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Journal of Chinese Integrative Medicine ›› 2010, Vol. 8 ›› Issue (9): 863-869.doi: 10.3736/jcim20100910

• Original Experimental Research • Previous Articles     Next Articles

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

Hai-sheng You a, Hai-feng Zhangb, Ya-lin Donga, Si-ying Chena, Mao-yi Wanga, Wei-hua Donga, Jian-Feng Xingc   

  1. a Department of Pharmacy, the First Affiliated Hospital of Medical College, Xi ’ an Jiaotong University,Xi'an 710061, Shaanxi Province, China
    b Department of Pharmacy, Tangdu Hospital, the Fourth Military Medical University, Xi'an 710038,Shaanxi Province, China
    c Department of Pharmacy,College of Medicine,Xi’an Jiaotong University,Xi’an 710061,Shaanxi Province,China;
  • Received:2010-02-05 Accepted:2010-05-28 Online:2010-09-20 Published:2010-09-15


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).

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.

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.

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

Table 1

Precisions and recovery of scutellarin and scutellarein"

Table 2

Transportation of scutellarin and scutellarein with HBSS solution in Caco-2 monolayer"

Table 3

Transportation of scutellarin and scutellarein with PBS solution in Caco-2 monolayer"

Figure 1

Transport amount from AP to BL or from BL to AP with scutellarin (100 μmol/L) and scutellarein (50 μmol/L)"

Table 4

Effects of different inhibitors of multidrug resistance-associated protein on scutellarin and scutellarein transportation"

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