野黄芩苷和野黄芩素在Caco-2细胞模型中的吸收转运特性

doi:10.3736/jcim20100910

Abstract

Objective

To investigate the absorption and transepithelial transport characteristics of scutellarin and scutellarein in the human colonic adenocarcinoma cell (Caco-2) monolayer model. The influence factors on these two compounds’ absorption were investigated, such as buffer solution, duration of culture, and inhibitors of multidrug resistance-associated protein 2 (MRP2), breast cancer drug resistance protein (BCRP) and P-glycoprotein (P-gp).
Methods

By using Caco-2 monolayer as an intestinal epithelial cell model, the transport process was studied from apical (AP) side to basolateral (BL) side or from BL to AP. The two compounds were determined by high-performance liquid chromatography coupled with diode-array-detector detection. Transport parameters and apparent permeability coeffients (Papp) were calculated.
Results

The Papp values of scutellarin and scutellarein were different in two buffer solutions, respectively. In phosphate buffered saline, scutellarin had no absorption from AP to BL, while its Papp value was 0.74×10–6 to 1.58×10–6 cm/s from BL to AP. The Papp values of scutellarein were 4.33×10–6 to 6.79×10–6 cm/s and 1.32×10–6 to 2.56×10–6 cm/s from AP to BL and from BL to AP, respectively. The Papp value gradually decreased with time. The absorption of scutellarein was better than that of scutellarin. The scutellarin absorption was improved by verapamil, MK-571 and reserpine. The scutellarein absorption was improved by verapamil whereas its excretion was improved by MK-571.
Conclusion

Absorption of scutellarin is difficult in Caco-2 monolayer cells, which contributes to its low bioavailability. Scutellarein absorption is better than scutellarin absorption. Scutellarein transepithelial transport is passive diffusion. The inhibitor of P-gp can improve scutellarin and scutellarein transportation. The inhibitors of MRP2 and BCRP can promote transportation of scutellarin. The inhibitor of MRP2 can promote efflux of scutellarein. The multidrug resistance-associated protein may be the second reason for low bioavailability of scutellarin.

Key words: Caco-2 monolayer cells, Scutellarin, Scutellarein, Apparent permeability coefficient

Hai-sheng You , Hai-feng Zhang, Ya-lin Dong, Si-ying Chen, Mao-yi Wang, Wei-hua Dong, Jian-Feng Xing. Absorption and transportation characteristics of scutellarin and scutellarein across Caco-2 monolayer model. Journal of Chinese Integrative Medicine, 2010, 8(9): 863-869.

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URL: http://www.jcimjournal.com/EN/10.3736/jcim20100910

http://www.jcimjournal.com/EN/Y2010/V8/I9/863

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Figures/Tables 5

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References 15

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Absorption and transportation characteristics of scutellarin and scutellarein across Caco-2 monolayer model

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