DSPE-PEG-cRGD 修飾脂質(zhì)體在靶向遞送OC-2 shRNA中的應(yīng)用研究

鏈接：https://www.mdpi.com/1999-4923/14/10/2157

作者：劉春燕，趙文麗，張立剛，孫華敏，陳曦和鄧寧

摘要：

陽離子脂質(zhì)體遞送干擾RNA（shRNA）在**中發(fā)揮著重要作用。設(shè)計(jì)了環(huán)狀精氨酸-甘氨酸-天冬氨酸（cRGD）修飾的陽離子脂質(zhì)體（cRGD-CL），用于將ONECUT2（OC-2）shRNA（pshOC-2）靶向遞送至乳腺癌細(xì)胞。陽離子脂質(zhì)體的表征分析表明，制備的cRGD-CL/pshOC-2脂質(zhì)體復(fù)合物粒徑均一（150±1.02 nm），zeta電位適中（19.8±0.249 mV），包封率高達(dá)96%。流式細(xì)胞儀檢測結(jié)果表明，cRGD的引入可顯著促進(jìn)脂質(zhì)體靶向*細(xì)胞。在MCF-7細(xì)胞中，pshOC-2能夠下調(diào)OC-2的表達(dá)，導(dǎo)致細(xì)胞凋亡、細(xì)胞劃痕修復(fù)受阻、遷移和集落形成受阻，其中Bcl-xL和Bcl-2信號通路被抑制，Bax和Cleaved Caspase-3信號通路被上調(diào)。在MCF-7異種移植瘤小鼠中，靜脈注射cRGD-CL/pshOC-2脂質(zhì)體復(fù)合物可有效降低*組織中OC-2的表達(dá)，產(chǎn)生明顯的**作用，提示該脂質(zhì)體復(fù)合物可能通過受體介導(dǎo)的胞吞轉(zhuǎn)運(yùn)作用深入*內(nèi)部。結(jié)果表明，陽離子脂質(zhì)體（cRGD-CL）是一種有效的OC-2 shRNA遞送系統(tǒng)，可能成為乳腺癌*的有效候選藥物。

譯文：

Cationic liposome delivery of interfering RNA (shRNA) plays an important role in tumor therapy. A cyclic arginine glycine aspartate (cRGD) modified cationic liposome (cRGD-CL) was designed for targeting ONECUT2 (OC-2) shRNA (pshOC-2) to breast cancer cells. The characterization analysis of cationic liposomes showed that the prepared cRGD-CL/pshOC-2 liposome complex had uniform particle size (150 ± 1.02 nm), moderate zeta potential (19.8 ± 0.249 mV), and an encapsulation efficiency of up to 96%. The results of flow cytometry analysis showed that the introduction of cRGD can significantly promote liposome targeting of tumor cells. In MCF-7 cells, pshOC-2 can downregulate the expression of OC-2, leading to cell apoptosis, impaired scratch repair, migration, and colony formation. The Bcl xL and Bcl-2 signaling pathways are inhibited, while the Bax and Cleaved Caspase-3 signaling pathways are upregulated. In MCF-7 xenograft tumor mice, intravenous injection of cRGD-CL/pshOC-2 liposome complex can effectively reduce the expression of OC-2 in tumor tissue and produce significant anti-tumor effects, suggesting that this liposome complex may penetrate deep into the tumor through receptor-mediated phagocytic transport. The results show that cationic liposomes (cRGD-CL) is an effective OC-2 shRNA delivery system and may become an effective candidate drug for breast cancer treatment.

西安pg電子官方生物提供相關(guān)產(chǎn)品：

DSPE-PEG-Tetrazine

DSPE-PEG-TMS

DSPE-PEG-TPP

DSPE-PEG-Transferrin 

DSPE-PEG-VE, MW:2000

DSPE-PEG-β-cyclodextrin

DSPE-PEG-Ald

DSPE-PEG-Dethiobiotin

DSPE-PEG-VS

DSPE-PEG-cRGD

DSPE-PEG-KRWWKWWRR

DSPE-PEG-TAT

DSPE-PEG-CTT2

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