Investigation of the Absorption Mechanism of Ginsenoside Compound K and Its Fatty Acid Ester Prodrugs Using Caco-2 Cell Monolayers Model

Zhu Xuemei; Zhang Bing; Luo Ting; Hu Jiangning; Li Hongyan; Deng Zeyuan

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Investigation of the Absorption Mechanism of Ginsenoside Compound K and Its Fatty Acid Ester Prodrugs Using Caco-2 Cell Monolayers Model

Zhu Xuemei 1,Zhang Bing 2,Luo Ting 2,Hu Jiangning 2 * #,Li Hongyan 2,Deng Zeyuan 2

1.College of Life Science and Food Engineering, Nanchang University, NanChang 330047

2.College of Life Science and Food Engineering, Nanchang University, 330047

*Correspondence author

#Submitted by

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Funding: Doctoral Fund of Ministry of Education of China （No.No.20103601120004）

Opened online: 7 August 2013

Accepted by: none

Citation: Zhu Xuemei,Zhang Bing,Luo Ting.Investigation of the Absorption Mechanism of Ginsenoside Compound K and Its Fatty Acid Ester Prodrugs Using Caco-2 Cell Monolayers Model[OL]. [ 7 August 2013] http://en.paper.edu.cn/en_releasepaper/content/4551903

Ginsenoside compound K (CK) is a bioactive compound with poor oral bioavailability due to its high hydrophilic polarity. In contrast, its novel lipophilic ester prodrugs, the butyl and octyl ester of CK (CK-B and CK-O), have excellent oral potency. The aim of this study was to examine the transport mechanisms of CK and its lipophilic ester prodrugs (CK-B and CK-O) using human Caco-2 cells. Results showed that CK had a low permeability coefficient (8.65±0.17×10-7 cm/s) for AP to BL transport over 10-50 μM, while the transport rate for AP to BL flux of CK-B (29.70±1.45×10-7 cm/s) and CK-O (28.39±1.72×10-7 cm/s) were significantly greater than that of CK. Furthermore, the major transport mechanism of CK was passive transcellular diffusion with active efflux mediated by P-gp involved, whereas CK-B and CK-O were not the substrate of efflux pump. These results suggested that improving the lipophilic of CK by acylation can increases the transport across Caco-2 cells significantly.

Keywords:food nutrition; compound K; fatty acid ester; Caco-2 cell; intestinal absorption; P-gp

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