| RRC ID |
58578
|
| 著者 |
Yeong KY, Khaw KY, Takahashi Y, Itoh Y, Murugaiyah V, Suzuki T.
|
| タイトル |
Discovery of gamma-mangostin from Garcinia mangostana as a potent and selective natural SIRT2 inhibitor.
|
| ジャーナル |
Bioorg Chem
|
| Abstract |
Studies have suggested that sirtuin inhibition may have beneficial effects on several age-related diseases such as neurodegenerative disorders and cancer. Garcinia mangostana is a well-known tropical plant found mostly in South East Asia with several positive health effects. Some of its phytochemicals such as α-mangostin was found to be able to modulate sirtuin activity in mice and was implicated with inflammation, diabetes and obesity. However, comprehensive studies on sirtuin activity by the prenylated xanthones extracted from Garcinia mangostana have yet to be reported. The present study led to the discovery and identification of γ-mangostin as a potent and selective SIRT2 inhibitor. It was demonstrated that γ-mangostin was able to increase the α-tubulin acetylation in MDA-MD-231 and MCF-7 breast cancer cells. It was also found to possess potent antiproliferative activity against both cell lines. In addition, it was able to induce neurite outgrowth in the N2a cells.
|
| 巻・号 |
94
|
| ページ |
103403
|
| 公開日 |
2020-1-1
|
| DOI |
10.1016/j.bioorg.2019.103403
|
| PII |
S0045-2068(19)30999-X
|
| PMID |
31711765
|
| MeSH |
Antineoplastic Agents, Phytogenic / chemistry
Antineoplastic Agents, Phytogenic / isolation & purification
Antineoplastic Agents, Phytogenic / pharmacology*
Cell Proliferation / drug effects
Dose-Response Relationship, Drug
Drug Discovery*
Drug Screening Assays, Antitumor
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / isolation & purification
Enzyme Inhibitors / pharmacology*
Garcinia mangostana / chemistry*
Humans
Molecular Docking Simulation
Molecular Structure
Sirtuin 2 / antagonists & inhibitors*
Sirtuin 2 / metabolism
Structure-Activity Relationship
Tumor Cells, Cultured
Xanthones / chemistry
Xanthones / isolation & purification
Xanthones / pharmacology*
|
| IF |
3.926
|
| 引用数 |
0
|
| リソース情報 |
| ヒト・動物細胞 |
MCF7(RCB1904) |
