Evaluation of in vitro antiprotozoal activity of Ajuga laxmannii and its secondary metabolites

Pharm Biol. 2016 Sep;54(9):1808-14. doi: 10.3109/13880209.2015.1129542. Epub 2016 Jan 6.

Abstract

Context Some Ajuga L. (Lamiaceae) species are traditionally used for the treatment of malaria, as well as fever, which is a common symptom of many parasitic diseases. Objective In the continuation of our studies on the identification of antiprotozoal secondary metabolites of Turkish Lamiaceae species, we have investigated the aerial parts of Ajuga laxmannii. Materials and methods The aerial parts of A. laxmannii were extracted with MeOH. The H2O subextract was subjected to polyamide, C18-MPLC and SiO2 CCs to yield eight metabolites. The structures of the isolates were elucidated by NMR spectroscopy and MS analyses. The extract, subextracts as well as the isolates were tested for their in vitro antiprotozoal activities against Plasmodium falciparum, Trypanasoma brucei rhodesiense, T. cruzi and Leishmania donovani at concentrations of 90-0.123 μg/mL. Results Two iridoid glycosides harpagide (1) and 8-O-acetylharpagide (2), three o-coumaric acid derivatives cis-melilotoside (3), trans-melilotoside (4) and dihydromelilotoside (5), two phenylethanoid glycosides verbascoside (6) and galactosylmartynoside (7) and a flavone-C-glycoside, isoorientin (8) were isolated. Many compounds showed moderate to good antiparasitic activity, with isoorientin (8) displaying the most significant antimalarial potential (an IC50 value of 9.7 μg/mL). Discussion and conclusion This is the first report on the antiprotozoal evaluation of A. laxmannii extracts and isolates. Furthermore, isoorientin and dihydromelilotoside are being reported for the first time from the genus Ajuga.

Keywords: Antiprotozoal activity; Isoorientin; Lamiaceae; flavonoid; iridoid glycosides; plasmodium.

Publication types

  • Comparative Study

MeSH terms

  • Ajuga* / metabolism
  • Animals
  • Antiprotozoal Agents / isolation & purification
  • Antiprotozoal Agents / pharmacology*
  • Cell Line
  • Humans
  • Leishmania donovani / drug effects
  • Leishmania donovani / growth & development
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Phytotherapy
  • Plant Components, Aerial
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Plants, Medicinal
  • Plasmodium falciparum / drug effects
  • Plasmodium falciparum / growth & development
  • Rats
  • Trypanosoma brucei rhodesiense / drug effects
  • Trypanosoma brucei rhodesiense / growth & development
  • Trypanosoma cruzi / drug effects
  • Trypanosoma cruzi / growth & development

Substances

  • Antiprotozoal Agents
  • Plant Extracts