Autoren:	Schirmeister, Tanja Oli, Swarna Wu, Hongmei Della Sala, Gerardo Costantino, Valeria Seo, Ean-Jeong Efferth, Thomas
Titel:	Cytotoxicity of endoperoxides from the Caribbean sponge Plakortis halichondrioides towards sensitive and multidrug-resistant leukemia cells : acids vs. esters activity evaluation
Online-Publikationsdatum:	21-Okt-2022
Erscheinungsdatum:	2017
Sprache des Dokuments:	Englisch
Zusammenfassung/Abstract:	The 6-epimer of the plakortide H acid (1), along with the endoperoxides plakortide E (2), plakortin (3), and dihydroplakortin (4) have been isolated from a sample of the Caribbean sponge Plakortis halichondrioides. To perform a comparative study on the cytotoxicity towards the drug-sensitive leukemia CCRF-CEM cell line and its multi-drug resistant subline CEM/ADR5000, the acid of plakortin, namely plakortic acid (5), as well as the esters plakortide E methyl ester (6) and 6-epi-plakortide H (7) were synthesized by hydrolysis and Steglich esterification, respectively. The data obtained showed that the acids (1, 2, 5) exhibited potent cytotoxicity towards both cell lines, whereas the esters showed no activity (6, 7) or weaker activity (3, 4) compared to their corresponding acids. Plakortic acid (5) was the most promising derivative with half maximal inhibitory concentration (IC50) values of ca. 0.20 µM for both cell lines.
DDC-Sachgruppe:	570 Biowissenschaften 570 Life sciences
Veröffentlichende Institution:	Johannes Gutenberg-Universität Mainz
Organisationseinheit:	FB 09 Chemie, Pharmazie u. Geowissensch.
Veröffentlichungsort:	Mainz
ROR:	https://ror.org/023b0x485
DOI:	http://doi.org/10.25358/openscience-8142
Version:	Published version
Publikationstyp:	Zeitschriftenaufsatz
Nutzungsrechte:	CC BY
Informationen zu den Nutzungsrechten:	https://creativecommons.org/licenses/by/4.0/
Zeitschrift:	Marine drugs 15 3
Seitenzahl oder Artikelnummer:	Art. 63
Verlag:	Molecular Diversity Preservation International
Verlagsort:	Basel
Erscheinungsdatum:	2017
ISSN:	1660-3397
URL der Originalveröffentlichung:	http://dx.doi.org/10.3390/md15030063
DOI der Originalveröffentlichung:	10.3390/md15030063
Enthalten in den Sammlungen:	DFG-OA-Publizieren (2012 - 2017)