二氢青蒿素-香豆素杂合体的设计、合成及作为潜在的抗神经炎症药物的机制研究。
Design, Synthesis, and Mechanism of Dihydroartemisinin⁻Coumarin Hybrids as Potential Anti-Neuroinflammatory Agents.
机构信息
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China.
School of life sciences and biological pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
出版信息
Molecules. 2019 Apr 28;24(9):1672. doi: 10.3390/molecules24091672.
Cancer patients frequently suffer from cancer-related fatigue (CRF), which is a complex syndrome associated with weakness and depressed mood. Neuroinflammation is one of the major inducers of CRF. The aim of this study is to find a potential agent not only on the treatment of cancer, but also for reducing CRF level of cancer patients. In this study, total-thirty new Dihydroartemisinin-Coumarin hybrids (DCH) were designed and synthesized. The in vitro cytotoxicity against cancer cell lines (HT-29, MDA-MB-231, HCT-116, and A549) was evaluated. Simultaneously, we also tested the anti-neuroinflammatory activity of DCH. DCH could inhibit the activated microglia N9 release of NO, TNF-α, and IL-6. The docking analysis was shown that MD-2, the coreceptor of TLR4, might be one of the targets of DCH.
癌症患者经常患有与癌症相关的疲劳（CRF），这是一种与虚弱和情绪低落有关的复杂综合征。神经炎症是 CRF 的主要诱因之一。本研究旨在寻找一种不仅能治疗癌症，而且能降低癌症患者 CRF 水平的潜在药物。在这项研究中，总共设计并合成了 30 种新型青蒿素-香豆素杂合化合物（DCH）。评估了它们对癌细胞系（HT-29、MDA-MB-231、HCT-116 和 A549）的体外细胞毒性。同时，我们还测试了 DCH 的抗神经炎症活性。DCH 可以抑制激活的小胶质细胞 N9 释放的 NO、TNF-α 和 IL-6。对接分析表明，TLR4 的核心受体 MD-2 可能是 DCH 的靶标之一。
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