ArticleJournal of enzyme inhibition and medicinal chemistry2012
Ionic derivatives of betulinic acid as novel HIV-1 protease inhibitors.
Article in Journal of enzyme inhibition and medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 40 citations in OpenAlex.
- Amphiphilic Semisynthetic Triterpenoids Impair Survival Pathways and Suppress Clonogenic Growth in Multidrug-Resistant High-Risk Neuroblastoma.International journal of molecular sciences · 2026Article
- Biological Potential and Physicochemical Properties of Ionic Liquids Bioinspired by Carboxylic Acids: A Review.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Antimicrobial Potential of Betulinic Acid and Investigation of the Mechanism of Action against Nuclear and Metabolic Enzymes with Molecular Modeling.Pathogens (Basel, Switzerland) · 2023Article
- Comparison of In Vitro Antimelanoma and Antimicrobial Activity of 2,3-Indolo-betulinic Acid and Its Glycine Conjugates.Plants (Basel, Switzerland) · 2023Article
- Article
- Endophytic Microbial Diversity: A New Hope for the Production of Novel Anti-tumor and Anti-HIV Agents as Future Therapeutics.Current microbiology · 2021Review
- Viral UL8 Is Involved in the Antiviral Activity of Oleanolic Acid Against HSV-1 Infection.Frontiers in microbiology · 2021Article
- The Role of Ionic Liquids in the Pharmaceutical Field: An Overview of Relevant Applications.International journal of molecular sciences · 2020Review
- Recent advances in natural anti-HIV triterpenoids and analogs.Medicinal research reviews · 2020Review
- Antiviral Activities of Oleanolic Acid and Its Analogues.Molecules (Basel, Switzerland) · 2018Review
- Effect of betulinic acid and its ionic derivatives on M-MuLV replication.Biochemical and biophysical research communications · 2018Article
- Structure and Anti-HIV Activity of Betulinic Acid Analogues.Current medical science · 2018Review
- Co-administration of betulinic acid and methamphetamine causes toxicity to dopaminergic and serotonergic nerve terminals in the striatum of late adolescent rats.Journal of neurochemistry · 2014Article
- New ionic derivatives of betulinic acid as highly potent anti-cancer agents.Bioorganic & medicinal chemistry letters · 2012Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Betulinic acid is a natural product possessing abundant and favourable biological activity, including anti-cancer, anti-malarial, anti-inflammatory and anti-HIV properties, while causing minimal toxicity to unaffected cells. The full biological potency of betulinic acid cannot be fully unlocked, however, for a number of reasons, a primary one being its limited solubility in aqueous and biologically pertinent organic media. Aiming to improve the water solubility of betulinic acid without disrupting its structurally related bioactivity, we have prepared different ionic derivatives of betulinic acid. Inhibition bioassays on HIV-1 protease-catalysed peptide hydrolysis indicate significantly improved performance resulting from converting the betulinic acid to organic salt form. Indeed, for one particular cholinium-based derivative, its water solubility is improved more than 100 times and the half maximal inhibitory concentration (IC(50)) value (22 μg mL(-1)) was one-third that of wide-type betulinic acid (60 μg mL(-1)). These encouraging results advise that additional studies of ionic betulinic acid derivatives as a therapeutic solution against HIV-1 infection are warranted.
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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.