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中国民间草药粗毛鳞盖蕨中的罕见苯并萘并氧杂蒽酮及其体外抗神经炎症活性。

Rare benzonaphthoxanthenones from Chinese folk herbal medicine Polytrichum commune and their anti-neuroinflammatory activities in vitro.

机构信息

School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.

School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, PR China.

出版信息

Bioorg Chem. 2020 Sep;102:104087. doi: 10.1016/j.bioorg.2020.104087. Epub 2020 Jul 10.

Abstract

Two new (1-2) as well as five known (3-7) compounds were isolated from Polytrichum commune, a folk herbal medicine in China, and three of them (2, 4, 5) belong to benzonaphthoxanthenones that are rarely found in nature. Their structures were elucidated by the approach to 1D and 2D NMR spectra. The absolute configuration of 2 was assigned by comparing its experimental and calculated ECD data. 1-5 were investigated for their anti-neuroinflammatory activity against LPS-induced BV-2 cells. 1 and 3 exhibited well protective effect at a concentration of 2.5 μmol/mL. Molecular docking studies were adopted to further investigate the possible mechanism, whose results suggested that 1 might exert anti-neuroinflammatory effect by inhibiting activity of p38α, JNK2 and TAK1 to reduce the liberation of pro-inflammatory cytokines.

摘要

从中国民间草药金发藓中分离得到两个新的(1-2)和五个已知的(3-7)化合物,其中三个(2、4、5)属于苯并萘并氧杂蒽酮类化合物,在自然界中很少见。通过对 1D 和 2D NMR 谱的研究,阐明了它们的结构。通过比较实验和计算的 ECD 数据,确定了 2 的绝对构型。研究了 1-5 对 LPS 诱导的 BV-2 细胞的抗炎活性。在 2.5μmol/mL 的浓度下,1 和 3 表现出很好的保护作用。采用分子对接研究进一步探讨了可能的机制,结果表明,1 可能通过抑制 p38α、JNK2 和 TAK1 的活性来减少促炎细胞因子的释放,从而发挥抗炎作用。

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