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Mar. Drugs 2017, 15(3), 63; doi:10.3390/md15030063

Cytotoxicity of Endoperoxides from the Caribbean Sponge Plakortis halichondrioides towards Sensitive and Multidrug-Resistant Leukemia Cells: Acids vs. Esters Activity Evaluation

1
Institute of Pharmacy and Biochemistry, Johannes Gutenberg University Mainz, Staudinger Weg 5, 55128 Mainz, Germany
2
The NeaNat Group, Dipartimento di Farmacia, Università degli Studi di Napoli Federico II, via D. Montesano 49, 80131 Napoli, Italy
*
Author to whom correspondence should be addressed.
Academic Editor: Friedemann Honecker
Received: 15 December 2016 / Revised: 15 February 2017 / Accepted: 16 February 2017 / Published: 3 March 2017
(This article belongs to the Collection Marine Compounds and Cancer)
View Full-Text   |   Download PDF [592 KB, uploaded 3 March 2017]   |  

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. View Full-Text
Keywords: Caribbean sponge; plakortide; endoperoxide; leukemia; multi-drug resistant leukemia; cytotoxicity Caribbean sponge; plakortide; endoperoxide; leukemia; multi-drug resistant leukemia; cytotoxicity
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MDPI and ACS Style

Schirmeister, T.; Oli, S.; Wu, H.; Della Sala, G.; Costantino, V.; Seo, E.-J.; Efferth, T. Cytotoxicity of Endoperoxides from the Caribbean Sponge Plakortis halichondrioides towards Sensitive and Multidrug-Resistant Leukemia Cells: Acids vs. Esters Activity Evaluation. Mar. Drugs 2017, 15, 63.

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