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目的研究石菖蒲、安息香和苏合香挥发油促进罗丹明-123(Rho-123)的肠吸收作用及其机制。方法制作大鼠肠外翻模型,向肠囊内注入1.0mL K-R营养液,将肠囊悬浮于45.0mL 37℃的K-R溶液中。向肠囊外溶液中分别加入浓度均为60μg/mL的石菖蒲、安息香和苏合香挥发油,孵育30min后加入Rho-123,用高效液相色谱-荧光检测法测定肠囊内Rho-123的含量。培养人结肠癌细胞Caco-2,分别加入浓度均为80μg/mL的石菖蒲、安息香和苏合香挥发油作用48h,应用流式细胞术检测P糖蛋白(P-gp)的表达;采用qPCR检测P-gp基因MDR1mRNA的表达。结果石菖蒲、安息香和苏合香挥发油均可增加大鼠空肠和回肠Rho-123的吸收速率常数和表观通透系数(P<0.01),降低P-gp及其基因MDR1 mRNA的表达(3者作用的降低率分别为53.15%、55.10%、61.86%及55.41%、16.24%、38.46%;P<0.01)。结论抑制P-gp及其基因的表达可能是石菖蒲、安息香和苏合香挥发油促进Rho-123肠吸收的主要机制之一。
Objective To study the intestinal absorption of rhodamine-123 (Rho-123) and its mechanism by using the volatile oil of Acorus calamus, Benzoin and Sulfuric acid. Methods The rat model of parenteral eversion was made by injecting 1.0 mL of K-R nutrient solution into the gut and suspending the gut in 45.0 mL of K-R at 37 ° C. To the extragalactic solution were added the concentration of 60μg / mL of Acorus calamus, benzoin and volatile oil of Soviet Union, after incubation for 30min by adding Rho-123, high performance liquid chromatography - fluorescence detection of intestinal tract Rho-123 content. Caco-2 was cultured in human colon cancer cells, and treated with 60μg / mL Acorus gramineus, benzoin and thujeprazole respectively for 48 hours. The expression of P-glycoprotein (P-gp) was detected by flow cytometry. gp gene MDR1 mRNA expression. Results Acorus gramineus, benzoin and fulgurone could increase the Rho-123 absorption rate constant and the apparent permeability coefficient (P <0.01), and decrease the expression of P-gp and its gene MDR1 mRNA in the jejunum and ileum The reduction rates were 53.15%, 55.10%, 61.86% and 55.41%, 16.24% and 38.46%, respectively; P <0.01). Conclusions Inhibition of P-gp and its gene expression may be one of the main mechanisms of intestinal absorption of Rho-123 by the volatile oil of Acorus calamus, Benzoin and Sukang.