Produção Nacional
Revisado por pares
In vitro effects of lapachol and β-lapachone against Leishmania amazonensis
2023; Associação Brasileira de Divulgação Científica; Volume: 56; Linguagem: Inglês
10.1590/1414-431x2023e12693
ISSN1414-431X
AutoresÁquila Carolina Fernandes Herculano Ramos‐Milaré, Bruna Gomes Sydor, Aline Ávila Brustolin, Daniele Stéfanie Sara Lopes Lera‐Nonose, Jully Oyama, Expedito Leite Silva, Wilker Caetano, K.S.S. Campanholi, Izabel Galhardo Demarchi, Thaís Gomes Verzignassi Silveira, Maria Valdrinez Campana Lonardoni,
Tópico(s)Synthesis and Biological Evaluation
ResumoLeishmaniasis is a neglected disease that affects millions of people worldwide, and special attention should be given to treatment because the available drugs have limitations, which can lead to low therapeutic adherence and parasitic resistance. This study evaluated the activity of the bioactive naphthoquinones, lapachol and β-lapachone, against Leishmania amazonensis. The cell alterations were evaluated in vitro on promastigote and amastigote forms. The lethal dose (LD50) at 24, 48, and 72 h on the promastigote's forms using lapachol was 75.60, 72.82, and 58.85 μg/mL and for β-lapachone was 0.65, 1.24, and 0.71 μg/mL, respectively. The naphthoquinones significantly inhibited the survival rate of L. amazonensis amastigotes at 83.11, 57.59, and 34.95% for lapachol (82.28, 41.14, and 20.57 µg/mL), and 78.49, 83.25, and 80.22% for β-lapachone (3.26, 1.63, and 0.815 µg/mL). The compounds on the promastigote's forms led to the loss of mitochondrial membrane potential, induced changes in the integrity of the membrane, caused damage to cells suggestive of the apoptotic process, and showed inhibition of tumor necrosis factor (TNF)-α and interleukin (IL)-6 production. The results showed that these naphthoquinones are promising candidates for research on new drugs with anti-Leishmania activity derived from natural products.
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