Wang Shaoxia, Wang Hong, Jing Haoran, Wang Shixiang, Kang Liyuan, Gao Xiumei, Hu Limin, Zheng Xiaohui
Tianjin Key Laboratory of Chinese Medicine Pharmacology, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, People's Republic of China.
Chin J Physiol. 2012 Dec 31;55(6):428-34. doi: 10.4077/CJP.2011.AMM045.
Down-regulation of microglial activation represents a practical strategy for combating diverse brain disorders such as stroke and neurodegenerative diseases. In the present study, we showed evidence that isopropyl 3-(3, 4-dihydroxyphenyl)-2-hydroxypropanoate (IDHP), a new bioactive metabolite of Danshen (Salvia miltiorrhiza Bunge), exerted an anti-inflammatory effect in lipopolysaccharide (LPS)- induced microglia. Our data showed that IDHP significantly reduced the production of nitric oxide (NO), tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) in LPS-induced BV-2 cells and rat primary microglia in a dose-dependent manner. IDHP also suppressed mRNA expression of LPSinduced inducible nitric oxide synthase (iNOS), TNF-α and IL-1β. Moreover, IDHP significantly suppressed the production of reactive oxygen species (ROS), nuclear factor κB (NF-κB) translocation and DNA binding activity induced by LPS treatment in BV-2 cells. These findings indicated that IDHP might be of value in the treatment of various microglia-mediated neuroinflammatory diseases.
小胶质细胞激活的下调是对抗多种脑部疾病（如中风和神经退行性疾病）的一种切实可行的策略。在本研究中，我们证明了丹参（Salvia miltiorrhiza Bunge）的一种新的生物活性代谢产物3-(3,4-二羟基苯基)-2-羟基丙酸异丙酯（IDHP）在脂多糖（LPS）诱导的小胶质细胞中发挥抗炎作用。我们的数据表明，IDHP以剂量依赖性方式显著降低LPS诱导的BV-2细胞和大鼠原代小胶质细胞中一氧化氮（NO）、肿瘤坏死因子-α（TNF-α）和白细胞介素-1β（IL-1β）的产生。IDHP还抑制LPS诱导的诱导型一氧化氮合酶（iNOS）、TNF-α和IL-1β的mRNA表达。此外，IDHP显著抑制LPS处理诱导的BV-2细胞中活性氧（ROS）的产生、核因子κB（NF-κB）易位和DNA结合活性。这些发现表明，IDHP可能在治疗各种小胶质细胞介导的神经炎症性疾病中具有价值。
