Mebendazole induces PINK1/Parkin-mediated mitophagy via regulating
mTOR/ULK1 signaling pathway by ROS accumulation deriving from
mitochondrial stress in melanom
Abstract
The development of safe and efficient drugs is urgently needed for
clinical melanoma treatment. The repurposing of existing drugs for new
clinical indications is an impressive strategy for the development of
antitumor drugs. In this study, we embarred on an exploration of
mebendazole, a well-established antiparasitic drug, to uncover its
potential antimelanoma effect and underlying mechanisms. Our findings
revealed that mebendazole possessed alluring antimelanoma activity with
good safety profiles both in vitro and in vivo. Specifically, the
antimelanoma function of mebendazole is derived from the inhibition of
cell proliferation, migration and invasion, epithelial-mesenchymal
transition (EMT), as well as the induction of endogenous apoptosis
through reactive oxygen species (ROS)-mediated PI3K/Akt/mTOR pathway.
Further studies have demonstrated that mebendazole can induce the
accumulation of intracellular ROS driven by activating oxidative stress
injury and causing a series of manifestations of mitochondrial
functional failure. Successively, mitochondrial stress activated
Ca2+-mediated and LKB1-mediated AMPK/mTOR/ULK1 pathway, which could
trigger PINK1/Parkin-mediated mitophagy. Notably, the ability of
mebendazole to induce apoptosis and inhibit proliferation in melanoma
cells was related to the induction of PINK1/Parkin-mediated mitophagy.
In summary, the present study revealed that mebendazole exerts
attractive antimelanoma effects by acting on mitochondria to regulate
ROS-mediated multiple signaling pathways.