DSPE-PEG-COOH用于制備DSPE-PEG-DOX的相關(guān)文獻（含合成路線）

文獻名: Peptide Engraftment on PEGylated Nanoliposomes for Bone Specific Delivery of PTH (1-34) in Osteoporosis

作者：

Taewon Hwang 1, Hee Dong Han, Chung Kil Song, Hasoo Seong, Jung Hyun Kim, Xiaoyuan Chen, Byung Cheol Shin

摘要：

抗癌藥物的腫瘤特異性遞送是藥物開發(fā)過程中面臨的主要挑戰(zhàn)之一。在這項研究中，我們通過將新合成的DSPE-PEG2000-DOX（DPD）作為脂質(zhì)成分摻入脂質(zhì)體中制備了阿霉素（DOX）偶聯(lián)脂質(zhì)體（DCL），并測試了其體內(nèi)抗腫瘤活性。通過酰胺鍵將DOX偶聯(lián)到DSPE-PEG2000-COOH上合成了DPD，并通過（1）H-NMR分析確認了所得DPD的化學結(jié)構(gòu)。通過薄膜澆鑄水合法制備了脂質(zhì)體尺寸為130nm的DCL。流式細胞術(shù)分析證實，DCL的細胞攝取明顯高于傳統(tǒng)脂質(zhì)體。DCL對小鼠B16F10黑色素瘤荷瘤小鼠的抗腫瘤活性表明，DCL比傳統(tǒng)脂質(zhì)體更有效地抑制腫瘤生長，這可能是由于DOX介導的內(nèi)吞過程。

實驗使用方法:

Synthesis ofConjugate (SDSSD-DSPE)

A lipid-PEG-peptide combination that may subsequently be added to liposomes forbone targeting was developed, SDSSD was conjugated to DSPE-PEG2000-C00H usingcarbodiimide chemistry, based on the previously described method by Wang et al. withmodi fications [32. Briefly, DSPE-PEG2000-COOH was dissolved in 0.1 M MES bufferat pH 6.0 and stirred at 2-8 °C for 10 min. Then, EDC.HCl and NHS (20 equivalentseach) were added to the reaction mixture and stirred for 60 min at 2-8 °C. A 7.4 pHadjustment was made to the reaction mixture, Finally, SDSSD, previously dissolved inMilli-Q water, was added to the reaction mixture and stirred overnight. The resultantmixture was dialyzed using a 2KD dialysis membrane for 48 h to remove unconjugatedSDSSD. Purifield SDSSD-DSPE (conjugate) was freeze-dried and characterized by'H-NMRMaldi-TOF, and a Scanning Electron Microscope (SEM) followed by Energy Dispersive。

反應結(jié)構(gòu)路線

重要檢測:

文獻核磁

重要實驗結(jié)果說明

Synthesis of DSPE-PEG2000-DOX (DPD)Covalent conjugation of DOX to DSPE.PEG2000-COOH was confirmed by HNMR (500 MHz, Auto Sampler-HRMAS.FT-NMR, Bruker, Switzerland) analysis ofDPD. 'HNMR spectra were obtained forcomb polymer solutions in deuteratedchloroform. As shown in a Figure 3, theproton peaks of DOX (1,2 and 3)andDSPE-PEG2000-C00H(4 and 5)wereobserved at 7.4~8.2 ppm and 1.2~3.7ppm, respectively.

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廠家:西安齊岳生物科技有限公司

用途:科研

狀態(tài)：固體/粉末/溶液

產(chǎn)地:西安

溫馨提醒:僅供科研，不能用于人體實驗!

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