Anti‐angiogenic effect of quercetin and its 8‐methyl pentamethyl ether derivative in human microvascular endothelial cells

Autor: Carmelina Daniela Anfuso, Mario Salmeri, Gabriella Lupo, Nunzia Caporarello, Maria Teresa Cambria, Anna Longo, Concetta Rocco, Mario C. Foti, Melania Olivieri, Guido Zanghì
Rok vydání: 2019
Předmět:
Male
Vascular Endothelial Growth Factor A
0301 basic medicine
8‐methylquercetin pentamethyl ether
Proto-Oncogene Proteins c-jun
Angiogenesis
Angiogenesis Inhibitors
quercetin dimer
Receptor tyrosine kinase
quercetin
angiogenesis
chemistry.chemical_compound
tumour angiogenesis
0302 clinical medicine
quercetin 8-methyl
Cell Movement
Blood-Retinal Barrier
Extracellular Signal-Regulated MAP Kinases
human retinal endothelial cells
Neovascularization
Pathologic

biology
Chemistry
Kinase
Vascular endothelial growth factor
medicine.anatomical_structure
030220 oncology & carcinogenesis
Molecular Medicine
Original Article
Rabbits
8-methylquercetin pentamethyl ether
Signal Transduction
Methyl Ethers
Cell Survival
Blood–retinal barrier
VEGFR‐2
Retina
Cell Line
03 medical and health sciences
medicine
Animals
Humans
Viability assay
Protein kinase B
6
8-dibromoquercetin

VEGFR-2
Cell Proliferation
Vascular Endothelial Growth Factor Receptor-1
6
8‐dibromoquercetin

Endothelial Cells
Original Articles
Cell Biology
Vascular Endothelial Growth Factor Receptor-3
Vascular Endothelial Growth Factor Receptor-2
peroxidation
030104 developmental biology
biology.protein
Cancer research
Endothelium
Vascular

Proto-Oncogene Proteins c-akt
Ex vivo
8-dibromoquercetin
Zdroj: Journal of Cellular and Molecular Medicine
23 (2019): 6565–6577. doi:10.1111/jcmm.14455
info:cnr-pdr/source/autori:Lupo G.; Cambria M.T.; Olivieri M.; Rocco C.; Caporarello N.; Longo A.; Zanghi G.; Salmeri M.; Foti M.C.; Anfuso C.D./titolo:Anti-angiogenic effect of quercetin and its 8-methyl pentamethyl ether derivative in human microvascular endothelial cells/doi:10.1111%2Fjcmm.14455/rivista:Journal of Cellular and Molecular Medicine (Print)/anno:2019/pagina_da:6565/pagina_a:6577/intervallo_pagine:6565–6577/volume:23
ISSN: 1582-4934
1582-1838
DOI: 10.1111/jcmm.14455
Popis: Angiogenesis is involved in many pathological states such as progression of tumours, retinopathy of prematurity and diabetic retinopathy. The latter is a more complex diabetic complication in which neurodegeneration plays a significant role and a leading cause of blindness. The vascular endothelial growth factor (VEGF) is a powerful pro‐angiogenic factor that acts through three tyrosine kinase receptors (VEGFR‐1, VEGFR‐2 and VEGFR‐3). In this work we studied the anti‐angiogenic effect of quercetin (Q) and some of its derivates in human microvascular endothelial cells, as a blood retinal barrier model, after stimulation with VEGF‐A. We found that a permethylated form of Q, namely 8MQPM, more than the simple Q, is a potent inhibitor of angiogenesis both in vitro and ex vivo. Our results showed that these compounds inhibited cell viability and migration and disrupted the formation of microvessels in rabbit aortic ring. The addition of Q and more significantly 8MQPM caused recoveries or completely re‐establish the transendothelial electrical resistance (TEER) to the control values and suppressed the activation of VEGFR2 downstream signalling molecules such as AKT, extracellular signal‐regulated kinase, and c‐Jun N‐terminal kinase. Taken together, these data suggest that 8MQPM might have an important role in the contrast of angiogenesis‐related diseases.
Databáze: OpenAIRE