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| Content Provider | Royal Society of Chemistry (RSC) |
|---|---|
| Author | Zhu, Shijun Khuri, Fadlo R. Zhang, Hongzheng Sun, Aiming Arrendale, Richard F. Lin, Xiaoqian Chen, Zhuo G. Snyder, James P. Culver, Deborah Fu, Haian Reddy, Prabhakar Shoji, Mamoru Evers, Taylor J. Shin, Dong M. Moore, Terry W. Morii, Nao Mancini, Alessandra Howard, Randy B. Sica, Gabriel |
| Copyright Year | 2012 |
| Abstract | Objectives are to examine the efficacy, pharmacokinetics, and toxicology of a synthetic curcumin analog EF31 in head and neck squamous cell carcinoma. The synthesis of EF31 was described for the first time. Solubility of EF24 and EF31 was compared using nephelometric analysis. Human head and neck squamous cell carcinoma Tu212 xenograft tumors were established in athymic nude mice and treated with EF31 i.p. once daily five days a week for about 5–6 weeks. The long term effect of EF31 on the NF-κB signaling system in the tumors was examined by Western blot analysis. EF31 at 25 mg kg−1, i.p. inhibited tumor growth almost completely. Solubilities of EF24 and EF31 are <10 and 13 μg mL−1 or <32 and 47 μM, respectively. The serum chemistry profiles of treated mice were within the limits of normal, they revealed a linear increase of Cmax. EF31 decreased the level of phosphorylation of NF-κB p65. In conclusion, the novel synthetic curcumin analog EF31 is efficacious in inhibiting the growth of Tu212 xenograft tumors and may be useful for treating head and neck squamous cell carcinoma. The long term EF31 treatment inhibited NF-κB p65 phosphorylation in xenografts, implicating downregulation of cancer promoting transcription factors such as angiogenesis and metastasis. |
| Starting Page | 633 |
| Ending Page | 640 |
| Page Count | 8 |
| File Format | HTM / HTML PDF |
| ISSN | 17579694 |
| Volume Number | 4 |
| Issue Number | 6 |
| Journal | Integrative Biology |
| DOI | 10.1039/c2ib20007d |
| Language | English |
| Publisher | Royal Society of Chemistry |
| Access Restriction | Open |
| Subject Keyword | Pharmacokinetics Toxicology Curcumin Carcinoma Human head Xenotransplantation Nude mouse NF-κB Western blot Chemistry Cmax (pharmacology) Phosphorylation Cancer Angiogenesis Metastasis |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Biochemistry Biophysics |
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