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3 results on '"plakortide"'

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

Author

Schirmeister, Tanja, Oli, Swarna, Wu, Hongmei, Della Sala, Gerardo, Costantino, Valeria, Ean-Jeong Seo, and Efferth, Thomas

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 themost promising derivativewith halfmaximal inhibitory concentration (IC50) values of ca. 0.20 &#181'M for both cell lines. [ABSTRACT FROM AUTHOR]

Published
2017
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2. Cytotoxicity of Endoperoxides from the Caribbean Sponge Plakortis halichondrioides towards Sensitive and Multidrug-Resistant Leukemia Cells: Acids vs. Esters Activity Evaluation

Author

Tanja Schirmeister, Swarna Oli, Hongmei Wu, Gerardo Della Sala, Valeria Costantino, Ean-Jeong Seo, and Thomas Efferth

Subjects
Caribbean sponge, plakortide, endoperoxide, leukemia, multi-drug resistant leukemia, cytotoxicity, Biology (General), QH301-705.5
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.

Published
2017
Full Text
View/download PDF

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

Author

Schirmeister, Tanja, Oli, Swarna, Wu, Hongmei, Sala, Gerardo Della, Costantino, Valeria, Seo, Ean-Jeong, Efferth, Thomas, Schirmeister, Tanja, Oli, Swarna, Wu, Hongmei, DELLA SALA, Gerardo, Costantino, Valeria, Seo, Ean Jeong, and Efferth, Thomas

Subjects
Leukemia, Caribbean sponge, plakortide, Esters, Antineoplastic Agents, Phytogenic, Drug Resistance, Multiple, Article, 570 Life sciences, Porifera, Dioxanes, lcsh:Biology (General), Caribbean Region, Drug Resistance, Neoplasm, Cell Line, Tumor, Plakortis, Animals, Humans, cytotoxicity, Drug Screening Assays, Antitumor, lcsh:QH301-705.5, Acids, endoperoxide, multi-drug resistant leukemia, 570 Biowissenschaften
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.

Published
2016

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