| Monoterpenoid indole alkaloid dimers from Kopsia arborea inhibit cyclin-dependent kinase 5 and tau phosphorylation |
| Chen, C; Liu, JW; Guo, LL; Xiong, F; Ran, XQ; Guo, YR; Yao, YG ; Hao, XJ; Luo, RC; Zhang, Y
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| 2022
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| 发表期刊 | PHYTOCHEMISTRY
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| ISSN | 0031-9422
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| 卷号 | 203 |
| 摘要 | Three undescribed monoterpenoid indole alkaloid dimers (kopoffines A-C, which are connected via a methylene unit) and with nine known alkaloids were isolated and identified from the fruits of Kopsia arborea Blume. Their structures, including their absolute configurations, were established by HRESIMS, NMR, single-crystal X-ray diffraction, and ECD analyses. Kopoffines A-C showed significant inhibition against cyclin-dependent kinase 5 (IC50: 0.34-2.18 mu M). Western blotting analyses showed that kopoffines A-C significantly decreased the protein levels of CDK5 and phospho-CDK5 (Tyr15) (pCDK5) at concentrations of 2.5 and 10 mu M. The levels of phospho-Tau (Thr217) (pTau217, a new biomarker of AD), and phospho-Tau (Ser396) (pTau396), which play major roles in the formation of neurofibrillary tangles , were decreased by the kopoffines A-C treatment. Molecular docking studies indicated that kopoffines A-C could form stable interactions with CDK5. |
| 收录类别 | sci
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| 语种 | 英语
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| 文献类型 | 期刊论文
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| 条目标识符 | http://ir.kiz.ac.cn/handle/152453/13497
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| 专题 | 科研部门_疾病机理遗传学和进化医学学科组（姚永刚）
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推荐引用方式
GB/T 7714 |
Chen, C,Liu, JW,Guo, LL,et al. Monoterpenoid indole alkaloid dimers from Kopsia arborea inhibit cyclin-dependent kinase 5 and tau phosphorylation[J]. PHYTOCHEMISTRY,2022,203.
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| APA |
Chen, C.,Liu, JW.,Guo, LL.,Xiong, F.,Ran, XQ.,...&Zhang, Y.(2022).Monoterpenoid indole alkaloid dimers from Kopsia arborea inhibit cyclin-dependent kinase 5 and tau phosphorylation.PHYTOCHEMISTRY,203.
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| MLA |
Chen, C,et al."Monoterpenoid indole alkaloid dimers from Kopsia arborea inhibit cyclin-dependent kinase 5 and tau phosphorylation".PHYTOCHEMISTRY 203(2022).
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