α-Methylene-γ-lactones as a Novel Class of Anti-leukemic Agents
Katarzyna Gach and Anna Janecka
Affiliation: Department of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, 92-215 Lodz, Poland.
Natural products are important leads in drug discovery. In recent years, the anti-leukemic properties of natural compounds
isolated from plants, containing an α-Methylene-γ-lactones skeleton, have attracted a lot of attention. Extensive research has been carried
out to characterize their molecular mechanisms of action and potential chemotherapeutic application in different types of cancer,
including leukemias. Sesquiterpene lactones, a group of α-Methylene-γ-lactones are plant-derived compounds, mostly of the Compositae
family, used in traditional medicine especially for the treatment of inflammation. However, they exhibit a broad spectrum of other
biological effects, including cytotoxic, anti-bacterial, anti-helminthic, and anti-tumor activity. Recently, a sesquiterpene lactone,
parthenolide, and several other compounds containing an α-methylene-γ-lactone skeleton have become topics of interest as potential antileukemic
agents. The recent research emphasizes their selective activity against leukemia cells while the normal hematopoietic cells
remain unaffected. In this review, we give a brief description of natural α-Methylene-γ-lactones isolated from plants and their derivates
with minor chemical modifications that possess anti-leukemic activity. We also discuss molecular mechanisms of action of these
compounds, in particular, their selectivity against leukemia cells.
Keywords: Alkylating agents, α-Methylene-γ-lactones, apoptosis, leukemia treatment, leukemia stem cells, sesquiterpene lactones.
Rights & PermissionsPrintExport