São Paulo State University (UNESP), School of Sciences, Humanities and Languages, Department of Biotechnology, Laboratory of Herbal Medicine and Natural Products, Assis, São Paulo, Brazil; São Paulo State University (UNESP), Institute of Chemistry, Araraquara, São Paulo, Brazil.
São Paulo State University (UNESP), School of Sciences, Humanities and Languages, Department of Biotechnology, Laboratory of Herbal Medicine and Natural Products, Assis, São Paulo, Brazil.
J Ethnopharmacol. 2025 Jan 30;337(Pt 2):118994. doi: 10.1016/j.jep.2024.118994. Epub 2024 Oct 24.
Mandevilla velutina (Mart. Ex Stadelm.) Woodson, known in Brazil as "infalível" and "jalapa", is a medicinal plant native from the Cerrado region (Brazilian Savannah). The underground organ (xylopodium) of this species is prepared as ethanolic extract or infusion and it is commonly used in traditional medicine to treat snake venom. Although, locals and indigenous populations from Cerrado have used M. velutina for the treatment of infection by Trypanosoma cruzi (Chagas' disease).
This study aimed to evaluate the in vitro antioxidant and anti-glycation activities of the crude hydroethanolic extract of M. velutina xylopodium. Besides, it aimed to evaluate its effect on parasitemia levels in vivo T. cruzi experimental infection. In addition, this study aimed to determine possible interactions between the main compound of the extract and molecular targets associated with survival and virulence of T. cruzi in silico approaches.
Determination of total polyphenols, flavonoids and steroidal aglycones content were performed. In addition, high performance liquid chromatography (HPLC) was carried out to identify main compounds of the extract. Antioxidant activity was determined by DPPH radical scavenging, ferric ion reducing power (FRAP), Thiobarbituric acid reactive species (TBARS) and Oxygen Radical Absorbance Capacity (ORAC) methods. Anti-glycation activity was demonstrated through relative mobility in electrophoresis (RME), determination of free amino groups and inhibition of AGEs formation. Determination of the action of extract in parasitemia levels was performed by T. cruzi experimental infection of mice and nitrite levels were measured in the serum of animals evaluated in this study. Molecular docking analyses of the main compound (Velutinol A) with DNA and molecular targets associated with survival and virulence of T. cruzi.
Phytoconstituents evaluation exhibited the presence polyphenols, flavonoids and steroidal aglycone, and HPLC identified the major presence of Velutinol A. Antioxidant and anti-glycation evaluations showed that the extract present significant activity in all methods evaluated. In addition, extract reduced the number of trypomastigotes and increased the survival of treated animals. The treatment using extract showed an interference in the synthesis of physiological nitric oxide as an immune response to infection. In silico assays demonstrated interaction between Velutinol A and DNA and molecular targets of T. cruzi.
The results showed that the hydroethanolic extract of M. velutina xylopodium contains bioactive compounds including polyphenols, flavonoids and steroidal aglycones (mainly Velutinol A) of which may be responsible for the antioxidant, anti-glycation and anti-parasitic activity against T. cruzi. Trypanocidal activity of M. velutina compounds may be linked to their influence on NO synthesis during infection and/or their capacity to bind and inhibit molecules associated to virulence and survival of T. cruzi.
曼德维拉·维鲁蒂娜（Mart. Ex Stadelm.）伍德森，在巴西被称为“infalível”和“jalapa”，是一种来自塞拉多地区（巴西稀树草原）的药用植物。该物种的地下器官（木栓质）被制成乙醇提取物或浸液，常用于传统医学治疗蛇毒。尽管如此，塞拉多地区的当地人以及土著居民也使用曼德维拉·维鲁蒂娜来治疗克氏锥虫（恰加斯病）感染。
本研究旨在评估曼德维拉·维鲁蒂娜木栓质的粗水醇提取物的体外抗氧化和抗糖化活性。此外，还旨在评估其对体内克氏锥虫实验感染时寄生虫血症水平的影响。此外，本研究旨在通过计算机模拟方法确定提取物的主要化合物与克氏锥虫存活和毒力相关的分子靶标之间的可能相互作用。
测定总多酚、类黄酮和甾体糖苷元的含量。此外，还进行了高效液相色谱（HPLC）以鉴定提取物的主要化合物。通过 DPPH 自由基清除、铁离子还原能力（FRAP）、硫代巴比妥酸反应性物质（TBARS）和氧自由基吸收能力（ORAC）方法测定抗氧化活性。通过电泳（RME）中的相对迁移率、测定游离氨基基团和抑制 AGEs 形成来证明抗糖化活性。通过克氏锥虫实验感染小鼠来确定提取物在寄生虫血症水平中的作用，并测量动物血清中的亚硝酸盐水平。对主要化合物（Velutinol A）与 DNA 和与克氏锥虫存活和毒力相关的分子靶标的分子对接分析。
植物成分评价显示存在多酚、类黄酮和甾体糖苷元，HPLC 鉴定出 Velutinol A 的主要存在。抗氧化和抗糖化评价表明，该提取物在所有评估方法中均表现出显著的活性。此外，提取物减少了锥虫数量并提高了治疗动物的存活率。该提取物的治疗作用显示出对生理一氧化氮的合成有干扰，这是对感染的免疫反应。计算机模拟试验表明 Velutinol A 与 DNA 和克氏锥虫的分子靶标之间存在相互作用。
结果表明，曼德维拉·维鲁蒂娜木栓质的水醇提取物含有生物活性化合物，包括多酚、类黄酮和甾体糖苷元（主要是 Velutinol A），这些化合物可能是其具有抗氧化、抗糖化和抗克氏锥虫活性的原因。曼德维拉·维鲁蒂娜化合物的杀锥虫活性可能与其对感染期间一氧化氮合成的影响有关，或者与其结合和抑制与克氏锥虫毒力和存活相关的分子的能力有关。
