School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa 519020, Macau, China.
Fitoterapia. 2024 Jun;175:105967. doi: 10.1016/j.fitote.2024.105967. Epub 2024 Apr 16.
Sulfur-containing natural products possess a variety of biological functions including antitumor, antibacterial, anti-inflammatory and antiviral activities. In this study, four previously undescribed sulfur-containing compounds asperteretals L and M, terreins A and B, together with 17 known compounds were obtained from a culture of marine fungus A. terreus supplemented with inorganic sulfur source NaSO. Their planar structures and absolute configurations were elucidated by NMR, HRESIMS, and ECD experiments. The in vitro cytotoxicities of compounds 1-21 against HCT-116 and Caco-2 were evaluated by SRB assay. Asperteretal M (2) exhibited activity against HCT-116 with the IC value at 30μM. The antiproliferative effect of asperteretal M was confirmed by colony formation assay and cell death staining. Furthermore, the preliminary study on the anti-colon cancer mechanism of asperteretal M was performed by RNA-seq analysis. Western blotting validated that asperteretal M significantly decreased the expression of cell-cycle regulatory proteins CDK1, CDK4, and PCNA in a concentration-dependent manner.
含硫天然产物具有多种生物功能，包括抗肿瘤、抗菌、抗炎和抗病毒活性。在本研究中，从海洋真菌 A. terreus 的培养物中获得了四种以前未描述的含硫化合物 Asperteretals L 和 M、 Terreins A 和 B，以及 17 种已知化合物，这些化合物是在添加无机硫源 NaSO 的情况下产生的。通过 NMR、HRESIMS 和 ECD 实验阐明了它们的平面结构和绝对构型。通过 SRB 测定法评估了化合物 1-21 对 HCT-116 和 Caco-2 的体外细胞毒性。Asperteretal M（2）对 HCT-116 表现出活性，IC 值为 30μM。Asperteretal M 的抗增殖作用通过集落形成测定和细胞死亡染色得到证实。此外，通过 RNA-seq 分析对 Asperteretal M 的抗结肠癌机制进行了初步研究。Western blotting 验证了 Asperteretal M 显著降低了细胞周期调节蛋白 CDK1、CDK4 和 PCNA 的表达，呈浓度依赖性。
