Highly efficient, nonpeptidic oligoguanidinium vectors that selectively internalize into mitochondria
Highly efficient, nonpeptidic oligoguanidinium vectors that selectively internalize into mitochondria
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DOI：
10.1021/ja044006q
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发表时间：
2005-01-26
影响因子：
15
通讯作者：
Giralt, E
中科院分区：
文献类型：
--
作者：
Fernandex-Carneado, J;Van Gool, M;Giralt, E
基于寡胍的细胞递送系统自十年前以来在药物递送领域获得了广泛的兴趣。因此，含精氨酸的肽如达特或Antp、寡精氨酸肽和衍生的类肽已被描述为用于在癌细胞内递送非渗透性药物的穿梭体。在这里，我们报告了一个新的家庭四胍细胞穿透载体有效地内化在人类肿瘤细胞。通过共聚焦显微镜和流式细胞术研究它们的高度内化，以及它们在线粒体中的特异性积累，使得这些新载体可能成为将抗癌药物靶向递送至线粒体的载体。
Oligoguandinium-based cell delivery systems have gained broad interest in the drug delivery field since one decade ago. Thus, arginine-containing peptides as Tat or Antp, oligoarginine peptides, and derived peptoids have been described as shuttles for delivering nonpermeant drugs inside cancer cells. Herein we report a new family of tetraguanidinium cell penetrating vectors efficiently internalized in human tumor cells. Their high internalization, studied by confocal microscopy and flow cytometry, as well as their specific accumulation in mitochondria makes these new vectors likely vehicles for the targeted delivery of anticancer drugs to mitochondria.