Xiao Xinru, Guo Wenwen, Ding Ziqi, Chen Nuo, Zhang Qian
Department of Respiratory and Critical Care Medicine, The Second People's Hospital of Changzhou, The Third Affiliated Hospital of Nanjing Medical University, Changzhou 213164, China.
Department of Respiratory and Critical Care Medicine, The Second People's Hospital of Changzhou, The Third Affiliated Hospital of Nanjing Medical University, Changzhou 213164, China; Changzhou Medical Center, Nanjing Medical University, Changzhou 213003, China.
Phytomedicine. 2025 Nov;147:157183. doi: 10.1016/j.phymed.2025.157183. Epub 2025 Aug 19.
Chronic obstructive pulmonary disease (COPD) is defined by chronic airway inflammation. Traditional Chinese herb Pinellia ternata is used to treat COPD, but its bioactive components and mechanisms are unclear.
To identify the key active component of Pinellia ternate and explore its therapeutic mechanisms in COPD.
The principal active components and their associated targets of Pinellia ternata were identified through network pharmacology analysis. Using the BEAS-2B cell, the effects of baicalein on oxidative stress, apoptosis, and inflammation induced by cigarette smoke extract (CSE) were evaluated. A COPD mouse model was established to assess the protective effects of baicalein on airway inflammation, mucus secretion, and lung tissue damage. Flow cytometry was used to analyze the proportion of immune cells in lung tissues. UPLC-Q/TOF-MS was employed to evaluate the metabolic profile changes in bronchoalveolar lavage fluid (BALF).
Pinellia ternata interacted with 70 COPD-related targets, with hypoxia-inducible factor 1-alpha (HIF1A) as a key target. Baicalein, one of the major components of Pinellia ternata, alleviates oxidative stress, apoptosis, and inflammation in CSE-treated BEAS-2B cells by inhibiting HIF1A. In COPD mice, baicalein alleviated airway inflammation and lung damage and decreased HIF1A expression. Baicalein modulated the CD4⁺/CD8⁺ T cell ratio in lung tissues, reducing the cytotoxicity of CD8⁺ T cells, and altered metabolic pathways in BALF.
Baicalein exerts anti-inflammatory effects in COPD by inhibiting HIF1A-mediated oxidative stress and apoptosis in bronchial epithelial cells and modulating CD8⁺ T cell cytotoxicity. This study provides a basis for developing baicalein as a potential COPD therapy.
慢性阻塞性肺疾病（COPD）由慢性气道炎症定义。传统中药半夏用于治疗COPD，但其生物活性成分和作用机制尚不清楚。
确定半夏的关键活性成分并探讨其在COPD中的治疗机制。
通过网络药理学分析确定半夏的主要活性成分及其相关靶点。使用BEAS-2B细胞，评估黄芩苷对香烟烟雾提取物（CSE）诱导的氧化应激、细胞凋亡和炎症的影响。建立COPD小鼠模型，以评估黄芩苷对气道炎症、黏液分泌和肺组织损伤的保护作用。采用流式细胞术分析肺组织中免疫细胞的比例。使用超高效液相色谱-四极杆/飞行时间质谱（UPLC-Q/TOF-MS）评估支气管肺泡灌洗液（BALF）中的代谢谱变化。
半夏与70个COPD相关靶点相互作用，其中缺氧诱导因子1α（HIF1A）为关键靶点。黄芩苷作为半夏的主要成分之一，通过抑制HIF1A减轻CSE处理的BEAS-2B细胞中的氧化应激、细胞凋亡和炎症。在COPD小鼠中，黄芩苷减轻气道炎症和肺损伤，并降低HIF1A表达。黄芩苷调节肺组织中CD4⁺/CD8⁺ T细胞比例，降低CD8⁺ T细胞的细胞毒性，并改变BALF中的代谢途径。
黄芩苷通过抑制HIF1A介导的支气管上皮细胞氧化应激和细胞凋亡以及调节CD8⁺ T细胞细胞毒性，在COPD中发挥抗炎作用。本研究为开发黄芩苷作为潜在的COPD治疗药物提供了依据。
