Description: 1-O-Acetylbritannilactone is an active compound isolated from Inula Britannica L. 1-O-Acetylbritannilactone inhibits VEGF-mediated activation of Src and FAK. 1-O-Acetylbritannilactone inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
IC50 & Target: Src, FAK
PGE2, COX-2, NF-κB
In Vitro: 1-O-Acetylbritannilactone (ABL) inhibits angiogenesis and lung cancer cell growth through regulating VEGF-Src-FAK signaling. 1-O-Acetylbritannilactone dose-dependently inhibits vascular endothelial growth factor (VEGF)-induced proliferation, migration, and capillary structure formation of cultured human umbilical vascular endothelial cells (HUVECs). Treatment of A549 NSCLC cells with 1-O-Acetylbritannilactone results in cell growth inhibition and Src-FAK in-activation. The potential effect of 1-O-Acetylbritannilactone is tested ton Src and FAK phosphorylation in A549 lung cancer cells. Significant high levels of Src and FAK phosphorylations are noticed a in A549 cells, which are both inhibited by treatment of 1-O-Acetylbritannilactone (5 μM and 10 μM). Src and FAK are both important for cancer cell proliferation. Thus, A549 cell growth, tested by MTT assay and clonogenicity assay,is remarkably inhibited by corresponding 1-O-Acetylbritannilactone treatment. The anti-A549 cell growth activity of 1-O-Acetylbritannilactone is again dose-dependent.1-O-acetylbritannilactone (ABL) isolated from Inula britannica-F., inhibits inflammatory responses in vascular smooth muscle cells (VSMCs). 1-O-Acetylbritannilactone (5, 10, 20 μM) has several concentration dependent effects, including inhibition of lipopolysaccharide (LPS)-induced PGE2 production and COX-2 expression, and blockade of NF-κB activation and translocation. In addition, 1-O-Acetylbritannilactone directly inhibits the binding of active NF-κB to specific DNA cis-element.
In Vivo: Administration of a single dose of 1-O-Acetylbritannilactone (12 mg/kg/day) remarkably suppresses growth of A549 xenografts in nude mice. In vivo microvessels formation and Src activation are also significantly inhibited in 1-O-Acetylbritannilactone -treated xenograft tumors. To investigate the potential activity of 1-O-Acetylbritannilactone in vivo, a nude mice xenograft model is applied. A single dose of 1-O-Acetylbritannilactone (12 mg/kg/day, i.p.) dramatically inhibits the growth of A549 xenografts in nude mice. Further, the weights of 1-O-Acetylbritannilactone-treated tumors are remarkably lighter than that of vehicle-treated tumors. Notably, 1-O-Acetylbritannilactone administration does not affect mice body weights.
|Contents||1 vial supplied at requested quantity.|
|Research Area||Cancer, Inflammation/Immunology|