丹酚酸B在心肌细胞和血管内皮细胞内的摄取特性  

Cellular uptake characteristics of salvianolic acid B in myocardial cells and blood vessel endothelial cells

作　　者：邵静萍[1] 张善飞 陈渊成[1] 杨文亮[1] 柳晓泉[1] 

机构地区：[1]中国药科大学药物代谢与动力学研究中心,南京210009 [2]正大青春宝药业有限公司,杭州310023

出　　处：《中国药科大学学报》2009年第3期263-268,共6页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30772609)~~

摘　　要：目的:研究丹参水溶性成分丹酚酸B在心肌细胞和血管内皮细胞中的摄取特性。方法:考察时间、温度、药物浓度、介质pH等因素对心肌细胞和血管内皮细胞摄取丹酚酸B的影响,采用LC/MS测定细胞内丹酚酸B的浓度。结果:心肌细胞和血管内皮细胞在37℃和4℃条件下对丹酚酸B的摄取符合对数模型,细胞摄取量与细胞外药物浓度成正比并随介质pH的减小而显著增加,同时丹参中其他水溶性成分明显促进丹酚酸B的摄取,使其摄取量增加30%以上。细胞能量代谢抑制剂能显著抑制丹酚酸B在心肌细胞和内皮细胞中的摄取。在温孵药液中加入乳酸和脂肪酸,心肌细胞和血管内皮细胞对丹酚酸B的摄取均增加20%以上。结论:pH是影响丹酚酸B摄取的主要因素,酸性介质促进了丹酚酸B在心肌细胞和血管内皮细胞中的摄取,提示心肌缺血等心血管疾病造成的内环境酸度增加能明显提高心肌细胞和血管内皮细胞对丹酚酸B的摄取,更好地发挥其心血管活性。Aim： To determine the uptake characteristics of salvianolic acid B（ Sal B） in myocardial cells and blood vessel endothelial cells. Method： The effects of various factors, such as time, temperature, drug concentration, pH of the medium, on the uptake of Sal B in myocardial cells and aorta endothelial cells were investigated. LC/MS was employed to determine the intraeellular concentration of Sal B. Results： Uptake kinetics of Sal B in the myocardial cells and aorta endothelial cells fitted well to the logarithmic model at 37 ℃ and 4 ℃. The amount of uptake was in direct proportion to the extracellular concentration of Sal B in the experimental concentration range. Uptake of Sal B both in the myocardial cells and blood vessel endothelial cells would significantly increase while the medium pH decreased, and some water-soluble components extracted from danshen would also facilitate the uptake of Sal B both in the myocardial cells and blood vessel endothelial cells obviously. The energy metabolism inhibitors would significantly inhibit the uptake of Sal B in the myocardial cells and blood vessel endothelial cells. When lactic acid and fatty acid were added to the incubation solution, the uptake of Sal B both in the myocardial cells and aorta endothelial cells increased more than 20%. Conclusion： pH is the most important factor influencing the cellular uptake of Sal B, and the amount of uptake tends to increase in acidic medium. Results suggest that the uptake of Sal B would increase in the acidified internal environment induced by myocardial ischemia, thus exerting better cardiovascular activities.

关 键 词：丹酚酸B 心肌细胞 血管内皮细胞 摄取 

分 类 号：R285[医药卫生—中药学]