Elawady Mohamed E, Hamed Ahmed A, Alsallami Wamedh M, Gabr Ebtsam Z, Abdel-Monem Mohamed O, Hassan Mervat G
Microbial Biotechnology Department, National Research Centre, El-Buhouth St. 33, Cairo 12622, Egypt.
Microbial Chemistry Department, National Research Centre, El-Buhouth St. 33, Cairo 12622, Egypt.
Microorganisms. 2023 Apr 19;11(4):1062. doi: 10.3390/microorganisms11041062.
Endophytic fungi are a highly unpredictable group of microorganisms that can create a diverse range of secondary metabolites with biological activity. These metabolites enhance the host's ability to tolerate stress caused by various factors, such as disease, insects, pathogens, and herbivores. The secondary metabolites produced by endophytic fungi may have potential applications in agriculture, pharmacy, and medicine. The purpose of this study was to examine the anti-acetylcholinesterase activity of secondary metabolites extracted from endophytic fungi. SB5 was one of the many endophytic fungi isolated from and identified genetically with accession number ON872302. Our study utilized fermentation and microbial cultivation techniques to obtain secondary metabolites. During the course of our investigation, we isolated a compound called Physcion (C1) from the endophytic fungus SB5. We subsequently identified that C1 possesses inhibitory activity against COX-2 and LOX-1, with IC50 values of 43.10 and 17.54 µg/mL, respectively, making it an effective anti-inflammatory agent. Moreover, we found that C1 also exhibited potent anticholinesterase activity (86.9 ± 1.21%). In addition to these promising therapeutic properties, our experiments demonstrated that C1 possesses strong antioxidant capacity, as evidenced by its ability to scavenge DPPH, ABTS, O2 radicals, and NO and inhibit lipid peroxidation. To further investigate the molecular mechanisms underlying C1 pharmacological properties, we employed SwissADME web tools to predict the compound's ADME-related physicochemical properties and used Molecular Operating Environment and PyMOL for molecular docking studies.
内生真菌是一类高度不可预测的微生物，能够产生多种具有生物活性的次生代谢产物。这些代谢产物可增强宿主耐受由各种因素（如疾病、昆虫、病原体和食草动物）引起的应激的能力。内生真菌产生的次生代谢产物可能在农业、制药和医学领域具有潜在应用。本研究的目的是检测从内生真菌中提取的次生代谢产物的抗乙酰胆碱酯酶活性。SB5是从[具体来源未给出]分离并通过基因鉴定的众多内生真菌之一，登录号为ON872302。我们的研究利用发酵和微生物培养技术来获取次生代谢产物。在研究过程中，我们从内生真菌SB5中分离出一种名为大黄素甲醚（C1）的化合物。随后我们确定C1对COX - 2和LOX - 1具有抑制活性，IC50值分别为43.10和17.54 µg/mL，使其成为一种有效的抗炎剂。此外，我们发现C1还表现出强大的抗胆碱酯酶活性（86.9 ± 1.21%）。除了这些有前景的治疗特性外，我们的实验表明C1具有很强抗氧化能力，这体现在其清除DPPH、ABTS、O2自由基和NO以及抑制脂质过氧化的能力上。为了进一步研究C1药理特性背后的分子机制，我们使用SwissADME网络工具预测该化合物与ADME相关的物理化学性质，并使用分子操作环境（Molecular Operating Environment）和PyMOL进行分子对接研究。
