ArticleMolecular pharmaceutics2017
Pharmacokinetics and Pharmacodynamics of the Triterpenoid Ursolic Acid in Regulating the Antioxidant, Anti-inflammatory, and Epigenetic Gene Responses in Rat Leukocytes.
Article in Molecular pharmaceutics, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 31 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
31 citing papers in PubMed, 59 citations in OpenAlex.
- Ursolic acid: context-dependent redox activity on oxidative stress and its toxicological implications.Archives of toxicology · 2026Review
- Natural products targeting cytokine-regulated SASP inflammation networks in Ovarian cancer: Implications on immune escape and molecular resistance.Inflammopharmacology · 2026Review
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- Micro- and Nanoplastics and Functional Nutrients in Human Health: Epigenetic Mechanisms and Cellular Resilience Signaling in Brain Insulin Resistance and the Risk of Alzheimer's Disease.International journal of molecular sciences · 2025Review
- Biotin-Linked Ursolic Acid Conjugates as Selective Anticancer Agents and Target-Identification Tools for Cancer Therapy.Molecules (Basel, Switzerland) · 2025Article
- Ursolic acid sensitizes bladder cancer to gemcitabine chemotherapy by concurrently targeting PI3K/AKT and JNK pathways.Translational andrology and urology · 2025Article
- Application of Physiologically-Based Pharmacokinetic (PBPK) Model in Drug Development and in Dietary Phytochemicals.Current pharmacology reports · 2025Review
- Oleaceae plants: a source of metabolites with atheroprotective potential.Frontiers in pharmacology · 2025Review
- Pharmacodynamics (PD), Pharmacokinetics (PK) and PK-PD Modeling of NRF2 Activating Dietary Phytochemicals in Cancer Prevention and in Health.Current pharmacology reports · 2025Review
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- Natural Bioactive Compounds Targeting Histone Deacetylases in Human Cancers: Recent Updates.Molecules (Basel, Switzerland) · 2022Review
- Redox signaling, mitochondrial metabolism, epigenetics and redox active phytochemicals.Free radical biology & medicine · 2022Review
- Comprehensive overview of Nrf2-related epigenetic regulations involved in ischemia-reperfusion injury.Theranostics · 2022Review
- 3Evidence-based complementary and alternative medicine : eCAM · 2022Article
- Triterpenoid ursolic acid drives metabolic rewiring and epigenetic reprogramming in treatment/prevention of human prostate cancer.Molecular carcinogenesis · 2022Article
- Natural Bioactive Compounds Targeting Epigenetic Pathways in Cancer: A Review on Alkaloids, Terpenoids, Quinones, and Isothiocyanates.Nutrients · 2021Review
- Antioxidant, Anti-Inflammatory, and Cytotoxic Activity of Extracts from Some Commercial Apple Cultivars in Two Colorectal and Glioblastoma Human Cell Lines.Antioxidants (Basel, Switzerland) · 2021Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
The triterpenoid ursolic acid (UA) has been proposed as a potential cancer chemopreventive agent in many preclinical and clinical studies. In the present work, we aimed to characterize the pharmacokinetics (PK) of UA and to quantitatively assess the antioxidative and anti-inflammatory effects of UA, which are potentially linked to its chemopreventive efficacy. UA was administered intravenously (i.v., 20 mg/kg) or by oral gavage (100 mg/kg) to male Sprague-Dawley rats, and blood samples were collected at a series of designated time points. The plasma concentration of UA was determined using a validated liquid chromatography-mass spectrometry (LC-MS) approach. A biexponential decline in the UA plasma concentration was observed after i.v. dosing and was fitted to a two-compartmental model. The expression levels of phase II drug metabolism (DM)/antioxidant genes and the inflammatory iNos gene in corresponding treatment arms were measured using qPCR as a pharmacodynamic (PD) marker. The expression of phase II DM/antioxidant genes increased and peaked approximately 3 h after 20 mg/kg UA treatment. In a lipopolysaccharide (LPS)-induced acute inflammation model, UA inhibited LPS-stimulated iNos expression and that of the epigenetic markers the DNA methyltransferases (DNMTs) and histone deacetylases (HDACs) in leukocytes. A PK-PD model using Jusko's indirect response model (IDR) with transition compartments (TC) was established to describe the time delay and magnitude of the gene expression elicited by UA. The PK-PD model provided reasonable fitting linking the plasma concentration of UA simultaneously with the PD response based on leukocyte mRNA expression. Overall, our results indicate that UA is effective at inducing various phase II DM/antioxidant genes and inhibiting pro-inflammatory genes in vivo. This PK-PD modeling approach may provide a conceptual framework for the future clinical evaluation of dietary chemopreventive agents in humans.
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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.