Cytotoxicity of Artesunic Acid Homo- and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells

6533b871fe1ef96bd12d1b07

RESEARCH PRODUCT

Cytotoxicity of Artesunic Acid Homo- and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells

Svetlana B. Tsogoeva Cindy Horwedel Thomas Efferth Thomas Efferth Shengwei Wei

subject

Spectrometry Mass Electrospray Ionization Magnetic Resonance Spectroscopy Cell Survival Apoptosis chemistry.chemical_compound Cell Line Tumor Drug Discovery medicine Humans Cytotoxicity chemistry.chemical_classification Reactive oxygen species Formazans Leukemia Betulin Cell Cycle Succinates Cell cycle Flow Cytometry medicine.disease Artemisinins Triterpenes Multiple drug resistance Leukemia chemistry Biochemistry Drug Resistance Neoplasm Cell culture Apoptosis Molecular Medicine Reactive Oxygen Species

description

A novel approach to circumvent multidrug resistance is hybridization of natural products in dimers. We analyzed homodimers of two artesunic acid molecules and heterohybrids of artesunic acid and betulin in human CCRF-CEM and multidrug-resistant P-glycoprotein-overexpressing CEM/ADR5000 leukemia cells. Multidrug-resistant cells were not cross-resistant to the novel compounds. Collateral sensitivity was observed for artesunic acid homodimer. Artesunic acid and artesunic acid homodimer induced G0/G1 cell cycle arrest, apoptosis, and formation of reactive oxygen species.

year	journal	country	edition	language
2010-06-08	Journal of Medicinal Chemistry

https://doi.org/10.1021/jm100404t

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