Novel bioactive peptides of Achillea eriophora show anticancer and antioxidant activities

Bioorg Chem. 2021 May:110:104777. doi: 10.1016/j.bioorg.2021.104777. Epub 2021 Feb 24.

Abstract

Despite the limitations of current methods in cancer treatment, the use of bioactive peptides can be as an alternative to treat today. Therefore, isolation and relative purification of bioactive peptides was carried out form Achillea eriophora using a Sep-Pak C18 SPE cartridge and Amicon® Ultra Centrifugal Filters. The presence of desired peptides was checked using RP-HPLC and confirmed using LC-MS. The results of anticancer assay showed that the peptide mixture inhibits the growth of MCF-7 cancerous cell line with the values of IC50, GI50, and LC50 equal to 18.73 ± 0.22, 7.52 ± 0.15, and 56.73 ± 0.18 µg/mL, respectively. It also showed DPPH radical scavenging activity and cupric-ion reducing power with the IC50 value of 5.095 ± 0.23 and 63.3 ± 0.44 µg/mL, respectively. Although flavonoids were present in the sample along with the peptides, their amount was trivial (18.097 ± 1.36 μg/mL). Nevertheless, the results of the LC-MS showed mass-to-charge ratios of 301.17, 261.22, and 243.25, which was a dipeptide or tripeptide in compression to enzyme-digested BSA as a standard. In addition, SEM analysis of the purified peptide mixture showed that it kills the MCF-7 cancerous cell line by creating pores in the membrane. Therefore, it might be valuable to these peptides sequenced and be studied for physicochemical properties. Animal and clinical studies could help its application in drug development.

Keywords: Anticancer; Bioactive peptide; Cupric-ion reducing power; DPPH radical scavenging; LC-MS; RP-HPLC.

MeSH terms

  • Achillea / chemistry*
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Antioxidants / chemistry
  • Antioxidants / isolation & purification
  • Antioxidants / pharmacology*
  • Biphenyl Compounds / antagonists & inhibitors
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Flowers / chemistry*
  • Humans
  • MCF-7 Cells
  • Molecular Docking Simulation
  • Molecular Structure
  • Picrates / antagonists & inhibitors
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents, Phytogenic
  • Antioxidants
  • Biphenyl Compounds
  • Picrates
  • 1,1-diphenyl-2-picrylhydrazyl