dihydrocelastrol

Dihydrocelastrol is a **synthetic derivative** of celastrol, produced through **hydrogenation** of celastrol, which is a triterpene isolated from the traditional Chinese medicinal plant *Tripterygium wilfordii* (Thunder of God Vine) and *Tripterygium regelii*. The compound has demonstrated **potent antitumor activity** across multiple hematological malignancies, including multiple myeloma, mantle cell lymphoma, and diffuse large B-cell lymphoma. Dihydrocelastrol exhibits **lower toxicity** compared to its parent compound celastrol, with reduced hepatic, renal, and reproductive toxicity. The compound works through multiple mechanisms: it **inhibits cell proliferation** by inducing G0/G1 phase cell cycle arrest through downregulation of cyclin D1 and cyclin-dependent kinases 4 and 6; it **promotes apoptosis** through both caspase-dependent extrinsic and intrinsic pathways; it **suppresses key signaling pathways** including IL-6/STAT3, ERK1/2, JAK2/STAT3, PI3K/Akt, and mTORC1/mTORC2; and it **inhibits angiogenesis** and nuclear translocation of transcription factors Jun B and p65. Notably, dihydrocelastrol has shown efficacy in **overcoming bortezomib resistance** in multiple myeloma by inhibiting STAT3-dependent PSMB5 regulation and demonstrates **synergistic effects** when combined with chemotherapeutic agents such as bortezomib, doxorubicin, and panobinostat (LBH589).

Other names

Triptohypol C