Central and peripheral analgesic active components of triterpenoid saponins from Stauntonia chinensis and their action mechanism

木瓜三萜皂苷的中枢及外周镇痛活性成分及其作用机制

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作者:Ji-Hong Gong #, Chang-Ming Zhang #, Bo Wu #, Zi-Xun Zhang, Zhong-Yan Zhou, Jia-Hui Zhu, Han Liu, Yi Rong, Qian Yin, Ya-Ting Chen, Rong Zheng, Guang-Zhong Yang, Xiao-Fei Yang, Su Chen

Abstract

Triterpenoid saponins from Stauntonia chinensis have been proven to be a potential candidate for inflammatory pain relief. Our pharmacological studies confirmed that the analgesic role of triterpenoid saponins from S. chinensis occurred via a particular increase in the inhibitory synaptic response in the cortex at resting state and the modulation of the capsaicin receptor. However, its analgesic active components and whether its analgesic mechanism are limited to this are not clear. In order to further determine its active components and analgesic mechanism, we used the patch clamp technique to screen the chemical components that can increase inhibitory synaptic response and antagonize transient receptor potential vanilloid 1, and then used in vivo animal experiments to evaluate the analgesic effect of the selected chemical components. Finally, we used the patch clamp technique and molecular biology technology to study the analgesic mechanism of the selected chemical components. The results showed that triterpenoid saponins from S. chinensis could enhance the inhibitory synaptic effect and antagonize the transient receptor potential vanilloid 1 through different chemical components, and produce central and peripheral analgesic effects. The above results fully reflect that "traditional Chinese medicine has multi-component, multi-target, and multi-channel synergistic regulation".

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