Institute of Biochemistry and Biophysics, P. O. Box 13145-1384, University of Tehran, Tehran, Iran.
Int J Biol Macromol. 2013 Sep;60:334-40. doi: 10.1016/j.ijbiomac.2013.06.013. Epub 2013 Jun 15.
Deposition of proteins is a key pathogenic feature of more than 20 amyloid-related diseases. Inhibiting or reversing amyloid aggregation via the use of small molecules is proposed as two useful approaches in hampering the development of these diseases. In this research, we examined the inhibitory and disruptive effects of apigenin, a common dietary flavonoid with multiple pharmacological properties, against human insulin fibrillization. Besides, we investigated the potential cytotoxicity of insulin fibrils on SK-N-MC cells in the presence and absence of apigenin. The increase in Thioflavin T (ThT) and anilinonaphthalene-8-sulfonic acid (ANS) fluorescent intensities and Congo red absorbance were inhibited by simultaneous incubation of various concentrations of apigenin with insulin, in a dose-dependent manner. The spectroscopy results were confirmed by transmission electron microscopy, where lower extent of fibrillar structures was observed in the presence of apigenin. In addition, the cell exposure to the co-incubated insulin amyloids with apigenin led to the increased viability and decreased LDH release dose-dependently, compared to cells exposed to insulin fibrils alone. Co-incubation with apigenin also attenuated the extent of apoptotic cell death induced by insulin fibrils. It can be concluded that apigenin possess in vitro anti-amyloidogenic activities as well as protective effects against insulin amyloids cytotoxicity.
蛋白质沉积是 20 多种淀粉样相关疾病的关键致病特征。通过使用小分子抑制或逆转淀粉样聚集被认为是阻碍这些疾病发展的两种有用方法。在这项研究中,我们研究了芹菜素(一种具有多种药理特性的常见饮食类黄酮)对人胰岛素纤维形成的抑制和破坏作用。此外,我们还研究了在存在和不存在芹菜素的情况下,胰岛素纤维对 SK-N-MC 细胞的潜在细胞毒性。随着胰岛素中各种浓度的芹菜素的同时孵育,硫黄素 T(ThT)和苯胺萘-8-磺酸(ANS)荧光强度和刚果红吸光度的增加呈剂量依赖性抑制。光谱结果通过透射电子显微镜得到证实,在存在芹菜素的情况下观察到纤维结构的程度较低。此外,与单独暴露于胰岛素纤维的细胞相比,细胞暴露于与芹菜素共孵育的胰岛素淀粉样物会导致细胞活力增加和 LDH 释放减少,呈剂量依赖性。与胰岛素纤维共孵育也能减轻胰岛素纤维诱导的细胞凋亡死亡的程度。可以得出结论,芹菜素具有体外抗淀粉样变性活性以及对胰岛素淀粉样毒性的保护作用。