Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi

Mikko Vahermo, Sara Krogerus, Abdelmajeed Nasereddin, Marcel Kaiser, Reto Brun, Charles L. Jaffe, Jari Yli-Kauhaluoma, Vânia M. Moreira

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

Derivatives of dehydroabietic acid bearing different amino acids scaffolds have potent antiprotozoal activity against Leishmania donovani and Trypanosoma cruzi, with good to high selectivity, and can therefore be regarded as good models for further development into new drugs to fight leishmaniasis and Chagas disease. Several of the tested compounds were able to kill parasites residing inside cells, with IC50 values ranging from 2.3 to 9 mu M (L. donovani) and 1.4 to 5.8 mu M (T. cruzi), reflecting their ability to fight these infections at the relevant stage responsible for disease. One of the compounds, bearing a 3-pyridyl-Dalanine side chain, was 1.5-fold more potent against T. cruzi amastigotes residing in L6 cells than the reference compound benznidazole.
LanguageEnglish
Pages457-463
Number of pages7
JournalMedChemComm
Volume7
Issue number3
Early online date25 Nov 2015
DOIs
Publication statusPublished - 1 Mar 2016

Fingerprint

Bearings (structural)
Leishmania donovani
Trypanosoma cruzi
Derivatives
Scaffolds
Leishmaniasis
Chagas Disease
Amino Acids
Inhibitory Concentration 50
Parasites
Pharmaceutical Preparations
Infection
dehydroabietic acid

Keywords

  • abietane diterpenoids
  • in-vitro
  • staphylococcus-aureus
  • trypanocidal activity
  • screening drugs
  • diseases
  • chemotherapy
  • amastigotes
  • organisms

Cite this

Vahermo, Mikko ; Krogerus, Sara ; Nasereddin, Abdelmajeed ; Kaiser, Marcel ; Brun, Reto ; Jaffe, Charles L. ; Yli-Kauhaluoma, Jari ; Moreira, Vânia M. / Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi. In: MedChemComm. 2016 ; Vol. 7, No. 3. pp. 457-463.
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Vahermo, M, Krogerus, S, Nasereddin, A, Kaiser, M, Brun, R, Jaffe, CL, Yli-Kauhaluoma, J & Moreira, VM 2016, 'Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi' MedChemComm, vol. 7, no. 3, pp. 457-463. https://doi.org/10.1039/c5md00498e

Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi. / Vahermo, Mikko; Krogerus, Sara; Nasereddin, Abdelmajeed; Kaiser, Marcel; Brun, Reto; Jaffe, Charles L.; Yli-Kauhaluoma, Jari; Moreira, Vânia M.

In: MedChemComm, Vol. 7, No. 3, 01.03.2016, p. 457-463.

Research output: Contribution to journalArticle

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