ABSTRACT
Currently, in developing countries, parasitic and bacterial diseases as amebiasis, giardiasis, trichonomiasis, leishmaniasis, trypanosomiasis, tuberculosis, and nocardiasis are a public health problem. The pharmacological treatment for these diseases is not completely effective and causes several side effects in patients. Therefore, the search for new compounds with biological activity is very important to develop new drugs safely and more efficiently. In this study, different organic extracts obtained from thirty-seven species of the Salvadoran flora were evaluated in several in vitro models to determine their potential activity against five protozoa (Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis, Leishmania mexicana, and Trypanosoma cruzi) and three bacteria (Acinetobacter baumanni, Mycobacterium tuberculosis, and Nocardia brasiliensis). The results showed the activity of eight extracts with IC50values of less than 100 µg/mL against L. mexicanaand five extracts with MICs values less than <50 µg/mL against M. tuberculosis. Besides, seven plant species showed MICs ≤3.125 µg/mL against N. brasiliensis. Additionally, secondary metabolites (flavonoids and monoterpene oxygenate) previously reported as active were fingerprint by UPLC-MS to establish a potential correlation with the biological activity showed.
Actualmente, en los países en vías de desarrollo, enfermedades parasitarias y bacterianas como la amebiasis, giardiasis, trichonomiasis, leishmaniasis, tripanosomiasis, tuberculosis y nocardiasis son un problema de salud pública. El tratamiento farmacológico de estas enfermedades no es del todo eficaz y provoca varios efectos secundarios en los pacientes. Por lo tanto, la búsqueda de nuevos compuestos con actividad biológica es muy importante para desarrollar nuevos fármacos, seguros y eficaces. En este estudio se evaluaron diferentes extractos orgánicos obtenidos de treinta y siete especies de la flora salvadoreña en varios modelos in vitro para determinar su actividad potencial contra cinco parásitos (Entamoeba histolytica, Giardia lamblia, Trichomonas vaginalis, Leishmania mexicana y Trypanosoma cruzi) y tres bacterias (Acinetobacter baumanni, Mycobacterium tuberculosis y Nocardia brasiliensis). Los resultados mostraron la actividad de ocho extractos con valores de CI50 menores a 100 µg/mL contra L. mexicana y cinco extractos con valores de CIMs <50 µg/mL contra M. tuberculosis. Además, siete especies de plantas presentaron CIM ≤3,125 µg/mL frente a N. brasilienses. Finalmente, los metabolitos secundarios (flavonoides y monoterpenos oxigenados) previamente reportados como activos fueron determinados por UPLC-MS para establecer una posible correlación con la actividad biológica mostrada.
Subject(s)
Plant Extracts/pharmacology , Flora , Anti-Bacterial Agents/therapeutic use , Antiparasitic Agents/therapeutic use , Plants, Medicinal , Communicable Diseases/drug therapy , El SalvadorABSTRACT
AbstractAphelandra scabra (Vahl) Sm., Acanthaceae, is a shrub widely used by some Mayan communities as carminative, antidote, and remedy for some infections. Bio-guided isolation of the methanol extract of leaves led us to the purification of the anti-giardial metabolites cirsimaritin and sorbifolin, along with the inactive metabolites cirsimarin, sorbifolin-6-O-β-glucopyranoside, and squalene. Cirsimaritin displayed high activity in the anti-giardial bioassay with an IC50 = 3.8 μM, being considered as outstanding when compared to previous reported metabolites, while sorbifolin showed a low activity with an IC50 = 75.6 μM. Additionally, both compounds proved not to be cytotoxic in an in vitro bioassay against HEK-293, a normal cell line. This is the first investigation on anti-giardial properties of A. scabra and its phytochemistry as well, thus the isolated compounds are considered as new for the plant genus and for the species.