Studzińska-Sroka Elżbieta, Majchrzak-Celińska Aleksandra, Bańdurska Monika, Rosiak Natalia, Szwajgier Dominik, Baranowska-Wójcik Ewa, Szymański Marcin, Gruszka Wojciech, Cielecka-Piontek Judyta
Department of Pharmacognosy, Poznan University of Medical Sciences, Rokietnicka 3 Str., 60-806 Poznań, Poland.
Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, Święcickiego 4 Str., 60-781 Poznań, Poland.
Antioxidants (Basel). 2022 Oct 20;11(10):2069. doi: 10.3390/antiox11102069.
Lichens are a source of various biologically active compounds. However, the knowledge about them is still scarce, and their use in medicine is limited. This study aimed to investigate the therapeutic potential of the lichen and its major metabolite caperatic acid in regard to their potential application in the treatment of central nervous system diseases, especially neurodegenerative diseases and brain tumours, such as glioblastoma. First, we performed the phytochemical analysis of the tested extracts based on FT-IR derivative spectroscopic and gas chromatographic results. Next the antioxidant properties were determined, and moderate anti-radical activity, strong chelating properties of Cu and Fe ions, and a mild effect on the antioxidant enzymes of the tested extracts and caperatic acid were proved. Subsequently, the influence of the tested extracts and caperatic acid on cholinergic transmission was determined by in vitro and in silico studies confirming that inhibitory effect on butyrylcholinesterase is stronger than against acetylcholinesterase. We also confirmed the anti-inflammatory properties of extracts and caperatic acid using a COX-2 and hyaluronidase inhibition models. Moreover, our studies show the cytotoxic and pro-apoptotic activity of the extracts against T98G and U-138 MG glioblastoma multiforme cell lines. In conclusion, it is possible to assume that extracts and especially caperatic acid can be regarded as the source of the valuable substances to finding new therapies of central nervous system diseases.
地衣是多种生物活性化合物的来源。然而，关于它们的知识仍然匮乏，其在医学上的应用也很有限。本研究旨在探讨地衣及其主要代谢产物石花酸在治疗中枢神经系统疾病，特别是神经退行性疾病和脑肿瘤（如胶质母细胞瘤）方面的治疗潜力。首先，我们基于傅里叶变换红外导数光谱和气相色谱结果对测试提取物进行了植物化学分析。接下来测定了抗氧化性能，结果证明测试提取物和石花酸具有适度的抗自由基活性、对铜和铁离子的强螯合性能以及对测试提取物和石花酸的抗氧化酶有轻微影响。随后，通过体外和计算机模拟研究确定了测试提取物和石花酸对胆碱能传递的影响，证实其对丁酰胆碱酯酶的抑制作用强于对乙酰胆碱酯酶的抑制作用。我们还使用COX - 2和透明质酸酶抑制模型证实了提取物和石花酸的抗炎特性。此外，我们的研究表明提取物对多形性胶质母细胞瘤T98G和U - 138 MG细胞系具有细胞毒性和促凋亡活性。总之，可以假设提取物，尤其是石花酸可被视为寻找中枢神经系统疾病新疗法的有价值物质的来源。
