HPLC-Based Activity Profiling for Antiprotozoal Compounds in the Endemic Iranian Medicinal Plant Helichrysum oocephalum

  • J Nat Prod. 2019 Apr 26;82(4):958-969. doi: 10.1021/acs.jnatprod.8b01031.
Maryam Akaberi  1  2 ,  Ombeline Danton  1 ,  Zahra Tayarani-Najaran  3 ,  Javad Asili  2 ,  Mehrdad Iranshahi  2 ,  S Ahmad Emami  2 ,  Matthias Hamburger  1
Affiliations
  • 1. Division of Pharmaceutical Biology, Department of Pharmaceutical Sciences , University of Basel , Klingelbergstrasse 50 , 4056 Basel , Switzerland.
  • 2. Department of Pharmacognosy, School of Pharmacy , Mashhad University of Medical Sciences , Mashhad , Iran.
  • 3. Biotechnology Research Center, Pharmaceutical Technology Institute , Mashhad University of Medical Sciences , Mashhad , Iran.
PMID: 30916554 DOI: 10.1021/acs.jnatprod.8b01031
Abstract

In a screening of Iranian Plants for antiprotozoal activity a dichlomethane extract from the aerial parts of Helichrysum oocephalum showed in vitro antiprotozoal activity against Plasmodium falciparum and Leishmania donovani, with IC50 values of 4.01 ± 0.50 and 5.08 ± 0.07 μg/mL, respectively. The activity in the extract was tracked by HPLC-based activity profiling, and subsequent targeted preparative isolation afforded 24 compounds, including pyrones 22-24, phloroglucinol derivatives 12-19, and compounds containing both structural motifs (1-11, 20, and 21). Of these, 15 compounds were new natural products. The in vitro antiprotozoal activity of isolates was determined. Compound 3 showed good potency and selectivity in vitro against L. donovani (IC50 1.79 ± 0.17 μM; SI 53).