三七总皂苷心肌靶向脂质体的体外靶向性研究  

Study on the Targeting Characteristics of Myocardial Targeting Panax Notoginseng Saponins Liposomes in vitro

作　　者：黄建春[1] 谢佳秀 陈红丽 韦柱梅 黄玉鹏 HUANG Jian-chun;XIE Jia-xiu;CHEN Hong-li;WEI Zhu-mei;HUANG Yu-peng(Pharmaceutical College, Guangxi Medical University,Nanning Guangxi,530021,China)

机构地区：[1]广西医科大学药学院,广西南宁530021

出　　处：《时珍国医国药》2022年第4期817-820,共4页Lishizhen Medicine and Materia Medica Research

基　　金：国家自然科学基金(81560587);广西自然科学基金项目(2018GXNSFAA050073);广西壮族自治区大学生创新创业训练计划项目(202010598148)。

摘　　要：目的研究三七总皂苷心肌靶向脂质体(PAC-L-PNS)的对心肌细胞的体外靶向性。方法将加载了罗丹明B(Rhodamine B,RHB)荧光染料的PAC-L-PNS(即PAC-L-PNS-RHB)和加载了RHB的三七总皂苷普通脂质体(即L-PNS-RHB)分别与H9C2心肌细胞在相同实验条件下共同培养一定时间,以每毫克细胞蛋白摄取的荧光值为指标,考察H9C2心肌细胞对不同脂质体的摄取量;将PAC-L-PNS-RHB和L-PNS-RHB分别与H9C2心肌细胞和HL-7702非心肌细胞在相同实验条件下共同培养一定时间,以每毫克细胞蛋白摄取的荧光值为指标,考察不同细胞对脂质体的摄取量;将PAC-L-PNS-RHB和L-PNS-RHB分别与H9C2心肌细胞在不同实验条件下共同培养一定时间,以每毫克细胞蛋白摄取的荧光值为指标,考察不同环境下心肌细胞对脂质体的摄取量。结果心肌细胞摄取PAC-L-PNS-RHB和L-PNS-RHB的量均随着培养时间的延长而增加,从1h开始,心肌细胞对PAC-L-PNS-RHB的摄取量显著高于L-PNS-RHB(P<0.01);心肌细胞对PAC-L-PNS-RHB的摄取量较非心肌细胞高4.97倍;在缺氧条件下,心肌细胞对PAC-L-PNS-RHB的摄取量较L-PNS-RHB高2.06倍;美托洛尔的加入导致心肌细胞对PAC-L-PNS-RHB的摄取量显著下降。结论PAC-L-PNS具有较强的体外心肌细胞靶向性,其原因可能是PAC-L-PNS与心肌细胞表面的β1-AR发生了特异性结合。Objective To study on the targeting characteristics of myocardial targeting Panax notoginseng saponins liposomes in vitro.Methods The PAC-L-PNS loaded with Rhodamine B(RHB)fluorescent dye(PAC-L-PNS-RHB)and Panax notoginseng saponins liposomes loaded with RHB(L-PNS-RHB)were co cultured with H9 c2 cardiomyocytes under the same experimental conditions for a certain period of time.The uptake of different liposomes by H9 C2 cardiomyocytes was evaluated by the fluorescence value of cellular protein uptake;PAC-L-PNS-RHB and L-PNS-RHB were co cultured with H9 C2 cardiomyocytes and HL-7702 non cardiomyocytes under the same experimental conditions for a certain period of time.The uptake of liposomes by different cells was measured by the fluorescence value of cell protein uptake;PAC-L-PNS-RHB and L-PNS-RHB were co cultured with H9 c2 cardiomyocytes under different experimental conditions for a certain period of time.The uptake of liposomes by cardiomyocytes under different conditions was evaluated by the fluorescence value of cell protein uptake.Results The uptake of both PAC-L-PNS-RHB and L-PNS-RHB by cardiomyocytes increased with the prolongation of culture time,and the uptake of PAC-L-PNS-RHB by cardiomyocytes was significantly higher than that of L-PNS-RHB from 1 h(P<0.01);the uptake of PAC-L-PNS-RHB by cardiomyocyte was 4.97-fold higher than that by nonmyocyte;Under hypoxia,the uptake of PAC-L-PNS-RHB by cardiomyocytes was 2.06 times higher than that of L-PNS-RHB.The uptake of PAC-L-PNS-RHB by cardiomyocytes was decreased significantly after the addition of Metoprold.Conclusion PAC-L-PNS has strong targeting ability to cardiomyocytes in vitro,this may be due to the specific interaction between PAC-L-PNS and the surface of cardiomyocytesβ1-AR.

关 键 词：三七总皂苷 心肌靶向 脂质体 体外靶向 

分 类 号：R285.5[医药卫生—中药学]