Drug intelligence / Profile preview

chelerythrine

Development stage
Preclinical
Lead developer
Immedica
Modality
Small Molecules
Administration
Intraperitoneal (experimental/animal Studies)[3][5]
01

Overview

Chelerythrine is a benzophenanthridine alkaloid isolated from plants such as Chelidonium majus and species of Zanthoxylum. It is primarily known as a potent and selective inhibitor of protein kinase C (PKC), acting as a cell-permeable small molecule. In addition to PKC inhibition, chelerythrine antagonizes G-protein-coupled CB1 receptors and inhibits pro-survival proteins like BclXL by blocking their binding to Bak BH3 peptides. This leads to the induction of apoptosis in various cancer cell lines through disruption of calcium homeostasis and mitochondrial function. Chelerythrine also exhibits antibacterial activity by disrupting bacterial cell walls and membranes. Its biological activities include antitumor, anti-inflammatory, antidiabetic effects and it has been used experimentally for its ability to induce apoptosis in cancer cells[1][2][4][6].

Other names
BroussonpapyrineCheleritrineToddalinToddaline1,2-dimethoxy-12-methyl(1,3)dioxolo)4',5':4,5)benzo(1,2-c)phenanthridinium(1,3)benzodioxolo(5,6-c)phenanthridinium, 1,2-dimethoxy-12-methyl-Chelerythrine chloride
02

Targets

PKC (Protein kinase C family)BCL2L1 (B-cell lymphoma-extra large protein)

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