Bio-Guided Investigation of Sideritis cypria Methanol Extract Driven by in Vitro Antioxidant and Cytotoxic Assays

Chem Biodivers. 2021 Mar;18(3):e2000966. doi: 10.1002/cbdv.202000966. Epub 2021 Feb 17.

Abstract

Sideritis cypria Post is an endemic and endangered species of Northern Cyprus. The overall aim of the present study was to evaluate the total phenolic content, the antioxidant, the cytotoxic and the antimicrobial activity of the methanol extract obtained from the aerial parts of cultivated S. cypria. A bio-guided approach led to the isolation of 27 chemical compounds by using various analytical techniques. Their structures were elucidated on the basis of 1D and 2D NMR spectroscopy. The crude extract exerted strong antioxidant activity (DPPH and FRAP assays) which was attributed to its high total phenolic content. Furthermore, groups rich in phenolic content showed highest antioxidant property, whereas groups with phytosterols, diterpenoids and apigenin derivatives exerted cytotoxic effects in MDA-MB231 cancer cell line by the MTT method. Moreover, the cytotoxic activity of four isolated apigenin derivatives was evaluated in the same cancer cells. The antimicrobial activity of the extract and groups were measured, demonstrating lack of activity. To the best of our knowledge, this survey is the first report on the biological activities of the methanol extract of S. cypria.

Keywords: antimicrobial activity; antioxidant activity; bio-guided; cultivated Sideritis cypria; cytotoxicity.

MeSH terms

  • 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 Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Methanol / chemistry
  • Molecular Structure
  • Picrates / antagonists & inhibitors
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Sideritis / chemistry*
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

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