Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i>
Leishmaniasis is a neglected tropical disease caused by protozoan parasites of the genus <i>Leishmania</i>. An estimated 700,000 to 1 million new cases occur annually. Current therapies are limited by high toxicity, cost, prolonged treatment period, and rising resistance in endemic regio...
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2025-02-01
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| author | Rachel Nápoles Rodríguez María Laura Arreguez Aldana M. Corlatti Hernán G. Bach César A. N. Catalán Laura C. Laurella Paola A. Barroso Valeria P. Sülsen |
| author_facet | Rachel Nápoles Rodríguez María Laura Arreguez Aldana M. Corlatti Hernán G. Bach César A. N. Catalán Laura C. Laurella Paola A. Barroso Valeria P. Sülsen |
| author_sort | Rachel Nápoles Rodríguez |
| collection | DOAJ |
| description | Leishmaniasis is a neglected tropical disease caused by protozoan parasites of the genus <i>Leishmania</i>. An estimated 700,000 to 1 million new cases occur annually. Current therapies are limited by high toxicity, cost, prolonged treatment period, and rising resistance in endemic regions. The Asteraceae family has emerged as a promising source of bioactive compounds with proven leishmanicidal activity. In this study, the assessment of the antileishmanial activity of <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> extracts, the isolation of the sesquiterpene lactones heliangin and glaucolide A, respectively, and the evaluation of the activity of the compounds were conducted. Dichloromethane extracts of <i>H. tuberosus</i> and <i>V. squamulosa</i> were active on <i>Leishmania amazonensis</i> promastigotes, inhibiting the replication of the parasites in 97.2 ± 3.1% and 89.1 ± 1.1%, respectively, at 100 μg/mL. Heliangin was active against promastigotes of <i>L. amazonensis</i> (IC<sub>50</sub> = 9.3 μM) and intracellular amastigotes (IC<sub>50</sub> = 0.8 μM), while glaucolide A exhibited moderate activity against promastigotes (IC<sub>50</sub> = 46.7 μM) and did not show activity against intracellular amastigotes. Based on these results, heliangin was further evaluated in an animal model of cutaneous leishmaniasis using BALB/c mice infected with <i>L. amazonensis</i>. Heliangin (8 mg/Kg), when administered in combination with Glucantime, significantly reduced lesion progression and parasite load compared to the vehicle-treated group (<i>p</i> < 0.001). These findings show that heliangin is a potential candidate for leishmaniasis treatment, especially in combination with therapeutic drugs. |
| format | Article |
| id | doaj-art-80f10a16244b454d97c39b07482a7be5 |
| institution | DOAJ |
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| spelling | doaj-art-80f10a16244b454d97c39b07482a7be52025-08-20T02:53:21ZengMDPI AGMolecules1420-30492025-02-01305103910.3390/molecules30051039Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i>Rachel Nápoles Rodríguez0María Laura Arreguez1Aldana M. Corlatti2Hernán G. Bach3César A. N. Catalán4Laura C. Laurella5Paola A. Barroso6Valeria P. Sülsen7CONICET-Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Autonomous City of Buenos Aires C1113AAD, ArgentinaCONICET-Universidad Nacional de Salta, Instituto de Patología Experimental (IPE), Salta A4400, ArgentinaCONICET-Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Autonomous City of Buenos Aires C1113AAD, ArgentinaInstituto Nacional de Tecnología Agropecuaria, Buenos Aires B1686, ArgentinaInstituto de Química Orgánica, Facultad de Bioquímica, Química y Farmacia, Universidad Nacional de Tucumán, San Miguel de Tucumán, Tucumán T4000INI, ArgentinaCONICET-Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Autonomous City of Buenos Aires C1113AAD, ArgentinaCONICET-Universidad Nacional de Salta, Instituto de Patología Experimental (IPE), Salta A4400, ArgentinaCONICET-Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Autonomous City of Buenos Aires C1113AAD, ArgentinaLeishmaniasis is a neglected tropical disease caused by protozoan parasites of the genus <i>Leishmania</i>. An estimated 700,000 to 1 million new cases occur annually. Current therapies are limited by high toxicity, cost, prolonged treatment period, and rising resistance in endemic regions. The Asteraceae family has emerged as a promising source of bioactive compounds with proven leishmanicidal activity. In this study, the assessment of the antileishmanial activity of <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> extracts, the isolation of the sesquiterpene lactones heliangin and glaucolide A, respectively, and the evaluation of the activity of the compounds were conducted. Dichloromethane extracts of <i>H. tuberosus</i> and <i>V. squamulosa</i> were active on <i>Leishmania amazonensis</i> promastigotes, inhibiting the replication of the parasites in 97.2 ± 3.1% and 89.1 ± 1.1%, respectively, at 100 μg/mL. Heliangin was active against promastigotes of <i>L. amazonensis</i> (IC<sub>50</sub> = 9.3 μM) and intracellular amastigotes (IC<sub>50</sub> = 0.8 μM), while glaucolide A exhibited moderate activity against promastigotes (IC<sub>50</sub> = 46.7 μM) and did not show activity against intracellular amastigotes. Based on these results, heliangin was further evaluated in an animal model of cutaneous leishmaniasis using BALB/c mice infected with <i>L. amazonensis</i>. Heliangin (8 mg/Kg), when administered in combination with Glucantime, significantly reduced lesion progression and parasite load compared to the vehicle-treated group (<i>p</i> < 0.001). These findings show that heliangin is a potential candidate for leishmaniasis treatment, especially in combination with therapeutic drugs.https://www.mdpi.com/1420-3049/30/5/1039Asteraceaesesquiterpene lactones<i>Leishmania amazonensis</i>in vitro and in vivo assays |
| spellingShingle | Rachel Nápoles Rodríguez María Laura Arreguez Aldana M. Corlatti Hernán G. Bach César A. N. Catalán Laura C. Laurella Paola A. Barroso Valeria P. Sülsen Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> Molecules Asteraceae sesquiterpene lactones <i>Leishmania amazonensis</i> in vitro and in vivo assays |
| title | Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> |
| title_full | Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> |
| title_fullStr | Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> |
| title_full_unstemmed | Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> |
| title_short | Bioactive Compounds with Leishmanicidal Potential from <i>Helianthus tuberosus</i> and <i>Vernonanthura squamulosa</i> |
| title_sort | bioactive compounds with leishmanicidal potential from i helianthus tuberosus i and i vernonanthura squamulosa i |
| topic | Asteraceae sesquiterpene lactones <i>Leishmania amazonensis</i> in vitro and in vivo assays |
| url | https://www.mdpi.com/1420-3049/30/5/1039 |
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