Dietary Flavonoids: Cardioprotective Potential with Antioxidant Effects and Their Pharmacokinetic, Toxicological and Therapeutic Concerns

Molecules. 2021 Jun 30;26(13):4021. doi: 10.3390/molecules26134021.

Abstract

Flavonoids comprise a large group of structurally diverse polyphenolic compounds of plant origin and are abundantly found in human diet such as fruits, vegetables, grains, tea, dairy products, red wine, etc. Major classes of flavonoids include flavonols, flavones, flavanones, flavanols, anthocyanidins, isoflavones, and chalcones. Owing to their potential health benefits and medicinal significance, flavonoids are now considered as an indispensable component in a variety of medicinal, pharmaceutical, nutraceutical, and cosmetic preparations. Moreover, flavonoids play a significant role in preventing cardiovascular diseases (CVDs), which could be mainly due to their antioxidant, antiatherogenic, and antithrombotic effects. Epidemiological and in vitro/in vivo evidence of antioxidant effects supports the cardioprotective function of dietary flavonoids. Further, the inhibition of LDL oxidation and platelet aggregation following regular consumption of food containing flavonoids and moderate consumption of red wine might protect against atherosclerosis and thrombosis. One study suggests that daily intake of 100 mg of flavonoids through the diet may reduce the risk of developing morbidity and mortality due to coronary heart disease (CHD) by approximately 10%. This review summarizes dietary flavonoids with their sources and potential health implications in CVDs including various redox-active cardioprotective (molecular) mechanisms with antioxidant effects. Pharmacokinetic (oral bioavailability, drug metabolism), toxicological, and therapeutic aspects of dietary flavonoids are also addressed herein with future directions for the discovery and development of useful drug candidates/therapeutic molecules.

Keywords: ROS scavenging; bioavailability and drug metabolism; cardioprotective effects; dietary flavonoids; drug discovery; myocardial dysfunction; toxicity.

Publication types

  • Review

MeSH terms

  • Antioxidants* / chemistry
  • Antioxidants* / pharmacokinetics
  • Antioxidants* / therapeutic use
  • Biological Availability
  • Cardiotonic Agents* / chemistry
  • Cardiotonic Agents* / pharmacokinetics
  • Cardiovascular Diseases* / metabolism
  • Cardiovascular Diseases* / pathology
  • Cardiovascular Diseases* / prevention & control
  • Flavonoids* / chemistry
  • Flavonoids* / pharmacokinetics
  • Flavonoids* / therapeutic use
  • Fruit / chemistry*
  • Humans
  • Vegetables / chemistry*

Substances

  • Antioxidants
  • Cardiotonic Agents
  • Flavonoids