Synthesis of folic acid-alliinase conjugate and its in situ inhibition of tumor cell proliferation by combination of alliin
10.11665/j.issn.1000-5048.20190613
- VernacularTitle:叶酸-蒜酶缀合物的合成及联合蒜氨酸原位抑制肿瘤细胞增殖作用
- Author:
Chunxia LUO
1
;
Li ZHU
;
Xinyu LI
;
Mutallip AMET
;
Yiliyaer NIJIATI
;
Xinxia LI
;
Ming GUAN
Author Information
1. 新疆师范大学化学化工学院
- Publication Type:Journal Article
- Keywords:
folic acid-alliinase conjugate;
coupling ratio;
targeting;
antitumor activity;
HeLa cells
- From:
Journal of China Pharmaceutical University
2019;50(6):721-727
- CountryChina
- Language:Chinese
-
Abstract:
To synthesize the folic acid-alliinase conjugate(FA-Alliinase), and to study its targeting and antitumor activity on cervical cancer HeLa cells. FA-Alliinase I and FA-Alliinase II were synthesized by two methods. The couping ratios of two conjugates measured were 12 and 31, respectively. The FA-Alliinase II with high coupling ratio was selected and its structure was characterized preliminarily. The activity of alliinase retained about 50% in FA-Alliinase II determined by HPLC. The specific effect of FA-Alliinase II on HeLa cells was observed by confocal laser and flow cytometry. The antitumor activity of conjugate combined with alliin was determined by MTT, and IC50 of alliin was(127. 6±2. 3)μmol/L. This study provides a direct evaluation method for the synthesis and optimization of FA-Alliinase.
