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Cytotoxic and apoptotic effects of leptocarpin, a plant-derived sesquiterpene lactone, on human cancer cell lines.

Abstract
Sesquiterpene lactones have attracted much attention in drug research because they present a series of biological activities such as anticancer, antifungal, anti-inflammatory, antimicrobial and antioxidant. Leptocarpin (LTC) is a sesquiterpene lactone isolated from a native Chilean plant, Leptocarpha rivularis, which has been widely used in traditional medicine by Mapuche people. Previous work has demonstrated that LTC decreases cell viability of cancer cell lines. In this contribution, we analyze the mechanism of LTC cytotoxicity on different cancer cell lines. The results show that in all cases LTC induces an apoptotic process and inhibition of NF-κB. Apoptosis has been confirmed by observing condensation of chromatin, nuclear fragmentation, release of cytochrome c into the cytosol, and increasing of caspase-3 activity. It has also been found that LTC is an effective inhibitor of NF-κB, which suggests that leptocarpin-induced cytotoxicity involves in some degree the inhibition of NF-κB signaling pathway. The concentration at which LTC inhibits NF-κB activity to the control level is similar or even lower than that found for parthenolide and others sesquiterpene lactones. These results indicate that leptocarpine is a very interesting molecule that could be considered as therapeutic agent for cancer treatment.
AuthorsClaudia Bosio, Giacomo Tomasoni, Rolando Martínez, Andrés F Olea, Héctor Carrasco, Joan Villena
JournalChemico-biological interactions (Chem Biol Interact) Vol. 242 Pg. 415-21 (Dec 05 2015) ISSN: 1872-7786 [Electronic] Ireland
PMID26562779 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2015 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Sesquiterpenes
  • leptocarpin
  • Cytochromes c
Topics
  • Antineoplastic Agents (pharmacology)
  • Apoptosis (drug effects)
  • Asteraceae (chemistry)
  • Cell Line, Tumor
  • Cytochromes c (metabolism)
  • Cytosol (drug effects, metabolism)
  • Humans
  • Sesquiterpenes (pharmacology)

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