In vivo activity of (8-hydroxymethylen)-trieicosanyl acetate against Trypanosoma cruzi during acute phase of the infection.

The antiprotozoal activity in vivo against Trypanosoma cruzi of (8-hydroxymethylen)-trieicosanyl acetate was evaluated in BALB/c mice during the acute phase of Chagas' disease (15 days after infection). Animals were treated during 15 days at doses of 16.8 and 33.6 µg/g, reduced parasitemia of 77.6 and 64.1% was observed respectively, in comparison with positive control mice (allopurinol 8.5 µg/g) which reduced only 29.7%. Also, amastigote nests in cardiac tissue were significant reduced in treated mice groups. The regression of effect induced after the suppression of the treatment with the compound was evaluated; animals were infected and simultaneously began the treatment with the compound during 20 days (16.8 and 33.6 µg/g). Mice were monitored after the end of the treatment for one more week. A good antitrypanosomal response was observed (66.1 and 68.9% less than untreated mice) during treatment, but 8 days after suspension of treatment, parasitemia level increased, reducing only 58.6 and 56.29 % respectively in treated animals compared with no treated.

Anti-trypanosomal activity of (8-hydroxymethylen)-trieicosanyl acetate against infective forms of Trypanosoma cruzi.

The activity of an (8-hydroxymethylen)-trieicosanyl acetate compound obtained from chloroform extracts of Senna villosa (Mill.) H.S. Irwin & Barneby (Leguminosae) against Trypanosoma cruzi was evaluated in vivo. Oral doses of 2.1, 8.4, and 33.6 microg/g were tested for 28 days in BALB/c mice infected with T. cruzi. Reduced parasitemia levels of 70.5%, 73.8%, and 80.9%, respectively, were observed. A significant reduction in amastigote nests was detected in the cardiac tissue of treated animals at doses of 8.4 and 33.6 microg/g. The LD50 of (8-hydroxymethylen)-trieicosanyl acetate was impossible to determine because none of the animals died, even at oral doses of 5000 microg/g; consequently, it was impossible to determine the acute oral toxicity in vivo.

Antiprotozoal activity of (8-hydroxymethylen)-trieicosanyl acetate isolated from Senna villosa.

A white solid compound was isolated from the chloroform extract of the leaves of Senna villosa. The material was identified by (1)H-NMR, (13)C-NMR, IR and EM methods as (8-hydroxymethylen)-trieicosanyl acetate, a new compound with biological activity, which was tested in vitro at concentrations of 1.65, 3.3 and 6.6 microg/ml for inhibition of the growth of Trypanosoma cruzi epimastigotes and tripomastigotes. We observed inhibition of growth at all concentrations tested, and the effect at concentrations of 3.3 and 6.6 microg/ml was greater than that of gentian violet (positive control). At the concentration of 6.6 microg/ml, the compound showed the greatest inhibitory effect against the growth of both forms of the parasite.

[Studies on chemical constituents from the root of Mirablis jalapa].

OBJECTIVE: To investigate the chemical constituents from the root of Mirabilis jalapa. METHOD: Compounds were isolated from 75% ethanolic extract of the titled herb by silica gel column chromatography, and their structures were elucidated by physical and chemical evidences and spectroscopic analysis. RESULT: Four compounds were obtained and identified as (2, 5-dioxoimidazolidin-4-yl)-urea (1), glycerin monoeicosate (2), boeravinone (3) and beta-sitosterol (4). CONCLUSION: Compound (2) is a new compound, and compound (1) was obtained from this plant for the first time.