An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection
Abstract Traditional Chinese medicine (TCM) treatment can be valuable therapeutic strategies. However, the active components and action mechanisms that account for its therapeutic effects remain elusive. Based on the hypothesis that the components of a formula which exert effect would be measurable...
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Nature Portfolio
2017
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oai:doaj.org-article:36c9b9030ea84df0b4f1d2160ba861132021-12-02T15:05:41ZAn integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection10.1038/s41598-017-05812-02045-2322https://doaj.org/article/36c9b9030ea84df0b4f1d2160ba861132017-07-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-05812-0https://doaj.org/toc/2045-2322Abstract Traditional Chinese medicine (TCM) treatment can be valuable therapeutic strategies. However, the active components and action mechanisms that account for its therapeutic effects remain elusive. Based on the hypothesis that the components of a formula which exert effect would be measurable in target tissue, a target tissue metabolomics-based strategy was proposed for screening of antipyretic components in Qingkaikling injection (QKLI). First, we detected the components of QKLI which could reach its target tissue (hypothalamus) by determining the hypothalamus microdialysate and discovered that only baicalin and geniposide could be detected. Then, by conducting hypothalamus metabolomics studies, 14 metabolites were screened as the potential biomarkers that related to the antipyretic mechanisms of QKLI and were used as its pharmacodynamic surrogate indices. Subsequently, the dynamic concentration of baicalin and geniposide in hypothalamus microdialysates and biomarkers in hypothalamus were measured and correlated with each other. The results indicated that only baicalin shown a good correlation with these biomarkers. Finally, a network pharmacology approach was established to validate the antipyretic activity of baicalin and the results elucidated its antipyretic mechanisms as well. The integrated strategy proposed here provided a powerful means for identifying active components and mechanisms contributing to pharmacological effects of TCM.Zhixin ZhangFang LuHaiyu LiuHuizhen ZhaoYuehong LiuShuang FuMeiling WangZiye XieHonghong YuZhenghai HuangYanling ZhangXiaoyan GaoNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-12 (2017) |
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Medicine R Science Q Zhixin Zhang Fang Lu Haiyu Liu Huizhen Zhao Yuehong Liu Shuang Fu Meiling Wang Ziye Xie Honghong Yu Zhenghai Huang Yanling Zhang Xiaoyan Gao An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection |
| description |
Abstract Traditional Chinese medicine (TCM) treatment can be valuable therapeutic strategies. However, the active components and action mechanisms that account for its therapeutic effects remain elusive. Based on the hypothesis that the components of a formula which exert effect would be measurable in target tissue, a target tissue metabolomics-based strategy was proposed for screening of antipyretic components in Qingkaikling injection (QKLI). First, we detected the components of QKLI which could reach its target tissue (hypothalamus) by determining the hypothalamus microdialysate and discovered that only baicalin and geniposide could be detected. Then, by conducting hypothalamus metabolomics studies, 14 metabolites were screened as the potential biomarkers that related to the antipyretic mechanisms of QKLI and were used as its pharmacodynamic surrogate indices. Subsequently, the dynamic concentration of baicalin and geniposide in hypothalamus microdialysates and biomarkers in hypothalamus were measured and correlated with each other. The results indicated that only baicalin shown a good correlation with these biomarkers. Finally, a network pharmacology approach was established to validate the antipyretic activity of baicalin and the results elucidated its antipyretic mechanisms as well. The integrated strategy proposed here provided a powerful means for identifying active components and mechanisms contributing to pharmacological effects of TCM. |
| format |
article |
| author |
Zhixin Zhang Fang Lu Haiyu Liu Huizhen Zhao Yuehong Liu Shuang Fu Meiling Wang Ziye Xie Honghong Yu Zhenghai Huang Yanling Zhang Xiaoyan Gao |
| author_facet |
Zhixin Zhang Fang Lu Haiyu Liu Huizhen Zhao Yuehong Liu Shuang Fu Meiling Wang Ziye Xie Honghong Yu Zhenghai Huang Yanling Zhang Xiaoyan Gao |
| author_sort |
Zhixin Zhang |
| title |
An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection |
| title_short |
An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection |
| title_full |
An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection |
| title_fullStr |
An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection |
| title_full_unstemmed |
An integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of Qingkaikling injection |
| title_sort |
integrated strategy by using target tissue metabolomics biomarkers as pharmacodynamic surrogate indices to screen antipyretic components of qingkaikling injection |
| publisher |
Nature Portfolio |
| publishDate |
2017 |
| url |
https://doaj.org/article/36c9b9030ea84df0b4f1d2160ba86113 |
| work_keys_str_mv |
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