The redox couple avarol/avarone in the fight with malignant gliomas: the case study of U-251 MG cells.

Abstract

This study aimed to screen in vitro antitumour activity of the redox couple avarol/avarone against the human malignant glioma cell line U-251 MG for the first time. Compared both with avarol and positive controls used (temozolomide and doxorubicin), avarone was found to be the most active compound with IC50 value below 1 μM (IC50 0.68 ± 0.04 μM, 96 h). Considerable less DNA damage in the cells treated with avarol and avarone vs. doxorubicin (105 & 123% vs. 299%, respectively; untreated U-251 MG cells were used as a control, 100%), coupled with no sign of cytotoxicity against the normal human foetal lung fibroblast MRC-5 cells (IC50 > 100 μM), has actually pointed out the importance of this marine sesquiterpenoid quinone structure as a promising lead compound in development of novel brain chemotherapeutics.

• Authors: Boris Pejin, Giuseppina Tommonaro, Miodrag Glumac, Dimitar Jakimov, Vesna Kojic
• Journal: Natural product research (Nat Prod Res) Vol. 32 Issue 5 Pg. 616-620 (Mar 2018) ISSN: 1478-6427 [Electronic] England
• PMID: 28504009 (Publication Type: Journal Article)

Chemical References

• Cyclohexenes
• Sesquiterpenes
• avarone
• Dacarbazine
• Doxorubicin
• avarol
• Temozolomide

Topics

• Antineoplastic Combined Chemotherapy Protocols (pharmacology)
• Brain Neoplasms (drug therapy, pathology)
• Cell Line, Tumor
• Comet Assay
• Cyclohexenes (administration & dosage, pharmacology)
• DNA Damage (drug effects)
• Dacarbazine (analogs & derivatives, pharmacology)
• Doxorubicin (pharmacology)
• Fibroblasts (drug effects)
• Glioma (drug therapy, pathology)
• Humans
• Oxidation-Reduction
• Sesquiterpenes (administration & dosage, pharmacology)
• Temozolomide