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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
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| 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： | 257 次 |
| 本月下载数： | 7 次 |
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