Synthesis,Characterization and Anti-tumor Effect Evaluation of Novel Ampelopsin Derivative Poly (γ-glutamic Acid)-ampelopsin Conjugate
- VernacularTitle: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
- Author:
Xiaoshan WU
1
;
Feng NI
1
;
Yuying GAO
1
;
Renjie HUANG
1
Author Information
1. Dept. of Pharmacy,Fujian Health College,Fuzhou 350101,China
- Publication Type:Journal Article
- Keywords:
Ampelopsin;
Poly(γ-glutamic acid);
Polymer compounds;
Synthesis;
Characterization;
Anti-tumor effect
- From:
China Pharmacy
2020;31(22):2720-2725
- CountryChina
- Language:Chinese
-
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.