A. Fournet et al., ANTIPROTOZOAL ACTIVITY OF QUINOLINE ALKALOIDS ISOLATED FROM GALIPEA-LONGIFLORA, A BOLIVIAN PLANT USED AS A TREATMENT FOR CUTANEOUS LEISHMANIASIS, PTR. Phytotherapy research, 8(3), 1994, pp. 174-178
The stem bark of Galipea longiflora is used by the Chimane Indians in
Bolivia for the treatment of cutaneous leishmaniasis produced by Leish
mania braziliensis. Petroleum ether and chloroform extracts of stem, r
oot bark and leaves were found active in vitro against Leishmania ssp
and Trypanosoma cruzi at 100 mu g/mL. The activity guided fractionatio
n of the extracts by chromatography afforded 12 active compounds ident
ified as 2-substituted quinoline alkaloids. BALB/c mice were infected
with Leishmania amazonensis (strain PH8 or H-142) and treated 24 h aft
er infection with the major alkaloids from the crude alkaloidal extrac
t; 2-phenylquinoline and 2-n-pentylquinoline. 2-phenylquinoline was as
potent as Glucantime (Rhone-Poulenc) against the strain H-142, but le
ss active than the reference drug against the virulent strain PH8 of L
. amazonensis. 2-n-pentylquinoline did not exhibit any activity. Assay
s of single local treatments on the rear footpad infection, 2 weeks af
ter the parasitic inoculation, indicated an effect for 2-phenylquinoli
ne by reducing the severity of lesion. However, this activity was foun
d to be slightly lower than that obtained using Glucantime.