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.