Georgieva Stela, Todorov Petar, Tchekalarova Jana
Department of Analytical Chemistry, University of Chemical Technology and Metallurgy, 1756 Sofia, Bulgaria.
Department of Organic Chemistry, University of Chemical Technology and Metallurgy, 1756 Sofia, Bulgaria.
Pharmaceuticals (Basel). 2025 Jan 5;18(1):53. doi: 10.3390/ph18010053.
This study explores the potential for the synthesis of peptide nanosystems comprising spinorphin molecules (with rhodamine moiety: Rh-S, Rh-S5, and Rh-S6) conjugated with nanoparticles (AuNPs), specifically peptide Rh-S@AuNPs, peptide Rh-S5@AuNPs, and peptide Rh-S6@AuNPs, alongside a comparative analysis of the biological activities of free and conjugated peptides. The examination of the microstructural characteristics of the obtained peptide systems and their physicochemical properties constitutes a key focus of this study. Zeta (ζ) potential, Fourier transformation infrared (FTIR) spectroscopy, circular dichroism (CD), scanning electron microscopy (SEM-EDS), transmission electron microscopy (TEM), and UV-Vis spectrophotometry were employed to elucidate the structure-activity correlations of the peptide@nano AuNP systems. The zeta potential values for all the Rh-S@AuNPs demonstrate that the samples are electrically stable and resistant to flocculation and coagulation. The absorption of energy quanta from UV-Vis radiation by the novel nanopeptide systems does not substantially influence the distinctive signal of AuNPs, which is situated at around 531 nm. The FTIR measurements indicate the signals associated with the unique functional groups of the peptides, whereas circular dichroism verifies the synthesis of the conjugated nanocomposites of the spinorphin@AuNP type. An analysis of the SEM and TEM data revealed that most AuNPs have a spherical morphology, with an average diameter of around 21.92 ± 6.89 nm. The results of the in vivo studies showed promising findings regarding the anticonvulsant properties of the nanocompounds, especially the Rh-S@AuNP formulation. : All the nanocompounds tested demonstrated the ability to reduce generalized tonic-clonic seizures. This suggests that these formulations may effectively target the underlying neuronal hyperexcitability. In addition, the prepared Rh-S@AuNP formulations also showed anticonvulsant activity in the maximal electroshock test performed in mice, which was evident after systemic (intraperitoneal) administration. The study's findings indicate that conjugates can be synthesized via a straightforward process, rendering them potential therapeutic agents with biological activity.
本研究探索了合成包含与纳米颗粒（金纳米颗粒，AuNPs）共轭的斯皮诺啡分子（带有罗丹明部分：Rh-S、Rh-S5和Rh-S6）的肽纳米系统的潜力，具体为肽Rh-S@AuNPs、肽Rh-S5@AuNPs和肽Rh-S6@AuNPs，并对游离肽和共轭肽的生物活性进行了对比分析。对所得肽系统的微观结构特征及其物理化学性质的研究是本研究的重点。采用zeta（ζ）电位、傅里叶变换红外（FTIR）光谱、圆二色性（CD）、扫描电子显微镜（SEM-EDS）、透射电子显微镜（TEM）和紫外可见分光光度法来阐明肽@纳米金颗粒系统的构效关系。所有Rh-S@AuNPs的zeta电位值表明样品在电学上是稳定的，抗絮凝和凝聚。新型纳米肽系统对紫外可见辐射能量量子的吸收对位于约531nm处的金纳米颗粒的独特信号没有实质性影响。FTIR测量表明了与肽的独特官能团相关的信号，而圆二色性验证了斯皮诺啡@AuNP型共轭纳米复合材料的合成。对SEM和TEM数据的分析表明，大多数金纳米颗粒呈球形，平均直径约为21.92±6.89nm。体内研究结果显示了关于纳米化合物抗惊厥特性的有前景的发现，尤其是Rh-S@AuNP制剂。：所有测试的纳米化合物都表现出减少全身强直阵挛性癫痫发作的能力。这表明这些制剂可能有效地靶向潜在的神经元过度兴奋。此外，制备的Rh-S@AuNP制剂在对小鼠进行的最大电休克试验中也显示出抗惊厥活性，在全身（腹腔内）给药后很明显。该研究结果表明共轭物可以通过简单的过程合成，使其成为具有生物活性的潜在治疗剂。
