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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
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引用本文:罗春霞,朱丽,李心雨,木塔力甫·艾买提,伊力亚尔·尼加提,李新霞,关明.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[J].中国药科大学学报,2019,50(6):721-727.
Cite:LUO Chunxia,ZHU Li,LI Xinyu,AMET Mutallip,NIJIATI Yiliyaer,LI Xinxia,GUAN Ming.Synthesis of folic acid-alliinase conjugate and its in situ inhibition of tumor cell proliferation by combination of alliin[J].J China Pharm Univ,2019,50(6):721-727.
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作者单位
罗春霞 新疆师范大学化学化工学院 
朱丽 新疆师范大学化学化工学院 
李心雨 新疆医科大学药学院 
木塔力甫·艾买提 新疆医科大学中心实验室 
伊力亚尔·尼加提 新疆医科大学中心实验室 
李新霞 新疆医科大学药学院 
关明 新疆师范大学化学化工学院 
基金项目:新疆维吾尔自治区联合基金资助项目(No.2016D01C157)#罗春霞和朱丽对本论文的贡献相同
中文摘要:合成叶酸-蒜酶缀合物(FA-Alliinase),采用宫颈癌HeLa细胞考察其对肿瘤细胞的靶向性和抑制肿瘤生长活性。采用两种方法合成叶酸-蒜酶缀合物FA-AlliinaseⅠ和FA-AlliinaseⅡ,测得两种缀合物的偶联比分别为12和31,选择高偶联比的FA-AlliinaseⅡ,对其结构进行初步的表征。高效液相色谱法测得FA-AlliinaseⅡ有约50%的蒜酶活力;激光共聚焦及流式细胞仪观察到FA-AlliinaseⅡ对HeLa细胞具有一定的靶向性,MTT法测得FA-AlliinaseⅡ联合蒜氨酸后对HeLa细胞增殖有抑制作用,以蒜氨酸计IC50为(127.6±2.3)μmol/L。该研究为类前药叶酸-蒜酶缀合物的合成优化提供了较为直接的评价方法。
中文关键词:叶酸-蒜酶缀合物  偶联比  靶向性  抗肿瘤活性  HeLa细胞
 
Synthesis of folic acid-alliinase conjugate and its in situ inhibition of tumor cell proliferation by combination of alliin
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.
keywords:folic acid-alliinase conjugate  coupling ratio  targeting  antitumor activity  HeLa cells
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