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源自皮洛蒂酸的一氧化氮供体的合成及其对PC12细胞多巴胺分泌影响的研究。

Synthesis of Nitric Oxide Donors Derived from Piloty's Acid and Study of Their Effects on Dopamine Secretion from PC12 Cells.

作者信息

Sanna Daniele, Rocchitta Gaia, Serra Maria, Abbondio Marcello, Serra Pier Andrea, Migheli Rossana, De Luca Lidia, Garribba Eugenio, Porcheddu Andrea

机构信息

Istituto CNR di Chimica Biomolecolare, Trav. La Crucca 3, 07040 Sassari, Italy.

Department of Clinical and Experimental Medicine, Medical School, University of Sassari, viale San Pietro 43/b, 07100 Sassari, Italy.

出版信息

Pharmaceuticals (Basel). 2017 Sep 5;10(3):74. doi: 10.3390/ph10030074.

Abstract

This study investigated the mechanisms and kinetics of nitric oxide (NO) generation by derivatives of Piloty's acid (NO-donors) under physiological conditions. In order to qualitatively and quantitatively measure NO release, electron paramagnetic resonance (EPR) was carried out with NO spin trapping. In addition, voltammetric techniques, including cyclic voltammetry and constant potential amperometry, were used to confirm NO release from Piloty's acid and its derivatives. The resulting data showed that Piloty's acid derivatives are able to release NO under physiological conditions. In particular, electron-withdrawing substituents favoured NO generation, while electron-donor groups reduced NO generation. In vitro microdialysis, performed on PC12 cell cultures, was used to evaluate the dynamical secretion of dopamine induced by the Piloty's acid derivatives. Although all the studied molecules were able to induce DA secretion from PC12, only those with a slow release of NO have not determined an autoxidation of DA itself. These results confirm that the time-course of NO-donors decomposition and the amount of NO released play a key role in dopamine secretion and auto-oxidation. This information could drive the synthesis or the selection of compounds to use as potential drugs for the therapy of Parkinson's disease (PD).

摘要

本研究调查了生理条件下皮洛蒂酸衍生物(一氧化氮供体)产生一氧化氮(NO)的机制和动力学。为了定性和定量测量NO释放,采用NO自旋捕获进行电子顺磁共振(EPR)。此外,还使用了包括循环伏安法和恒电位安培法在内的伏安技术来确认皮洛蒂酸及其衍生物释放NO的情况。所得数据表明,皮洛蒂酸衍生物在生理条件下能够释放NO。特别是,吸电子取代基有利于NO生成,而供电子基团则减少NO生成。对PC12细胞培养物进行的体外微透析用于评估皮洛蒂酸衍生物诱导的多巴胺动态分泌。尽管所有研究的分子都能够诱导PC12分泌多巴胺,但只有那些NO释放缓慢的分子才不会导致多巴胺自身的自氧化。这些结果证实,NO供体分解的时间进程和释放的NO量在多巴胺分泌和自氧化中起关键作用。这些信息可以推动化合物的合成或选择,以用作治疗帕金森病(PD)的潜在药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bad1/5620618/599d5e9d740f/pharmaceuticals-10-00074-g001.jpg

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