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Acevaltrate is a natural iridoid valepotriate isolated from plants of the *Valeriana* genus, including *Valeriana jatamansi* and *Valeriana glechomifolia*. It is being investigated as a multi-target antineoplastic agent with the ability to induce various forms of regulated cell death. Preclinical studies have demonstrated that acevaltrate induces ferroptosis in colorectal cancer cells by targeting the iron chaperones PCBP1/2 and the antioxidant enzyme GPX4. It also triggers pyroptosis in bortezomib-resistant multiple myeloma cells through a Caspase-3 and GSDME-dependent mechanism. Furthermore, acevaltrate has been shown to inhibit the accumulation of hypoxia-inducible factor-1α (HIF-1α) by suppressing its synthesis and promoting its degradation via the mTOR/p70S6K/4E-BP1 pathway. Additional research indicates its potential in glioblastoma by suppressing the USP10/CCND1 axis and in myeloma by inhibiting the Otub1/c-Maf axis. Preclinical models suggest it may overcome therapeutic resistance and exhibits a favorable safety profile compared to some first-line clinical drugs.
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