In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside
Abstract 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 as anti-inflammatory, anti-depression, anti-oxidation and anti-atherosclerosis. However, the compound had poor bioavailab...
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| Format: | Article |
| Language: | English |
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BMC
2020-01-01
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| Series: | BMC Pharmacology and Toxicology |
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| Online Access: | https://doi.org/10.1186/s40360-020-0384-9 |
| _version_ | 1818393381087215616 |
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| author | Cheng Wang Yimeng Zhou Xiaohong Gong Li Zheng Yunxia Li |
| author_facet | Cheng Wang Yimeng Zhou Xiaohong Gong Li Zheng Yunxia Li |
| author_sort | Cheng Wang |
| collection | DOAJ |
| description | Abstract 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 as anti-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-pass intestinal perfusion model to 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 was concluded that the gastrointestinal absorption the most unique active ingredient and considered as the mechanisms of TSG involved processes passive transport and the participation of efflux transporters. |
| first_indexed | 2024-12-14T05:44:24Z |
| format | Article |
| id | doaj.art-afd6d89c95f2424e9edeee368a114b8f |
| institution | Directory Open Access Journal |
| issn | 2050-6511 |
| language | English |
| last_indexed | 2024-12-14T05:44:24Z |
| publishDate | 2020-01-01 |
| publisher | BMC |
| record_format | Article |
| series | BMC Pharmacology and Toxicology |
| spelling | doaj.art-afd6d89c95f2424e9edeee368a114b8f2022-12-21T23:14:55ZengBMCBMC Pharmacology and Toxicology2050-65112020-01-0121111310.1186/s40360-020-0384-9In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucosideCheng Wang0Yimeng Zhou1Xiaohong Gong2Li Zheng3Yunxia Li4School of Pharmacy, Chengdu University of Traditional Chinese MedicineSchool of Pharmacy, Chengdu University of Traditional Chinese MedicineSchool of Pharmacy, Chengdu University of Traditional Chinese MedicineSchool of Pharmacy, Chengdu University of Traditional Chinese MedicineSchool of Pharmacy, Chengdu University of Traditional Chinese MedicineAbstract 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 as anti-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-pass intestinal perfusion model to 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 was concluded that the gastrointestinal absorption the most unique active ingredient and considered as the mechanisms of TSG involved processes passive transport and the participation of efflux transporters.https://doi.org/10.1186/s40360-020-0384-92,3,5,4′-tetrahydroxystilbence-2-O-β-D-glucosideAbsorption mechanismCaco-2 cellIntestinal perfusionP-gpMRP2 |
| spellingShingle | Cheng Wang Yimeng Zhou Xiaohong Gong Li Zheng Yunxia Li In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside BMC Pharmacology and Toxicology 2,3,5,4′-tetrahydroxystilbence-2-O-β-D-glucoside Absorption mechanism Caco-2 cell Intestinal perfusion P-gp MRP2 |
| title | In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside |
| title_full | In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside |
| title_fullStr | In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside |
| title_full_unstemmed | In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside |
| title_short | In vitro and in situ study on characterization and mechanism of the intestinal absorption of 2,3,5,4′-tetrahydroxy-stilbene-2-O-β-D-glucoside |
| title_sort | in vitro and in situ study on characterization and mechanism of the intestinal absorption of 2 3 5 4 tetrahydroxy stilbene 2 o β d glucoside |
| topic | 2,3,5,4′-tetrahydroxystilbence-2-O-β-D-glucoside Absorption mechanism Caco-2 cell Intestinal perfusion P-gp MRP2 |
| url | https://doi.org/10.1186/s40360-020-0384-9 |
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