Study on the hypotensive effect and mechanism of hawthorn (Crataegus pinnatifida) fruits and hyperoside in spontaneously hypertensive rats.

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 in vivo 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.