摘要
目的:研究延胡索季铵碱成分在Caco-2细胞模型中的吸收转运。方法:采用高效液相法测定药物浓度,计算表观渗透系数(Papp),研究延胡索活性部位中7个主要季铵碱成分非洲防己碱、蓝堇辛、脱氢紫堇鳞茎碱、13-甲基巴马土宾、巴马汀、小檗碱和脱氢延胡索碱在Caco-2细胞模型中的双向转运。结果:小檗碱、脱氢紫堇鳞茎碱、脱氢延胡索碱、非洲防己碱和巴马汀的吸收渗透系数(PAB)较小,分别为9.83×10-7、2.64×10-7、2.15×10-7、1.65×10-7、1.52×10-7 cm.s-1,而蓝堇辛和13-甲基巴马土宾的吸收渗透系数相对较大,分别为6.12×10-6、5.43×10–6 cm.s-1;7个季铵碱的分泌渗透系数(PBA)都比其相应的吸收渗透系数要大,其中脱氢延胡索碱和巴马汀的分泌渗透系数分别是其吸收渗透系数的31.9倍和19.6倍。结论:延胡索季铵碱成分的肠道吸收较差,所检测的7种季铵碱的转运则可能是依靠载体介导的主动转运。相对地,蓝堇辛和13-甲基巴马土宾的吸收要好于其他5种生物碱。
OBJECTIVE To study the absorption and transportation of quaternary alkaloids in Corydalis yanhusuo by using Caco-2 cell monolayer model. METHODS Caco-2 cell monolayer model was used to study the bi-direction transport of colum- bamine, fumaricine, dehydrocorybulbine, 13-methyl palmatrubine, palmatine, berberine and dehydrocorydaline. The concen- tration of the seven alkaloids in cell culture medium was measured by HPLC and the apparent permeability coefficients （Papp） were calculated. RESULTS The absorptive permeability coefficients （P_AB） of columbamine, fumaricine, dehydrocorybulbine, l 3 methyl-palmatrubine, palmatine, berberine and dehydrocorydaline were 9. 83 × 10^- 7,6. 12 × 10 ^-6 , 2. 64 × 10^-7,5.43 × 10^-6 , 2.15 × 10^-7,1.65 × 10^-7 and 1.52 × 10^-7 cm.s-1 , respectively. Except fumaricine and 13 methyl palmatrubine, the other five alkaloids had lower permeabilities, and the secretive permeabilities （PBA） of all the alkaloids were larger than their absorptive permeabilities. Among them, the PBA of dehydrocorydaline and berberine were 31.9 and 19. 6 times as much as the PABrespec- tively. CONCLUSION The results suggest that the intestinal absorption of quaternary alkaloids in Corydalis yanhusuo are low- er, which might have efflux mechanism by transporters, and the absorption of fumaricine and 13-methyl-palmatrubine are bet- ter than that of other 5 alkaloids, relatively.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2013年第2期89-92,共4页
Chinese Journal of Hospital Pharmacy
基金
"重大新药创制"科技重大专项(编号:2009ZX09301-003
2009ZX09103-382
2012ZX09301-002)
国家自然科学基金项目(编号:31070319)
关键词
延胡索
季铵碱
CACO-2细胞单层模型
表观渗透系数
Corydalis yanhusuo
quaternary alkaloids
Caco-2 cell monolayer model
permeability coefficients
