RGDS peptide contains the Arg-Gly-Asp (RGD) motif that mediates the interaction between extracellular matrix proteins and cell integrins and is widely used to probe integrin function[1]. RGDS peptide demonstrates significant antibacterial potential as an antibiotic adjuvant[2]. RGDS peptide covalently functionalized ND (NDCO-RGDS) can also be a tumor-targeting carrier of VEGF-siRNA[3].
In vitro, treatment of osteoblast-like cells with 0.2mM RGDS peptide for three days completely blocked apoptosis induced by staurosporine, the Ca2+·Pi ion pair, and sodium nitroprusside[4]. Following 500μg/mL RGDS peptide treatment for 2, 6, 16, and 24h, SK-MEL-110 cells internalized RGDS peptide in a time-dependent manner and exhibited marked anti-proliferative and pro-apoptotic effects independent of any extracellular anti-adhesive action[5].
In vivo, a single intraperitoneal injection of RGDS peptide 1h before lipopolysaccharide (LPS) challenge (1, 2.5, or 5mg/kg) dose-dependently suppressed the LPS-induced increases in neutrophil and macrophage counts, total protein content, TNF-α and macrophage inflammatory protein (MIP)-2 levels, and matrix metalloproteinase-9 activity in bronchoalveolar lavage fluid[6]. In Balb/c mice, a single intraperitoneal injection of RGDS peptide (5mg/kg) 30min before LPS (50μg/kg) and D-GalN (800mg/kg) markedly reduced hepatic injury and mortality[7].
References:
[1] Ortega-Velázquez R, Díez-Marqués ML, Ruiz-Torres MP, et al. Arg-Gly-Asp-Ser (RGDS) peptide stimulates transforming growth factor beta1 transcription and secretion through integrin activation. FASEB J. 2003;17(11):1529-1531.
[2] Feng Y, Xie W, Wan Z, et al. Harnessing RGDS peptides to regulate bacterial-host interfaces for targeted antimicrobial therapy. J Control Release. 2025;384:113922.
[3] Cui C , Wang Y , Zhao W , et al. RGDS covalently surfaced nanodiamond as a tumor targeting carrier of VEGF-siRNA: synthesis, characterization and bioassay. J Mater Chem B. 2015;3(48):9260-9268.
[4] Grigoriou V, Shapiro IM, Cavalcanti-Adam EA, et al. Apoptosis and survival of osteoblast-like cells are regulated by surface attachment. J Biol Chem. 2005;280(3):1733-1739.
[5] Aguzzi MS, Fortugno P, Giampietri C, et al. Intracellular targets of RGDS peptide in melanoma cells. Mol Cancer. 2010;9:84.
[6] Moon C, Han JR, Park HJ, et al. Synthetic RGDS peptide attenuates lipopolysaccharide-induced pulmonary inflammation by inhibiting integrin signaled MAP kinase pathways. Respir Res. 2009;10(1):18.
[7] Yin X, Gong X, Jiang R, et al. Synthetic RGDS peptide attenuated lipopolysaccharide/D-galactosamine-induced fulminant hepatic failure in mice. J Gastroenterol Hepatol. 2014;29(6):1308-1315.
















