- 作者：Lushan Yu ; Qi Shen ; Quan Zhou ; Huidi Jiang ; Huichang Bi ; Min Huang ; Hui Zhou ; Su Zeng
- 关键词：MDR1 ; reverse multidrug resistance 1 ; P-gp ; P-glycoprotein ; MRP2 ; MDR-associated protein 2 ; GF120918 ; N-(4-[2-(1 ; 2 ; 3 ; 4-tetrahydro-6 ; 7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9 ; 10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide ; CsA ; cyclosporin A ; Calcein AM ; Calcein acetoxymethyl ester ; Rho-123 ; rhodamine 123 ; ER ; efflux ratio ; NER ; net efflux ratio ; TEER ; transepithelial electrical resistance ; Papp ; apparent permeability coefficient ; AP ; apical side ; BL ; basolateral side ; MDCK ; Madin-Darby can
- 刊名：Journal of Ethnopharmacology
- 出版年：25 November, 2013
- 年：2013
- 卷：150
- 期：2
- 页码：485-491
- 全文大小：477 K
Ethnopharmacological relevance
Lotus plumule, the dried young cotyledon and radicle of the Nelumbo nucifera Gaertn. (Fam. Nymphaeaceae) ripe seed, is a famous Traditional Chinese Medicine to remove heat from the heart, anchor the mind, improve seminal emission, and arrest bleeding for centuries in China. Liensinine and its analogs neferine and isoliensinine are the major active components in lotus plumule. Aim of the study is to investigate the association of liensinine, neferine, and isoliensinine with efflux transporters.Materials and methods
Caco-2, MDCK, MDCK-MDR1, and MDCK-MRP2 were used as cell models for the transcellular transport and accumulation studies.
Results
The results obtained in Caco-2 cells suggested that P-glycoprotein (P-gp) might be involved in transcellular transport. Cellular accumulation and transport experiments were further performed in MDCK-MDR1 cells. GF120918 and cyclosporine A were found to completely inhibit the efflux, and the net efflux ratios of these alkaloids exhibited saturation over the concentration range. No significant differences in liensinine accumulation and transport were observed between MDCK and MDCK-MRP2 cells.
Conclusions
These results demonstrated that liensinine, neferine, and isoliensinine are substrates of P-gp, whereas MRP2 is not involved in the transport process, suggesting that P-gp might be responsible for the absorption and distribution of the 3 alkaloids.