Anti-tumor activity of N-thiolated β-lactam antibiotics

被引:43
作者
Chen, Di [1 ]
Falsetti, Samuel C. [2 ,3 ]
Frezza, Michael [1 ]
Milacic, Vesna [1 ]
Kazi, Aslamuzzaman [2 ,3 ]
Cui, Qiuzhi Cindy [1 ,4 ]
Long, Timothy E. [4 ]
Turos, Edward [4 ]
Dou, Q. Ping [1 ]
机构
[1] Wayne State Univ, Sch Med, Dept Pathol, Prevent Program,Barbara Ann Karmanos Canc Inst, Detroit, MI 48201 USA
[2] Univ S Florida, Coll Med, H Lee Moffitt Canc Ctr & Res Inst, Dept Biochem & Mol Biol,Drug Discovery Program, Tampa, FL 33612 USA
[3] Univ S Florida, Drug Discovery Program, H Lee Moffitt Canc Ctr & Res Inst, Dept Interdisciplinary Oncol,Coll Med, Tampa, FL 33612 USA
[4] Univ S Florida, Dept Chem, Ctr Mol Divers Drug Design Discovery & Delivery, Tampa, FL 33620 USA
关键词
beta-lactam; DNA damage; apoptosis; anti-tumor activity; breast cancer;
D O I
10.1016/j.canlet.2008.03.047
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
An ongoing strategy for cancer treatment is selective induction of apoptosis in cancer over normal cells. N-thiolated beta-lactams were found to induce DNA damage, growth arrest and apoptosis in cultured human cancer cells. However, whether these compounds have a similar effect in vivo has not been studied. We report here that treatment with the P-lactam L-1 caused a significant inhibition of tumor growth in a breast cancer xenograft mouse model, associated with induction of DNA damage and apoptosis in vivo. These results suggest that the synthetic antibiotic N-thiolated beta-lactams hold great potential to be developed as novel anti-cancer drugs. Published by Elsevier Ltd.
引用
收藏
页码:63 / 69
页数:7
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