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氟奋乃静与金纳米颗粒共轭物的光谱性质及生物活性

Spectroscopic Properties and Biological Activity of Fluphenazine Conjugates with Gold Nanoparticles.

作者信息

Kowalska Oliwia, Piergies Natalia, Barbasz Anna, Niemiec Piotr, Gnacek Patrycja, Duraczyńska Dorota, Oćwieja Magdalena

机构信息

Jerzy Haber Institute of Catalysis and Surface Chemistry, Polish Academy of Sciences, Niezapominajek 8, PL-30239 Krakow, Poland.

Institute of Nuclear Physics, Polish Academy of Sciences, PL-31342 Krakow, Poland.

出版信息

Molecules. 2024 Dec 17;29(24):5948. doi: 10.3390/molecules29245948.

DOI:10.3390/molecules29245948
PMID:39770038
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11676885/
Abstract

Fluphenazine (FPZ) is a well-known neuroleptic that has attracted considerable scientific interest due to its biocidal, virucidal, and antitumor properties. Although methods for encapsulating and delivering FPZ to enhance its activity and reduce side effects have been developed, there is still limited knowledge about its conjugates with gold nanoparticles (AuNPs). Therefore, the aim of this research was to develop a preparation method for stable FPZ-AuNP conjugates and to investigate their physicochemical and biological properties. FPZ-AuNP conjugates were synthesized via a ligand exchange process on the surface of gold nanoparticles (AuNPs) with an average size of 17 ± 5 nm. Electrokinetic measurements revealed that the zeta potential of FPZ-AuNPs is affected by both their composition and pH. The FPZ-AuNPs exhibited an isoelectric point due to the acid-base properties of FPZ. Surface-enhanced Raman spectroscopy (SERS), combined with density functional theory (DFT), was used to determine the adsorption structure of FPZ after conjugation. Studies with human neuroblastoma cells (SH-SY5Y) revealed that FPZ-AuNP conjugates more effectively reduced cell viability compared to citrate-stabilized AuNPs alone or free FPZ molecules. The reduction in SH-SY5Y cell viability was found to be dependent on the FPZ-AuNP concentration.

摘要

氟奋乃静（FPZ）是一种著名的抗精神病药物，因其具有杀菌、杀病毒和抗肿瘤特性而引起了相当大的科学关注。尽管已经开发出了用于包裹和递送FPZ以增强其活性并减少副作用的方法，但关于其与金纳米颗粒（AuNPs）的共轭物的知识仍然有限。因此，本研究的目的是开发一种稳定的FPZ-AuNP共轭物的制备方法，并研究其物理化学和生物学特性。通过在平均尺寸为17±5nm的金纳米颗粒（AuNPs）表面进行配体交换过程合成了FPZ-AuNP共轭物。电动测量表明，FPZ-AuNPs的zeta电位受其组成和pH值的影响。由于FPZ的酸碱性质，FPZ-AuNPs表现出一个等电点。表面增强拉曼光谱（SERS）结合密度泛函理论（DFT）用于确定共轭后FPZ的吸附结构。对人神经母细胞瘤细胞（SH-SY5Y）的研究表明，与单独的柠檬酸盐稳定的AuNPs或游离的FPZ分子相比，FPZ-AuNP共轭物更有效地降低了细胞活力。发现SH-SY5Y细胞活力的降低取决于FPZ-AuNP的浓度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/fec5e22a6a0b/molecules-29-05948-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/40769297c1c0/molecules-29-05948-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/e2cfb0594b6d/molecules-29-05948-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/4efce67e8741/molecules-29-05948-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/bc4d8ee5f967/molecules-29-05948-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/b9a35e2b3088/molecules-29-05948-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/76d9113be908/molecules-29-05948-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/988c0767f24f/molecules-29-05948-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/64a2a4853fea/molecules-29-05948-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/fec5e22a6a0b/molecules-29-05948-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/40769297c1c0/molecules-29-05948-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/e2cfb0594b6d/molecules-29-05948-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/4efce67e8741/molecules-29-05948-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/bc4d8ee5f967/molecules-29-05948-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/b9a35e2b3088/molecules-29-05948-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/76d9113be908/molecules-29-05948-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/988c0767f24f/molecules-29-05948-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/64a2a4853fea/molecules-29-05948-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ce07/11676885/fec5e22a6a0b/molecules-29-05948-g009.jpg

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本文引用的文献

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The Adsorption of Chlorpromazine on the Surface of Gold Nanoparticles and Its Effect on the Toxicity to Selected Mammalian Cells.氯丙嗪在金纳米颗粒表面的吸附及其对所选哺乳动物细胞毒性的影响。
Materials (Basel). 2024 Sep 28;17(19):4774. doi: 10.3390/ma17194774.
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Spectroscopic studies under properties of chlorpromazine conjugated to gold nanoparticles.氯丙嗪与金纳米粒子偶联的光谱性质研究。
Spectrochim Acta A Mol Biomol Spectrosc. 2024 Nov 5;320:124588. doi: 10.1016/j.saa.2024.124588. Epub 2024 Jun 3.
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Repurposing phenothiazines for cancer therapy: compromising membrane integrity in cancer cells.
将吩噻嗪类药物用于癌症治疗的新用途：破坏癌细胞的膜完整性
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