Advances in the activity of resveratrol and its derivatives in cardiovascular diseases
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Yaling Peng1, Xing Zheng1,2, Si Zhang2
1Institute of Pharmacy and Pharmacology, Hengyang Medicinal School, University of South China, Hengyang, Hunan, China.
Insights
Resveratrol (RSV) shows cardiovascular protection but is unstable. This review explores RSV derivatives, their synthesis, structure-activity relationships, and mechanisms for treating cardiovascular diseases (CVDs).
Area of Science:
- Pharmacology and Medicinal Chemistry
- Cardiovascular Medicine
- Natural Product Chemistry
Background:
- Cardiovascular diseases (CVDs) are the leading global cause of mortality.
- Resveratrol (RSV), a natural compound, exhibits antioxidant and cardioprotective properties.
- Clinical use of RSV is hindered by its poor stability and rapid metabolism.
Purpose of the Study:
- To review the activity, synthesis, and structure-activity relationships (SAR) of resveratrol derivatives.
- To elucidate the mechanisms by which RSV and its derivatives exert protective effects against CVDs.
- To highlight recent advancements in optimizing RSV for cardiovascular applications.
Main Methods:
- Literature review of scientific databases (e.g., PubMed, Scopus).
- Analysis of studies on resveratrol synthesis and derivatization.
- Examination of research on the pharmacological mechanisms of RSV in cardiovascular models.
Main Results:
- RSV derivatives demonstrate improved stability and bioavailability compared to native RSV.
- Structure-activity relationship studies reveal key modifications enhancing cardioprotective effects.
- RSV's mechanisms in CVDs involve antioxidant, anti-inflammatory, and signaling pathway modulation.
Conclusions:
- Optimizing resveratrol structure through derivatization offers a promising strategy to overcome its limitations for CVD treatment.
- Further research into RSV derivatives holds potential for developing novel cardiovascular therapeutics.
- Understanding SAR and mechanisms is crucial for designing effective RSV-based drugs.
Abstract:
Cardiovascular diseases (CVDs), the leading cause of human death worldwide, are diseases that affect the heart and blood vessels and include arrhythmias, coronary atherosclerotic heart disease, hypertension, and so on. Resveratrol (RSV) is a natural nonflavonoid phenolic compound with antioxidant, anti-inflammatory, anticancer, and cardiovascular protection functions. RSV has shown significant protective effects against CVD. However, RSV's clinical application is limited by its tendency to be oxidized and metabolized easily. Therefore, it is necessary to optimize the RSV structure. This review will introduce the activity, synthesis, and structure-activity relationships of RSV derivatives, and the mechanism of the action of RSV in CVDs in recent years.
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