Guo Fei-Fei, Tang Xuan, Tang Li-Ying, Wei Jun-Ying, Xiao Jun-Ping, Yang Hong-Jun
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China.
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China Tianjin University of Traditional Chinese Medicine Tianjin 301617, China.
Zhongguo Zhong Yao Za Zhi. 2020 Apr;45(8):1800-1807. doi: 10.19540/j.cnki.cjcmm.20200107.401.
The difference in pharmacological activities and active components between leaves, barks and flowers of Eucommia ulmoides(EU) are still unclear. However, clarifying the differences in pharmacological effects of different parts of EU is of great significance for the development of EU products, and their corresponding active components provide basis for quality control of different parts of EU. Based on the chemical compositions of different parts of EU, integrated strategy of target prediction and target analysis of the compounds was used to investigate the difference in the pharmacological effects of leaves, barks and followers. The "component-target-function" association network was constructed to mine the specific material basis corresponding to specific efficacy of different parts of EU. In this study, the author found that EU may have the activities of anti-oxidation, neuromodulation, blood pressure regulation, myo-cardial expansion, and anti-apoptosis according to target prediction and function analysis. However, the effects of different parts of EU were different. Leaves were involved in the process of bone development such as osteoblast differentiation and bone mineralization in a specific way. In addition, the leaves may affect the process of bone development by regulating the metabolism of vitamin D and affecting the absorption of calcium. Leaves may also specifically act on estrogen and estradiol response processes where estrogen receptors were involved. Regarding its protective function for the liver, leaves may play a role by regulating vitamin A-related pathways. As compared with leaves, the specific pharmacological effects of barks may be related to the development of the urinary system. Flowers specifically participate in functions related to pain sensation, glutamate signaling pathway, and excitatory postsynaptic potential. Based on the hie-rarchical network of "component-target-pathway", we further found that specific activities of different parts of EU were inseparable from its specific chemical compositions. Phenylpropanoids, terpenoids and rings, iridoids, flavonoids and other components which are specific in leaves can target the specific effects of leaves, while the flavonoids in barks and the quinones in flowers may be the material basis for their respective specific effects. The prediction of the activities of different parts of EU provides a new basis for the focuses and differences in subsequent Eucommia product development. At the same time, the material basis research based on differential efficacy also provides a basis for the quality control of Eucommia differentiated products.
杜仲叶、皮和花的药理活性及活性成分差异尚不清楚。然而,明确杜仲不同部位的药理作用差异对杜仲产品的开发具有重要意义,其相应的活性成分可为杜仲不同部位的质量控制提供依据。基于杜仲不同部位的化学成分,采用化合物靶点预测与靶点分析的整合策略,研究杜仲叶、皮和花的药理作用差异。构建“成分-靶点-功能”关联网络,挖掘杜仲不同部位特定功效对应的具体物质基础。在本研究中,作者通过靶点预测和功能分析发现,杜仲可能具有抗氧化、神经调节、血压调节、心肌扩张和抗凋亡等活性。然而,杜仲不同部位的作用效果有所不同。杜仲叶以特定方式参与成骨细胞分化和骨矿化等骨骼发育过程。此外,叶可能通过调节维生素D代谢和影响钙吸收来影响骨骼发育过程。叶还可能特异性作用于涉及雌激素受体的雌激素和雌二醇反应过程。关于其对肝脏的保护作用,叶可能通过调节维生素A相关途径发挥作用。与叶相比,杜仲皮的特定药理作用可能与泌尿系统发育有关。花则特异性参与与痛觉、谷氨酸信号通路和兴奋性突触后电位相关的功能。基于“成分-靶点-通路”层次网络,我们进一步发现杜仲不同部位的特定活性与其特定化学成分密不可分。叶中特有的苯丙素类、萜类和环烯醚萜类、黄酮类等成分可靶向叶的特定作用,而皮中的黄酮类和花中的醌类可能是其各自特定作用的物质基础。杜仲不同部位活性的预测为后续杜仲产品开发的重点和差异提供了新依据。同时,基于差异药效的物质基础研究也为杜仲差异化产品的质量控制提供了依据。