A new polyoxygenated cyclohexane and other constituents from <i>Kaempferia rotunda</i> and their cytotoxic activity

<div><p>The isolation of secondary metabolites from a methanolic extract of <i>Kaempferia rotunda</i> yielded 12 compounds (<b>1</b>–<b>12</b>), including a new polyoxygenated cyclohexane compound, (–)-3-acetyl-4-benzoyl-1-benzoyloxymethyl-1,6-diepoxycyclohexan-2,3,4,5-tetrol (<b>1</b>). The structures of the isolated compounds were determined based on their spectroscopic data and comparison with references. All of the isolated compounds were tested for their cytotoxic activity against pancreatic (PSN-1) and breast (MDA-MB231) cancer cell lines. Compound <b>12</b> showed moderate cytotoxic activity against PSN-1 and MDA-MB231 without showing any cytotoxicity against the normal cell line, TIG-3.</p></div

Chemical Constituents of Thai <i>Citrus hystrix</i> and Their Antiausterity Activity against the PANC‑1 Human Pancreatic Cancer Cell Line

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 <i>Citrus hystrix</i> 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 (<b>1</b>–<b>10</b>) including a new furanocoumarin (<b>1</b>). 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 (<b>7</b>) was identified as the most active constituent. In real-time live imaging, <b>7</b> was found to induce cell shrinkage, membrane blebbing, and disintegration of organelles in PANC-1 cells. Bergamottin (<b>7</b>) was also found to inhibit PANC-1 cell migration and colony formation. Mechanistically, <b>7</b> inhibited key survival proteins in the Akt/mTOR signaling pathway. Bergamottin (<b>7</b>) and related compounds are potential antiausterity candidates for drug development against pancreatic cancer

Chemical Constituents of Thai <i>Citrus hystrix</i> and Their Antiausterity Activity against the PANC‑1 Human Pancreatic Cancer Cell Line

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 <i>Citrus hystrix</i> 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 (<b>1</b>–<b>10</b>) including a new furanocoumarin (<b>1</b>). 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 (<b>7</b>) was identified as the most active constituent. In real-time live imaging, <b>7</b> was found to induce cell shrinkage, membrane blebbing, and disintegration of organelles in PANC-1 cells. Bergamottin (<b>7</b>) was also found to inhibit PANC-1 cell migration and colony formation. Mechanistically, <b>7</b> inhibited key survival proteins in the Akt/mTOR signaling pathway. Bergamottin (<b>7</b>) and related compounds are potential antiausterity candidates for drug development against pancreatic cancer

Constituents of the Rhizomes of <i>Boesenbergia pandurata</i> and Their Antiausterity Activities against the PANC‑1 Human Pancreatic Cancer Line

Human pancreatic cancer cell lines have a remarkable tolerance to nutrition starvation, which enables them to survive under a tumor microenvironment. The search for agents that preferentially inhibit the survival of cancer cells under low nutrient conditions represents a novel antiausterity strategy in anticancer drug discovery. In this investigation, a methanol extract of the rhizomes of <i>Boesenbergia pandurata</i> showed potent preferential cytotoxicity against PANC-1 human pancreatic cancer cells under nutrient-deprived conditions, with a PC₅₀ value of 6.6 μg/mL. Phytochemical investigation of this extract led to the isolation of 15 compounds, including eight new cyclohexene chalcones (<b>1</b>–<b>8</b>). The structures of the new compounds were elucidated by NMR spectroscopic data analysis. Among the isolated compounds obtained, isopanduratin A1 (<b>14</b>) and nicolaioidesin C (<b>15</b>) exhibited potent preferential cytotoxicity against PANC-1 human pancreatic cancer cells under nutrition-deprived conditions, with PC₅₀ values of 1.0 and 0.84 μM, respectively