Preparation of curcumin prodrugs and theirin vitro anti-tumor activities |
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Authors: | Lu Peng Tong Qiangsong Jiang Fengchao Zheng Liduan Chen Fangmin Zeng Fuqing Dong Jihua Du Yuefeng |
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Institution: | (1) Department of Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430022 Wuhan, China;(2) Department of Pathology, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430022 Wuhan, China;(3) Department of Central Laboratory, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430022 Wuhan, China;(4) Department of Pharmical Chemistry, Tongji College of Pharmacy, Huazhong University of Science and Technology, 430030 Wuhan, China |
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Abstract: | Summary 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.
LU Peng, male, born in 1977, M. D., Ph. D.
This project was supported by a grant from the National Natural Sciences Foundation of China (No. 30200284). |
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Keywords: | curcumin prodrug tumor cells |
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