Planta Med 2015; 81 - PW3
DOI: 10.1055/s-0035-1556431

Flavonoids modulating c-Met and ALK activity

SY Han 1, YO Choi 2, HH Song 2, YM Kim 2, YW Chin 2
  • 1College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, Gyeongnam 660 – 701, Republic of Korea
  • 2BK21PLUS R-FIND team and College of Pharmacy, Dongguk University-Seoul, Goyang, Gyeonggi-do 410 – 820, Republic of Korea

Bioactivity-guided separation of the roots of Scutellaria baicalensis, using c-Met kinase assay, led to the isolation of 19 flavonoids. Of these isolates, norwogonin and baicalin were found to be active in the c-Met assay. Further investigation for c-Met inhibitory compounds in the ALK assay revealed that norwogonin and baicalin were active. Norwogonin and baicalin were found to inhibit both c-Met (IC50 6.24 and 13.4µM, respectively) and ALK kinases (IC50 7.62 and 0.93µM, respectively). Furthermore, the binding mode of norwogonin in the ATP binding site of c-Met was disclosed in docking study.