Evaluation of Tributyrin Lipid Emulsion with Affinity to Low-Density Lipoprotein: Pharmacokinetics in Adult Male Wistar Rats and Cellular Activity on Caco-2 and HepG2 Cell Lines
The Journal of Pharmacology and Experimental Therapeutics, ISSN: 0022-3565, Vol: 316, Issue: 1, Page: 62-70
2006
- 24Citations
- 16Captures
Metric Options: CountsSelecting the 1-year or 3-year option will change the metrics count to percentiles, illustrating how an article or review compares to other articles or reviews within the selected time period in the same journal. Selecting the 1-year option compares the metrics against other articles/reviews that were also published in the same calendar year. Selecting the 3-year option compares the metrics against other articles/reviews that were also published in the same calendar year plus the two years prior.
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations24
- Citation Indexes24
- 24
- CrossRef20
- Captures16
- Readers16
- 16
Article Description
The tributyrin lipid emulsion was proved to be able to bind to low-density lipoprotein (LDL) in vitro. The aim of this study was to investigate the pharmacokinetics of the emulsion in vivo and the cellular activity in vitro. The pharmacokinetics of tributyrin and its metabolite, butyrate, was evaluated in male Wistar rats after administration with pure tributyrin or tributyrin emulsion. After oral administration, maximal plasma concentration ( C max ), time to reach maximal plasma concentration ( T max ), and elimination half-life ( T 1/2 ) of butyrate were 87.6 μM and 25.3 and 63.0 min, respectively, for the pure tributyrin compared with 1344.5 μM and 8.5 and 19.8 min for the 10% (v/v) tributyrin emulsion. C max and mean residence time of tributyrin were 2.74 μM and 87.9 min and 4.2 μM and 132.0 min for pure tributyrin and 10% emulsion, respectively. The bioavailabilities of the pure tributyrin versus tributyrin emulsion were 15.3 versus 65.7% and 34.9 versus 64.5% calculated from butyrate and tributyrin, respectively. After the rats were treated with 17α-ethynylestradiol (an LDL receptor up-regulator), the distribution volumes calculated from both butyrate and tributyrin were significantly increased after oral administration or infusion of the 10% tributyrin emulsion. The increased distribution volume after coadministration with a LDL receptor up-regulator suggested the increased uptake of tributyrin/butyrate by tissues with increased expression of LDL receptors. The selective uptake of the emulsion by the cellular LDL receptors was further confirmed by testing the cellular viability in the presence of competing LDL. The viable cells can reach 92% of control at IC 50 in Caco-2 and 77% in HepG2 incubated with emulsion in the presence of LDL.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0022356524324024; http://dx.doi.org/10.1124/jpet.105.090464; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=29244471995&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/16188956; https://linkinghub.elsevier.com/retrieve/pii/S0022356524324024; https://dx.doi.org/10.1124/jpet.105.090464; https://jpet.aspetjournals.org/content/316/1/62
Elsevier BV
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