Akrami Mohammad, Balalaie Saeed, Hosseinkhani Saman, Alipour Mohsen, Salehi Fahimeh, Bahador Abbas, Haririan Ismaeil
Department of Pharmaceutical Biomaterials and Medical Biomaterials Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
Peptide Chemistry Research Center, K. N. Toosi University of Technology, Tehran, Iran.
Sci Rep. 2016 Aug 4;6:31030. doi: 10.1038/srep31030.
Pro-apoptotic peptides induce intrinsic apoptosis pathway in cancer cells. However, poor cellular penetration of the peptides is often associated with limited therapeutic efficacy. In this report, a series of peptide-gold nanoparticle platforms were developed to evaluate the anticancer activity of a novel alpha-lipoic acid-peptide conjugate, LA-WKRAKLAK, with respect to size and shape of nanoparticles. Gold nanoparticles (AuNPs) were found to enhance cell internalization as well as anticancer activity of the peptide conjugates. The smaller nanospheres showed a higher cytotoxicity, morphological change and cellular uptake compared to larger nanospheres and nanorods, whereas nanorods showed more hemolytic activity compared to nanospheres. The findings suggested that the anticancer and biological effects of the peptides induced by intrinsic apoptotic pathway were tuned by peptide-functionalized gold nanoparticles (P-AuNPs) as a function of their size and shape.
促凋亡肽可诱导癌细胞的内源性凋亡途径。然而，肽的细胞穿透性较差往往与治疗效果有限相关。在本报告中，开发了一系列肽-金纳米颗粒平台，以评估一种新型α-硫辛酸-肽缀合物LA-WKRAKLAK在纳米颗粒大小和形状方面的抗癌活性。发现金纳米颗粒（AuNPs）可增强肽缀合物的细胞内化以及抗癌活性。与较大的纳米球和纳米棒相比，较小的纳米球显示出更高的细胞毒性、形态变化和细胞摄取，而纳米棒与纳米球相比显示出更多的溶血活性。研究结果表明，内源性凋亡途径诱导的肽的抗癌和生物学效应可通过肽功能化金纳米颗粒（P-AuNPs）根据其大小和形状进行调节。
