Authors:	Schirmeister, Tanja Oli, Swarna Wu, Hongmei Della Sala, Gerardo Costantino, Valeria Seo, Ean-Jeong Efferth, Thomas
Title:	Cytotoxicity of endoperoxides from the Caribbean sponge Plakortis halichondrioides towards sensitive and multidrug-resistant leukemia cells : acids vs. esters activity evaluation
Online publication date:	21-Oct-2022
Year of first publication:	2017
Language:	english
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:	570 Biowissenschaften 570 Life sciences
Institution:	Johannes Gutenberg-Universität Mainz
Department:	FB 09 Chemie, Pharmazie u. Geowissensch.
Place:	Mainz
ROR:	https://ror.org/023b0x485
DOI:	http://doi.org/10.25358/openscience-8142
Version:	Published version
Publication type:	Zeitschriftenaufsatz
License:	CC BY
Information on rights of use:	https://creativecommons.org/licenses/by/4.0/
Journal:	Marine drugs 15 3
Pages or article number:	Art. 63
Publisher:	Molecular Diversity Preservation International
Publisher place:	Basel
Issue date:	2017
ISSN:	1660-3397
Publisher URL:	http://dx.doi.org/10.3390/md15030063
Publisher DOI:	10.3390/md15030063
Appears in collections:	DFG-OA-Publizieren (2012 - 2017)