ArticleMolecules (Basel, Switzerland)2016
ent-Pimarane and ent-Kaurane Diterpenes from Aldama discolor (Asteraceae) and Their Antiprotozoal Activity.
Article in Molecules (Basel, Switzerland), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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11 citing papers in PubMed.
- Epoxidation of ent-pimara-8(14),15-dien-19-oic acid by whole cells of the endophytic fungus Aspergillus sclerotiorum.International microbiology : the official journal of the Spanish Society for Microbiology · 2026Article
- Application of Data-Centric Supervised Machine Learning to Predict Phenotypic Activity Against Clinically Relevant Stages ofPharmaceutics · 2025Article
- Multi-target Compounds against Trypanosomatid Parasites andCurrent drug targets · 2024Review
- Antimicrobial Activity and Molecular Docking Studies of the Biotransformation of Diterpene Acanthoic Acid Using the FungusAntibiotics (Basel, Switzerland) · 2023Article
- Kaurane-Type Diterpenoids as Potential Inhibitors of Dihydrofolate Reductase-Thymidylate Synthase in New WorldAntibiotics (Basel, Switzerland) · 2023Article
- Plant Terpenoids as Hit Compounds against Trypanosomiasis.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Identification of Kaurane-Type Diterpenes as Inhibitors of Leishmania Pteridine Reductase I.Molecules (Basel, Switzerland) · 2021Article
- Pimarane Diterpenoids from the Seeds ofMolecules (Basel, Switzerland) · 2020Article
- Untargeted LC-MS metabolomic studies of Asteraceae species to discover inhibitors of Leishmania major dihydroorotate dehydrogenase.Metabolomics : Official journal of the Metabolomic Society · 2019Article
- Asteraceae Plants as Sources of Compounds Against Leishmaniasis and Chagas Disease.Frontiers in pharmacology · 2019Review
- Anti-Trypanosomatid Elemanolide Sesquiterpene Lactones from Vernonia lasiopus O. Hoffm.Molecules (Basel, Switzerland) · 2017Article
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5 authors.
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Abstract
Aldama discolor (syn.Viguiera discolor) is an endemic Asteraceae from the Brazilian "Cerrado", which has not previously been investigated for its chemical constituents and biological activity. Diterpenes are common secondary metabolites found in Aldama species, some of which have been reported to present potential antiprotozoal and antimicrobial activities. In this study, the known ent-3-α-hydroxy-kaur-16-en-18-ol (1), as well as three new diterpenes, namely, ent-7-oxo-pimara-8,15-diene-18-ol (2), ent-2S,4S-2-19-epoxy-pimara-8(3),15-diene-7β-ol (3) and ent-7-oxo-pimara-8,15-diene-3β-ol (4), were isolated from the dichloromethane extract of A. discolor leaves and identified by means of MS and NMR. The compounds were assayed in vitro against Trypanosoma brucei rhodesiense, T. cruzi and Leishmania donovani, Plasmodium falciparum and also tested for cytotoxicity against mammalian cells (L6 cell line). The ent-kaurane 1 showed significant in vitro activity against both P. falciparum (IC 50 = 3.5 μ M) and L. donovani (IC 50 = 2.5 μ M) and ent-pimarane 2 against P. falciparum (IC 50 = 3.8 μ M). Both compounds returned high selectivity indices (SI >10) in comparison with L6 cells, which makes them interesting candidates for in vivo tests. In addition to the diterpenes, the sesquiterpene lactone budlein A (5), which has been reported to possess a strong anti-T. b. rhodesiense activity, was identified as major compound in the A. discolor extract and explains its high activity against this parasite (100% growth inhibition at 2 μ g/mL).
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