Polyketides with Anti-neuroinflammatory Activity from Theissenia cinerea
Polyketides with Anti-neuroinflammatory Activity from Theissenia cinerea
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DOI：
10.1021/acs.jnatprod.0c01307
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发表时间：
2021-06-29
影响因子：
5.1
通讯作者：
Lee, Tzong-Huei
中科院分区：
文献类型：
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作者：
Hsieh, Meng-Hsuan;Hsiao, George;Lee, Tzong-Huei
灰茶菜(Theissenia Cinerea)89091602是一株先前报道的植物来源的生物活性真菌菌株，从其深层培养物中分离出的活性成分在细胞研究和动物实验中都显示出强大的抗神经炎活性。在我们先前对该真菌生物活性物质的研究的基础上，进行了固态发酵，试图使生物活性次生代谢物多样化。在本研究中，通过光谱分析和与文献数据的比较，分离并鉴定了5个未见报道的多酮化合物，它们分别是异森苯酚(1)、异环氧化物(2)、异千里内酯D(3)、异森酮(4)和异千异色满酮(5)，以及已知的异千里内酯B(6)、异千内酯C(7)和芳香酮(8)。通过单晶X-射线衍射数据分析，进一步证实了异环氧化物(2)和异色满酮(5)的构型。西洋参内酯(4)、西洋参内酯B(6)、西洋参内酯C(7)和芳香草酮(8)对小鼠脑小胶质细胞BV-2具有明显的一氧化氮生成抑制作用，其IC50值分别为5.0+/-1.0、4.5+/-0.6、1.1+/-0.1和3.2+/-0.3 mU，无明显的细胞毒作用。
Theissenia cinerea 89091602 is a previously reported plant-derived bioactive fungal strain, and the active principles separated from the extracts of its submerged culture were shown to exhibit potent anti-neuroinflammatory activities in both cellular study and animal testing. In a continuation of our previous investigation on the bioactive entities from this fungus, solid state fermentation was performed in an attempt to diversify the bioactive secondary metabolites. In the present study, five previously unreported polyketides, theissenophenol (1), theissenepoxide (2), theissenolactone D (3), theissenone (4), and theissenisochromanone (5), together with the known theissenolactone B (6), theissenolactone C (7), and arthrinone (8), were isolated and characterized through spectroscopic analysis and comparison with the literature data. The configurations of theissenepoxide (2) and theissenisochromanone (5) were further corroborated by single-crystal X-ray diffraction data analysis. Theissenone (4), theissenolactone B (6), theissenolactone C (7), and arthrinone (8) exhibited potent nitric oxide production inhibitory activities in murine brain microglial BV-2 cells with IC50 values of 5.0 +/- 1.0, 4.5 +/- 0.6, 1.1 +/- 0.1, and 3.2 +/- 0.3 mu M, respectively, without any significant cytotoxic effects.