Institute for Environmental and Climate Research, Jinan University, Guangzhou 511443, China.
CAS Key Laboratory of Tropical Marine Bio-Resources and Ecology, Guangdong Key Laboratory of Marine Materia Medica, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China.
Mar Drugs. 2023 May 26;21(6):327. doi: 10.3390/md21060327.
To discover bioactive natural products from mangrove sediment-derived microbes, a chemical investigation of the two Beibu Gulf-derived fungi strains, sp. SCSIO 41050 and sp. SCSIO 41411, led to the isolation of 23 natural products. Five of them were identified as new ones, including two polyketide derivatives with unusual acid anhydride moieties named cordyanhydride A ethyl ester () and maleicanhydridane (), and three hydroxyphenylacetic acid derivatives named stachylines H-J (-). Their structures were determined by detailed nuclear magnetic resonance (NMR) and mass spectroscopic (MS) analyses, while the absolute configurations were established by theoretical electronic circular dichroism (ECD) calculation. A variety of bioactive screens revealed three polyketide derivatives (-) with obvious antifungal activities, and displayed moderate cytotoxicity against cell lines A549 and WPMY-1. Compounds and at 10 μM exhibited obvious inhibition against phosphodiesterase 4 (PDE4) with inhibitory ratios of 49.7% and 39.6%, respectively, while , , and showed the potential of inhibiting acetylcholinesterase (AChE) by an enzyme activity test, as well as in silico docking analysis.
为了从红树林沉积物来源的微生物中发现具有生物活性的天然产物，对北部湾来源的两株真菌菌株， sp. SCSIO 41050 和 sp. SCSIO 41411 进行了化学研究，分离得到了 23 种天然产物。其中有 5 种被鉴定为新化合物，包括两个具有不寻常酸酐部分的聚酮衍生物，分别命名为 cordyanhydride A 乙酯（）和 maleicanhydridane（），以及三个羟基苯乙酸衍生物，命名为 stachylines H-J（-）。它们的结构通过详细的核磁共振（NMR）和质谱（MS）分析确定，而绝对构型则通过理论电子圆二色性（ECD）计算确定。多种生物活性筛选显示，三种聚酮衍生物（-）具有明显的抗真菌活性，而 对细胞系 A549 和 WPMY-1 表现出中等的细胞毒性。化合物（-）在 10 μM 时对磷酸二酯酶 4（PDE4）表现出明显的抑制作用，抑制率分别为 49.7%和 39.6%，而 、 和 具有抑制乙酰胆碱酯酶（AChE）的潜力，通过酶活性测试以及计算机对接分析得到证实。
