Hennig Dorle, Schubert Stephanie, Dargatz Harald, Kostenis Evi, Fahr Alfred, Schubert Ulrich S, Heinzel Thorsten, Imhof Diana
Center for Molecular Biomedicine, Institute of Biochemistry and Biophysics, Department of Biochemistry, Friedrich Schiller University Jena, Hans-Knöll-Str. 2, D-07745, Jena, Germany.
Macromol Biosci. 2014 Jan;14(1):69-80. doi: 10.1002/mabi.201300213. Epub 2013 Aug 21.
The use of different nanoparticles (NPs) for successful encapsulation of bioactive substances is discussed. The inclusion efficiency into liposomes, acetalated dextran (Ac-Dex), and variants of poly[(lactic acid)-co-(glycolic acid)] (PLGA) NPs is analyzed after chemical degradation. Efficient inclusion of SIRT1 inhibitor Ex527 in liposomes, Ac-Dex- and PLGA-NPs is observed for all procedures used. Activity of Ex527 is demonstrated by monitoring the acetylation status of SIRT1-target p53. In contrast, small peptides are only incorporated into acid-terminated PLGA-NPs and marginally into Ac-Dex-NPs. The yield depends on peptide sequence and terminal modifications. Activity is exemplified for angiotensin II using the dynamic mass redistribution technology.
讨论了使用不同的纳米颗粒（NPs）成功包封生物活性物质的情况。在化学降解后，分析了生物活性物质包入脂质体、乙酰化葡聚糖（Ac-Dex）和聚（乳酸-共-乙醇酸）（PLGA）纳米颗粒变体中的包封效率。对于所有使用的方法，均观察到SIRT1抑制剂Ex527能有效包入脂质体、Ac-Dex和PLGA纳米颗粒中。通过监测SIRT1靶标p53的乙酰化状态来证明Ex527的活性。相比之下，小肽仅能掺入酸封端的PLGA纳米颗粒中，且少量掺入Ac-Dex纳米颗粒中。产率取决于肽序列和末端修饰。使用动态质量再分布技术以血管紧张素II为例证明了其活性。
