文献类型：期刊文章

作　　者：郑怡然[1] 吴秀稳[1] 杨秀伟[1]

机构地区：[1]北京大学医学部药学院天然药物学系天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》

基　　金：The National New Drug R&D Program(Grant No.2011BAI07B08;2009ZX09301-010)of China

年　　份：2017

卷　　号：26

期　　号：8

起止页码：566-573

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2017_2018、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：The blood-brain barrier permeability of 20（S） and 20（R）-protopanaxatriol epimers and dammar-20（22）E,24-diene- 313,6α,12β-triol were investigated using the MDCK-pHaMDR cell monolayer model. The bidirectional permeability tests were carried out, and the apparent permeability coefficients （Papp） were calculated. The two protopanaxatriol epimers showed good permeability with Papp values of-10^-5 cm/s, whereas dammar-20（22）E,24-diene-3β,6α, 12β-triol showed poor permeability with Papp of 〈1 × 10^-7 cm/s. The three compounds showed differences in intracellular accumulations due to their different structures. Inhibition of P-gp with verapamil showed that the transport mechanisms in MDCK-pHaMDR cell monolayer for compounds 1 and 2 epimers were not only simple passive diffusion but also involving an effiux way mediated by P-gp. These findings provided new basis for the further study of compounds 1 and 2 acting on the brain.

关 键 词：20（S）-Protopanaxatriol  20（R）-Protopanaxatriol  Dammar-20（22）E,24-diene-3β,6α,12β-triol  MDCK-pHaMDR  Permeability  Blood-brain barrier  

分 类 号：R285[中药学类]