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Inhibition of capsaicin and dihydrocapsaicin derivatives towards histonedeacetylase and molecular docking studies |
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| รหัสดีโอไอ | |
| Creator | 1. Pakit Kumboonma 2. Thanaset Senawong 3. Khatcharin Siriwong 4. Chavi Yenjai 5. Chanokbhorn Phaosiri |
| Title | Inhibition of capsaicin and dihydrocapsaicin derivatives towards histonedeacetylase and molecular docking studies |
| Publisher | Research and Development Office, Prince of Songkla University |
| Publication Year | 2016 |
| Journal Title | Songklanakarin Journal of Science and Technology (SJST) |
| Journal Vol. | 38 |
| Journal No. | 4 |
| Page no. | 399-406 |
| Keyword | red chili pepper,Capsicum annuum,histone deacetylase,HeLa cell,anticancer |
| ISSN | 0125-3395 |
| Abstract | The natural products, capsaicin and dihydrocapsaicin, were modified at double-bond and phenolic moieties to providetwelve capsaicin and dihydrocapsaicin derivatives. The natural products and synthesized compounds were evaluated ashistone deacetylase inhibitors via in vitro fluorometric assay at 500 mM concentrations. The results revealed that a methylester derivative and a silyl-protected dihydrocapsaicin were the best histone deacetylase inhibitors among the testedcompounds with 87% and 85% inhibitions, respectively. Molecular docking experiments were conducted on the obtainedcompounds with the human HDAC8 enzyme. These data show a new method for providing putative histone deacetylaseinhibitors from common natural products. |
