Preparation of Curcumin Prodrugs and Their in Vitro Anti-tumor Activities

被引：0

作者：

陆鹏 ^{[1
]}

童强松 ^{[1
]}

姜凤超 ^{[2
]}

郑丽端 ^{[3
]}

陈方敏 ^{[1
]}

曾甫清 ^{[1
]}

董继华 ^{[4
]}

杜岳峰 ^{[1
]}

机构：

[1] Department of Surgery

[2] Department of Pharmical Chemistry, Tongji College of Pharmacy, Huazhong University of Science and Technology, Wuhan , China

[3] Department of Pathology

[4] Department of Central Laboratory, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan , China

来源：

华中科技大学学报(医学英德文版) | 2005年 / 06期

关键词：

curcumin; prodrug; tumor cells;

D O I：

暂无

中图分类号：

R730.5 [肿瘤治疗学];

学科分类号：

100214 ;

摘要：

The curcumin prodrugs, which could be selectively activated in tumor cells, were prepared to establish a basis for the targeted chemotherapy for cancer. On the basis of the molecular structure of curcumin, the N-maleoyl-L-valine-curcumin (NVC), N-maleoyl- glycine-curcumin (NGC) were chemically synthesized and identified by IR and NMR spectroscopy. After treatment with these two prodrugs for 6-24 h, the rates of growth inhibition on human bladder cancer EJ cells and renal tubular epithelial (HKC) cells were detected by MTT colorimetry. Our results showed that after the treatment with 20 μmol/L-40 μmol/L NVC and NGC for 6-24 h, the growth inhibitory effects on EJ cells were 6.71 %-65.13 % (P<0.05), 10.96 %-73.01 % (P<0.05), respectively, in both dose- and time-dependent manners. When compared with the curcumin of same concentrations, the growth inhibitory effects of these two prodrugs on HKC cells were significantly decreased (P<0.01). It is concluded that activation of curcumin prodrugs via hydrolysis functions of cellular esterase could inhibit the growth activities of tumor cells, and reduce the side effects on normal diploid cells. This provided a novel strategy for further exploration of tumor-targeted chemotherapeutic drugs.

引用

页码：668 / 670+678 +678

页数：4