A. Fournet et al., ANTILEISHMANIAL ACTIVITY OF A TETRALONE ISOLATED FROM AMPELOCERA-EDENTULA, A BOLIVIAN PLANT USED AS A TREATMENT FOR CUTANEOUS LEISHMANIASIS, Planta medica, 60(1), 1994, pp. 8-12
The stem bark of Ampelocera edentula Kuhlm. (Ulmaceae) is used by the
Chimanes Indians from Bolivia for the treatment of cutaneous leishmani
asis caused by the protozoan Leishmania braziliensis. A chloroform ext
ract of the stem barks was found to be active against extracellular fo
rms of Leishmania ssp. and Trypanosoma cruzi at 50 mu g/ml. Bioassay-g
uided fractionation of this extract allowed us to isolate one active c
ompound. Its structure was elucidated by spectral and chemical studies
as 4-hydroxyl-1-tetralone. BALB/e mice infected with L. amazonensis (
PH8) or L. venezuelensis were treated one day after the parasitic infe
ction with 4-hydroxy-1-tetralone (25 mg/ kg/day) or with reference dru
g, Glucantime(R) (56 mg Sb-v/kg/day) for 14 days. Lesion development w
as the criteria used to evaluate the disease severity. 4-Hydroxy-1-tet
ralone was slightly less effective than the reference drug against L.
amazonensis or L. venezuelensis. Single treatment near the site of inf
ection, 14 days after infection with L. amazonensis, with 4-hydroxy-1-
tetralone (50 mg/kg) was more effective than Glucantime (112 mg/kg). T
his study is, to our knowledge, the first to show the activity of a te
tralone for the experimental treatment of New World cutaneous leishman
iasis.