Ana Carolina Bolela Bovo Candido, Mariana Cintra Pagotti, Daiane Albino Dos Santos, Lucas Antonio de Lima Paula, Rodrigo Cássio Sola Veneziani, Jairo Kenupp Bastos, Sérgio Ricardo Ambrósio, Lizandra Guidi Magalhães
{"title":"Efficacy of Diterpene Polyalthic Acid Combined with Amphotericin B against <i>Leishmania amazonensis</i> In Vitro.","authors":"Ana Carolina Bolela Bovo Candido, Mariana Cintra Pagotti, Daiane Albino Dos Santos, Lucas Antonio de Lima Paula, Rodrigo Cássio Sola Veneziani, Jairo Kenupp Bastos, Sérgio Ricardo Ambrósio, Lizandra Guidi Magalhães","doi":"10.3390/ph17091243","DOIUrl":null,"url":null,"abstract":"<p><p><b>Background/Objectives:</b> Leishmaniasis, a neglected disease caused by <i>Leishmania</i> spp. including <i>L. amazonensis</i>, urgently requires new treatments. Polyalthic acid (PA), a natural diterpene from <i>Copaifera</i> spp., has previously demonstrated significant antiparasitic potential. This study evaluated the leishmanicidal effects of polyalthic acid (PA), alone and with amphotericin B (AmpB), on <i>L. amazonensis</i> promastigote and amastigote forms. <b>Results:</b> PA showed significant activity against promastigotes, with 50% effective concentration (EC<sub>50</sub>) values of 2.01 μM at 24 h and an EC<sub>50</sub> of 3.22 μM against amastigotes after 48 h. The PA and AmpB combination exhibited a synergistic effect on both forms without inducing cytotoxicity or hemolysis. Morphological changes in promastigotes, including vacuole formation and cell rounding, were more pronounced with the combination. <b>Conclusions:</b> These findings suggest that PA and AmpB together could form a promising new treatment strategy against <i>Leishmania</i> infections, offering enhanced efficacy without added toxicity.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":4.3000,"publicationDate":"2024-09-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11434928/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceuticals","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.3390/ph17091243","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Background/Objectives: Leishmaniasis, a neglected disease caused by Leishmania spp. including L. amazonensis, urgently requires new treatments. Polyalthic acid (PA), a natural diterpene from Copaifera spp., has previously demonstrated significant antiparasitic potential. This study evaluated the leishmanicidal effects of polyalthic acid (PA), alone and with amphotericin B (AmpB), on L. amazonensis promastigote and amastigote forms. Results: PA showed significant activity against promastigotes, with 50% effective concentration (EC50) values of 2.01 μM at 24 h and an EC50 of 3.22 μM against amastigotes after 48 h. The PA and AmpB combination exhibited a synergistic effect on both forms without inducing cytotoxicity or hemolysis. Morphological changes in promastigotes, including vacuole formation and cell rounding, were more pronounced with the combination. Conclusions: These findings suggest that PA and AmpB together could form a promising new treatment strategy against Leishmania infections, offering enhanced efficacy without added toxicity.