Division of Stem Cell Regulation and Application, Key Laboratory for Quality Evaluation of Bulk Herbs of Hunan Province, Hunan University of Chinese Medicine, Changsha 410208, Hunan, China.
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
Pharmacol Res. 2018 Oct;136:172-180. doi: 10.1016/j.phrs.2018.09.002. Epub 2018 Sep 6.
Artemisinin (Qinghaosu) and its semi-synthetic derivatives have been demonstrated to alleviate neuroinflammatory response in the central nerve system (CNS). In this review, we summarized that artemisinins are capable to treat neuroinflammtion-related CNS diseases in both direct (via regulating inflammatory process in the CNS, exerting anti-oxidative stress and neuroprotective effect, and preventing Aβ accumulation) and indirect (via maintaining BBB integrity, suppressing systemic inflammation and alleviating intestinal inflammtion) manner. However, the precise mechanism of their anti-neuroinflammatory effects and potential neurotoxicity, which hindered further progress in these aspects, remains unclear. We suggest that further understanding of the PK/PD properties and structure-action relationship of atemisinin and its derivatives will facilitate the development of new therapeutics with better curative effects and safety.
青蒿素（qinghaosu）及其半合成衍生物已被证明可减轻中枢神经系统（CNS）中的神经炎症反应。在这篇综述中，我们总结了青蒿素类药物能够通过直接（通过调节中枢神经系统中的炎症过程、发挥抗氧化应激和神经保护作用以及防止 Aβ 积累）和间接（通过维持 BBB 完整性、抑制全身炎症和缓解肠道炎症）方式治疗与神经炎症相关的 CNS 疾病。然而，其抗炎作用的确切机制以及潜在的神经毒性，这阻碍了这些方面的进一步进展，目前尚不清楚。我们建议，进一步了解青蒿素及其衍生物的药代动力学/药效学特性和构效关系将有助于开发具有更好疗效和安全性的新型治疗药物。
