Thiohydantoin and Hydantoin Derivatives from the Roots of Armoracia rusticana and Their Neurotrophic and Anti-neuroinflammatory Activities.,Journal of Natural Products

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Thiohydantoin and Hydantoin Derivatives from the Roots of Armoracia rusticana and Their Neurotrophic and Anti-neuroinflammatory Activities.
Journal of Natural Products ( IF 3.3 ) Pub Date : 2019-10-18 , DOI: 10.1021/acs.jnatprod.9b00527
Tae Hyun Lee ₁ , Zahra Khan _{2,

3} , Sun Yeou Kim _{2,

3} , Kang Ro Lee ₁

Affiliation

Two new thiohydantoins (1 and 3) and three new hydantoins (2, 4, and 5) along with three known compounds (6-8) were isolated from roots of horseradish. Physical data analysis including NMR (1H and 13C NMR, 1H-1H COSY, HSQC, and HMBC), HRESIMS, and ECD were employed for structure elucidation of the new compounds 1-5. Potential neuroprotective effects of all compounds (1-8) on nerve growth factor (NGF) induction in C6 glioma were also evaluated. Among these compounds, 1b and 2a exhibited potent NGF secretion stimulation activities (NGF secretion levels: 153.59 ± 5.44% and 141.99 ± 5.21%, respectively). Their anti-neuroinflammatory activities were also assessed based on their inhibitory effects on nitric oxide (NO) production in lipopolysaccharide-stimulated murine microglia. Compound 7 marginally inhibited NO production with an IC50 value of 32.6 μM.

中文翻译：

乡村结缕草根中的硫代乙内酰脲和乙内酰脲衍生物及其神经营养和抗神经炎活性。

从辣根中分离出两个新的硫代乙内酰脲（1和3）和三个新的乙内酰脲（2、4和5）以及三个已知的化合物（6-8）。物理数据分析包括NMR（1H和13C NMR，1H-1H COSY，HSQC和HMBC），HRESIMS和ECD用于阐明新化合物1-5。还评估了所有化合物（1-8）对C6胶质瘤中神经生长因子（NGF）诱导的潜在神经保护作用。在这些化合物中，1b和2a表现出有效的NGF分泌刺激活性（NGF分泌水平：分别为153.59±5.44％和141.99±5.21％）。还基于它们对脂多糖刺激的鼠小胶质细胞中一氧化氮（NO）产生的抑制作用，评估了它们的抗神经炎活性。化合物7以32.6μM的IC50值略微抑制了NO的产生。

更新日期：2019-10-19

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