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Description

Canthardin is a toxin initially produced by the blister beetle, Canarthis vesicatoria. Canthardin competitively inhibits serine/threonine phosphatases such as protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A). Canthardin exhibits anticancer and anti-resorptive activities. In cancer cells, canthardin upregulates expression of caspase 1 and the NGF receptor and downregulates expression of Bcl-2-like protein 10, Fas ligand, and TNF-α. In colorectal cancer cells, canthardin inhibits heat shock factor 1 and downstream HSP70- and BAG3-related signaling, inhibiting cell proliferation. Additionally, cantharidin displays pro-inflammatory activity in vivo, producing increases in MCP-1, IL-6, IL-1β, and myeloperoxidase. In vitro, this compound inhibits RANKL-induced expression of Fra-2 and cathepsin K and inhibits activation of ERK and MAPK signaling; these actions result in inhibition of differentiation and resorptive activity.

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Chen X, Liu J, Zhang Y. Cantharidin impedes the activity of protein serine/threonine phosphatase in Plutella xylostella. Mol Biosyst. 2013 Nov 19. [Epub ahead of print]. PMID: 24253262.

Kadioglu O, Kermani NS, Kelter G, et al. Pharmacogenomics of Cantharidin in Tumor Cells. Biochem Pharmacol. 2013 Nov 11. pii: S0006-2952(13)00709-0. Epub ahead of print]. PMID: 24231507.

Kim JA, Kim Y, Kwon BM, et al. The natural compound cantharidin induces cancer cell death through inhibition of heat shock protein 70 (HSP70) and Bcl-2-associated athanogene domain 3 (BAG3) expression by blocking heat shock factor 1 (HSF1) binding to promoters. J Biol Chem. 2013 Oct 4;288(40):28713-26. PMID: 23983126.

Ivetic Tkalcevic V, Hrvacic B, Bosnar M, et al. Cantharidin-induced inflammation in mouse ear model for translational research of novel anti-inflammatories. Transl Res. 2012 Aug;160(2):137-45. PMID: 22677362.

Kim MH, Shim KS, Kim SH. Inhibitory effect of cantharidin on osteoclast differentiation and bone resorption. Arch Pharm Res. 2010 Mar;33(3):457-62. PMID: 20361312.