Natural potential neuroinflammatory inhibitors from Alhagi sparsifolia Shap
Natural potential neuroinflammatory inhibitors from Alhagi sparsifolia Shap
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来自 Alhagi sparsifolia Shap 的天然潜在神经炎症抑制剂。
DOI：
10.1016/j.bmcl.2016.12.075
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发表时间：
2017-02-15
影响因子：
2.7
通讯作者：
Li, Ning
中科院分区：
文献类型：
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作者：
Zhou, Di;Wei, Hongyan;Li, Ning
神经炎症是神经退行性疾病中神经元损伤的关键因素。在我们之前关于天然有效的神经炎症抑制剂的研究中，广泛分布于新疆的民间药材骆驼刺（豆科）因其显著的抗神经炎症作用引起了我们的关注。因此，我们对其生物活性物质基础进行了进一步研究。结果，通过色谱和光谱方法分别对33种主要成分进行了表征和鉴定。此外，在脂多糖诱导的N9细胞体外实验中评估了提取物和纯化成分的抗神经炎症作用。结果显示，化合物1、2、3、5、6、8、11、15、16、17、22、23、25、26、28、30、33在其有效浓度下可表现出显著的抑制活性，且无明显细胞毒性。特别是，异鼠李素（1）（半数抑制浓度为17.87μM）、槲皮素（2）（10.22μM）、3',7 - 二羟基 - 4' - 甲氧基异黄酮（5）（17.43μM）、3',7 - 二羟基 - 4',6 - 二甲氧基异黄酮（6）（11.21μM）、丁香脂素（16）（2.68μM）、博马辛醇A（17）（7.61μM）、橙黄胡椒酰胺（23）（14.91μM）和1,3,3,4 - 四甲基环戊烯（33）（2.63μM）显示出比阳性对照米诺环素（19.89μM）更强的抑制作用。因此，这些有效成分可能是该草药表现出显著的神经炎症抑制活性的原因。此外，化合物16和33可能是开发针对神经退行性疾病的潜在治疗药物的良好先导化合物。（C）2017爱思唯尔有限公司。保留所有权利。
Neuroinflammation is a key contributor to neuronal damage in neurodegenerative diseases. In our previous work on natural effective neuroinflammatory inhibitors, Alhagi sparsifolia Shap. (Leguminosae), a folk medicine widely distributed in Xinjiang, attracted our attention because of its significant anti-neuroinflammatory effect. Therefore, further investigation of the bioactive material basis was carried out. As a result, 33 major components were characterized and identified by chromatographic and spectral methods, respectively. Furthermore, the anti-neuroinflammatory effects of the extract and purified constituents were evaluated in LPS-induced N9 cells in vitro. The results displayed that compounds 1, 2, 3, 5, 6, 8, 11, 15, 16, 17, 22, 23, 25, 26, 28, 30, 33 could exhibit significant inhibitory activities without obvious cytotoxicities at their effective concentrations. Especially, isorhamnetin (1) (IC50 17.87 mu M), quercetin (2) (10.22 mu M), 3',7-dihydroxyl-4'-methoxylisoflavone (5) (17.43 mu M), 3',7-dihydroxy1-4',-6dimethoxylisoflavone (6) (11.21 mu M), syringgaresinol (16) (2.68 mu M), bombasinol A (17) (7.61 mu M), aurantiamide (23) (14.91 mu M) and 1,3,3,4-tetramethyl cyclopentene (33) (2.63 mu M) showed much stronger inhibiting effect than that of the positive control minocycline (19.89 mu M). Therefore, the effective compositions might be responsible for the significant neuroinflammation inhibitory activities exhibited by the herb. Moreover, compounds 16 and 33 could be good leading compounds for the development of potential therapeutic agents against neurodegenerative diseases. (C) 2017 Elsevier Ltd. All rights reserved.