In vitro effects of rebaudioside A, stevioside and steviol on porcine cytochrome p450 expression and activity

Thøgersen, Rebekka; Petrat-Melin, Bjørn; Zamaratskaia, Galia; Grevsen, Kai; Young, Jette F.; Rasmussen, Martin Krøyer

doi:10.1016/j.foodchem.2018.03.055

Cited by 11 publications

(5 citation statements)

References 41 publications

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“…The following conditions were used: 2 min at 50 • C, 10 min at 95 • C, followed by 40 cycles at 95 • C for 15 s and 1 min at 60 • C. Specific primer and probes were designed using pig-specific sequences obtained from Ensemble (Sscrofa 11.1), according to Knudsen et al 2018. [46] The primer and probe sequences of CYP1A2, CYP2B22, CYP2E1, and CYP3A29, and β-actin have been given earlier [65], and the remaining sequences are given in Supplementary Material S1, Table S3.…”

Section: Real-time Polymerase Chain Reaction (Rt Pcr)mentioning

confidence: 99%

Background Diet Influences TMAO Concentrations Associated with Red Meat Intake without Influencing Apparent Hepatic TMAO-Related Activity in a Porcine Model

et al. 2020

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Red meat has been associated with an increased cardiovascular disease (CVD) risk, possibly through gut microbial-derived trimethylamine-N-oxide (TMAO). However, previous reports are conflicting, and influences from the background diet may modulate the impact of meat consumption. This study investigated the effect of red and white meat intake combined with two different background diets on urinary TMAO concentration and its association with the colon microbiome in addition to apparent hepatic TMAO-related activity. For 4 weeks, 32 pigs were fed chicken or red and processed meat combined with a prudent or western background diet. 1 H NMR-based metabolomics analysis was conducted on urine samples and hepatic Mrna expression of TMAO-related genes determined. Lower urinary TMAO concentrations were observed after intake of red and processed meat when consumed with a prudent compared to a western background diet. In addition, correlation analyses between urinary TMAO concentrations and relative abundance of colon bacterial groups suggested an association between TMAO and specific bacterial taxa. Diet did not affect the hepatic Mrna expression of genes related to TMAO formation. The results suggest that meat-induced TMAO formation is regulated by mechanisms other than alterations at the hepatic gene expression level, possibly involving modulations of the gut microbiota.

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Section: Real-time Polymerase Chain Reaction (Rt Pcr)mentioning

confidence: 99%

Background Diet Influences TMAO Concentrations Associated with Red Meat Intake without Influencing Apparent Hepatic TMAO-Related Activity in a Porcine Model

et al. 2020

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“…25 Moreover, hepatocyte systems were reported to be more suitable for measuring the activity of UGTs or the expression of both CYPs and UGTs than human liver microsome in vitro systems. 26,27 Thus, using a cocktail compound in hepatocytes (such as L-02 and HepG2 cells) in vitro has been considered a reliable, mature, and rapid approach to determine CYP or UGT activities and expression.…”

Section: Introductionmentioning

confidence: 99%

Stereoisomers of octahydrocurcumin, the hydrogenated metabolites of curcumin, display stereoselective activity on the CYP2E1 enzyme in L-02 cells

et al. 2023

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“…RA is a steviol glycoside -a diterpene with a steviol backbone and mono-and trisaccharide carbohydrate residues at the C13 and C19 positions ( Figure S1). 2 This combination of both hydrophobic diterpene and hydrophilic sugar side chain(s) in its structure allows RA to form micelles in aqueous solutions. Therefore, RA is of considerable clinical interest due to its potential for use as a nanotechnological drug delivery system.…”

Section: Introductionmentioning

confidence: 99%

Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin

Hou

Wang

Zhang

et al. 2019

IJN

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PurposeRebaudioside A (RA) has nanocarrier characteristics that allow it to self-assemble into micelles in aqueous solutions. The purpose of this study was to determine if a self-nanomicellizing solid dispersion based on RA could be utilized as an oral nano-drug delivery system.Materials and methodsCurcumin (Cur) served as a model hydrophobic drug, and a Cur-loaded self-nanomicellizing solid dispersion based on RA (RA-Cur) was formulated. The properties of RA-Cur in the solid state and in aqueous solution were characterized. The antioxidant activity and mechanism of RA-Cur endocytosis were also investigated. The pharmacokinetics, biodistribution in the intestinal tract, and anti-inflammation properties were also evaluated in vivo.ResultsRA-Cur could be easily fabricated, and it self-assembled into ultrasmall micelles (particle size ~4 nm) in a homogeneous distribution state (polydispersity index <0.2) when dissolved in water. Cur was readily encapsulated into RA micelles and this improved its water solubility (to 14.34±1.66 mg/mL), as well as its in vitro release and membrane permeability. The antioxidant activities of Cur in RA-Cur were also significantly improved. Biodistribution in the intestinal tract confirmed a significant enhancement of Cur absorption in the duodenum, jejunum, and ileum by encapsulation in RA-Cur, and the absorption of RA-Cur was governed by mixed transcytosis mechanisms. Pharmacokinetic tests of RA-Cur in rats revealed a dramatic 19.06-fold enhancement of oral bioavailability when compared to free Cur. More importantly, oral administration of RA-Cur could efficiently ameliorate ulcerative colitis in a mouse model induced by dextran sodium sulfate.ConclusionSelf-nanomicellizing solid dispersions based on RA have great potential as novel oral nano-drug delivery systems for hydrophobic drugs such as Cur.

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In vitro effects of rebaudioside A, stevioside and steviol on porcine cytochrome p450 expression and activity

Cited by 11 publications

References 41 publications

Background Diet Influences TMAO Concentrations Associated with Red Meat Intake without Influencing Apparent Hepatic TMAO-Related Activity in a Porcine Model

Background Diet Influences TMAO Concentrations Associated with Red Meat Intake without Influencing Apparent Hepatic TMAO-Related Activity in a Porcine Model

Stereoisomers of octahydrocurcumin, the hydrogenated metabolites of curcumin, display stereoselective activity on the CYP2E1 enzyme in L-02 cells

Novel self-nanomicellizing solid dispersion based on rebaudioside A: a potential nanoplatform for oral delivery of curcumin

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