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

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...

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Published inJournal of natural products (Washington, D.C.) Vol. 80; no. 7; pp. 2146 - 2150
Main Authors Liu, Rongxia, Heiss, Elke H, Schachner, Daniel, Jiang, Baohong, Liu, Wanhui, Breuss, Johannes M, Dirsch, Verena M, Atanasov, Atanas G
Format Journal Article
LanguageEnglish
Published United States American Chemical Society and American Society of Pharmacognosy 28.07.2017
Subjects
Animals
Becaplermin
Cell Movement
Cell Proliferation
chalcone
Disease Models, Animal
Dose-Response Relationship, Drug
Flavonoids - chemistry
Flavonoids - isolation & purification
Flavonoids - pharmacology
hops
Humulus - chemistry
inhibitory concentration 50
MAP Kinase Signaling System
Mice
Molecular Structure
Muscle, Smooth, Vascular - metabolism
myocytes
Myocytes, Smooth Muscle - metabolism
Neointima - chemically induced
Neointima - metabolism
Oxazines - metabolism
Phosphorylation
platelet-derived growth factor
Platelet-Derived Growth Factor - drug effects
Propiophenones - chemistry
Propiophenones - isolation & purification
Propiophenones - pharmacology
Proto-Oncogene Proteins c-sis
Rats
Rats, Sprague-Dawley
Signal Transduction
smooth muscle
Wound Healing - drug effects
Xanthenes - metabolism
Online AccessGet full text
ISSN0163-3864
1520-6025
1520-6025
DOI10.1021/acs.jnatprod.7b00268

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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.
AbstractList 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.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.
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.
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.
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 (IC = 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.
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 (IC 50 = 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.
Author Liu, Wanhui
Atanasov, Atanas G
Jiang, Baohong
Liu, Rongxia
Schachner, Daniel
Dirsch, Verena M
Breuss, Johannes M
Heiss, Elke H
AuthorAffiliation State Key Laboratory of Drug Research
Department of Pharmacognosy
Yantai University
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
University of Vienna
Center for Physiology and Pharmacology, Institute for Vascular Biology and Thrombosis Research
Institute of Genetics and Animal Breeding of the Polish Academy of Sciences
Medical University of Vienna
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Snippet 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...
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...
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SubjectTerms Animals
Becaplermin
Cell Movement
Cell Proliferation
chalcone
Disease Models, Animal
Dose-Response Relationship, Drug
Flavonoids - chemistry
Flavonoids - isolation & purification
Flavonoids - pharmacology
hops
Humulus - chemistry
inhibitory concentration 50
MAP Kinase Signaling System
Mice
Molecular Structure
Muscle, Smooth, Vascular - metabolism
myocytes
Myocytes, Smooth Muscle - metabolism
Neointima - chemically induced
Neointima - metabolism
Oxazines - metabolism
Phosphorylation
platelet-derived growth factor
Platelet-Derived Growth Factor - drug effects
Propiophenones - chemistry
Propiophenones - isolation & purification
Propiophenones - pharmacology
Proto-Oncogene Proteins c-sis
Rats
Rats, Sprague-Dawley
Signal Transduction
smooth muscle
Wound Healing - drug effects
Xanthenes - metabolism
Title Xanthohumol Blocks Proliferation and Migration of Vascular Smooth Muscle Cells in Vitro and Reduces Neointima Formation in Vivo
URI http://dx.doi.org/10.1021/acs.jnatprod.7b00268
https://www.ncbi.nlm.nih.gov/pubmed/28627872
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