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Open AccessArticle

Intestinal Absorption of Triterpenoids and Flavonoids from Glycyrrhizae radix et rhizoma in the Human Caco-2 Monolayer Cell Model

1
School of Life Science and Technology, Beijing Institute of Technology, No. 5, Zhongguancun South Street, Haidian District, Beijing 100081, China
2
State Key Laboratory of Natural and Biomimetic Drugs, Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Peking University, No. 38, Xueyuan Road, Haidian District, Beijing 100191, China
*
Authors to whom correspondence should be addressed.
Molecules 2017, 22(10), 1627; https://doi.org/10.3390/molecules22101627
Received: 12 September 2017 / Revised: 23 September 2017 / Accepted: 27 September 2017 / Published: 29 September 2017
(This article belongs to the Collection Herbal Medicine Research)
Glycyrrhizae radix et rhizoma has been used as a traditional Chinese medicine for the treatment of various diseases. Triterpenoids and flavonoids from the plant have many beneficial effects and their chemical structures are modified in the gastrointestinal tract after oral administration. However, absorption of these triterpenoids and flavonoids still needs to be defined. Here, the uptake and transepithelial transport of the selected major triterpenoids, glycyrrhizin (1), glycyrrhetic acid-3-O-mono-β-d-glucuronide (2), and glycyrrhetinic acid (3); and the selected major flavonoids, licochalcone A (4), licochalcone B (5), licochalcone C (6), echinatin (7), isoliquiritin apioside (8), liquiritigenin (9), liquiritin apioside (10) isolated from Glycyrrhizae radix et rhizoma, were investigated in the human intestinal epithelium-like Caco-2 cell monolayer model. Compounds 3, 57, and 9 were designated as well-absorbed compounds, 2 and 4 were designated as moderately absorbed ones, and 1, 8, and 10 were assigned for the poorly absorbed ones. The absorption mechanism of well and moderately absorbed compound was mainly passive diffusion to pass through the human intestinal Caco-2 cell monolayer. These findings provided useful information for predicting their oral bioavailability and the clinical application. View Full-Text
Keywords: Glycyrrhizae radix et rhizoma; triterpenoids; flavonoids; human intestinal Caco-2 cell monolayer model; passive diffusion Glycyrrhizae radix et rhizoma; triterpenoids; flavonoids; human intestinal Caco-2 cell monolayer model; passive diffusion
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Wang, X.-X.; Liu, G.-Y.; Yang, Y.-F.; Wu, X.-W.; Xu, W.; Yang, X.-W. Intestinal Absorption of Triterpenoids and Flavonoids from Glycyrrhizae radix et rhizoma in the Human Caco-2 Monolayer Cell Model. Molecules 2017, 22, 1627.

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