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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| Main Authors: | , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-02-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/30/5/1039 |
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| Summary: | 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. |
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| ISSN: | 1420-3049 |