Reference - Detail
| RRC ID | 67316 |
|---|---|
| Author | Sun S, Phrutivorapongkul A, Dibwe DF, Balachandran C, Awale S. |
| Title | Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line. |
| Journal | 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. |
| Volume | 81(8) |
| Pages | 1877-1883 |
| Published | 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 |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | X(Twitter) |
| Total number of mentions | 7 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | PANC-1(RCB2095) |