中国药理学通报
中國藥理學通報
중국약이학통보
CHINESE PHARMACOLOGICAL BULLETIN
2014年
9期
1306-1310,1311
,共6页
兰燕宇%刘跃%曹旭%牟景丽%王爱民%郑林
蘭燕宇%劉躍%曹旭%牟景麗%王愛民%鄭林
란연우%류약%조욱%모경려%왕애민%정림
杜仲提取物%Caco-2 细胞%摄取%UPLC-MS/MS%pH值%被动扩散
杜仲提取物%Caco-2 細胞%攝取%UPLC-MS/MS%pH值%被動擴散
두중제취물%Caco-2 세포%섭취%UPLC-MS/MS%pH치%피동확산
Eucommia ulmoides extract%Caco-2 cell%uptake%UPLC-MS/MS%pH value%passive diffusion
目的:研究杜仲提取物中京尼平苷酸、原儿茶酸、松脂醇二葡萄糖苷、松脂醇单葡萄糖苷在Caco-2细胞的摄取特性。方法以Caco-2细胞单层模型研究杜仲提取物的细胞摄取规律,采用UPLC-MS/MS法测定Caco-2细胞中京尼平苷酸、原儿茶酸、松脂醇二葡萄糖苷、松脂醇单葡萄糖苷的浓度,考察时间、pH值、药物浓度、温度及抑制剂对Caco-2细胞摄取杜仲提取物的影响。结果杜仲提取物中京尼平苷酸、原儿茶酸、松脂醇二葡萄糖苷、松脂醇单葡萄糖苷4种成分在Caco-2细胞中的摄取具有一定的时间、浓度依懒性,其摄取表现为被动扩散;在pH 4条件下,杜仲提取物中上述4种成分的细胞摄取量明显高于pH 8;在4℃、25℃、37℃条件下,杜仲提取物在37℃下的摄取量最高;加入维拉帕米、环孢菌素A后,杜仲提取物中原儿茶酸的细胞摄取量有明显变化,其余3个成分没有变化。结论杜仲提取物中京尼平苷酸、原儿茶酸、松脂醇二葡萄糖苷、松脂醇单葡萄糖苷4种成分的细胞摄取机制主要是被动转运;P-糖蛋白参与其原儿茶酸的摄取过程。
目的:研究杜仲提取物中京尼平苷痠、原兒茶痠、鬆脂醇二葡萄糖苷、鬆脂醇單葡萄糖苷在Caco-2細胞的攝取特性。方法以Caco-2細胞單層模型研究杜仲提取物的細胞攝取規律,採用UPLC-MS/MS法測定Caco-2細胞中京尼平苷痠、原兒茶痠、鬆脂醇二葡萄糖苷、鬆脂醇單葡萄糖苷的濃度,攷察時間、pH值、藥物濃度、溫度及抑製劑對Caco-2細胞攝取杜仲提取物的影響。結果杜仲提取物中京尼平苷痠、原兒茶痠、鬆脂醇二葡萄糖苷、鬆脂醇單葡萄糖苷4種成分在Caco-2細胞中的攝取具有一定的時間、濃度依懶性,其攝取錶現為被動擴散;在pH 4條件下,杜仲提取物中上述4種成分的細胞攝取量明顯高于pH 8;在4℃、25℃、37℃條件下,杜仲提取物在37℃下的攝取量最高;加入維拉帕米、環孢菌素A後,杜仲提取物中原兒茶痠的細胞攝取量有明顯變化,其餘3箇成分沒有變化。結論杜仲提取物中京尼平苷痠、原兒茶痠、鬆脂醇二葡萄糖苷、鬆脂醇單葡萄糖苷4種成分的細胞攝取機製主要是被動轉運;P-糖蛋白參與其原兒茶痠的攝取過程。
목적:연구두중제취물중경니평감산、원인다산、송지순이포도당감、송지순단포도당감재Caco-2세포적섭취특성。방법이Caco-2세포단층모형연구두중제취물적세포섭취규률,채용UPLC-MS/MS법측정Caco-2세포중경니평감산、원인다산、송지순이포도당감、송지순단포도당감적농도,고찰시간、pH치、약물농도、온도급억제제대Caco-2세포섭취두중제취물적영향。결과두중제취물중경니평감산、원인다산、송지순이포도당감、송지순단포도당감4충성분재Caco-2세포중적섭취구유일정적시간、농도의라성,기섭취표현위피동확산;재pH 4조건하,두중제취물중상술4충성분적세포섭취량명현고우pH 8;재4℃、25℃、37℃조건하,두중제취물재37℃하적섭취량최고;가입유랍파미、배포균소A후,두중제취물중원인다산적세포섭취량유명현변화,기여3개성분몰유변화。결론두중제취물중경니평감산、원인다산、송지순이포도당감、송지순단포도당감4충성분적세포섭취궤제주요시피동전운;P-당단백삼여기원인다산적섭취과정。
Aim To observe the uptake process of geniposidic acid , protocatechuic acid , pinoresinol diglucoside and pnoresinol singleglucoside in Caco-2 cell. Methods The concentration of the four componds in cells was detected by UPLC-MS/MS, and the mechanism of the four componds absorption in cells was explored by studying the time, pH, drug concen-tration and inhibitors on the uptake of Eucommia ul-moides extract in cells. Results Eucommia ulmoides extract in Caco-2 cell uptake was time-dependent. Eu-commia ulmoides extract at 0.2~5 g·L-1 concentra-tion range of uptake increased linearly, consistent with passive diffusion process. The drug uptake amount un-der pH 4.0 was significantly higer than pH 8 . 0 ( P<0.05 ) . The drug uptake amount was the highest in
<br> 37℃. Compared with control group, geniposidic acid, protocatechuic acid, pinoresinol diglucoside and pnoresinol singleglucoside cell uptake was not signifi-cantly higher after additional treatment with verapamil and cyclosporin A, and protocatechuic acid cell uptake was significantly higher after additional treatment with verapamil and cyclosporin A, Conclusion The mech-anism of Eucommia ulmoides extract absorption in cells was mainly through passive transport, and P-glycopro-teins participates in the conveying process of protocate-chuic acid in Caco-2 cells.