College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan 250355, China.
Experimental Center, Shandong University of Traditional Chinese Medicine, Jinan 250355, China.
Food Funct. 2024 May 20;15(10):5627-5640. doi: 10.1039/d3fo02641h.
Hawthorn fruits have a sweet and sour taste, besides having beneficial therapeutic effects on hyperlipidemia, hypertension, and coronary heart disease, making them widely used in food and clinical medicine. However, their hypotensive effects and potential mechanisms of anti-hypertension still need to be elucidated. This study aims to explore the antihypertensive effect of hawthorn and its monomer hyperoside on spontaneously hypertensive rats through pharmacodynamics, serum metabolomics, and mechanism studies. After 7 weeks of intervention with hawthorn extract and hyperoside, the blood pressure was significantly reduced. Aortic vascular staining results showed that the injury was significantly improved after intervention with hawthorn extract and hyperoside. According to the serum metabolomics study, the main metabolic pathway regulating blood pressure in hawthorn extract and hyperoside groups was the primary bile acid biosynthesis pathway. Quantitative experiments confirmed that the level of bile acid in the model group was significantly different from that in the normal group, while that in the hawthorn group and the hyperoside group was close to that in the normal group. Based on the prediction of bile acid-hypertension related targets and the literature, nine genes involved in bile acid metabolism and inflammatory pathways were selected for further study. The FXR, TGR5, ET-1, NOS3, Akt1, TNF-α, Ptgs2, ACE2 and Kdr mRNA expression levels in the hawthorn extract and hyperoside groups were significantly different from those in the model groups. In summary, hawthorn extract and hyperoside have a hypotensive effect on spontaneously hypertensive rats through bile acid and inflammation related targets. Hence, hawthorn extract has the potential to become a functional food or an alternative therapy for hypertension.
山楂果实酸甜可口，除对高脂血症、高血压、冠心病等具有有益的治疗作用外，还广泛应用于食品和临床医学。然而，其降压作用及其潜在的降压机制仍需阐明。本研究旨在通过药效学、血清代谢组学和机制研究，探讨山楂及其单体金丝桃苷对自发性高血压大鼠的降压作用。山楂提取物和金丝桃苷干预 7 周后，血压明显降低。主动脉血管染色结果表明，山楂提取物和金丝桃苷干预后损伤明显改善。根据血清代谢组学研究，山楂提取物和金丝桃苷组调节血压的主要代谢途径是初级胆汁酸生物合成途径。定量实验证实，模型组胆汁酸水平与正常组差异显著，而山楂组和金丝桃苷组接近正常组。基于胆汁酸-高血压相关靶点的预测和文献，选择了九个与胆汁酸代谢和炎症途径相关的基因进行进一步研究。山楂提取物和金丝桃苷组中 FXR、TGR5、ET-1、NOS3、Akt1、TNF-α、Ptgs2、ACE2 和 Kdr 的 mRNA 表达水平与模型组有显著差异。综上所述，山楂提取物和金丝桃苷通过胆汁酸和炎症相关靶点对自发性高血压大鼠具有降压作用。因此，山楂提取物具有成为功能性食品或高血压替代疗法的潜力。
