TY - JOUR
T1 - Nortopsentins as Leads from Marine Organisms for Anticancer and Anti-Inflammatory Agent Development
AU - Pecoraro, Camilla
AU - Terrana, Francesca
AU - Panzeca, Giovanna
AU - Parrino, Barbara
AU - Cascioferro, Stella
AU - Diana, Patrizia
AU - Giovannetti, Elisa
AU - Carbone, Daniela
N1 - Funding Information: This work was partially supported by the following grants: PRIN2017, Prot. No. 2017E84AA4 (to P.D.) and AIRC-IG grant, No. 24444 (to E.G.). Publisher Copyright: © 2023 by the authors.
PY - 2023/9/1
Y1 - 2023/9/1
N2 - 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 in vitro 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). In vivo 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.
AB - 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 in vitro 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). In vivo 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.
KW - anti-inflammatory agents
KW - anticancer agents
KW - marine alkaloids
KW - natural products
KW - nortopsentin derivatives
UR - http://www.scopus.com/inward/record.url?scp=85172801926&partnerID=8YFLogxK
U2 - https://doi.org/10.3390/molecules28186450
DO - https://doi.org/10.3390/molecules28186450
M3 - Review article
SN - 1420-3049
VL - 28
JO - Molecules
JF - Molecules
IS - 18
M1 - 6450
ER -