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Acevaltrate is an iridoid valepotriate that has been found in V. glechomifolia and has diverse biological activities.1,2,3 It inhibits Na+/K+-ATPase in isolated rat kidney that endogenously expresses this transporter (IC50 = 22.8 µM) and H+/K+-ATPase activity by 60.7% in isolated rat gastric epithelium, which endogenously expresses H+/K+-ATPase, when used at a concentration of 100 µM.2 Acevaltrate (1-4 µM) induces pyroptosis in OCI-My5 and OPM-2 multiple myeloma cells.3 It increases the production of reactive oxygen species (ROS), inhibits glutathione peroxidase 4 (GPX4), and induces ferroptosis in RKO colon cancer cells when used at a concentration of 5 µM.1 In vivo, acevaltrate (10, 25, and 50 mg/kg) reduces tumor volume and increases intratumoral malondialdehyde (MDA) levels in an RKO mouse xenograft model.
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1. Acevaltrate as a novel ferroptosis inducer with dual targets of PCBP1/2 and GPX4 in colorectal cancer. Signal Transduct. Target Ther. 10(1), 211 (2025).
2. In vitro effect of valepotriates isolated from Valeriana glechomifolia on rat P-
3. Acevaltrate overcomes myeloma resistance to bortezomib via pyroptosis by promoting BAX translocalization to mitochondria. Eur. J. Pharmacol. 996, 177572 (2025).