Vascular endothelial growth factor receptor-2 (VEGFR2) plays a pivotal role in promoting angiogenesis and contributing to the growth and progression of renal cancer. Hence, the current investigation was undertaken with the aim of identifying safe and potent phytochemicals from whole plant extract (AiWE) that can efficiently suppress the overexpression of VEGFR2. HPLC analysis identified and quantified 11 polyphenols in considerable amounts in AiWE. All the compounds showed good binding energies with VEGFR2 in the molecular docking study, except catechin hydrate and rutin hydrate. However, among the polyphenols, myricetin exhibited an almost similar hydrogen bonding pattern with the active site of VEGFR2. The all-atom molecular dynamic simulation revealed that myricetin showed a very stable interaction with the active site of VEGFR2 throughout the simulation. Based on these results, it is suggested that myricetin may inhibit angiogenesis by suppressing the VEGFR2 signaling, thereby impeding the growth and progression of renal cancer.
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http://dx.doi.org/10.1016/j.heliyon.2025.e41749 | DOI Listing |
Molecules
February 2025
BB21 Plus Program, Department of Chemistry, Pukyong National University, Busan 48513, Republic of Korea.
Angiogenesis, primarily driven by the vascular endothelial growth factor (VEGF) and its receptor, the VEGFR, plays a key role in various pathological processes such as cancer progression. Here, we investigated the anti-angiogenic effects of Lucknolide A (LA), a marine -derived compound, and evaluated its potential as a VEGFR2 inhibitor. LA selectively inhibited the proliferation of human endothelial cells EA.
View Article and Find Full Text PDFACS Nano
March 2025
Department of Ophthalmology, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, No. 100 Haining Road, Shanghai 200080, China.
Small interfering RNA (siRNA) has garnered tremendous interest as a potential therapeutic tool because of its intriguing gene-silencing ability. Toward the success in the manufacture of siRNA therapeutics for the potential treatment of choroidal neovascularization (CNV), siRNA conjugated with dual functional units of membrane-penetrating heptafluoropropyl and age-related macular degeneration-targeting cyclic Arg-Gly-Asp (RGD) peptide was attempted for transcellular transportation into the cell interiors. Of note, cyclic RGD allowed selective affinities toward the angiogenic endothelial cells in the pathological CNV.
View Article and Find Full Text PDFPurpose Receptor tyrosine kinase (RTK) concentrations on the plasma membrane correlate with angiogenic functions in vitro and in rodent models. The intracellular RTK pool also regulates plasma membrane receptor availability and signaling pathways. Organs have specialized angiogenic functions essential to their distinct roles, supporting the hypothesis that plasma membrane and intracellular RTK concentrations vary across endothelial cells (ECs) from different organs.
View Article and Find Full Text PDFFront Cardiovasc Med
February 2025
School of Pharmacy, Jining Medical University, Rizhao, China.
Background: Myocardial fibrosis (MF) is a prevalent pathological condition associated with various heart diseases, such as heart failure and arrhythmias, which disrupt electrical signals and reduce pumping efficiency. This research explored the therapeutic effects and potential mechanisms of L. fruit polysaccharide (LVFP) on MF.
View Article and Find Full Text PDFJ Microbiol
February 2025
Department of Parasitology, College of Medicine, The Catholic University of Korea, Seoul 06591, Republic of Korea.
Chronic toxoplasmosis is caused by Toxoplasma gondii bradyzoites. This study assessed six candidate small molecule kinase inhibitors (SMKIs) against bradyzoites (ME49 strain), the reactivated form of the parasite resulting from the rupture of brain cysts. Bradyzoites were obtained from mouse brain cysts, cultured in ARPE-19 cells, and treated with afatinib and neratinib (HER2/HER4 inhibitors), ACTB-1003 and regorafenib (VEGFR-2 inhibitors), or altiratinib and foretinib (c-MET inhibitors).
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