Olive Leaf Metabolites as Covalent Human Topoisomerase II Poisons Academic Article uri icon

abstract

  • Topoisomerase II plays many essential roles in genome maintenance. To carry out its physiological functions, the enzyme generates transient double-stranded breaks in the DNA to help resolve topological problems that naturally occur. Thus, while essential to cell survival, topoisomerase II has the potential to fragment the genome. Beyond its critical cellular functions, human topoisomerase II is the target for a number of widely prescribed anticancer drugs that act by increasing levels of enzyme-mediated DNA strand breaks. Many of these “topoisomerase II poisons” are derived from natural sources. Identification and characterization of topoisomerase II poisons from natural sources can provide novel drug scaffolds. Therefore, a series of water-soluble extracts from Mediterranean plants were screened for activity against human topoisomerase IIα. An extract from Phillyrhea latifolia …

publication date

  • April 1, 2016