从红树林沉积物来源的微生物中发现生物活性天然产物,对北部湾两种真菌菌株的化学研究,Talaromycessp.SCSIO41050和青霉菌。SCSIO41411,导致23天然产物的分离。其中五个被确定为新的,包括两种具有不寻常酸酐部分的聚酮化合物衍生物,命名为苯甲酸酐A乙酯(1)和马来酸酐(4),和三种羟基苯乙酸衍生物,命名为粗线H-J(10-12)。通过详细的核磁共振(NMR)和质谱(MS)分析确定了它们的结构,而绝对构型是通过理论电子圆二色性(ECD)计算确定的。多种生物活性筛选显示三种聚酮衍生物(1-3)具有明显的抗真菌活性,和4显示对细胞系A549和WPMY-1的中等细胞毒性。化合物1和6在10μM时对磷酸二酯酶4(PDE4)有明显的抑制作用,抑制率分别为49.7%和39.6%,分别,而5、10和11通过酶活性测试显示出抑制乙酰胆碱酯酶(AChE)的潜力,以及硅对接分析。
To discover bioactive natural products from mangrove sediment-derived microbes, a chemical investigation of the two Beibu Gulf-derived fungi strains, Talaromyces sp. SCSIO 41050 and Penicillium 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 (1) and maleicanhydridane (4), and three hydroxyphenylacetic acid derivatives named stachylines H-J (10-12). 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 (1-3) with obvious antifungal activities, and 4 displayed moderate cytotoxicity against cell lines A549 and WPMY-1. Compounds 1 and 6 at 10 μM exhibited obvious inhibition against phosphodiesterase 4 (PDE4) with inhibitory ratios of 49.7% and 39.6%, respectively, while 5, 10, and 11 showed the potential of inhibiting acetylcholinesterase (AChE) by an enzyme activity test, as well as in silico docking analysis.