Mohamed Sayed H A, Mahmoud Yehia A-G, Bediway Mohamed Y, Elsilk Sobhy E, Yosri Mohammed, Metwally Kamel, Abo-Dya Nader E, Yahya Galal, Almostafa Mervt, El-Hela Atef A
Botany and Microbiology Department, Faculty of Science, Tanta University, Tanta 31527, Egypt.
The Regional Center for Mycology and Biotechnology, Al-Azhar University, Nasr City, Cairo 11787, Egypt.
Molecules. 2025 Sep 8;30(17):3650. doi: 10.3390/molecules30173650.
Fungi are a prolific source of diverse bioactive metabolites, yet many remain unexplored. Among these, depsidones are a rare class of compounds with significant biological potential, but they are seldom reported in mushrooms. This study investigated the medicinal fungus , known for its extensive therapeutic use in traditional medicine. Fruiting bodies were extracted using petroleum ether, ethyl acetate, n-butanol, and methanol. Extracts were screened phytochemically and assessed for total phenolic content and antioxidant activity using the DPPH assay. Ethyl acetate extract exhibited the highest phenolic yield and antioxidant potential and was subsequently evaluated for cytotoxicity against HepG2, HCT116, MCF7, and A549 cancer cell lines. It showed notable anticancer activity with minimal toxicity to normal Vero cells. UHPLC/Q-TOF-MS/MS analysis of ethyl acetate extract tentatively identified nine minor depsidones including mollicellin G, simplicildone I, mollicellin B, talaromyone B, simplicildone A, purpactin C, emeguisin B, mollicellin E, and simplicildone D on the basis of high-resolution negative-mode detection and characteristic MS/MS fragmentation patterns. Molecular docking revealed strong binding affinities between these compounds and cancer-related targets (AKT1, CDK2, ERK1, TNFα), with simplicildone D and mollicellin G demonstrating particularly high interactions. These findings provide mechanistic insights into the observed bioactivity and highlight as a promising source of therapeutic depsidones for future anticancer drug development.
真菌是多种生物活性代谢物的丰富来源，但许多仍未被探索。其中，缩酚酸酮是一类具有重要生物学潜力的稀有化合物，但在蘑菇中很少被报道。本研究调查了这种在传统医学中具有广泛治疗用途的药用真菌。子实体用石油醚、乙酸乙酯、正丁醇和甲醇进行提取。对提取物进行植物化学筛选，并使用DPPH法评估总酚含量和抗氧化活性。乙酸乙酯提取物表现出最高的酚类产量和抗氧化潜力，随后对其针对HepG2、HCT116、MCF7和A549癌细胞系的细胞毒性进行评估。它显示出显著的抗癌活性，对正常Vero细胞的毒性最小。基于高分辨率负离子模式检测和特征性MS/MS裂解模式，对乙酸乙酯提取物进行的超高效液相色谱/四极杆飞行时间串联质谱分析初步鉴定出九种次要缩酚酸酮，包括莫利塞林G、单环缩酚酸酮I、莫利塞林B、塔拉霉素B、单环缩酚酸酮A、紫菌素C、埃梅吉辛B、莫利塞林E和单环缩酚酸酮D。分子对接揭示了这些化合物与癌症相关靶点（AKT1、CDK2、ERK1、TNFα）之间有很强的结合亲和力，其中单环缩酚酸酮D和莫利塞林G表现出特别高的相互作用。这些发现为观察到的生物活性提供了机制见解，并突出了该真菌作为未来抗癌药物开发中有前景的治疗性缩酚酸酮来源。
