新型蛇葡萄素衍生物γ-聚谷氨酸蛇葡萄素酯的合成、表征及抗肿瘤作用评价
x

请在关注微信后,向客服人员索取文件

篇名: 新型蛇葡萄素衍生物γ-聚谷氨酸蛇葡萄素酯的合成、表征及抗肿瘤作用评价
TITLE: Synthesis,Characterization and Anti-tumor Effect Evaluation of Novel Ampelopsin Derivative Poly (γ-glutamic Acid)-ampelopsin Conjugate
摘要: 目的:设计合成γ-聚谷氨酸蛇葡萄素酯(γ-PGA-AMP),并进行表征和体外抗肿瘤活性评价。方法:利用酯化反应将蛇葡萄素接载在γ-聚谷氨酸上生成合成产物。采用紫外光谱法、傅里叶红外光谱法、氢-1核磁共振法及元素分析等方法对合成产物的结构进行表征;采用紫外吸收光谱法在293nm波长处测定合成产物中蛇葡萄素的含量。以5-氟尿嘧啶为阳性对照,采用MTT法检测γ-PGA-AMP、蛇葡萄素对人乳腺癌细胞MCF-7、人肝癌细胞HepG2、人肺癌细胞A549的抑制作用,计算半数抑制浓度(IC50)。结果:表征结果显示,蛇葡萄素的7位游离羟基与γ-聚谷氨酸a位碳上的羧基已发生了酯化反应,合成产物即为γ-PGA-AMP(产率为55.7%),其中蛇葡萄素含量为32.3%。γ-PGA-AMP和蛇葡萄素对MCF-7、HepG2和A549细胞均有明显的抑制作用;γ-PGA-AMP对上述3种肿瘤细胞的IC50分别为40.19、28.29、55.23μg/mL,蛇葡萄素的IC50分别为105.30、81.23、130.10μg/mL,5-FU的IC50分别为24.72、87.98、30.99μg/mL。结论:成功合成具有体外抗肿瘤活性的γ-PGA-AMP,且抗肿瘤活性强于蛇葡萄素。
ABSTRACT: OBJECTIVE:To desig n and sy nthesize poly (γ-glutamic acid )-ampelopsin(γ-PGA-AMP),and to characterize it and evaluate its anti-tumor activity in vitro . METHODS :Synthetic product was produced through an esterification reaction between γ-PGA and ampelopsin. The structure of synthetic product was characterized by the UV spectrophotometry ,Fourier transform infrared(FT-IR)spectroscopy,1H-NMR spectra and the quantitative elemental analysis. The content of ampelopsin in synthetic product was determined by UV absorption spectrometry at 292 nm. Using 5-FU as positive control ,MTT assay was used to determine inhibitory effects of γ-PGA-AMP and ampelopsin on human breast cancer cell MCF- 7,human liver cancer cell HepG 2 and human lung cancer cell A 549. The IC 50 was calculated. RESULTS :The results showed that the free 7-hydroxyl group of ampelopsin and the a-carboxyl group of γ-polyglutamic acid had been esterified to obtain γ-PGA-AMP;the yield of γ-PGA-AMP was 55.7%,and the content of ampelopsin was 32.3%. The inhibitory effect of γ-PGA-AMP and ampelopsin on MCF- 7,HepG2 and A 549 cells was obvious. IC 50 of γ-PGA-AMP(to 3 above tumor cells )were 40.19,28.29 and 55.23 μg/mL,those of ampelopsin were 105.30,81.23,130.10 μg/mL,those of 5-FU were 24.72,87.98,30.99 μg/mL,respectively. CONCLUSIONS :γ-PGA-AMP with anti-tumor effect in vitro is synthesized successfully ,and its anti-tumor effect is stronger than that of ampelopsin.
期刊: 2020年第31卷第22期
作者: 吴晓珊,倪峰,高毓瀅,黄仁杰
AUTHORS: WU Xiaoshan ,NI Feng,GAO Yuying ,HUANG Renjie
关键字: 蛇葡萄素;γ-聚谷氨酸;高分子化合物;合成;表征;抗肿瘤作用
KEYWORDS: Ampelopsin;Poly(γ-glutamic acid);Polymer compounds ;Synthesis;Characterization;Anti-tumor effect
阅读数: 26 次
本月下载数: 3 次

* 注:未经本站明确许可,任何网站不得非法盗链资源下载连接及抄袭本站原创内容资源!在此感谢您的支持与合作!