基于肝癌化疗增效减毒的5,3′,4′,3″,4″,5″-六-O-乙基-EGCG的合成及其脂质体制备与表征  

Synthesis, Preparation and Characterization of 5,3′,4′,3",4 ",5"-hexa-Oethyl-EGCG based on Synergistic and Attenuative Chemotherapy for Hepatocellular Carcinoma

作　　者：韦爽 梁庆瑶 陈铁寓[1] 梁钢[1] Wei Shuang;Liang Qingyao;Chen Tieyu;Liang Gang(College of Pharmacy,Guangxi Medical University,Nanning 530021,China)

机构地区：[1]广西医科大学药学院,广西南宁530021

出　　处：《广东化工》2022年第6期42-44,共3页Guangdong Chemical Industry

摘　　要：目的:设计合成表没食子儿茶素没食子酸酯(EGCG)六乙基化衍生物5,3′,4′,3″,4″,5″-六-O-乙基-EGCG(Y6)并初步研究制备其脂质体。方法:以EGCG为原料,(CH;CH;O);SO;为乙基供体,丙酮为反应介质,碳酸钾催化反应,制备EGCG衍生物Y6粗品。采用乙醇注入法制备Y6脂质体,纳米粒度电位仪测定脂质体粒径、zeta电位及多分散系数(PDI),透射电镜法观察分析脂质体形态结构,透析法进行脂质体的分离,并用高效液相法测定并计算脂质体的包封率和载药量。结果:成功制备EGCG衍生物Y6,所得Y6产率为14.4%。乙醇注入法制备所得Y6脂质体粒径大小为(152.1±0.7)nm,zeta电位为(-13.8±1.1)mV,PDI为0.247±0.003,包封率为83.11%,载药量为8.90%。结论:本课题通过优化表没食子儿茶素没食子酸酯,所得Y6具有较好的稳定性;其脂质体粒径分布较小、较为稳定,可为EGCG衍生物的发现、结构优化及剂型改进提供理论参考依据。Objective:The hexaethylated derivative 5,3′,4′,3",4",5"-6-o-ethyl-EGCG (Y6) of Epigallocatechin gallate (EGCG) was designed and synthesized and the Y6 liposome was prepared.Methods:EGCG was used as starting,(CH;CH;O);SO;as ethyl donor,acetone as reaction medium and K;CO;was use as catalyst,EGCG derivative Y6 crude was prepared.Y6 liposomes were prepared by ethanol injection method.The particle size,zeta potential and PDI were measured by Zetasizer Nano ZS.The morphological structure of liposomes was observed and analyzed by TEM.The liposomes were separated by dialysis,and the entrapment efficiency and drug loading were measured by HPLC.Results:Y6 were successfully prepared with yield of 14.4%.The particle size was (152.1±0.7) nm,zeta potential was (-13.8±1.1) MV,PDI was 0.247±0.003.The entrapment efficienc y was 83.11%,and the drug loading was 8.90%.Conclusion:In this paper,Y6 has good stability with good liposomes yield.Our study could provide a theoretical reference for the discovery,structure and dosage form optimization of EGCG derivatives.

关 键 词：EGCG 衍生物 Y6 脂质体 合成 

分 类 号：TQ[化学工程]