In vitro effects of lapachol and β-lapachone against Leishmania amazonensis
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 na...
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| Format: | Article |
| Language: | English |
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Associação Brasileira de Divulgação Científica
2023-05-01
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| Series: | Brazilian Journal of Medical and Biological Research |
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| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2023000100635&lng=en&tlng=en |
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| author | Á.C.F.H. Ramos-Milaré B.G. Sydor A.Á. Brustolin D.S.S.L. Lera-Nonose J. Oyama E.L. Silva W. Caetano K.S.S. Campanholi I.G. Demarchi T.G.V. Silveira M.V.C. Lonardoni |
| author_facet | Á.C.F.H. Ramos-Milaré B.G. Sydor A.Á. Brustolin D.S.S.L. Lera-Nonose J. Oyama E.L. Silva W. Caetano K.S.S. Campanholi I.G. Demarchi T.G.V. Silveira M.V.C. Lonardoni |
| author_sort | Á.C.F.H. Ramos-Milaré |
| collection | DOAJ |
| description | 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 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. |
| first_indexed | 2024-03-13T08:43:46Z |
| format | Article |
| id | doaj.art-17f3a4b9f6644ce595bec2bc1d555887 |
| institution | Directory Open Access Journal |
| issn | 1414-431X |
| language | English |
| last_indexed | 2024-03-13T08:43:46Z |
| publishDate | 2023-05-01 |
| publisher | Associação Brasileira de Divulgação Científica |
| record_format | Article |
| series | Brazilian Journal of Medical and Biological Research |
| spelling | doaj.art-17f3a4b9f6644ce595bec2bc1d5558872023-05-30T07:33:19ZengAssociação Brasileira de Divulgação CientíficaBrazilian Journal of Medical and Biological Research1414-431X2023-05-015610.1590/1414-431x2023e12693In vitro effects of lapachol and β-lapachone against Leishmania amazonensisÁ.C.F.H. Ramos-Milaréhttps://orcid.org/0000-0001-9068-7958B.G. Sydorhttps://orcid.org/0000-0001-7556-8328A.Á. Brustolinhttps://orcid.org/0000-0001-5051-5369D.S.S.L. Lera-Nonosehttps://orcid.org/0000-0002-6717-6022J. Oyamahttps://orcid.org/0000-0002-9055-4634E.L. Silvahttps://orcid.org/0000-0002-5975-0063W. Caetanohttps://orcid.org/0000-0002-9402-8324K.S.S. Campanholihttps://orcid.org/0000-0001-5156-8542I.G. Demarchihttps://orcid.org/0000-0001-5764-9511T.G.V. Silveirahttps://orcid.org/0000-0002-5527-9358M.V.C. Lonardonihttps://orcid.org/0000-0003-2185-4163Leishmaniasis 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.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2023000100635&lng=en&tlng=enLeishmaniasisCutaneous leishmaniasisLeishmaniaNaphthoquinonesNatural products |
| spellingShingle | Á.C.F.H. Ramos-Milaré B.G. Sydor A.Á. Brustolin D.S.S.L. Lera-Nonose J. Oyama E.L. Silva W. Caetano K.S.S. Campanholi I.G. Demarchi T.G.V. Silveira M.V.C. Lonardoni In vitro effects of lapachol and β-lapachone against Leishmania amazonensis Brazilian Journal of Medical and Biological Research Leishmaniasis Cutaneous leishmaniasis Leishmania Naphthoquinones Natural products |
| title | In vitro effects of lapachol and β-lapachone against Leishmania amazonensis |
| title_full | In vitro effects of lapachol and β-lapachone against Leishmania amazonensis |
| title_fullStr | In vitro effects of lapachol and β-lapachone against Leishmania amazonensis |
| title_full_unstemmed | In vitro effects of lapachol and β-lapachone against Leishmania amazonensis |
| title_short | In vitro effects of lapachol and β-lapachone against Leishmania amazonensis |
| title_sort | in vitro effects of lapachol and β lapachone against leishmania amazonensis |
| topic | Leishmaniasis Cutaneous leishmaniasis Leishmania Naphthoquinones Natural products |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2023000100635&lng=en&tlng=en |
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