Yan Xi-Tao, Chen Jiang-Xian, Wang Zi-Xuan, Zhang Rui-Qi, Xie Jin-Yan, Kou Rong-Wei, Zhou Hui-Fang, Zhang An-Ling, Wang Min-Chang, Ding Yan-Xia, Gao Jin-Ming
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, People's Republic of China.
State Key Laboratory of Fluorine & Nitrogen Chemicals, Xi'an Modern Chemistry Research Institute, Xi'an 710065, People's Republic of China.
J Nat Prod. 2023 Jan 27;86(1):119-130. doi: 10.1021/acs.jnatprod.2c00810. Epub 2022 Dec 29.
Nine new sesquiterpenes, hyperhubeins A-I (-), and 14 known analogues (-) were isolated from the aerial portions of . Their structures and absolute configurations were determined unambiguously via spectroscopic analysis, single-crystal X-ray diffraction, and electronic circular dichroism calculations. Compounds - possess an unprecedented sesquiterpene carbon skeleton. Further, a plausible biosynthetic pathway from farnesyl diphosphate (FPP) is proposed. The isolated phytochemicals were evaluated for neuroprotective and anti-neuroinflammatory properties in vitro. Compounds , , -, , and displayed notable neuroprotective activity against hydrogen peroxide (HO)-induced lesions in PC-12 cells at 10 μM. Additionally, compounds , , , and exhibited inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in BV-2 microglial cells, with their IC values ranging from 4.92 to 6.81 μM. Possible interactions between these bioactive compounds and inducible nitric oxide synthase (iNOS) were predicted via molecular docking. Moreover, Western blotting indicated that compound exerted anti-neuroinflammatory activity by suppressing LPS-stimulated expression of toll-like receptor-4 (TLR-4) and inhibiting consequent activation of nuclear factor-kappa-B (NF-κB) signaling.
从……的地上部分分离出9种新的倍半萜类化合物，即过湖北素A - I（-），以及14种已知类似物（-）。通过光谱分析、单晶X射线衍射和电子圆二色性计算，明确确定了它们的结构和绝对构型。化合物……具有前所未有的倍半萜碳骨架。此外，还提出了一条从法尼基二磷酸（FPP）出发的合理生物合成途径。对分离得到的植物化学物质进行了体外神经保护和抗神经炎症特性评估。化合物……在10 μM浓度下，对过氧化氢（HO）诱导的PC - 12细胞损伤表现出显著的神经保护活性。此外，化合物……在BV - 2小胶质细胞中对脂多糖（LPS）诱导的一氧化氮（NO）产生具有抑制作用，其IC值范围为4.92至6.81 μM。通过分子对接预测了这些生物活性化合物与诱导型一氧化氮合酶（iNOS）之间可能的相互作用。此外，蛋白质印迹法表明化合物……通过抑制LPS刺激的Toll样受体4（TLR - 4）表达并抑制随后的核因子κB（NF - κB）信号通路激活，发挥抗神经炎症活性。
