RESUMO
Lantana camara (L.) is employed by several ethnical groups to treat numerous diseases. Although there are no ethnomedical reports on its use against leishmaniasis, organic extracts prepared from L. camara were shown to display leishmanicidal activity. In the present study, we carried out a bioassay-guided fractionation of the dichloromethane extract from Mexican L. camara in order to identify the compounds responsible for the leishmanicidal activity. Eighteen chromatographic fractions (FIâ»FXVIII) were evaluated in vitro against Leishmania mexicana and L. amazonensis. FII, FX, FXI, FXV, and FXVI showed significant activity against both Leishmania strains, the most potent of which was FXV. Eicosane (1), squalene (2), ß-ionone (3), caryophyllene oxide (4), ß-caryophyllene (5), hexanoic acid (6), tiglic acid (7), a mixture of lantanilic (8) and camaric (9) acids, and lantadene B (10) were identified and obtained from the active fractions and evaluated for their leishmanicidal activity. The mixture of lantanilic (8) and camaric (9) acids (79%/21%) was the most potent one (half maximal inhibitory concentration (IC50) = 12.02 ± 0.36 µM). This study indicates that this cultivar of L. camara has high potential for the development of phytomedicines or as a source of natural products, which might represent lead compounds for the design of new drugs against leishmaniasis.
Assuntos
Antiprotozoários/farmacologia , Lantana/química , Leishmania/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Animais , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Morte Celular/efeitos dos fármacos , Misturas Complexas/farmacologia , Concentração Inibidora 50 , México , Camundongos Endogâmicos BALB C , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificaçãoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Cleoserrata serrata (Jacq.) Iltis are widely used in South-Central Mexico to treat wounds and bacterial skin infections and in Panama by Kuna, Ngöbe-Buglé, and Teribe Indians for tropical warm baths and by Kunas in the form of "Ina kuamakalet" for snakebites. AIMS OF THE STUDY: To evaluate the effect of Cleoserrata serrata extract on growth and viability of L. mexicana amastigotes and promastigotes in vitro, as well as on bacteria that usually co-infect skin ulcers. MATERIALS AND METHODS: Cleoserrata serrata was collected in La Chontalpa, Tabasco, Mexico. The antiproliferative effect of the extract was tested on growth of Leishmania mexicana amastigotes and promastigotes in vitro, as well as on bacteria that usually co-infect skin ulcers. RESULTS: Our data show that Cleoserrata serrata significantly inhibits parasite growth (which was more important in infective amastigotes) and additionally inhibits growth of the co-infective bacteria Staphylococcus aureus and Pseudomonas aeruginosa. Confocal microscopy showed a leishmanicidal effect. CONCLUSION: We conclude that Cleoserrata serrata extract is potentially an optimal treatment alternative for patients with cutaneous leishmaniasis infected with Leishmania mexicana, since it controls both the parasite as well as bacterial co-infections. Furthermore, it can be applied topically. The precise metabolites responsible for the anti-Leishmania and anti-bacterial effects remain to be established.
Assuntos
Antibacterianos/farmacologia , Antiprotozoários/farmacologia , Leishmania mexicana/efeitos dos fármacos , Magnoliopsida , Extratos Vegetais/farmacologia , Animais , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Escherichia coli/efeitos dos fármacos , Escherichia coli/crescimento & desenvolvimento , Humanos , Leishmania mexicana/crescimento & desenvolvimento , Leishmaniose Cutânea , Camundongos Endogâmicos BALB C , Folhas de Planta , Raízes de Plantas , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/crescimento & desenvolvimento , Saccharomyces cerevisiae/efeitos dos fármacos , Saccharomyces cerevisiae/crescimento & desenvolvimento , Sementes , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/crescimento & desenvolvimentoRESUMO
This study focused on the assessment of the vasorelaxant activity of the organic and aqueous extracts obtained from leaves and fruits of a Mexican hawthorn (Crataegus gracilior) on isolated rat aorta, and on the purification and identification of some of their secondary metabolites by the use of chromatographic and spectroscopic techniques. The results obtained showed that the methanol extract has a significantly more potent and effective vasorelaxant effect than the other tested extracts, with an EC50 = 8.69 ± 4.34 µg/mL and an Emax = 94.6% ± 11.30%, values that are close to that of acetylcholine, the positive control. From the same extract, two major triterpenes were isolated and identified as ursolic and corosolic acids by comparison of their experimental NMR spectroscopic data with those reported in the literature. Chlorogenic acid, rutin, quercetin, kaempferol and (+)-catechin were also identified using HPLC coupled with PDAD. All these compounds have already been proven to possess on their own antihypertensive effect and other benefits on cardiovascular diseases and they can support, at least in part, the traditional use of this plant species.