Tectochrysin, a natural product isolated and purified from the heartwood of Pinus strobus L., leads to apoptotic cell death in NSCLC cells through activation of DR3 and Fas expression via inhibition of STAT3 phosphorylation.
Tectochrysin is one of the major flavonoids of Alpinia oxyphylla Miquel. Tectochrysin (at 1, 5, 10 μg/mL) suppressed the growth of SW480 and HCT116 human colon cancer cells. Tectochrysin inhibits SW480 cells growth with IC50 value of 6.3 μg/mL and HCT116 cells growth with IC50 value of 8.4 μg/mL. Morphologic observation shows that the cells are reduced in size by the treatment of NSC 80687 (10 μg/mL) in SW480 cells and HCT116 cells. Tectochrysin treatment also inhibited activity of NF-κB. Techtochrysin binds directly to the p50 unit. Tectochrysin concentration-dependently inhibits the translocation of p50 and p65 into the nucleus through inhibition of the phosphorylation of IκB. In vivo, tumor weights and volumes in mice were reduced when treated with tectochrysin (5 mg/kg). Tectochrysin leads to apoptotic cell death in colon cancer cells through activation of death receptors expression via the inhibition of NF-κB[3]. 1 mM tectochrysin was sufficient to fully sensitize mutant ABCG2-transfected cells, whereas higher concentrations were required for the wild-type ones[4]. Tectochrysin could inhibit the differentiation of BMMCs into osteoclasts induced by receptor activator of nuclear factor-κΒ ligand (RANKL) and macrophage colony-stimulating factor (M-CSF) in a concentration-dependent manner in vitro[5].
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