CAJ | 학술논문

目的：通过研究P-糖蛋白（P-gp）底物罗丹明123（R123）在空肠、回肠和结肠转运时辣椒素的作用，探究辣椒素对肠粘膜上P-gp功能的影响。方法使用体外扩散池法技术，分别取SD雄性大鼠的空肠、回肠和结肠肠段标本，计算各肠段中吸收方向（mucosa to serosa, M-S）和分泌方向（serosa to mucosa, S-M）R123的表观渗透速率（Papp）。用荧光分光光度计测定R123和荧光素钠（CF）在接收室中的浓度。结果在辣椒素作用下，R123经空肠粘膜透过时，吸收方向与空白组相比显著增高，分泌方向显著降低，但其在回肠及结肠M-S组及S-M组表观渗透系数Papp与空白组相比均没有显著性差异。CF经空肠粘膜透过时，M-S组及S-M组Papp与空白组相比均显著增高；经回肠和结肠粘膜透过与空白组相比没有显著性差异。结论辣椒素影响P-gp底物R123和细胞旁转运药物CF经肠粘膜透过的作用具有肠段差异性，对R123和CF的影响仅存在于空肠，表明辣椒素是一种较弱的P-gp抑制剂和粘膜通道改善剂。可能与P-gp和紧密连接在肠粘膜上的逐渐变化的分布有关。
목적：통과연구P-당단백（P-gp）저물라단명123（R123）재공장、회장화결장전운시랄초소적작용，탐구랄초소대장점막상P-gp공능적영향。방법사용체외확산지법기술，분별취SD웅성대서적공장、회장화결장장단표본，계산각장단중흡수방향（mucosa to serosa, M-S）화분비방향（serosa to mucosa, S-M）R123적표관삼투속솔（Papp）。용형광분광광도계측정R123화형광소납（CF）재접수실중적농도。결과재랄초소작용하，R123경공장점막투과시，흡수방향여공백조상비현저증고，분비방향현저강저，단기재회장급결장M-S조급S-M조표관삼투계수Papp여공백조상비균몰유현저성차이。CF경공장점막투과시，M-S조급S-M조Papp여공백조상비균현저증고；경회장화결장점막투과여공백조상비몰유현저성차이。결론랄초소영향P-gp저물R123화세포방전운약물CF경장점막투과적작용구유장단차이성，대R123화CF적영향부존재우공장，표명랄초소시일충교약적P-gp억제제화점막통도개선제。가능여P-gp화긴밀련접재장점막상적축점변화적분포유관。
Objective To investigate the role of capsaicin in regulating permeation of P-gp substrate rhodamine 123 (R123) across the jejunum, ileum and colon membranes of rats. Methods The permeability of R123 or fluorescein sodium (CF) across the jejunum, ileum and colon membranes of male SD rats was evaluated using a Ussing chamber. The concentration of R123 or CF in the receptor was determined using fluorospectrophotometry to calculate the apparent permeability coefficient (Papp). Results Compared with the blank control group, capsaicin increased the permeability of R123 across jejunal membranes in the mucosal-to-serosal (M-S) direction and decreased its permeability in the serosal-to-mucosal (S-M) direction, but produced no obvious effect on R123 transport across the ileum or colon membranes. Capsaicin caused a regional increase in the permeability of CF across the jejunal membranes compared with the control group, but CF transport across the ileum and colon membranes was not affected. Conclusion Capsaicin can affect the transport of R123 and CF across rat jejunal membranes, and this effect is shows an obvious intestine segment-related difference probably because of the different distribution of P-gp or tight junction in the intestines. This finding suggests that capsaicin is a weak P-gp inhibitor and an improver of mucous membrane channels.