Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development
The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several chemical...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-09-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/28/18/6450 |
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| author | Camilla Pecoraro Francesca Terrana Giovanna Panzeca Barbara Parrino Stella Cascioferro Patrizia Diana Elisa Giovannetti Daniela Carbone |
| author_facet | Camilla Pecoraro Francesca Terrana Giovanna Panzeca Barbara Parrino Stella Cascioferro Patrizia Diana Elisa Giovannetti Daniela Carbone |
| author_sort | Camilla Pecoraro |
| collection | DOAJ |
| description | The marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several chemical subclasses. In this review, we focus on the bis-indolyl alkaloid Nortopsentins and their derivatives with antiproliferative properties. Nortopsentins A–C were found to exhibit <i>in vitro</i> cytotoxicity against the P388 murine leukaemia cell line. Their structural manipulation provided a wide range of derivatives with significant anti-tumour activity against human cell lines derived from different cancer types (bladder, colon, gastric, CNS, liver, lung, breast, melanoma, ovarian, pancreatic, prostate, pleural mesothelioma, renal, sarcoma, and uterus). <i>In vivo</i> assays on animal models also proved that Nortopsentins and related bis-indolyl compounds have potent anti-inflammatory activity. These remarks set the foundation for future investigations into the development of new Nortopsentin derivatives as new anticancer and anti-inflammatory agents. |
| first_indexed | 2024-03-10T22:24:58Z |
| format | Article |
| id | doaj.art-35f42eb732474d3ca1a712d0e6773846 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T22:24:58Z |
| publishDate | 2023-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-35f42eb732474d3ca1a712d0e67738462023-11-19T12:07:32ZengMDPI AGMolecules1420-30492023-09-012818645010.3390/molecules28186450Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent DevelopmentCamilla Pecoraro0Francesca Terrana1Giovanna Panzeca2Barbara Parrino3Stella Cascioferro4Patrizia Diana5Elisa Giovannetti6Daniela Carbone7Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyDepartment of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyDepartment of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyDepartment of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyDepartment of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyDepartment of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyDepartment of Medical Oncology, Cancer Center Amsterdam, Amsterdam UMC, VU University Medical Center (VUmc), De Boelelaan 1117, 1081 HV Amsterdam, The NetherlandsDepartment of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, PA, ItalyThe marine environment is an excellent source of molecules that have a wide structural diversity and a variety of biological activities. Many marine natural products (MNPs) have been established as leads for anticancer drug discovery. Most of these compounds are alkaloids, including several chemical subclasses. In this review, we focus on the bis-indolyl alkaloid Nortopsentins and their derivatives with antiproliferative properties. Nortopsentins A–C were found to exhibit <i>in vitro</i> cytotoxicity against the P388 murine leukaemia cell line. Their structural manipulation provided a wide range of derivatives with significant anti-tumour activity against human cell lines derived from different cancer types (bladder, colon, gastric, CNS, liver, lung, breast, melanoma, ovarian, pancreatic, prostate, pleural mesothelioma, renal, sarcoma, and uterus). <i>In vivo</i> assays on animal models also proved that Nortopsentins and related bis-indolyl compounds have potent anti-inflammatory activity. These remarks set the foundation for future investigations into the development of new Nortopsentin derivatives as new anticancer and anti-inflammatory agents.https://www.mdpi.com/1420-3049/28/18/6450natural productsmarine alkaloidsnortopsentin derivativesanticancer agentsanti-inflammatory agents |
| spellingShingle | Camilla Pecoraro Francesca Terrana Giovanna Panzeca Barbara Parrino Stella Cascioferro Patrizia Diana Elisa Giovannetti Daniela Carbone Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development Molecules natural products marine alkaloids nortopsentin derivatives anticancer agents anti-inflammatory agents |
| title | Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development |
| title_full | Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development |
| title_fullStr | Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development |
| title_full_unstemmed | Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development |
| title_short | Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development |
| title_sort | nortopsentins as leads from marine organisms for anticancer and anti inflammatory agent development |
| topic | natural products marine alkaloids nortopsentin derivatives anticancer agents anti-inflammatory agents |
| url | https://www.mdpi.com/1420-3049/28/18/6450 |
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