論文 - 詳細
| RRC ID | 67316 |
|---|---|
| 著者 | Sun S, Phrutivorapongkul A, Dibwe DF, Balachandran C, Awale S. |
| タイトル | Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line. |
| ジャーナル | J Nat Prod |
| Abstract |
Human pancreatic cancer cells have an extreme tolerance to nutrition starvation, enabling them to survive in a hypovascular tumor microenvironment. Searching for agents that preferentially inhibit cancer cell viability under nutrition starvation conditions is a novel antiausterity strategy in anticancer drug discovery. In the present study, a hexane extract of the peels of Citrus hystrix fruits showed preferential cytotoxicity against PANC-1 human pancreatic cancer cells using a nutrient-deprived medium. Phytochemical investigation of this bioactive extract led to the isolation of 10 coumarins (1-10) including a new furanocoumarin (1). The isolated compounds were tested for their preferential cytotoxic activity against three different human pancreatic cancer cell lines [PANC-1, MIA PaCa-2, and PSN-1]. Among these, bergamottin (7) was identified as the most active constituent. In real-time live imaging, 7 was found to induce cell shrinkage, membrane blebbing, and disintegration of organelles in PANC-1 cells. Bergamottin (7) was also found to inhibit PANC-1 cell migration and colony formation. Mechanistically, 7 inhibited key survival proteins in the Akt/mTOR signaling pathway. Bergamottin (7) and related compounds are potential antiausterity candidates for drug development against pancreatic cancer. |
| 巻・号 | 81(8) |
| ページ | 1877-1883 |
| 公開日 | 2018-8-24 |
| DOI | 10.1021/acs.jnatprod.8b00405 |
| PMID | 30070833 |
| MeSH | Antineoplastic Agents, Phytogenic / pharmacology* Cell Line, Tumor Cell Membrane / drug effects Cell Membrane / ultrastructure Cell Movement / drug effects Cell Size / drug effects Citrus / chemistry* Coumarins / isolation & purification Coumarins / pharmacology Drug Screening Assays, Antitumor Humans Molecular Structure Organelles / drug effects Organelles / ultrastructure Pancreatic Neoplasms / drug therapy* Thailand Tumor Microenvironment Tumor Stem Cell Assay Wound Healing / drug effects |
| IF | 3.782 |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | X(Twitter) |
| 各媒体での言及数の合計 | 7 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | PANC-1(RCB2095) |