A review of the design and modification of lactoferricins and their derivatives

Biometals. 2018 Jun;31(3):331-341. doi: 10.1007/s10534-018-0086-6. Epub 2018 Feb 17.

Abstract

Lactoferricin (Lfcin), a multifunction short peptide with a length of 25 residues, is derived from the whey protein lactoferrin by acidic pepsin hydrolysis. It has potent nutritional enhancement, antimicrobial, anticancer, antiviral, antiparasitic, and anti-inflammatory activities. This review describes the research advantages of the above biological functions, with attention to the molecular design and modification of Lfcin. In this examination of design and modification studies, research on the identification of Lfcin active derivatives and crucial amino acid residues is also reviewed. Many strategies for Lfcin optimization have been studied in recent decades, but we mainly introduce chemical modification, cyclization, chimera and polymerization of this peptide. Modifications such as incorporation of D-amino acids, acetylation and/or amidation could effectively improve the activity and stability of these compounds. Due to their wide array of bio-functions and applications, Lfcins have great potential to be developed as biological agents with multiple functions involved with nutritional enhancement, as well as disease preventive and therapeutic effects.

Keywords: Biological agent; Lactoferricin; Modification; Nutritional enhancement; Preventive and therapeutic activity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Acetylation
  • Amides / chemistry
  • Amino Acid Sequence
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / therapeutic use
  • Antiviral Agents / chemistry
  • Antiviral Agents / therapeutic use
  • Humans
  • Lactoferrin / chemistry*
  • Lactoferrin / therapeutic use
  • Peptides / chemistry*
  • Peptides / therapeutic use
  • Whey Proteins / chemistry
  • Whey Proteins / therapeutic use

Substances

  • Amides
  • Anti-Infective Agents
  • Antiviral Agents
  • Peptides
  • Whey Proteins
  • lactoferricin B
  • Lactoferrin