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.
RGDS peptide含有可介导细胞外基质蛋白与细胞整合素相互作用的Arg-Gly-Asp（RGD）序列，被广泛用于研究整合素功能[1]。RGDS peptide作为抗生素佐剂亦表现出显著的抗菌潜力[2]。共价修饰的RGDS peptide功能化纳米金刚石（NDCO-RGDS）还可作为VEGF-siRNA的肿瘤靶向递送载体[3]。
在体外，0.2mM的RGDS peptide处理类成骨细胞3天，可完全阻断由星形孢菌素、Ca2+·Pi离子对和硝普钠诱导的细胞凋亡[4]。以500μg/mL的RGDS peptide处理SK-MEL-110细胞2、6、16和24小时后，RGDS peptide被细胞以时间依赖性方式摄取，并表现出显著的抗增殖和促凋亡效应，且该效应独立于其胞外抗黏附作用[5]。
在体内，于脂多糖（LPS）刺激前1小时单次腹腔注射1、2.5或5mg/kg的RGDS peptide，可剂量依赖性地抑制LPS诱导的支气管肺泡灌洗液中中性粒细胞和巨噬细胞数量、总蛋白含量、TNF-α和巨噬细胞炎症蛋白（MIP）-2水平以及基质金属蛋白酶-9活性的升高[6]。在Balb/c小鼠中，于LPS（50μg/kg）和D-GalN（800mg/kg）刺激前30分钟单次腹腔注射5mg/kg的RGDS peptide，可显著减轻肝损伤并降低死亡率[7]。