Antiproliferative and antimicrobial activities of alkylbenzoquinone derivatives from Ardisia kivuensis

Pharm Biol. 2014 Mar;52(3):392-7. doi: 10.3109/13880209.2013.837076. Epub 2013 Nov 5.

Abstract

Context: Medicinal plants are continuously screened for their pharmacological properties. Despite the diversity and the numerous phytochemicals found in Ardisia (Myrsinaceae) species, its full biological potential has not been fully explored.

Objective: Four naturally occurring alkylbenzoquinone derivatives, namely ardisiaquinone N (1), ardisiaquinone J (2), ardisiaquinone K (3) and a mixture of ardisiaquinone P (4) and K (3) from Ardisia kivuensis Taton (Myrsinaceae) were investigated in vitro for their cytotoxicity and antimicrobial activity.

Materials and methods: Minimal inhibitory concentration (MIC) was determined using the broth micro-dilution assay. Tumor cells growth inhibition was performed by sulphorhodamine B (SRB) assay while sub-diploid DNA fraction was measured by flow cytometry.

Results: Compounds 1, 2 and 3 showed significant antimicrobial activity against two Gram-positive bacteria and one fungus (with MICs varying between 3.12 and 6.25 µg/ml). The four compounds exhibited remarkable antiproliferative activity against the leukemia cell line TPH-1 with IC₅₀ inhibition values between 2 and 2.1 µg/ml. Cytotoxic activity was found to be related to apoptosis induction.

Discussion and conclusion: These findings suggest that natural compounds herein studied are interesting potential candidates for the development of new therapeutic agents, especially against leukemia and Gram-positive bacterial infections.

MeSH terms

  • Anti-Infective Agents / administration & dosage
  • Anti-Infective Agents / isolation & purification
  • Anti-Infective Agents / pharmacology
  • Antineoplastic Agents, Phytogenic / administration & dosage
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Apoptosis / drug effects
  • Ardisia / chemistry*
  • Benzoquinones / administration & dosage
  • Benzoquinones / isolation & purification
  • Benzoquinones / pharmacology*
  • Cell Line, Tumor
  • Flow Cytometry
  • Fungi / drug effects
  • Gram-Positive Bacteria / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Plant Extracts / administration & dosage
  • Plant Extracts / pharmacology*

Substances

  • Anti-Infective Agents
  • Antineoplastic Agents, Phytogenic
  • Benzoquinones
  • Plant Extracts