Curcumin and its demethoxy derivatives possess p300 HAT inhibitory activity and suppress hypertrophic responses in cardiomyocytes
| Autor: | Satoshi Shimizu, Mai Genpei, Kana Shimizu, Shogo Sono, Hiromichi Wada, Yusuke Miyazaki, Morio Ueno, Eriko Morimoto, Tatsuya Morimoto, Hideaki Kakeya, Yasufumi Katanasaka, Koji Hasegawa, Yoichi Sunagawa, Masafumi Funamoto, Maki Komiyama |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Curcumin Cardiomyocyte hypertrophy p300 030204 cardiovascular system & hematology Pharmacology Bisdemethoxycurcumin Inhibitory postsynaptic potential Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound Curcuma 0302 clinical medicine Diarylheptanoids parasitic diseases Animals Humans Myocytes Cardiac p300-CBP Transcription Factors Demethoxycurcumin Curcuminoid Cells Cultured Heart Failure biology lcsh:RM1-950 Biological activity Hypertrophy Histone acetyltransferase biology.organism_classification lcsh:Therapeutics. Pharmacology 030104 developmental biology chemistry biology.protein Molecular Medicine Cattle Rabbits Phytotherapy |
| Zdroj: | Journal of Pharmacological Sciences, Vol 136, Iss 4, Pp 212-217 (2018) |
| ISSN: | 1347-8613 |
| DOI: | 10.1016/j.jphs.2017.12.013 |
| Popis: | The natural compound, curcumin (CUR), possesses several pharmacological properties, including p300-specific histone acetyltransferase (HAT) inhibitory activity. In our previous study, we demonstrated that CUR could prevent the development of cardiac hypertrophy by inhibiting p300-HAT activity. Other major curcuminoids isolated from Curcuma longa including demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC) are structural analogs of CUR. In present study, we first confirmed the effect of these three curcuminoid analogs on p300-HAT activity and cardiomyocyte hypertrophy. Our results showed that DMC and BDMC inhibited p300-HAT activity and cardiomyocyte hypertrophy to almost the same extent as CUR. As the three compounds have structural differences in methoxy groups at the 3-position of their phenol rings, our results suggest that these methoxy groups are not involved in the inhibitory effects on p300-HAT activity and cardiac hypertrophy. These findings provide useful insights into the structure–activity relationship and biological activity of curcuminoids for p300-HAT activity and cardiomyocyte hypertrophy. |
| Databáze: | OpenAIRE |
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