Faculty of Health Science, Sinop University, Sinop, Turkey.
Department of Pharmacology, Faculty of Veterinary, Mustafa Kemal University, Hatay, Turkey.
Clin Exp Pharmacol Physiol. 2020 Nov;47(11):1834-1842. doi: 10.1111/1440-1681.13359. Epub 2020 Aug 19.
Iron overload is a key target in drug development. This study aimed to investigate the coordination of Fe(III) ions with a curcumin-oxime ligand that may be used in the treatment of iron overload. The synthesis of the curcumin-oxime ligand and curcumin-oxime-Fe(III) complex was successfully made and characterized in its solid-state and solution-state using FT-IR, UV-Vis, elemental analysis, and H-NMR. However, in this study, we investigated the apoptotic effects of the curcumin-oxime Fe (III) complex on SW480. SW480 cells were exposed to 99.2% medium for 48 hours. After 48 hours, the incubation period, cells were harvested by centrifugation and washed in phosphate-buffered saline (PBS) and lysed in radio-immunoprecipitation assay (RIPA) buffer for 20 minutes and supernatants were taken and pellets were discarded. ELISA test was used to examine the expression, and activity of cleaved caspase-3, Bax, and Bcl-2 proteins in SW480 cells. ELISA test results indicated that the activities of apoptotic proteins Bax, caspase 3 and Bcl-2 in human SW480 cell lines significantly increased in 48 hours treatment. Also, the activity of Bcl-2 was observed to decrease significantly. Catalase activities of the complex were investigated. The findings showed that the complex has a catalase activity. The findings suggest that this type of complex may constitute a new and interesting basis for the future search of new and more potent drugs. The SOD activity of the result showed that the complexes possessed a considerable SOD activity with an IC50 value of 7.685 µM. Also, when compared with the control, a complex increased the SOD levels (P < .05). Electrochemistry studies in the literature have shown that the Fe /Fe couple redox process occurs in low potential. This value is within the range of compounds that are expected to show superoxide dismutase activity. The I /I shows that one electron transport takes place in the complex. Our results suggest that curcumin-oxime may represent a new approach in the treatment of iron overload.
铁过载是药物开发的一个关键目标。本研究旨在研究与姜黄素肟配体配位的铁(III)离子，该配体可能用于治疗铁过载。成功地在固态和溶液态下合成了姜黄素肟配体和姜黄素肟-Fe(III)配合物，并通过 FT-IR、UV-Vis、元素分析和 1H-NMR 对其进行了表征。然而，在这项研究中，我们研究了姜黄素肟 Fe(III)配合物对 SW480 的凋亡作用。SW480 细胞暴露于 99.2%的培养基中 48 小时。孵育 48 小时后，收集细胞，用磷酸盐缓冲盐水 (PBS) 洗涤，然后在放射性免疫沉淀分析 (RIPA) 缓冲液中裂解 20 分钟，取上清液，丢弃沉淀。ELISA 试验用于检测 SW480 细胞中裂解的 caspase-3、Bax 和 Bcl-2 蛋白的表达和活性。ELISA 试验结果表明，在 48 小时处理后，人 SW480 细胞系中凋亡蛋白 Bax、caspase 3 和 Bcl-2 的活性显著增加。此外，还观察到 Bcl-2 的活性显著降低。还研究了配合物的过氧化氢酶活性。结果表明，该配合物具有过氧化氢酶活性。研究结果表明，这种类型的配合物可能为未来寻找新的、更有效的药物提供一个新的、有趣的基础。结果显示，该复合物具有相当的 SOD 活性，IC50 值为 7.685µM。此外，与对照组相比，复合物增加了 SOD 水平 (P<.05)。文献中的电化学研究表明，Fe/Fe 偶联的氧化还原过程发生在低电位。这个值在预计具有超氧化物歧化酶活性的化合物范围内。I/I 表明在配合物中发生了一个电子传递。我们的研究结果表明，姜黄素肟可能代表一种治疗铁过载的新方法。
