Carbosilane ruthenium metallodendrimer作为三阴性乳腺癌小鼠模型中替代性的抗癌药物载体：初步研究。
Carbosilane ruthenium metallodendrimer as alternative anti-cancer drug carrier in triple negative breast cancer mouse model: a preliminary study.
发表日期：2023 Feb 27
作者：
Sylwia Michlewska, Marek Maly, Dagmara Wójkowska, Kamil Karolczak, Elżbieta Skiba, Marcin Hołota, Małgorzata Kubczak, Paula Ortega, Cezary Watala, F Javier de la Mata, Maria Bryszewska, Maksim Ionov
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICS
摘要：
基于芳烃配合物Ru(II)与亚胺-吡啶表面基团配位的碳硅烷金属树状高分子G1-[[NCPh(o-N)Ru(η6- p-cymene)Cl]Cl]4（CRD13）已与抗癌药物偶联。正电荷树状高分子结构中的钌使得这种纳米粒子可以被认为是一种抗癌药物载体，因为钌有抗癌特性，使其效率更高。使用zeta电位测量、透射电子显微镜（TEM）和计算机模拟评估了CRD13与多柔比星（DOX）、5-氟尿嘧啶（5-Fu）和甲氨蝶呤（MTX）形成复合物的能力。结果表明，它与所有这些药物形成稳定的纳米复合物，增强了它们对MDA-MB-231癌细胞的作用。体内实验表明，CRD13/DOX系统导致三阴性乳腺癌小鼠肿瘤重量下降。然而，注射裸露的树状高分子时，肿瘤缩小最为明显。版权所有©2023 Elsevier B.V.。
The carbosilane metallodendrimer G1-[[NCPh(o-N)Ru(η6- p-cymene)Cl]Cl]4 (CRD13), based on an arene Ru(II) complex coordinated to imino-pyridine surface groups, has been conjugated with anti-cancer drugs. Ruthenium in the positively-charged dendrimer structure allows this nanoparticle to be considered as an anticancer drug carrier, made more efficient because ruthenium has anticancer properties. The ability of CRD13 to form complexes with Doxorubicin (DOX), 5-Fluorouracil (5-Fu), and Methotrexate (MTX) has been evaluated using zeta potential measurement, transmission electron microscopy (TEM) and computer simulation. The results show that it forms stable nanocomplexes with all those drugs, enhancing their effectiveness against MDA-MB-231 cancer cells. In vivo tests indicate that the CRD13/DOX system caused a decrease of tumor weight in mice with triple negative breast cancer. However, the tumors were most visibly reduced when naked dendrimers were injected.Copyright © 2023 Elsevier B.V. All rights reserved.