Plants of Brazilian restingas with tripanocide activity against Trypanosoma cruzi strains

Abstract

Chagas disease is caused by the Trypanosoma cruzi affecting millions of people, and widespread throughout Latin America. This disease exhibits a problematic chemotherapy. Benznidazole, which is the drug currently used as standard treatment, lamentably evokes several adverse reactions. Among other options, natural products have been tested to discover a novel therapeutic drug for this disease. A lot of plants from the Brazilian flora did not contain studies about their biological effects. Restinga de Jurubatiba from Brazil is a sandbank ecosystem poorly studied in relation to plant biological activity. Thus, three plant species from Restinga de Jurubatiba were tested against in vitro antiprotozoal activity. Among six extracts obtained from leaves and stem parts and 2 essential oils derived from leave parts, only 3 extracts inhibited epimastigote proliferation. Substances present in the extracts with activity were isolated (quercetin, myricetin, and ursolic acid), and evaluated in relation to antiprotozoal activity against epimastigote Y and Dm28 Trypanosoma cruzi strains. All isolated substances were effective to reduce protozoal proliferation. Essentially, quercetin and myricetin did not cause mammalian cell toxicity. In summary, myricetin and quercetin molecule can be used as a scaffold to develop new effective drugs against Chagas's disease.

Ursolic acid‐rich extract presents trypanocidal action in vitro but worsens mice under experimental acute Chagas disease

“…Faria et al tested a mixture containing ursolic acid, quercetin and myricetin against epimastigotes forms of T. cruzi (Y). They obtained an inhibition near 80% after 72 h at 10 μg/mL concentration, while the CPE reached similar inhibition in the highest concentration tested (300 μg/mL) 21 . A nanoemulsion of ursolic acid against the amastigotes of T. cruzi reached an IC 50 of 8.22 μg/mL, demonstrating a candidate for trypanocidal drug 22 .…”

“…in the highest concentration tested (300 μg/mL). 21 A nanoemulsion of ursolic acid against the amastigotes of T. cruzi reached an IC 50 of 8.22 μg/mL, demonstrating a candidate for trypanocidal drug. 22 However, the other metabolite found in the CPE extract, β-sitosterol, did not exert antiprotozoal activity, as previously reported in the literature.…”

Actividad tripanocida de cinco plantas latinoamericanas

“…El consumo de plantas medicinales ha sido ampliamente difundido debido a que, existen hasta 5 000 especies con potencial terapéutico; esto para tratar afecciones causadas por microorganismos, entre ellos los parásitos (Pérez-Molphe et al, 2018;Ramírez-Moreno et al, 2017;Sharma et al, 2017). Es por lo antes mencionado, que se han realizado estudios con diferentes partes de las plantas (principalmente corteza, flores, hojas, frutos, y raíces) y usando solventes orgánicos para su extracción con la finalidad de ser evaluadas en contra el parasito T. Cruzi (Abe et al, 2002;Bortoluzzi et al, 2021;Faria et al, 2017;Pérez-Treviño et al, 2017). Sin embargo, una gran cantidad de especies vegetales carecen de registro biológico, como las que se describen a continuación.…”

“…En 2012, Muñoz-Calderón et al evaluó in vitro dichos antiparasitarios en contra de T. cruzi en estadío de epimastigote, encontrando una IC 50 de 2.34 ± 0.72 ppm para Nifurtimox y para el Benznidazol la IC 50 fue de 13.12 ± 2.45 ppm. Así mismo, Faria et al (2017), utilizó el Benznidazol como control positivo en su ensayo tripanocida, encontrando una concentración efectiva 50 de entre 14.63 µg/mL y 16.6 µg/mL. Sin embargo, la distribución de estos medicamentos se encuentra estrictamente regulada por la Secretaría de Salud en México (Callejas et al, 2022), lo que desencadena un difícil acceso (distribución), además se han reportado efectos adversos, debido a la hipersensibilidad a los componentes de la fórmula (Abdel-Sattar et al, 2010; Centro para el Control y Prevención de Enfermedades [CDC], 2023; Jackson et al, 2020).…”

Molluskicidal nanoemulsion of Neomitranthes obscura (DC.) N. Silveira for schistosomiasis control

“…The geographic distribution occurs only in Espírito Santo and Rio de Janeiro in Brazil and is popularly used as food and medicine, mainly for the treatment of intestinal disorders. Some biological activities are known, such as Trypanosoma cruzi proliferation and cholinesterase activity inhibition (Marques, 2001;Ramos et al, 2010;Faria et al, 2017).…”