Drug intelligence / Profile preview

harringtonolide

Development stage
Preclinical
Modality
Classical Binding Small Molecules → Small Molecules
01

Overview

Harringtonolide is a bioactive diterpenoid tropone natural product isolated from the plant Cephalotaxus harringtonia. It possesses a unique cage-like polycyclic structure featuring a tropone ring, bridged lactone, and tetrahydrofuran ring. Harringtonolide exhibits potent antiproliferative and cytotoxic activity against various cancer cell lines (e.g., HCT-116, A375, A549, Huh-7), with reported IC50 values in the nanomolar range for some tumor cells. Its mechanism of action involves direct binding to receptor for activated C kinase 1 (RACK1), leading to inhibition of the epithelial–mesenchymal transition (EMT) process and suppression of cell proliferation by affecting the FAK/Src/STAT3 signaling pathway. These activities make it an effective antitumor agent candidate[1][2][4][8].

Other names
hainanolide
02

Targets

RACK1 (Receptor for activated C kinase 1)

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