Cephalomannine, a natural product isolated and purified from the barks of Cephalotaxus sinensis (Rehd. et Wils.) Li, is a taxol derivative with antitumor, antiproliferative properties.
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Cephalomannine is an alkaloidal analog of Paclitaxel, derived from various Cephalotaxus species. It functions as an orally active anti-tumor agent and is employed in chemotherapy for cancer research[1][2][3].
体内研究
In vivo, Cephalomannine administered at a dose of 0.4 mg/kg through intraperitoneal injection over a span of 10 days significantly curtails the growth of lung cancer cells in a nude mouse xenograft model, all while exhibiting no apparent side effects[3].
The mechanism by which Cephalomannine operates includes disrupting the interaction between APEX1 and HIF-1α through competitive binding with APEX1, highlighting its potential therapeutic action in tumor environments, particularly under hypoxic conditions[3].
体外研究
In cellular studies, Cephalomannine has shown significant anti-proliferative effects on lung cancer cell lines such as H460, A549, and H1299 under normal oxygen conditions, with IC50 values of 0.18, 0.20, and 0.37 μM respectively. Furthermore, Cephalomannine effectively reduces cell viability under hypoxic conditions as well[3].
Cephalomannine impacts the viability, reactive oxygen species (ROS) production, intracellular pH, migration of hypoxic lung cancer cells, and angiogenesis in hypoxic human umbilical vein endothelial cells (HUVECs). This is achieved through its inhibition of the interaction between APEX1 and HIF-1α in H460 and A549 cell lines over time periods of 0, 12, and 24 hours[3].
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