文献：DOPC-Detergent Conjugates: Fusogenic Carriers for Improved In Vitro and In Vivo Gene Delivery

作者：Philippe Pierrat, Anne Casset, Dimitri Kereselidze, Marie Lux, Françoise Pons, Luc Lebeau

文献链接：https://onlinelibrary.wiley.com/doi/abs/10.1002/mabi.201600012

摘要：

Phospholipid-detergent conjugates are proposed as fusogenic carriers for gene delivery. Eleven compounds are prepared and their properties are investigated. The ability of the conjugates to promote fusion with a negatively charged model membrane is determined. Their DNA delivery efficiency and cytotoxicity are assessed in vitro. Lipoplexes are administered in the mouse lung, and transgene expression Indeterminate inflammatory activity are measured. The results show that conjugation of 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) with C12E4 produces a carrier that can efficiently deliver DNA to cells, with negligible ­associated toxicity. Fusogenicity of the conjugates shows good correlation with in vitro transfection efficiency and crucially depends on the length of the polyether moiety of the detergent. Finally, DOPC-C12E4 reveals highly potent for in vivo DNA delivery and favorably compares to GL67A, the current golden standard for gene delivery to the airway, opening the way for further promising developments.

磷脂洗涤剂偶联物被提出作为基因递送的融合载体。制备了11种化合物，并对其性质进行了研究。测定偶联物促进与带负电荷的模型膜融合的能力。

在体外评估它们的DNA递送效率和细胞毒性。在小鼠肺部施用Lipoplex，并测量转基因表达不确定的炎症活性。

结果表明，1,2-二油酰基-sn-甘油-3-磷酸胆碱（DOPC）与C12E4的偶联产生了一种载体，可以有效地将DNA递送到细胞，相关毒性可以忽略不计。

偶联物的融合原性与体外转染效率具有良好的相关性，并且在很大程度上取决于洗涤剂聚醚部分的长度。

最后，DOPC-C12E4在体内DNA递送方面表现出色，与目前用于气道基因递送的金标准GL67A相比具有优势，为进一步有前景的发展开辟了道路。

相关推荐：

DOPE-PEG-CH2COOH

DOPE-PEG-FA

DOPE-PEG-Mal

DOPE-PEG-NH2

DOPE-PEG-SC

DOPE-PEI

DPPE-Cap-Biotin

DPPE-Cap-Folate

DPPE-ICG

DPPE-mPEG

DPPE-PEG2-NH-Mal

以上文章内容来源各类期刊或文献，如有侵权请联系我们删除！