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Research article
In vitro and in situ study on characterizationand mechanismofthe intestinal absorptionof 2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glucoside
Yunxia Li
Corresponding Author
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This work is licensed under a CC BY 4.0 License. Read Full License
View the published version at BMC Pharmacology and Toxicology.
Background: 2,3,5,4'-tetrahydroxystilbence-2-O-β-D-glucoside(TSG) is a polyhydroxyphenolic compound, which exhibited a broad spectrum of pharmacological activities, such asanti-inflammatory, anti-depression, anti-oxidation and anti-atherosclerosis.However, the compound had poor bioavailability and the underlying absorption mechanisms had not been studied. Therefore, the purpose of this study was to investigate the intestinal absorption mechanism of TSG. Methods: This study used Caco-2 cell monolayer model and single-passintestinal perfusion modelto explore the gastrointestinal absorption mechanisms of TSG. The effects of basic parameters such as drug concentration, time and pH on the intestinal absorption of TSG were analyzed by high performance liquid chromatography.The absorption susceptibility of TSG to three inhibitors, P-gp inhibitors verapamil hydrochloride and quinidine, and MRP2 inhibitor probenecid were also assessed.
Results: TSG was poorly absorbed in the intestines and the absorption of TSG in stomach is much higher than that in intestine. Both in vitro and in situ experiments showed that the absorption of TSG was saturated with increasing concentration and it was better absorbed in a weakly acidic environment pH 6.4. Moreover, TSG interacts with P-gp and MRP2, and TSG was not only the substrate of the P-gp and MRP2, but also affected the expression of P-gp and MRP2.
Conclusions: It wasconcluded that the gastrointestinalabsorption mechanisms ofTSG involved processes passive transport and the participation ofefflux transporters.
Keywords
2,3,5,4'-tetrahydroxystilbence-2-O-β-D-glucoside, Absorption mechanism, Caco-2 cell, Intestinal perfusion, P-gp, MRP2
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CURRENT STATUS: Published
Version 3
Posted 09 Jan, 2020
Published
On 22 Jan, 2020
No community comments so far
Editorial decision: Accept
On 08 Jan, 2020
Editor assigned
On 06 Jan, 2020
Submission checks complete
On 05 Jan, 2020
Editor invited
On 05 Jan, 2020
No comments provided
Editorial decision: Minor revision
On 03 Jan, 2020
Reviewers invited
Invitations sent on 01 Nov, 2019
Editor assigned
On 29 Oct, 2019
Submission checks complete
On 28 Oct, 2019
Editor invited
On 28 Oct, 2019
No comments provided
Review #2 received
Received 22 Oct, 2019
Editorial decision: Minor revision
On 22 Oct, 2019
Review #1 received
Received 20 Oct, 2019
Reviewer #2 agreed
On 08 Oct, 2019
Reviewer #1 agreed
On 06 Oct, 2019
Reviewers invited
Invitations sent on 05 Oct, 2019
Editor assigned
On 18 Sep, 2019
Submission checks complete
On 17 Sep, 2019
Editor invited
On 17 Sep, 2019
Metrics
Comments: 0
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This preprint is under consideration at BMC Pharmacology and Toxicology. A preprint is a preliminary version of a manuscript that has not completed peer review at a journal. Research Square does not conduct peer review prior to posting preprints. The posting of a preprint on this server should not be interpreted as an endorsement of its validity or suitability for dissemination as established information or for guiding clinical practice.
Learn more about In Review
Research article
In vitro and in situ study on characterizationand mechanismofthe intestinal absorptionof 2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glucoside
Yunxia Li
Corresponding Author
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
Peer Review Timeline
CURRENT STATUS: Published
Version 3
Posted 09 Jan, 2020
Published
On 22 Jan, 2020
No community comments so far
Editorial decision: Accept
On 08 Jan, 2020
Editor assigned
On 06 Jan, 2020
Submission checks complete
On 05 Jan, 2020
Editor invited
On 05 Jan, 2020
No comments provided
Editorial decision: Minor revision
On 03 Jan, 2020
Reviewers invited
Invitations sent on 01 Nov, 2019
Editor assigned
On 29 Oct, 2019
Submission checks complete
On 28 Oct, 2019
Editor invited
On 28 Oct, 2019
No comments provided
Review #2 received
Received 22 Oct, 2019
Editorial decision: Minor revision
On 22 Oct, 2019
Review #1 received
Received 20 Oct, 2019
Reviewer #2 agreed
On 08 Oct, 2019
Reviewer #1 agreed
On 06 Oct, 2019
Reviewers invited
Invitations sent on 05 Oct, 2019
Editor assigned
On 18 Sep, 2019
Submission checks complete
On 17 Sep, 2019
Editor invited
On 17 Sep, 2019
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
License:
This work is licensed under a CC BY 4.0 License. Read Full License
View the published version at BMC Pharmacology and Toxicology.
Background: 2,3,5,4'-tetrahydroxystilbence-2-O-β-D-glucoside(TSG) is a polyhydroxyphenolic compound, which exhibited a broad spectrum of pharmacological activities, such asanti-inflammatory, anti-depression, anti-oxidation and anti-atherosclerosis.However, the compound had poor bioavailability and the underlying absorption mechanisms had not been studied. Therefore, the purpose of this study was to investigate the intestinal absorption mechanism of TSG. Methods: This study used Caco-2 cell monolayer model and single-passintestinal perfusion modelto explore the gastrointestinal absorption mechanisms of TSG. The effects of basic parameters such as drug concentration, time and pH on the intestinal absorption of TSG were analyzed by high performance liquid chromatography.The absorption susceptibility of TSG to three inhibitors, P-gp inhibitors verapamil hydrochloride and quinidine, and MRP2 inhibitor probenecid were also assessed.
Results: TSG was poorly absorbed in the intestines and the absorption of TSG in stomach is much higher than that in intestine. Both in vitro and in situ experiments showed that the absorption of TSG was saturated with increasing concentration and it was better absorbed in a weakly acidic environment pH 6.4. Moreover, TSG interacts with P-gp and MRP2, and TSG was not only the substrate of the P-gp and MRP2, but also affected the expression of P-gp and MRP2.
Conclusions: It wasconcluded that the gastrointestinalabsorption mechanisms ofTSG involved processes passive transport and the participation ofefflux transporters.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7