中文摘要：

背景渗透房间的肽(hCPPs ) 表明的发卡由分子的调节激活的一个有趣的特征。我们假设了那 hCPPs 有潜力有选择地交付一根顺磁的金轧探针进矩阵 metalloproteinase 2 ( MMP-2 )积极人的卵巢腺癌房间排队， SKOV-3.Methods hCPPs 被综合并且用 1,4,7,10-tetraazacyclododecane-N 标记，并且， N “，并且“ -tetraacetic 酸金轧()( Gd-DOTA )并且由用一个标准的 f-moc 策略的荧光黄 isothiocyanate ( FITC )固体阶段肽合成协议。MMP-2 表示和活动被反向的 transcriptase 聚合酶链反应(RT-PCR ) 和 zymography 表明。在 SKOV-3 房间的 hCPPs 的成为主观和地点被荧光黄成像和流动 cytometery 观察。在 SKOV-3 房间的 Gd-DOTA 的选择交货被磁性的回声成像(MRI ) 和由 SKOV-3 房间的 hCPPs 的举起取决于的传播电子显微镜学(TEM ).Results 观察 MMP-2 的活动。与 Gd-DOTA-hCPPs 对待的 SKOV-3 房间的 T1WI 信号建议 Gd-DOTA-hCPPs 的举起在一时间增加了 --(r=0.990， P 0.01 ) 并且集中依赖者举止(r=0.964， P 0.001 ) ，但是被一个 MMP-2 禁止者禁止。电子显微镜学证明了 gadolinium.Conclusions hCPPs 的细胞内部的穿入的传播在细胞质和原子核观察的电子稠密的粒子能被用作有效向量让一根 MRI 分子的探针估计 MMP-2 的活动。

英文摘要：

Background The hairpin cell-penetrating peptides （hCPPs） demonstrate an interesting characteristic of conditioned activation by molecules. We hypothesized that hCPPs have the potential to selectively deliver a paramagnetic gadolinium probe into the matrix metalloproteinase 2 （MMP-2） positive human ovary adenocarcinoma cell lines, SKOV-3. Methods hCPPs were synthesized and labeled with 1,4,7,10-tetraazacyclododecane-N,N＇,N＂,N＂＇-tetraacetic acid gadolinium （111） （Gd-DOTA） and fluorescein isothiocyanate （FITC） by f-moc strategy using a standard solid phase peptide synthesis protocol. MMP-2 expression and activity were demonstrated by reverse transcriptase polymerase chain reaction （RT-PCR） and zymography. Internalization and location of hCPPs in SKOV-3 cells were observed by fluorescein imaging and flow cytometery. Selective delivery of Gd-DOTA in SKOV-3 cells was observed by magnetic resonance imaging （MRI） and transmission electron microscopy （TEM）. Results The uptake of hCPPs by SKOV-3 cells depended on the activity of MMP-2. T1WI signals of SKOV-3 cells treated with Gd-DOTA-hCPPs suggested the uptake of Gd-DOTA-hCPPs increased in a time- （r=0.990, P 〈0.01） and concentration-dependent manner （r=0.964, P 〈0.001）, but was inhibited by a MMP-2 inhibitor. Electron-dense particles observed in the cytoplasm and nucleus by transmission electron microscopy proved the intracellular penetration of gadolinium. Conclusions hCPPs can be used as an effective vector for an MRI molecular probe to assess the activity of MMP-2.