Competitive ELISA-based screening of plant derivatives for the inhibition of VEGF family members interaction with vascular endothelial growth factor receptor 1.
The activation of vascular endothelial growth factor receptor-1 (VEGFR-1, also known as Flt-1) is crucial in many physiological and pathological conditions, like angiogenesis, cancer, inflammation, hematopoiesis, bone marrow precursors/stem cells recruitment in tumor angiogenesis, and metastasis formation. Many recent reports indicate that molecules able to antagonize Flt-1 activity have gained a strong interest in the view of therapeutic approaches. In order to identify new compounds able to interfere in the Flt-1 recognition by VEGFs family members, we have developed a highly sensitive competitive ELISA-based screening to study plant extracts and derivatives. Several fractions of the N-butanol extract of Pteleopsis suberosa leaves and of the chloroform extract of Parinari campestris leaves demonstrated by a bioassay-guided fractionation an evident inhibition of VEGF-A or placental growth factor (PlGF) interaction with Flt-1, with an inhibition over 50 % in particular for the VEGF-A/Flt-1 interaction at a concentration of 100 microg/mL. This activity seems be due to the presence of a combination of compounds acting synergistically.
Ponticelli
Salvatore
S
Angiogenesis Lab and Stem Cell Fate Lab, Istituto di Genetica e Biofisica 'Adriano Buzzati-Traverso', CNR, Napoli, Italy.
Braca
Alessandra
A
De Tommasi
Nunziatina
N
De Falco
Sandro
S
D004797:Enzyme-Linked Immunosorbent Assay; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry* / Q000494:pharmacology; D010944:Plants / Q000737:chemistry*; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors*; D040281:Vascular Endothelial Growth Factor Receptor-1 / Q000037:antagonists & inhibitors*
D010936:Plant Extracts; D042461:Vascular Endothelial Growth Factor A; D040281:Vascular Endothelial Growth Factor Receptor-1