ArticleMalaria journal2014
Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
Article in Malaria journal, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers, 1 of them a synthesis that pooled it.
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Who cites it
13 citing papers in PubMed, 1 synthesis or guideline pooled it, 55 citations in OpenAlex.
- Use of Brazilian flora as the main source of new antimalarials: a systematic review.Memorias do Instituto Oswaldo Cruz · 2025Pooled it
- Design, Synthesis, and Evaluation of Halogenated Indoles Amines as Acetylcholinesterase Inhibitors: Integrated In-Vitro and In-Silico Approaches.Chemistry & biodiversity · 2026Article
- In silico ligand self-assembly drives binding recognition of natural products intoIn silico pharmacology · 2025Article
- Strychnos alkaloids: total synthesis, characterization, DFT investigations, and molecular docking with AChE, BuChE, and HSA.Heliyon · 2022Article
- Antihypertensive Activity of the Alkaloid Aspidocarpine in Normotensive Wistar Rats.Molecules (Basel, Switzerland) · 2022Article
- Nutritional and Phytochemical Variation of Marula (International journal of food science · 2022Article
- Biosynthesis and synthetic biology of psychoactive natural products.Chemical Society reviews · 2021Review
- Studies on Activities and Chemical Characterization of Medicinal Plants in Search for New Antimalarials: A Ten Year Review on Ethnopharmacology.Frontiers in pharmacology · 2021Review
- Role of Melatonin in the Synchronization of Asexual Forms in the ParasiteBiomolecules · 2020Review
- Antiplasmodial natural products: an update.Malaria journal · 2019Review
- Aspidosperma pyrifolium, a medicinal plant from the Brazilian caatinga, displays a high antiplasmodial activity and low cytotoxicity.Malaria journal · 2018Article
- Aspidosperma species as sources of anti-malarials: uleine is the major anti-malarial indole alkaloid from Aspidosperma parvifolium (Apocynaceae).Malaria journal · 2015Article
- Amino acid-derived defense metabolites from plants: A potential source to facilitate novel antimicrobial development.The Journal of biological chemistryReview
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7 authors at 2 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
backgroundSeveral species of Aspidosperma (Apocynaceae) are used as treatments for human diseases in the tropics. Aspidosperma olivaceum, which is used to treat fevers in some regions of Brazil, contains the monoterpenoid indole alkaloids (MIAs) aspidoscarpine, uleine, apparicine, and N-methyl-tetrahydrolivacine. Using bio-guided fractionation and cytotoxicity testing in a human hepatoma cell line, several plant fractions and compounds purified from the bark and leaves of the plant were characterized for specific therapeutic activity (and selectivity index, SI) in vitro against the blood forms of Plasmodium falciparum.
methodsThe activity of A. olivaceum extracts, fractions, and isolated compounds was evaluated against chloroquine (CQ)-resistant P. falciparum blood parasites by in vitro testing with radiolabelled [3H]-hypoxanthine and a monoclonal anti-histidine-rich protein (HRPII) antibody. The cytotoxicity of these fractions and compounds was evaluated in a human hepatoma cell line using a 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay, and the SI was calculated as the ratio between the toxicity and activity. Two leaf fractions were tested in mice with Plasmodium berghei.
resultsAll six fractions from the bark and leaf extracts were active in vitro at low doses (IC50 < 5.0 μg/mL) using the anti-HRPII test, and only two (the neutral and basic bark fractions) were toxic to a human cell line (HepG2). The most promising fractions were the crude leaf extract and its basic residue, which had SIs above 50. Among the four pure compounds evaluated, aspidoscarpine in the bark and leaf extracts showed the highest SI at 56; this compound, therefore, represents a possible anti-malarial drug that requires further study. The acidic leaf fraction administered by gavage to mice with blood-induced malaria was also active.
conclusionUsing a bio-monitoring approach, it was possible to attribute the anti-P. falciparum activity of A. olivaceum to aspidoscarpine and, to a lesser extent, N-methyl-tetrahydrolivacine; other isolated MIA molecules were active but had lower SIs due to their higher toxicities. These results stood in contrast to previous work in which the anti-malarial activity of other Aspidosperma species was attributed to uleine.
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