文献：线粒体、溶酶体和内质网：哪个是光疗的最佳靶点？

链接：https://www.sciencedirect.com/science/article/abs/pii/S0168365922006320

作者：李艳红 ，贾浩然 ，王洪 银，华先武 ，鲍彦文 ，吴福 根

节选：

为了实现上述目标，我们开发了一种基于含PS脂质胶束的新型药物递送系统（方案1）。该胶束由PS共轭的1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-聚乙二醇（DSPE-PEG）分子（称为DSPE-PEG-Ce6）自组装而成，该分子由含羧基的二氢卟酚e6（Ce6）与含胺基的脂质1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-N- [氨基（聚乙二醇）-5000]（铵盐）（DSPE-PEG 5000 -NH 2）一步反应合成（原料DSPE-PEG 5000 -NH 2和产物DSPE-PEG-Ce6的分子结构见图S1）。结果表明，制备的DSPE-PEG-Ce6能够被癌细胞有效内化并从线粒体迁移到溶酶体，最终到达内质网（ER）。此外，我们能够通过调节DSPE-PEG-Ce6的细胞孵育浓度来精细地调节其细胞内化量到相似的水平，并准确地比较其分别驻留在三种不同细胞器中的*效果。结果清楚地表明，与溶酶体和内质网靶向的光动力*相比，线粒体定位的光动力*取得了最*的*效果。总之，我们在此提供了一个理想的含PS胶束平台，实现了DSPE-PEG-Ce6在细胞器间的动态跟踪，并通过精确的时间和空间*增强了光动力*的疗效，这可能代表了精准医疗的进步。

To achieve the above-mentioned goal, we developed a novel drug delivery system based on PS-containing lipid micelles (Scheme 1). The micelles were self-assembled by a PS-conjugated 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-polyethylene glycol (DSPE-PEG) molecule (termed DSPE-PEG-Ce6) synthesized by a one-step reaction between the carboxyl-containing chlorin e6 (Ce6) and the amine-containing lipid 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[amino(polyethylene glycol)-5000] (ammonium salt) (DSPE-PEG5000-NH2) (the molecular structures of the raw material DSPE-PEG5000-NH2 and the product DSPE-PEG-Ce6 can be found in Fig. S1). The results showed that the as-prepared DSPE-PEG-Ce6 could be efficiently internalized by cancer cells and migrate from mitochondrion to lysosome and ultimately to endoplasmic reticulum (ER). In addition, we were able to carefully tune the cellular internalization quantity of DSPE-PEG-Ce6 to a similar level by modulating its cell incubation concentration and accurately compare its therapeutic efficacy when it separately resided in the three different organelles. The results clearly showed that compared with the lysosome- and ER-targeted PDT, the mitochondrion-localized PDT achieved the most excellent therapeutic outcome. Taken together, we herein provided an ideal PS-containing micellar platform and realized the inter-organelle dynamic tracking of DSPE-PEG-Ce6 and enhanced PDT efficacy through precise temporal and spatial treatment, which may represent an advancement in precision medicine.

西安齐岳生物提供相关产品：

APRPG-PEG-DSPE

NGR-PEG-DSPE

NGR(c(GGCNGRC))-PEG-DSPE

RVG29-PEG-DSPE

THRPPMWSPVWP-PEG-DSPE

M2pep-PEG-DSPE

EB1-PEG-DSPE

CPP-PEG-DSPE

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！