Son So-Ri, Ju In Gyong, Kim Jinhee, Park Keon-Tae, Oh Myung Sook, Jang Dae Sik
Department of Biomedical and Pharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, Korea.
Department of Oriental Pharmaceutical Science, College of Pharmacy and Kyung Hee East-West Pharmaceutical Research Institute, Kyung Hee University, Seoul 02447, Korea.
Plants (Basel). 2022 Jul 27;11(15):1954. doi: 10.3390/plants11151954.
Neuroinflammation, predominantly mediated by microglial activation, is a key immunological response in the pathogenesis of neurodegenerative disorders. In our preliminary study, the aerial part of inhibits LPS-induced microglial activation. The present study aims to identify chemical constituents with anti-neuroinflammatory properties in the aerial parts of . . Two new guaianolide sesquiterpenes, iwayomogins A and B ( and ), along with thirteen known sesquiterpene lactones (-), one diterpene glycoside (), and nine phenolic compounds (-) were isolated from the aerial parts of . by repeated chromatography. The structures of the isolates were elucidated by their spectroscopic data. All isolates were evaluated for their inhibitory activities on nitric oxide (NO) production in LPS-induced BV-2 microglial cells. 2,3-Dehydro-1--asperilin () exhibited the strongest inhibitory effect on NO production (IC value of 1.78 μM). In the molecular docking study, three compounds (, , and ) showed good binding affinities with iNOS. Additionally, compounds , , and inhibit pro-inflammatory cytokines (TNF-α and IL-6) in dose-dependent manners. The present study demonstrates that the chemical constituents from . inhibit NO production and pro-inflammatory cytokine release in BV-2 cells. However, further evaluation with biological experiments utilizing in vivo models is necessary.
神经炎症主要由小胶质细胞激活介导，是神经退行性疾病发病机制中的关键免疫反应。在我们的初步研究中，[植物名称]的地上部分可抑制脂多糖诱导的小胶质细胞激活。本研究旨在鉴定[植物名称]地上部分具有抗神经炎症特性的化学成分。通过反复色谱法从[植物名称]的地上部分分离得到了两种新的愈创木烷型倍半萜，即岩木香内酯A和B（[具体化学式1]和[具体化学式2]），以及13种已知的倍半萜内酯（[具体化合物1] - [具体化合物13]）、1种二萜糖苷（[具体化合物14]）和9种酚类化合物（[具体化合物15] - [具体化合物23]）。通过光谱数据阐明了分离物的结构。评估了所有分离物对脂多糖诱导的BV - 2小胶质细胞中一氧化氮（NO）产生的抑制活性。2,3 - 脱氢 - 1 - [具体基团] - 曲霉红素（[具体化学式3]）对NO产生表现出最强的抑制作用（IC值为1.78 μM）。在分子对接研究中，三种化合物（[具体化合物4]、[具体化合物5]和[具体化合物6]）与诱导型一氧化氮合酶（iNOS）显示出良好的结合亲和力。此外，化合物[具体化合物7]、[具体化合物8]和[具体化合物9]以剂量依赖方式抑制促炎细胞因子（肿瘤坏死因子 - α和白细胞介素 - 6）。本研究表明，[植物名称]的化学成分可抑制BV - 2细胞中NO的产生和促炎细胞因子的释放。然而，有必要利用体内模型进行进一步的生物学实验评估。
