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  • Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome.

Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome.

Biochemical and biophysical research communications (2018-01-23)
Elodie Bosc, Jhennifer Nastri, Valérie Lefort, Marilia Valli, Fernando Contiguiba, Renan Pioli, Maysa Furlan, Vanderlan da Silva Bolzani, Chahrazade El Amri, Michèle Reboud-Ravaux
ABSTRACT

The natural small molecule piperlongumine A is toxic selectively to cancer cells in vitro and in vivo. This toxicity has been correlated with cancer cell ROS, DNA damage and apoptotic cell death increases. We demonstrate here a new mechanistic property of piperlongumine: it inhibits selectively human immunoproteasome with no noticeable inhibition of human constitutive proteasome. This result suggests that immunoproteasome inhibition, a mechanism independent of ROS elevation, may also partly play a role in the anticancer effects observed with piperlongumine. Structure-activity relationships of piperlongumine analogs suggest that the lactam (piperidonic) ring of piperlongumine A may be replaced by the linear olefin -NHCO-CH2=CH2 to improve both in vitro inhibitory efficiency against immunoproteasome and cellular toxicity.

MATERIALS
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Product Description

Roche
Cell Proliferation Kit II (XTT), liquid, pkg of 1 kit, suitable for cell analysis, suitable for tissue culture