促进细胞穿透肽及其介导的生物分子从内含体逃逸的几种策略  

Strategies for enhancement of endosome escape during cytosolic delivery of cell penetrating peptides and bioactive cargoes

作　　者：王琥[1] 柳长柏[1] 

机构地区：[1]三峡大学分子生物学研究所,湖北宜昌443002

出　　处：《中国新药与临床杂志》2009年第1期57-61,共5页Chinese Journal of New Drugs and Clinical Remedies

基　　金：国家自然科学基金项目(20774094/B040203)

摘　　要：细胞穿透肽(CPPs)是一类可穿透细胞膜、向细胞内输送各种大分子生物活性物质的短肽。几乎所有CPPs及其介导的生物活性分子都是以内吞形式进入细胞,之后局限于内含体内,以至于最终被溶酶体消化降解,从而影响了CPPs的运输效率,故寻找辅助CPPs及其介导的生物活性分子从内含体中逃逸进入胞浆的方法尤为重要。目前的体外研究多用氯喹或Ca2+处理以提高CPPs的运输效率。最近有学者报道使用天然多肽或微生物的某些"元件"(如,流感病毒的HA2肽)来协助CPPs从内含体逃逸,将有助于CPPs作为高效运载工具向细胞内输送生物活性分子。Cell penetrating peptides （CPPs） , as a powerful vehicle, are able to deliver a variety of bioactive macromolecular substance into the cells by penetrating through the cell membrane. However, cellular uptake of most CPPs and the cargo occur mainly through endophagocytic pathways, and are retained in the endosome compartment of the cell, and the conjugates will be degradated in lysosome finally, thus influencing the delivery efficacy of CPPs. Several strategies （e.g. chloroquine or Ca^2＋ treatment） that can induce endosomal disruption have been shown to improve the bioavailability of CPPs and cargoes for facilitating the release from endosomal compartment to cytosol. Evidences have shown recently that some natural peptides from microorganism, such as HA2 peptide of influenza virus, are able to assist CPPs and cargoes to release from endosome into the cytosol, in vitro. This review lays focus on the main progress in this field.

关 键 词：肽类 胞吞作用 溶酶体 细胞穿透朕 内含体逃逸 药物输送 

分 类 号：R966[医药卫生—药理学]