ArticleMalaria journal2013
Two series of new semisynthetic triterpene derivatives: differences in anti-malarial activity, cytotoxicity and mechanism of action.
Article in Malaria journal, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers, 1 of them a synthesis that pooled it.
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Who cites it
17 citing papers in PubMed, 1 synthesis or guideline pooled it, 43 citations in OpenAlex.
- Use of Brazilian flora as the main source of new antimalarials: a systematic review.Memorias do Instituto Oswaldo Cruz · 2025Pooled it
- Natural triterpenic phenolic esters target PfA-M17 in Plasmodium falciparum.Malaria journal · 2026Article
- Molecular Diversity of Lupane Hybrids in Drug Design and Materials Science.Molecules (Basel, Switzerland) · 2025Review
- Article
- Betulinic Acid-Brosimine B Hybrid Compound Has a Synergistic Effect with Imatinib in Chronic Myeloid Leukemia Cell Line, Modulating Apoptosis and Autophagy.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Optimization of Ursolic Acid Extraction in Oil from Annurca Apple to Obtain Oleolytes with Potential Cosmeceutical Application.Antioxidants (Basel, Switzerland) · 2023Article
- Phytochemicals Derived from Agricultural Residues and Their Valuable Properties and Applications.Molecules (Basel, Switzerland) · 2023Review
- Potential of Triterpenic Natural Compound Betulinic Acid for Neglected Tropical Diseases New Treatments.Biomedicines · 2022Review
- Chemical Strategies towards the Synthesis of Betulinic Acid and Its More Potent Antiprotozoal Analogues.Molecules (Basel, Switzerland) · 2021Review
- The Knockout for G Protein-Coupled Receptor-Like PfSR25 Increases the Susceptibility of Malaria Parasites to the Antimalarials Lumefantrine and Piperaquine but Not to Medicine for Malaria Venture Compounds.Frontiers in microbiology · 2021Article
- Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, AgainstMolecular & cellular proteomics : MCP · 2020Article
- Identification of antiplasmodial triterpenes from Keetia species using NMR-based metabolic profiling.Metabolomics : Official journal of the Metabolomic Society · 2019Article
- Triterpene Derivatives as Relevant Scaffold for New Antibiofilm Drugs.Biomolecules · 2019Article
- Recent Developments in the Functionalization of Betulinic Acid and Its Natural Analogues: A Route to New Bioactive Compounds.Molecules (Basel, Switzerland) · 2019Review
- Anti-Trichomonas vaginalis activity of ursolic acid derivative: a promising alternative.Parasitology research · 2018Article
- In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts.Malaria journal · 2017Article
- Triterpenes as potentially cytotoxic compounds.Molecules (Basel, Switzerland) · 2015Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThe discovery and development of anti-malarial compounds of plant origin and semisynthetic derivatives thereof, such as quinine (QN) and chloroquine (CQ), has highlighted the importance of these compounds in the treatment of malaria. Ursolic acid analogues bearing an acetyl group at C-3 have demonstrated significant anti-malarial activity. With this in mind, two new series of betulinic acid (BA) and ursolic acid (UA) derivatives with ester groups at C-3 were synthesized in an attempt to improve anti-malarial activity, reduce cytotoxicity, and search for new targets. In vitro activity against CQ-sensitive Plasmodium falciparum 3D7 and an evaluation of cytotoxicity in a mammalian cell line (HEK293T) are reported. Furthermore, two possible mechanisms of action of anti-malarial compounds have been evaluated: effects on mitochondrial membrane potential (ΔΨm) and inhibition of β-haematin formation.
resultsAmong the 18 derivatives synthesized, those having shorter side chains were most effective against CQ-sensitive P. falciparum 3D7, and were non-cytotoxic. These derivatives were three to five times more active than BA and UA. A DiOC(6)(3) ΔΨm assay showed that mitochondria are not involved in their mechanism of action. Inhibition of β-haematin formation by the active derivatives was weaker than with CQ. Compounds of the BA series were generally more active against P. falciparum 3D7 than those of the UA series.
conclusionsThree new anti-malarial prototypes were obtained from natural sources through an easy and relatively inexpensive synthesis. They represent an alternative for new lead compounds for anti-malarial chemotherapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.