2. Academic Validation
  3. Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2

Scutellarin inhibits Hela cell growth and glycolysis by inhibiting the activity of pyruvate kinase M2

  • Bioorg Med Chem Lett. 2017 Dec 15;27(24):5404-5408. doi: 10.1016/j.bmcl.2017.11.011.
Lin You 1,  Hong Zhu 1,  Chun Wang 1,  Fang Wang 1,  Yongjun Li 1,  Yan Li 2,  Yonglin Wang 1,  Bin He 3
Affiliations

Affiliations

  • 1 Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Provincial Key Laboratory of Pharmaceutics, School of Pharmacy, National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang, Guizhou 550004, China.
  • 2 School of Basic Medicine, Guizhou Medical University, Guiyang, Guizhou 550004, China.
  • 3 Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Provincial Key Laboratory of Pharmaceutics, School of Pharmacy, National Engineering Research Center of Miao's Medicines, Guizhou Medical University, Guiyang, Guizhou 550004, China. Electronic address: binhe@gmc.edu.cn.
PMID: 29157862 DOI: 10.1016/j.bmcl.2017.11.011
Abstract

Scutellarin, one of natural Flavonoids, is widely and clinically used for treating many diseases in China. Recently, scutellarin has demonstrated a broad spectrum of anti-proliferative activities against multiple Cancer cell lines. However, the molecular mechanism of action remains to be investigated. We herein report the design and synthesis of biotinylated scutellareins as probes, which can be applied to discover scutellarein interacting proteins. Finally, we show that scutellarin directly targets Pyruvate Kinase M2 (PKM2) and inhibits its cytosolic activity to decrease glycolytic metabolism; on the Other hand, scutellarin may also participate in regulating cell cycle and apoptotic proteins by activating MEK/ERK/PIN1 signaling pathway to promote the nuclear translocation of PKM2.

Keywords

Antitumor activity; Inhibitor; PKM2; Scutellarein; Scutellarin.

Figures
Products