Natural Phenolics as Inhibitors of the Human Neutrophil Elastase (HNE) Release: An Overview of Natural Anti-inflammatory Discoveries during Recent Years

Antiinflamm Antiallergy Agents Med Chem. 2018;17(2):70-94. doi: 10.2174/1871523017666180910104946.

Abstract

Serine protease, Human Neutrophil Elastase (HNE), has been shown to be useful in medical science, however, its over production and malfunctioning may produce devastating effects and cause serious damage to the host. Unfortunately, the present approved drug, sivelestat, only alleviates the symptoms of the diseases caused by malfunction of HNE but not the disease progression. Therefore, there is a crucial need to search potent and safer molecules as elastase inhibitors and to develop better anti-inflammatory drugs in future. In addition, nature is the best architect that may provide a safer future drug candidate as HNEproduction/ activity inhibitor. Since phenolic natural products are already known as antiinflammatory compounds, either by acting as antioxidants or by any other mechanism, thus, this review article summarizes the discovery and elastase inhibitory activity of ∼180 phenolics isolated from diverse natural sources during more than one decade, i.e. 2005-2017.

Keywords: Anti-inflammatory compounds; disease; human neutrophil elastase; inhibitory activity; phenolics; secondary metabolites..

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Humans
  • Leukocyte Elastase / antagonists & inhibitors*
  • Leukocyte Elastase / metabolism
  • Molecular Structure
  • Neutrophils / drug effects*
  • Neutrophils / enzymology
  • Phenols / chemistry
  • Phenols / pharmacology*
  • Secretory Pathway / drug effects
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Phenols
  • Serine Proteinase Inhibitors
  • Leukocyte Elastase