-AmB) and in one patient receiving AmB colloidal dispersion (ABCD). Biliary and plasma AmB levels were quantified by high-performance liquid chromatography after purification by solid-phase extraction. For assessment of biliary AmB activity, isolates of Candida albicans, Candida tropicalis, Candida glabrata and Candida krusei were incubated in porcine bile at AmB concentrations of 0.025-5.00 mg/L. In addition, patient bile samples retrieved for AmB quantification were inoculated with the same Candida strains. Biliary AmB concentrations were lower and displayed a slower rise and decline than plasma levels. The highest penetration ratio, as expressed by the ratio between the area under the AmB concentration-time curve in bile and plasma (liberated AmB) over the sampling period (AUC0-n bile/AUC0-n LI plasma), was 0.28. Proliferation of C. albicans and C. tropicalis in bile was similar to that in culture medium, whereas growth of C. glabrata was diminished and proliferation of C. krusei was absent in bile. In comparison with culture medium, AmB activity decreased in spiked porcine bile. In all but one patient bile sample, fungal growth was delayed or lacking even when AmB was not detectable. However, no fungicidal effect was observed in patient bile at AmB concentrations up to 1.28 mg/L. Thus, a reliable response of fungal cholangitis to treatment with L-AmB or ABCD cannot be anticipated. Biliary AMB concentrations were lower and displayed a slower rise and decline than plasma levels. The highest penetration ratio as expressed by the ratio between the area under the time-AMB-concentration curve in bile and plasma (liberated AMB) over the sampling period (AUC 0-n bile /AUC 0-n LI plasma ) amounted to 0.28. Proliferation of C. albicans and C. tropicalis in bile was similar to that in culture medium whereas growth of C. glabrata was diminished and proliferation of C. krusei was absent in bile. In comparison with medium, AMB activity decreased in spiked porcine bile. In all but one patient bile sample, fungal growth was delayed or lacking, even when AMB was not detectable. However, no fungicidal effect was observed in patient bile at AMB concentrations of up to 1.28 mg/L. Thus, a reliable response of fungal cholangitis to treatment with LAMB or ABCD cannot be anticipated.

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“…Cholic acid (CA), an endogenous small molecule secreted in mammalian bile, plays a pivotal role as a physiological cleanser by efficiently solubilizing dietary fats, fat-soluble vitamins, and cholesterol [24] Due to its ready availability, non-toxic nature, and amphiphilic properties, which facilitate easy adsorption onto hydrophobic particles [25], it plays a crucial role in maintaining metabolic homeostasis as an essential component. Moreover, CA exhibits antifungal properties [26] and has been demonstrated to enhance the oral absorption of Sporanox ® pellets encapsulated in capsules [8,21], which makes it more attractive as a stabilizer for ITZ nanocrystals. In this study, CA was selected as a stabilizer, and a combination of microprecipitation and high-pressure homogenization methods was employed to prepare the nanocrystals of itraconazole (ITZ-Nanos).…”

Section: Introductionmentioning

confidence: 99%

The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer

Chang,

Yang,

Liu

et al. 2024

Molecules

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The aim of this study was to develop cholic-acid-stabilized itraconazole nanosuspensions (ITZ-Nanos) with the objective of enhancing drug dissolution and oral absorption. A laboratory-scale microprecipitation–high-pressure homogenization method was employed for the preparation of the ITZ-Nanos, while dynamic light scattering, transmission electron microscope analysis, X-ray diffraction, differential scanning calorimetry, and high-performance liquid chromatography analysis were utilized to evaluate their physicochemical properties. The absorption and bioavailability of the ITZ-Nanos were assessed using Caco-2 cells and rats, with Sporanox® pellets as a comparison. Prior to lyophilization, the particle size of the ITZ-Nanos measured approximately 225.7 nm. Both X-ray diffraction and differential scanning calorimetry confirmed that the ITZ remained crystalline within the nanocrystals. Compared to the pellets, the ITZ-Nanos exhibited significantly higher levels of supersaturation dissolution and demonstrated enhanced drug uptake by the Caco-2 cells. The AUC(0–t) value for the ITZ-Nanos in rats was 1.33-fold higher than that observed for the pellets. These findings suggest that cholic acid holds promise as a stabilizer for ITZ nanocrystals, as well as potentially other nanocrystals.

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Antifungal evaluation of cholic acid and its derivatives on Candida albicans by microcalorimetry and chemometrics

Cited by 19 publications

References 36 publications

Intra-species Genomic and Physiological Variability Impact Stress Resistance in Strains of Probiotic Potential

Intra-species Genomic and Physiological Variability Impact Stress Resistance in Strains of Probiotic Potential

Biliary amphotericin B pharmacokinetics and pharmacodynamics in critically ill liver transplant recipients receiving treatment with amphotericin B lipid formulations

The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer

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