RESUMO
Onchocerciasis caused by Onchocerca volvulus Leuckart, 1893 is the second-world infection responsible for human blindness. Except Ivermectin which has as targets the microfilariae of that parasite, specific treatment for this disease does not exist and in developing countries, medicinal plants seem to remedy that health problem. For that, aqueous and hydro-ethanolic leaf, bark, and root extracts of Calotropis procera and Faidherbia albida were evaluated in vitro, against the most popular bovine model, Onchocerca ochengi and the free-resistant nematode Caenorhabditis elegans. O. ochengi microfilariae and adults extracted from the bovine nodules and skins as well as the free strains of C. elegans were exposed to the various concentrations of the plant parts extracts and Ivermectin. In results, all the plant parts extracts were rich in tannins, saponins, alkaloids, flavonoids, phenols, coumarins, and glycosides. Phenols (175.45 ± 0.01 mg EGA/g DM), flavonoids (158.98 ± 0.05 mg EC/g DM), and tannins (89.98 ± 2.56 mg ETA/g DM) contents were high in the bark hydro-ethanolic extract of F. albida. The leaf hydro-ethanolic extract of F. albida induced high activity against O. ochengi microfilariae (CL50 = 0.13 mg/mL). The bark hydro-ethanolic extract of F. albida was also the most effective on O. ochengi adults and particularly on female adults (CL50 = 0.18 mg/mL). Against the parasite strain resistant to Ivermectin, F. albida leaf hydro-ethanolic extract appeared more active with CL50 = 0.13 mg/mL. Similarly, the bark hydro-ethanolic extract of F. albida was the most potent on the wild strain of C. elegans. Thus, this study validates the use of these plants by traditional healers in the management of onchocerciasis and suggests a new source of isolation of the potential plant compounds against Onchocerca.
RESUMO
Phytochemical investigation of the rhyzomes of Rumex abyssinicus (Polygonaceae) afforded six anthraquinones viz chrysophanol (1), physcion (2), emodin (3), mixture of physcion-8-O-ß,D-glucopyranoside (4) and chrypsophanol-8-O-ß,D-glucopyranoside (5), and emodin-8-O-ß,D-glucopyranoside (6). All the compounds were characterised and identified by comparison of their MS and NMR data with available literature data. The isolated compounds were evaluated for their antileishmanial activity. Emodin (3) was the most active compounds with IC50 13.82 and 0.26 µg/mL against Leishmania donovani amastigotes and promastigotes, respectively. Emodin-8-O-ß,D-glucopyranoside (6) also showed a moderate activity with IC50 27.53 and 37.08 µg/mL. This is the first report of antileishmanial compounds from R. abyssinicus and the antileishmanial activities of compounds 2, 4, 5 and 6 are here reported for the first time.
RESUMO
Two new compounds, an isoquinoline (1) and caloneuramide (2), a ceramide were isolated from the stem bark of Discoglypremna caloneura together with seven known compounds namely aurantiamide acetate (3), acetylaleuritolic acid (4), 3α-hydroxylaleuritolic acid 2α-p-hydroxybenzoate (5), mixture of stigmasterol (6) and ß-sitosterol (7), mixture of 7-oxo-stigmasterol (8) and 7-oxo-ß-sitosterol (9). Their structures were determined based on data from literature and spectroscopic methods. Derivatization reactions on the isoquinoline led to two new compounds, the methylated (10) and acetylated (11) derivatives. Some compounds and extracts were evaluated for their cytotoxic and antiproteinase activity. Antiproteinase effect of compounds 1, 10 and 11 exhibited IC50 values of 10.77, 1.19 and 3.61 µg/mL respectively; significantly low compared to the standard drug, acetyl salicylic acid (IC50 = 20.28 µg/mL). Ethyl acetate and methanol extract exhibited moderate cytotoxicity activity on Chang liver cells with CC50 values of 167.90 ± 2.20 and 106.30 ± 2.03 µg/mL compared to the reference drug cucurmin (CC50 = 11.05 ± 1.04 µg/mL).
Assuntos
Euphorbiaceae , Ceramidas/farmacologia , Euphorbiaceae/química , Isoquinolinas , Casca de Planta/química , Extratos Vegetais/química , Estigmasterol/análiseRESUMO
BACKGROUND: Within the framework to control mosquitoes, ovicidal, larvicidal and pupicidal activity of Annona senegalensis leaf extract and its 4 fractions against Anopheles gambiae and Culex quinquefasciatus were evaluated in the laboratory conditions. METHODS: Ovicidal test was performed by submitting at least 100 eggs of mosquitoes to 125, 250, 500, 1000 and 2000 ppm concentrations, while larvicidal and pupicidal effects were assessed by submitting 25 larvae or pupae to the concentrations of 2500, 1250, 625 and 312.5 ppm of plant extract or fractions of A. senegalensis. RESULTS: The eggs of An. gambiae were most affected by N-hexane (0.00% hatchability) and chloroform (03.67% hatchability) fractions compared to Cx. quinquefasciatus where at least 25 % hatchability were recorded at 2000 ppm. For larvicidal test, N-hexane (LC50= 298.8 ppm) and chloroform (LC50= 418.3 ppm) fractions were more effective than other fractions on An. gambiae larvae while, a moderate effectiveness was also observed with N-hexane (LC50= 2087.6 ppm), chloroform (LC50= 9010.1 ppm) fractions on Cx. quinquefasciatus larvae. The highest mortality percent of the pupae were also recorded with N-hexane and chloroform fractions on An. gambiae at 2500 ppm. As for Cx. quinquefasciatus only 50 % and 36 % mortality were recorded with N-hexane and chloroform fractions respectively. CONCLUSION: The extract of A. senegalensis was toxic on immature stage of mosquito species tested. By splitting methanolic crude extract, only N-hexane and chloroform fractions were revealed to possess a mosquitocidal effects and could be considered and utilized for future immature mosquito vectors control.
