Pharmacological Activities and Synthesis of Esculetin and Its Derivatives: A Mini-Review

Molecules. 2017 Mar 2;22(3):387. doi: 10.3390/molecules22030387.

Abstract

Esculetin, synonymous with 6,7-dihydroxycoumarin, is the main active ingredient of the traditional Chinese medicine Cortex Fraxini. The twig skin or trunk bark of Cortex Fraxini are used by herb doctors as a mild, bitter liver and gallbladder meridians' nontoxic drug as well as dietary supplement. Recently, with a variety of novel esculetin derivatives being reported, the molecular mechanism research as well as clinical application of Cortex Fraxini and esculetin are becoming more attractive. This mini-review will consolidate what is known about the biological activities, the mechanism of esculetin and its synthetic derivatives over the past decade in addition to providing a brief synopsis of the properties of esculetin.

Keywords: coumarin; esculetin; molecular mechanism; pharmacological activity; synthetic derivatives.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Infective Agents / chemical synthesis
  • Anti-Infective Agents / pharmacology
  • Anti-Inflammatory Agents / chemical synthesis
  • Anti-Inflammatory Agents / pharmacology
  • Antineoplastic Agents, Phytogenic / chemical synthesis
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Antioxidants / chemical synthesis
  • Antioxidants / pharmacology
  • Drugs, Chinese Herbal
  • Humans
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / pharmacology
  • Medicine, Chinese Traditional
  • Molecular Structure
  • Umbelliferones / chemical synthesis*
  • Umbelliferones / pharmacology*

Substances

  • Anti-Infective Agents
  • Anti-Inflammatory Agents
  • Antineoplastic Agents, Phytogenic
  • Antioxidants
  • Drugs, Chinese Herbal
  • Hypoglycemic Agents
  • Umbelliferones
  • esculetin