Cholesterol: Bioactivities, Structural Modification, Mechanisms of Action, and Structure-Activity Relationships

Mini Rev Med Chem. 2021;21(14):1830-1848. doi: 10.2174/1389557521666210105123320.

Abstract

Cholesterol, steroid alcohol, was discovered by M.E. Chevreul in 1815. Cholesterol and its derivatives showed a large variety of biological properties such as anticancer activity, anticardiac activity, anti-inflammatory activity, antimicrobial activity, anti-psychotic activity, antioxidant activity, drug-loaded activity, etc. In this mini-review, the advances of structural modification of cholesterol from 2014 to 2020 are summarized. In addition, the bioactivities, mechanisms of action and structureactivity relationships of cholesterol and its related derivatives are also discussed.

Keywords: Cholesterol derivatives; biological activities; mechanisms of action; structural modification; structure-activity relationships..

Publication types

  • Review

MeSH terms

  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / chemistry*
  • Anti-Inflammatory Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Survival / drug effects
  • Cholesterol / chemical synthesis
  • Cholesterol / chemistry*
  • Cholesterol / metabolism
  • Cholesterol / pharmacology
  • Drug Carriers / chemistry
  • Humans
  • Neutrophils / cytology
  • Neutrophils / drug effects
  • Neutrophils / metabolism
  • Oxidation-Reduction
  • Reactive Oxygen Species / metabolism
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Antineoplastic Agents
  • Drug Carriers
  • Reactive Oxygen Species
  • Cholesterol