Celastrol: A Promising Agent Fighting against Cardiovascular Diseases
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Updated: Aug 31, 2025

Network Pharmacology Prediction and Metabolomics Validation of the Mechanism of Fructus Phyllanthi against Hyperlipidemia
Published on: April 7, 2023
Zhexi Li1, Jingyi Zhang2, Xulei Duan1
1Department of Cardiology, Life Science Research Center, The First Affiliated Hospital of Xinxiang Medical University, Weihui 453100, China.
Insights
Celastrol, a compound from Tripterygium wilfordii, shows promise for treating cardiovascular diseases (CVD) by protecting heart cells and reducing inflammation and oxidation. Further research is needed due to pharmacokinetic limitations.
Area of Science:
- Pharmacology
- Cardiology
- Natural Products
Background:
- Cardiovascular diseases (CVD) represent a major global health burden.
- There is an urgent need for novel therapeutic strategies to combat CVD.
- Celastrol, a natural compound, has emerged as a potential therapeutic agent for CVD.
Purpose of the Study:
- To review the beneficial effects of celastrol against various cardiovascular diseases (CVD).
- To elucidate the underlying mechanisms of celastrol's cardioprotective actions.
- To discuss pharmacokinetic limitations and future directions for celastrol's clinical application.
Main Methods:
- Literature review of in vitro and in vivo preclinical studies.
- Analysis of celastrol's effects on cardiomyocyte health, oxidation, and inflammation.
- Evaluation of pharmacokinetic data and clinical potential.
Main Results:
- Celastrol demonstrates protective effects against a wide range of CVD, including obesity, diabetes, atherosclerosis, and heart failure.
- Mechanisms involve direct protection of cardiomyocytes and indirect modulation of oxidative stress and inflammation.
- Preclinical studies support celastrol's therapeutic potential for cardiovascular conditions.
Conclusions:
- Celastrol exhibits significant therapeutic potential for cardiovascular diseases (CVD) through multifaceted mechanisms.
- Pharmacokinetic challenges need to be addressed for successful clinical translation.
- Further research is warranted to optimize celastrol-based therapies for CVD management.
Abstract:
Cardiovascular diseases (CVD) are leading causes of morbidity and mortality worldwide; therefore, seeking effective therapeutics to reduce the global burden of CVD has become increasingly urgent. Celastrol, a bioactive compound isolated from the roots of the plant Tripterygium wilfordii (TW), has been attracting increasing research attention in recent years, as it exerts cardiovascular treatment benefits targeting both CVD and their associated risk factors. Substantial evidence has revealed a protective role of celastrol against a broad spectrum of CVD including obesity, diabetes, atherosclerosis, cerebrovascular injury, calcific aortic valve disease and heart failure through complicated and interlinked mechanisms such as direct protection against cardiomyocyte hypertrophy and death, and indirect action on oxidation and inflammation. This review will mainly summarize the beneficial effects of celastrol against CVD, largely based on in vitro and in vivo preclinical studies, and the potential underlying mechanisms. We will also briefly discuss celastrol's pharmacokinetic limitations, which hamper its further clinical applications, and prospective future directions.
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