PNC27抗癌肽作为靶向配体，显著提高了阿霉素在表达HDM2的细胞中的抗肿瘤疗效。
PNC27 anticancer peptide as targeting ligand significantly improved antitumor efficacy of Doxil in HDM2-expressing cells.
作者信息
Darban Shahrzad Amiri, Badiee Ali, Jaafari Mahmoud Reza
机构信息
Biotechnology Research Center, Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad 91775-1365, Iran.
Nanotechnology Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad 91775-1365, Iran.
出版信息
Nanomedicine (Lond). 2017 Jun;12(12):1475-1490. doi: 10.2217/nnm-2017-0069. Epub 2017 Jun 1.
AIM
To investigate the potential of PNC27 peptide, 12-26 of p53 with high affinity for HDM2 protein, as targeting ligand for Doxil to improve its antitumor activity.
MATERIALS & METHODS: Doxil postinserted with 25, 50, 100 and 200 PNC27 peptides per liposome. Flow cytometry and confocal analysis were performed on C26 colon carcinoma (HDM2 positive) and B16F0 melanoma (HDM2 negative) cells. In vivo studies were performed on BALB/c mice bearing C26 and C57BL/6 mice bearing B16F0 tumor models.
RESULTS
PNC27-Doxil showed significant cellular uptake and cytotoxicity in C26 cells compared with Doxil. PNC27-Doxil (100 PNC27 peptide) significantly improved therapeutic efficacy of Doxil without compromising its biodistribution in C26 tumor. However, these results were not observed in B16F0 cells.
CONCLUSION
PNC27 is a promising targeting ligand for Doxil against HDM2-positive cancers.
目的
研究对HDM2蛋白具有高亲和力的p53的12 - 26位PNC27肽作为阿霉素脂质体（Doxil）靶向配体以提高其抗肿瘤活性的潜力。
材料与方法
每个脂质体后插入25、50、100和200个PNC27肽的阿霉素脂质体。对C26结肠癌（HDM2阳性）和B16F0黑色素瘤（HDM2阴性）细胞进行流式细胞术和共聚焦分析。对携带C26肿瘤模型的BALB/c小鼠和携带B16F0肿瘤模型的C57BL/6小鼠进行体内研究。
结果
与阿霉素脂质体相比，PNC27 - 阿霉素脂质体在C26细胞中显示出显著的细胞摄取和细胞毒性。PNC27 - 阿霉素脂质体（100个PNC27肽）显著提高了阿霉素脂质体的治疗效果，且不影响其在C26肿瘤中的生物分布。然而，在B16F0细胞中未观察到这些结果。
结论
PNC27是一种有前景的针对HDM2阳性癌症的阿霉素脂质体靶向配体。
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