Journal
BRAZILIAN JOURNAL OF MEDICAL AND BIOLOGICAL RESEARCH
Volume 56, Issue -, Pages -Publisher
ASSOC BRAS DIVULG CIENTIFICA
DOI: 10.1590/1414-431X2023e12693
Keywords
Leishmaniasis; Cutaneous leishmaniasis; Leishmania; Naphthoquinones; Natural products
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This study evaluated the activity of bioactive naphthoquinones against Leishmania amazonensis and found that they significantly inhibited the survival rate of the parasite and induced changes in cell function. These naphthoquinones may be promising candidates for research on new drugs with anti-Leishmania activity derived from natural products.
Leishmaniasis 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 p-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 mu g/mL and for p-lapachone was 0.65, 1.24, and 0.71 mu g/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 mu g/mL), and 78.49, 83.25, and 80.22% for p-lapachone (3.26, 1.63, and 0.815 mu g/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)-a 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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