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Design, Synthesis, and Mechanism of Dihydroartemisinin?Coumarin Hybrids as Potential Anti-Neuroinflammatory Agents.

ABSTRACT: 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-?, and IL-6. The docking analysis was shown that MD-2, the coreceptor of TLR4, might be one of the targets of DCH.

SUBMITTER: Yu H

PROVIDER: S-EPMC6539525 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Mechanism of Dihydroartemisinin⁻Coumarin Hybrids as Potential Anti-Neuroinflammatory Agents.

Yu Haonan H Hou Zhuang Z Yang Xiaoguang X Mou Yanhua Y Guo Chun C

Molecules (Basel, Switzerland) 20190428 9

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 ...[more]

PMID: 31035404

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