Matairesinol discovered as a key active ingredient in Chinese dark tea protects against high-fat induced endothelial injury via activating AMPK phosphorylation

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Journal of ethnopharmacology Pub Date : 2025-03-07 DOI:10.1016/j.jep.2025.119576
Wenjie Bi , Yougang Zhang , Zixu Lu , Huanxin Zhao , Haiyang Wang , Songsong Wang , Rajiv Kumar Malhotra , Xiaojing Wang , Liwen Han
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Abstract

Ethnopharmacological relevance

As a traditional health beverage in China, Dark Tea (DT) have been proved to effectively mitigate vascular lesions induced by hyperlipidemia. However, key active ingredient of DT and the potential pharmacological mechanism protecting vascular endothelium is still unclear.
Aim of the study: This study aimed to investigate the key active ingredient in DT and reveal underlying mechanism responsible for its protective effect on vascular endothelium.

Materials and methods

The protective effect of DT on vascular endothelium was evaluated using a high-fat diet-induced zebrafish model. The chemical ingredients of DT were analyzed by ultra-high performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UHPLC-Q/TOF-MS), and the active ingredients were identified using a multidimensional molecular data mining approach. Molecular biology experiments were used to explore the underlying mechanisms of DT and its active components.

Results

The results showed that DT could significantly prevent the deposition of circulatory lipids on the vascular wall, inhibit inflammatory cell aggregation, and reduce microvascular hyperplasia in zebrafish models. An integrated multi-dimensional data mining technique was successfully employed to identify a key active lignan in DT, matairesinol. Furthermore, DT and matairesinol significantly protected endothelial cells by activating AMPK phosphorylation, thereby inhibiting downstream HMGCR protein expression and promoting PPARγ phosphorylation.

Conclusions

Matairesinol has been characterized as a key active ingredient in DT. It protects against high-fat-induced vascular endothelial damage by activating AMPK and downstream signaling pathways. These findings offer new insights into the therapeutic potential of DT as a daily dietary supplement for maintaining vascular health.

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materesinol是中国黑茶中发现的一种关键活性成分,通过激活AMPK磷酸化来防止高脂肪诱导的内皮损伤。
民族药理学相关性:作为中国传统的保健饮料,黑茶(DT)已被证明能有效减轻高脂血症引起的血管病变。然而,DT的关键活性成分及其保护血管内皮的潜在药理机制尚不清楚。研究目的:研究丹参中关键活性成分,揭示其对血管内皮保护作用的机制。材料与方法:采用高脂饮食诱导的斑马鱼模型,观察DT对血管内皮的保护作用。采用超高效液相色谱-四极杆/飞行时间质谱(UHPLC-Q/TOF-MS)分析了DT的化学成分,并采用多维分子数据挖掘方法鉴定了其有效成分。通过分子生物学实验,探讨其作用机制及其有效成分。结果:在斑马鱼模型中,DT能明显阻止循环脂质在血管壁上的沉积,抑制炎症细胞聚集,减少微血管增生。采用集成的多维数据挖掘技术,成功地鉴定了DT中一个关键的活性木脂素。此外,DT和mataresinol通过激活AMPK磷酸化,从而抑制下游HMGCR蛋白表达,促进PPARγ磷酸化,从而显著保护内皮细胞。结论:mattaresinol是DT的关键活性成分。它通过激活AMPK和下游信号通路来防止高脂肪诱导的血管内皮损伤。这些发现为DT作为维持血管健康的日常膳食补充剂的治疗潜力提供了新的见解。
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来源期刊
Journal of ethnopharmacology
Journal of ethnopharmacology 医学-全科医学与补充医学
CiteScore
10.30
自引率
5.60%
发文量
967
审稿时长
77 days
期刊介绍: The Journal of Ethnopharmacology is dedicated to the exchange of information and understandings about people''s use of plants, fungi, animals, microorganisms and minerals and their biological and pharmacological effects based on the principles established through international conventions. Early people confronted with illness and disease, discovered a wealth of useful therapeutic agents in the plant and animal kingdoms. The empirical knowledge of these medicinal substances and their toxic potential was passed on by oral tradition and sometimes recorded in herbals and other texts on materia medica. Many valuable drugs of today (e.g., atropine, ephedrine, tubocurarine, digoxin, reserpine) came into use through the study of indigenous remedies. Chemists continue to use plant-derived drugs (e.g., morphine, taxol, physostigmine, quinidine, emetine) as prototypes in their attempts to develop more effective and less toxic medicinals.
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