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 |
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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 |
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