New histone deacetylase inhibitors from the twigs of Melanorrhoea usitata
| Autor: | Pakit Kumboonma, Chanokbhorn Phaosiri, Chavi Yenjai, Thanaset Senawong, Somprasong Saenglee |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Gene isoform biology 010405 organic chemistry Histone deacetylase 2 Chemistry Organic Chemistry HDAC7 HDAC8 biology.organism_classification 01 natural sciences HDAC4 In vitro 0104 chemical sciences 03 medical and health sciences 030104 developmental biology Biochemistry Melanorrhoea usitata Histone deacetylase General Pharmacology Toxicology and Pharmaceutics |
| Zdroj: | Medicinal Chemistry Research. 27:2004-2015 |
| ISSN: | 1554-8120 1054-2523 |
| Popis: | Two new compounds, melanorrone (1) and melanorric acid (2), as well as 19 known compounds were isolated and identified from the twigs of Melanorrhoea usitata. Their structures were determined by spectroscopic methods (IR, 1H-NMR, 13C-NMR, 2D-NMR, MS, and ECD). The histone deacetylase (HDAC) inhibitory activities of the obtained compounds were evaluated. Melanorrone (1) along with five known compounds acted as good HDAC inhibitors at 100 μM. Molecular docking experiments of these compounds with representatives of class I (HDAC2 and HDAC8) and class II (HDAC4 and HDAC7) HDAC isoforms displayed potential isoform-selective HDAC inhibitors. Molecular docking data showed consistent results to the in vitro experiments with the high selectivity towards HDAC4 and HDAC8. |
| Databáze: | OpenAIRE |
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