Synthesis of folic acid-alliinase conjugate and its<i> in situ</i> inhibition of tumor cell proliferation by combination of alliin

LUO Chunxia; ZHU Li; LI Xinyu; AMET Mutallip; NIJIATI Yiliyaer; LI Xinxia; GUAN Ming

doi:10.11665/j.issn.1000-5048.20190613

Journal of China Pharmaceutical University > 2019 > 50(6): 721-727. > DOI: 10.11665/j.issn.1000-5048.20190613

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]. Journal of China Pharmaceutical University, 2019, 50(6): 721-727. DOI: 10.11665/j.issn.1000-5048.20190613

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Synthesis of folic acid-alliinase conjugate and its in situ inhibition of tumor cell proliferation by combination of alliin

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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.
- folic acid-alliinase conjugate,
- coupling ratio,
- targeting,
- antitumor activity,
- HeLa cells

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Synthesis of folic acid-alliinase conjugate and its in situ inhibition of tumor cell proliferation by combination of alliin

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