Reference - Detail
| RRC ID | 58578 |
|---|---|
| Author | Yeong KY, Khaw KY, Takahashi Y, Itoh Y, Murugaiyah V, Suzuki T. |
| Title | Discovery of gamma-mangostin from Garcinia mangostana as a potent and selective natural SIRT2 inhibitor. |
| Journal | 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. |
| Volume | 94 |
| Pages | 103403 |
| Published | 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 |
| Times Cited | 0 |
| Altmetric score |
オルトメトリクス指標項目
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| Total number of mentions | 0 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | MCF7(RCB1904) |