5-FU-乙酸鬼臼酯的合成及稳定性研究

5-FU-乙酸鬼臼酯的合成及稳定性研究

向蓉, 张辅民, 倪京满^*, 田瑄

1.兰州大学药学院;
2.兰州大学功能有机分子化学国家重点实验室;
3.兰州中医骨伤科医院, 甘肃兰州 730000

收稿日期:2006-11-10 修回日期:2007-02-10 出版日期:2007-03-15 发布日期:2007-03-15
通讯作者: 倪京满*

Synthesis and stability evaluation of 5-FU-acetic podophyllic ester as anti-tumor agent

Rong Xiang, Fu-Min Zhang, Jing-Man Ni^*, Xuan Tian

1. School of Pharmacy, Lanzhou University;
2. Sates Key Laboratory of Applied Organic Chemistry, Lanzhou University;
3. Hospital of Traditional China Medicine Traumatocomium of Lanzhou, Lanzhou 730000, China

Received:2006-11-10 Revised:2007-02-10 Online:2007-03-15 Published:2007-03-15
Contact: Jing-Man Ni*

摘要/Abstract

摘要： 目的研究一种新型鬼臼类抗肿瘤药物。方法根据拼合原理合成一种新的鬼臼类似物,并测定了其体外对肿瘤细胞的活性及在多种介质中的稳定性。结果合成的化合物在体外对P-388, A-549和Bel-7402肿瘤细胞表现出比VP-16更强的抑制活性。同时固体样品对温度、光等因素的改变较稳定, 而在人工胃液(AGJ)及pH较高的缓冲溶液中和高湿度条件下稳定性较差。结论本试验的结果为该化合物的进一步研究提供了研究基础。

关键词: 鬼臼毒素, 鬼臼毒素, 鬼臼毒素, 5-氟尿嘧啶, 5-氟尿嘧啶, 5-氟尿嘧啶, 抗肿瘤活性, 抗肿瘤活性, 抗肿瘤活性, 稳定性, 稳定性, 稳定性

Abstract:

Aim To study a new anti-cancer drug 5-FU-acetic podophyllic ester derivatized from podophyllotoxin. Methods A novel derivative of podophyllotoxin was synthesized. Its inhibitory effects against P-388, A-549, Bel-7402 and HL-60 in vitro were tested. The stability tests under different kinds of conditions were carried out. Results The novel derivative showed stronger inhibitory activities against P-388, A-549 and Bel-7402 in vitro than VP-16. The novel derivative was found to be stable at 60 ℃ and 4500 lx light in solid-state, but was less stable in humid condition. It was more stable in methanol (4 ℃) and chloroform (25 ℃) than in methanol (25 ℃), and less stable in artificial gastric juice(AGJ, 37 ℃). Its stabilities were decreased while increasing the pH of buffer solutions. Conclusion These results could provide useful information for further study of this compound.

Key words: Podophyllotoxin, Podophyllotoxin, 5-Fluorouracil, 5-Fluorouracil, Anti-tumor activity, Anti-tumor activity, Stabilities, Stabilities

中图分类号:

R916

Supporting:

Foundation item: National Natural Science Foundation of Gansu Province (3ZS051-A25-101) & Fund of the Ministry of Education of China (No.204142).

^*Corresponding author. Tel.: 86-0931-8915683; fax: 86-0931-8911255

向蓉, 张辅民, 倪京满^*, 田瑄. 5-FU-乙酸鬼臼酯的合成及稳定性研究[J]. .

Rong Xiang, Fu-Min Zhang, Jing-Man Ni^*, Xuan Tian. Synthesis and stability evaluation of 5-FU-acetic podophyllic ester as anti-tumor agent[J]. .

参考文献

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