Wang Yang-Chen, Geng Ruo-Yu, Yang Jian-Hua, Ma Chong, Dai Wu, Guo Ya-Li, Zhang Han-Teng, Xu Zi-Xuan, Li Xin-Yue, Ma Xin-Xin, Hu Jun-Ping, Wen Li-Mei
School of Clinical Medicine, Xinjiang Medical University Urumqi 830017, China.
College of Pharmacy,Xinjiang Medical University Urumqi 830017, China Xinjiang Key Laboratory of Clinical Drug Research Urumqi 830011, China.
Zhongguo Zhong Yao Za Zhi. 2024 Sep;49(17):4607-4616. doi: 10.19540/j.cnki.cjcmm.20240516.701.
This study aims to investigate the therapeutic effect and mechanism of Panax notoginseng saponins(PNS) on diabetic kidney disease(DKD) based on network pharmacology, molecular docking, animal experiments. Network pharmacology was employed to screen the potential targets, and STRING was employed to build the protein-protein interaction network. Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) enrichment analyses were carried out for the core targets screened out, and a ″components-targets-pathways″ visualization network was constructed to predict the potential mechanism of PNS in treating DKD. Five active ingredients were screened from PNS, the core targets of which for treating DKD were AKT1, STAT3, ESR1, HSP90AA1, MTOR, et al. The KEGG enrichment analysis showed that the pathways related to PNS for treating DKD included the pathway in cancer, chemical carcinogenesis-receptor activation, and PI3K-AKT signaling pathway. GO analysis revealed that protein binding, homologous protein binding, enzyme binding, and ATP binding were the main biological processes involved in the treatment of DKD with PNS. Male 6-week-old db/db mice were randomized into model, dapagliflozin, and low-dose and high-dose PNS groups, with 10 mice in each group. Ten 6-week-old db/m mice were used as the control group. Mice were administrated with corresponding drugs or distilled water(control and model groups) by gavage once a day for 8 weeks. The body weight, fasting blood glucose, kidney index, microalbuminuria, creatinine, microalbuminuria/creatinine ratio, and urea nitrogen content in the urine of mice were determined. Hematoxylin-eosin(HE) staining, periodic acid-Schiff(PAS) staining, and Masson staining were performed to observe the protective effect of PNS on the renal tissues in db/db mice. The results showed that PNS could significantly reduce the fasting blood glucose level and improve the renal damage in db/db mice. Western blot results showed that PNS down-regulated the protein levels of p-AKT1 and p-STAT3 and decreased the p-AKT1/AKT1 and p-STAT3/STAT3 ratios. In addition, high-dose PNS down-regulated the protein level of PIK3CA. In conclusion, PNS may exert the kidney-protecting effects in DKD by inhibiting STAT3 via the PI3K-AKT signaling pathway.
本研究旨在基于网络药理学、分子对接、动物实验探讨三七总皂苷(PNS)对糖尿病肾病(DKD)的治疗作用及机制。采用网络药理学筛选潜在靶点,利用STRING构建蛋白质-蛋白质相互作用网络。对筛选出的核心靶点进行基因本体论(GO)和京都基因与基因组百科全书(KEGG)富集分析,并构建“成分-靶点-通路”可视化网络以预测PNS治疗DKD的潜在机制。从PNS中筛选出5种活性成分,其治疗DKD的核心靶点有AKT1、STAT3、ESR1、HSP90AA1、MTOR等。KEGG富集分析表明,PNS治疗DKD的相关通路包括癌症通路、化学致癌作用-受体激活以及PI3K-AKT信号通路。GO分析显示,蛋白质结合、同源蛋白质结合、酶结合和ATP结合是PNS治疗DKD涉及的主要生物学过程。将6周龄雄性db/db小鼠随机分为模型组、达格列净组、低剂量和高剂量PNS组,每组10只。选取10只6周龄db/m小鼠作为对照组。小鼠每天经口灌胃给予相应药物或蒸馏水(对照组和模型组),持续8周。测定小鼠体重、空腹血糖、肾脏指数、微量白蛋白尿、肌酐、微量白蛋白尿/肌酐比值以及尿中尿素氮含量。进行苏木精-伊红(HE)染色、过碘酸-希夫(PAS)染色和Masson染色,观察PNS对db/db小鼠肾组织的保护作用。结果表明,PNS可显著降低db/db小鼠的空腹血糖水平并改善肾脏损伤。蛋白质印迹结果显示,PNS下调p-AKT1和p-STAT3的蛋白水平,并降低p-AKT1/AKT1和p-STAT3/STAT3比值。此外,高剂量PNS下调PIK3CA的蛋白水平。综上所述,PNS可能通过PI3K-AKT信号通路抑制STAT3发挥对DKD的肾脏保护作用。