| รหัสดีโอไอ | 10.14456/sjst-psu.2022.192 |
|---|---|
| Creator | 1. La-or Somsakeesit 2. Anupong Joompang 3. Santi Phosri 4. Pattaravadee Srikoon 5. Pakit Kumboonma 6. Thanaset Senawong 7. Chanokbhorn Phaosiri |
| Title | Evaluation of histone deacetylase inhibitory andantiproliferative activity of piperine and its derivatives |
| Publisher | Research and Development Office, Prince of Songkla University |
| Publication Year | 2022 |
| Journal Title | Songklanakarin Journal of Science an Technology (SJST) |
| Journal Vol. | 44 |
| Journal No. | 6 |
| Page no. | 1481-1488 |
| Keyword | piper nigrum l., piperine, piperine derivative, HDAC, hela cell |
| URL Website | https://sjst.psu.ac.th/ |
| ISSN | 0125-3395 |
| Abstract | Piperine (1) was obtained from the seeds of Piper nigrum L. It could act as a pan-histone deacetylase (HDAC)inhibitor. This lead compound was structurally modified to six derivatives that exhibited improved HDAC inhibitory activity.Based on the preliminary results, amide derivatives (1e and 1f) with the highest HDAC inhibitory activity were further studied.The results indicated that the derivatives 1e and 1f showed HDAC inhibitory activity with IC50 of 85.61 ? 3.32 ?M and 111.27 ?2.13 ?M, respectively. A molecular docking study suggested that piperine (1) had a high selectivity for HDAC1, while 1e and 1fshowed high selectivity for HDAC2. These derivatives were predicted to interact with HDAC active site using hydrogen bond,hydrophobic interaction, as well as chelation with Zn2+. The antiproliferative activity obtained from MTT assay against the HeLacell line indicated that 1f potentially inhibits HeLa cells with an IC50 of 10.38 ? 2.13 g/mL. These results suggest potentialHDAC inhibitors for further development to anti-cancer agents. |
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Digital File |