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Antiprotozoal activity of Jatrogrossidione from Jatropha grossidentata and Jatrophone from Jatropha isabellii
Author(s) -
SchmedaHirschmann G.,
Razmilic I.,
Sauvain M.,
Moretti C.,
Muñoz V.,
Ruiz E.,
Balanza E.,
Fournet A.
Publication year - 1996
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/(sici)1099-1573(199608)10:5<375::aid-ptr847>3.0.co;2-#
Subject(s) - antiprotozoal , amastigote , pentamidine , in vivo , trypanosoma cruzi , pharmacology , leishmania infantum , leishmania , biology , microbiology and biotechnology , in vitro , ketoconazole , leishmaniasis , medicine , parasite hosting , immunology , biochemistry , antifungal , visceral leishmaniasis , world wide web , computer science , pneumonia
The activity of jatrogrossidione, the main diterpene of Jatropha grossidentata and jatrophone from Jatropha isabellii was determined against Leishmania and Trypanosoma cruzi strains in vitro as well as against Leishmania amazonensis in vivo. Jatrogrossidione showed a strong in vitro leishmanicidal and trypanocidal activity with IC 100 of 0.75 and 1.5–5.0 μg/mL, respectively. Under similar conditions, the IC 100 of glucantime, ketoconazole and pentamidine towards Leishmania strains were >100, 50–100 and 1 μg/mL, respectively. The IC 50 of jatrogrossidione was <0.25 μg/mL against amastigote forms of Leishmania infecting macrophages, with toxicity at concentrations higher than 0.5 μg/mL. BALB/c mice infected with L. amazonensis strain PH 8 were treated 24 h after infection with jatrogrossidione and jatrophone for 13 consecutive days. Jatrophone at 25 mg/kg/day subcutaneously administered was significantly active ( p <0.05) against the virulent strain PH 8 of L. amazonesis ; it was more active than Glucantime at 112 mg Sb v per kg/day. Subcutaneous administration of jatrophone, however, proved to be too toxic under our assay conditions. Assays of single local treatment on the footpad infection 2 weeks after inoculation of L. amazonensis indicated that jatrogrossidione and jatrophone were inactive at the selected doses.