Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line
Copyright © 2018 American Chemical Society and American Society of Pharmacognosy. 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...
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th-cmuir.6653943832-625742018-11-29T07:55:57Z Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line Sijia Sun Ampai Phrutivorapongkul Dya Fita Dibwe Chandrasekar Balachandran Suresh Awale Biochemistry, Genetics and Molecular Biology Chemistry Medicine Pharmacology, Toxicology and Pharmaceutics Copyright © 2018 American Chemical Society and American Society of Pharmacognosy. 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. 2018-11-29T07:32:43Z 2018-11-29T07:32:43Z 2018-08-24 Journal 15206025 01633864 2-s2.0-85052553843 10.1021/acs.jnatprod.8b00405 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85052553843&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/62574 |
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Biochemistry, Genetics and Molecular Biology Chemistry Medicine Pharmacology, Toxicology and Pharmaceutics Sijia Sun Ampai Phrutivorapongkul Dya Fita Dibwe Chandrasekar Balachandran Suresh Awale Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line |
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Copyright © 2018 American Chemical Society and American Society of Pharmacognosy. 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. |
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Journal |
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Sijia Sun Ampai Phrutivorapongkul Dya Fita Dibwe Chandrasekar Balachandran Suresh Awale |
author_facet |
Sijia Sun Ampai Phrutivorapongkul Dya Fita Dibwe Chandrasekar Balachandran Suresh Awale |
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Sijia Sun |
title |
Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line |
title_short |
Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line |
title_full |
Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line |
title_fullStr |
Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line |
title_full_unstemmed |
Chemical Constituents of Thai Citrus hystrix and Their Antiausterity Activity against the PANC-1 Human Pancreatic Cancer Cell Line |
title_sort |
chemical constituents of thai citrus hystrix and their antiausterity activity against the panc-1 human pancreatic cancer cell line |
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2018 |
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https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85052553843&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/62574 |
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