ArticleMolecules (Basel, Switzerland)2012
Synthesis and antiplasmodial activity of betulinic acid and ursolic acid analogues.
Article in Molecules (Basel, Switzerland), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 82 citations in OpenAlex.
- Isolation, purification and characterization of betulinic acid derivative from the root bark ofInternational journal of biochemistry and molecular biology · 2026Article
- Molecular Diversity of Lupane Hybrids in Drug Design and Materials Science.Molecules (Basel, Switzerland) · 2025Review
- Betulinic and ursolic acids from Nauclea latifolia roots mediate their antimalarial activities through docking with PfEMP-1 and PfPKG proteins.BMC complementary medicine and therapies · 2024Article
- Optimization of Ursolic Acid Extraction in Oil from Annurca Apple to Obtain Oleolytes with Potential Cosmeceutical Application.Antioxidants (Basel, Switzerland) · 2023Article
- A Betulinic Acid Derivative, BA5, Induces G0/G1 Cell Arrest, Apoptosis Like-Death, and Morphological Alterations inFrontiers in pharmacology · 2022Article
- Bio-guided isolation of anti-leishmanial natural products from Diospyros gracilescens L. (Ebenaceae).BMC complementary medicine and therapies · 2021Article
- Chemical Strategies towards the Synthesis of Betulinic Acid and Its More Potent Antiprotozoal Analogues.Molecules (Basel, Switzerland) · 2021Review
- Evaluating the Potential of Ursolic Acid as Bioproduct for Cutaneous and Visceral Leishmaniasis.Molecules (Basel, Switzerland) · 2020Article
- A Highly Active Triterpene Derivative Capable |of Biofilm Damage to ControlBiomolecules · 2019Article
- Ursolic Acid Derivatives as Potential Agents AgainstPathogens (Basel, Switzerland) · 2019Article
- Ursolic Acid and Its Derivatives as Bioactive Agents.Molecules (Basel, Switzerland) · 2019Review
- 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
- Betulinic acid attenuates liver fibrosis by inducing autophagy via the mitogen-activated protein kinase/extracellular signal-regulated kinase pathway.Journal of natural medicines · 2019Article
- In vitro and in vivo anthelmintic efficacy of two pentacyclic triterpenoids, ursolic acid and betulinic acid against mice pinworm,Journal of parasitic diseases : official organ of the Indian Society for Parasitology · 2018Article
- In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts.Malaria journal · 2017Article
- Asiatic acid influences parasitaemia reduction and ameliorates malaria anaemia in P. berghei infected Sprague-Dawley male rats.BMC complementary and alternative medicine · 2016Article
- In vitro anthelmintic assessment of selected phytochemicals against Hymenolepis diminuta, a zoonotic tapeworm.Journal of parasitic diseases : official organ of the Indian Society for Parasitology · 2016Article
- Antiplasmodial phloroglucinol derivatives from Syncarpia glomulifera.Bioorganic & medicinal chemistry · 2016Article
- Ursolic Acid--A Pentacyclic Triterpenoid with a Wide Spectrum of Pharmacological Activities.Molecules (Basel, Switzerland) · 2015Review
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
More than 40% of the World population is at risk of contracting malaria, which affects primarily poor populations in tropical and subtropical areas. Antimalarial pharmacotherapy has utilised plant-derived products such as quinine and artemisinin as well as their derivatives. However, worldwide use of these antimalarials has caused the spread of resistant parasites, resulting in increased malaria morbidity and mortality. Considering that the literature has demonstrated the antimalarial potential of triterpenes, specially betulinic acid (1) and ursolic acid (2), this study investigated the antimalarial activity against P. falciparum chloroquine-sensitive 3D7 strain of some new derivatives of 1 and 2 with modifications at C-3 and C-28. The antiplasmodial study employed flow cytometry and spectrofluorimetric analyses using YOYO-1, dihydroethidium and Fluo4/AM for staining. Among the six analogues obtained, compounds 1c and 2c showed excellent activity (IC₅₀ = 220 and 175 nM, respectively) while 1a and b demonstrated good activity (IC₅₀ = 4 and 5 μM, respectively). After cytotoxicity evaluation against HEK293T cells, 1a was not toxic, while 1c and 2c showed IC₅₀ of 4 μM and a selectivity index (SI) value of 18 and 23, respectively. Moreover, compound 2c, which presents the best antiplasmodial activity, is involved in the calcium-regulated pathway(s).
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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.