2. Academic Validation
  3. Xanthohumol Blocks Proliferation and Migration of Vascular Smooth Muscle Cells in Vitro and Reduces Neointima Formation in Vivo

Xanthohumol Blocks Proliferation and Migration of Vascular Smooth Muscle Cells in Vitro and Reduces Neointima Formation in Vivo

  • J Nat Prod. 2017 Jul 28;80(7):2146-2150. doi: 10.1021/acs.jnatprod.7b00268.
Rongxia Liu 1,  Elke H Heiss 2,  Daniel Schachner 2,  Baohong Jiang 3,  Wanhui Liu 1,  Johannes M Breuss 4,  Verena M Dirsch 2,  Atanas G Atanasov 2 5
Affiliations

Affiliations

  • 1 School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University , Yantai, 264005, People's Republic of China.
  • 2 Department of Pharmacognosy, University of Vienna , Vienna, 1090, Austria.
  • 3 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai, 201203, People's Republic of China.
  • 4 Center for Physiology and Pharmacology, Institute for Vascular Biology and Thrombosis Research, Medical University of Vienna , Vienna, 1090, Austria.
  • 5 Institute of Genetics and Animal Breeding of the Polish Academy of Sciences , 05-552 Jastrzebiec, Poland.
PMID: 28627872 DOI: 10.1021/acs.jnatprod.7b00268
Abstract

Xanthohumol (1) is a principal prenylated chalcone found in hops. The aim of this study was to examine its influence on platelet-derived growth factor (PDGF)-BB-triggered vascular smooth muscle cell (VSMC) proliferation and migration in vitro and on experimentally induced neointima formation in vivo. Quantification of resazurin conversion indicated that 1 can inhibit PDGF-BB-induced VSMC proliferation concentration-dependently (IC50 = 3.49 μM). Furthermore, in a wound-healing assay 1 potently suppresses PDGF-BB-induced VSMC migration at 15 μM. Tested in a mouse femoral artery cuff model, 1 significantly reduces neointima formation. Taken together, we show that 1 represses PDGF-BB-induced VSMC proliferation and migration in vitro as well as neointima formation in vivo. This novel activity suggests 1 as an interesting candidate for further studies addressing a possible therapeutic application to counteract vascular proliferative disease.

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