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

doi:10.1039/c5md00498e

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

Strathclyde Institute Of Pharmacy And Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

23 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.

Original language	English
Pages (from-to)	457-463
Number of pages	7
Journal	MedChemComm
Volume	7
Issue number	3
Early online date	25 Nov 2015
DOIs	https://doi.org/10.1039/c5md00498e
Publication status	Published - 1 Mar 2016

Keywords

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

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title = "Antiprotozoal activity of dehydroabietic acid derivatives against Leishmania donovani and Trypanosoma cruzi",

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.",

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author = "Mikko Vahermo and Sara Krogerus and Abdelmajeed Nasereddin and Marcel Kaiser and Reto Brun and Jaffe, {Charles L.} and Jari Yli-Kauhaluoma and Moreira, {V{\^a}nia M.}",

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AU - Vahermo, Mikko

AU - Krogerus, Sara

AU - Nasereddin, Abdelmajeed

AU - Kaiser, Marcel

AU - Brun, Reto

AU - Jaffe, Charles L.

AU - Yli-Kauhaluoma, Jari

AU - Moreira, Vânia M.

PY - 2016/3/1

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AB - 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.

KW - abietane diterpenoids

KW - in-vitro

KW - staphylococcus-aureus

KW - trypanocidal activity

KW - screening drugs

KW - diseases

KW - chemotherapy

KW - amastigotes

KW - organisms

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

Abstract

Keywords

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