Faculty of Chemistry, University of Wroclaw, F. Joliot-Curie 14, 50-383 Wroclaw, Poland.
Spectrochim Acta A Mol Biomol Spectrosc. 2019 Jun 5;216:15-24. doi: 10.1016/j.saa.2019.03.011. Epub 2019 Mar 6.
Phenothiazine molecules are effective and commonly used antipsychotic drugs, especially in the treatment of schizophrenia. However, they produce strong extrapyramidal side-effects manifested by drug-induced parkinsonism. Because Parkinson's disease as a neurodegenerative illness is associated with the formation of amyloid fibrils in neuronal cells, it is postulated that the development of phenothiazine-induced parkinsonism may be related to the phenothiazine-induced formation of fibrillar aggregates. The effect of phenothiazine compounds (fluphenazine (FPh), chlorpromazine (ChP) and propionylpromazine (PP)) on the fibrillogenesis of poly-l-lysine (PLL) was studied using Fourier-transform infrared (FTIR) spectroscopy supported by principal component analysis (PCA), vibrational circular dichroism (VCD), transmission electron microscopy (TEM) and Congo red binding assay. The fibrillogenesis of PLL is accompanied by fibril formation with charged or uncharged polypeptides with PPII (polyproline-like extended helix), α-helix or β-sheet conformations. All of the phenothiazine molecules investigated effectively reduced the temperature required to induce the formation of β-sheet-rich fibrils from α-helix-rich fibrils of PLL.
吩噻嗪类分子是有效的、常用的抗精神病药物,尤其在治疗精神分裂症方面。然而,它们会产生强烈的锥体外系副作用,表现为药物诱导的帕金森病。由于帕金森病是一种神经退行性疾病,与神经元细胞中淀粉样纤维的形成有关,因此推测吩噻嗪类药物诱导的帕金森病的发展可能与吩噻嗪类药物诱导的纤维状聚集物的形成有关。使用傅里叶变换红外(FTIR)光谱结合主成分分析(PCA)、振动圆二色性(VCD)、透射电子显微镜(TEM)和刚果红结合测定法,研究了吩噻嗪类化合物(氟奋乃静(FPh)、氯丙嗪(ChP)和丙酰奋乃静(PP))对聚-l-赖氨酸(PLL)的原纤维形成的影响。PLL 的原纤维形成伴随着带电荷或不带电荷的多肽的原纤维形成,具有 PPII(类脯氨酸延伸螺旋)、α-螺旋或β-折叠构象。研究的所有吩噻嗪类分子都有效地降低了 PLL 从富含α-螺旋的原纤维向富含β-折叠的原纤维形成所需的温度。