Citation: Ru Ding, Yong Jian, Hong Kan, Zhong-Ying Liu, Shu Liu, Zhi-Qiang Liu, Jun Zhou. Studies on the intestinal absorption of the alkaloids in the Gancaofuzi decoction in a Caco-2 cell culture system by UPLC–MS/MS analysis[J]. Chinese Chemical Letters, ;2016, 27(6): 915-919. doi: 10.1016/j.cclet.2016.03.001 shu

Studies on the intestinal absorption of the alkaloids in the Gancaofuzi decoction in a Caco-2 cell culture system by UPLC–MS/MS analysis

Ru Ding ^a,c, ,
Yong Jian ^a,c ,
Hong Kan ^a,d ,
Zhong-Ying Liu ^a ,
Shu Liu ^b ,
Zhi-Qiang Liu ^b ,
Jun Zhou ^e

a School of Pharmacy, Jilin University, Changchun 130021, China;
b National Centre of Mass Spectrometry in Changchun & Jilin Province Key Laboratory of Chinese Medicine Chemistry and Mass Spectrometry, Changchun Institute of Applied Chemistry, Chinese Academy of Science, Changchun 130022, China;
c Guizhou Province and Chinese Academy of Sciences, Key Laboratory of Chemistry for Natural Products, Guiyang 550002, China;
d College of Chinese Medicine Material, Jilin Agricultural University, Changchun 130118, China;
e Department of Orthopedics, The Fourth People's Hospital of Guiyang, Guiyang 550000, China

Received Date: 15 December 2015
Revised Date: 29 January 2016

Fund Project: This research was supported by the National Natural Science Foundation of China (No. 81173507) and the Science Foundation of Jilin province (No. 20150414040GH).

In this study, the Caco-2 cell monolayer model was used to research the characteristic absorption and efflux of five diterpenoid alkaloids in Gancaofuzi decoction. An ultra performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS) method was developed for the determination of the simulated intestinal transport of five diterpenoid alkaloids with reserpine as internal standard. The use of the apparent permeability coefficient (Papp) and efflux rate (Er) was instituted to evaluate the intestinal absorption of the alkaloids. Transport of the five alkaloids in Caco-2 cell monolayer model was observed to better understand whether the intestinal absorption of alkaloids was influenced by the compatibility of four herbs in Gancaofuzi decoction. The results show that the Papp values of the five diterpenoid alkaloids were all more than 1×10^-6 cm/s, confirming that the processes of permeability were valid. The flux of the alkaloids was time-dependent, and the intestinal absorption mechanism of the five alkaloids was mainly based on passive transport. The compatibility of Heishunpian, Baizhu, Guizhi and Gancao can reduce the intestinal absorption of alkaloids, especially the most toxic hypaconitine, and the attenuated effect of mixed herbal water extracts was better than that of different herbs' water extracts combination. The results prove that compatibility of four herbs in Gancaofuzi decoction is rational.
- Gancaofuzi decoction,
- Caco-2 cell,
- Alkaloids,
- Combination,
- Ultra performance liquid chromatography,
- coupled with tandem mass spectrometry,
- (UPLC-MS/MS)
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