ArticleMolecules (Basel, Switzerland)2016
Cardamonin, a Novel Antagonist of hTRPA1 Cation Channel, Reveals Therapeutic Mechanism of Pathological Pain.
Article in Molecules (Basel, Switzerland), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 26 citations in OpenAlex.
- Identification of Phialomustin‑B (PHL-B) as a Novel Natural TRPA1 Channel Inhibitor.ACS omega · 2025Article
- A new horizon for neuroscience: terahertz biotechnology in brain research.Neural regeneration research · 2025Article
- Regulation of transient receptor potential ankyrin 1 by traditional Chinese medicine drugs and their active ingredients.Frontiers in pharmacology · 2025Review
- Anesthetic- and Analgesic-Related Drugs Modulating Both Voltage-Gated NaBiomolecules · 2024Review
- Fluorescence-Based HTS Assays for Ion Channel Modulation in Drug Discovery Pipelines.ChemMedChem · 2024Review
- From Plant to Chemistry: Sources of Active Opioid Antinociceptive Principles for Medicinal Chemistry and Drug Design.Molecules (Basel, Switzerland) · 2023Review
- Cardamonin suppressed the migration, invasion, epithelial mesenchymal transition (EMT) and lung metastasis of colorectal cancer cells by down-regulating ADRB2 expression.Pharmaceutical biology · 2022Article
- Function and therapeutic potential of transient receptor potential ankyrin 1 in fibrosis.Frontiers in pharmacology · 2022Review
- Emerging roles of cardamonin, a multitargeted nutraceutical in the prevention and treatment of chronic diseases.Current research in pharmacology and drug discovery · 2021Review
- Possible Participation of Ionotropic Glutamate Receptors and l-Arginine-Nitric Oxide-Cyclic Guanosine Monophosphate-ATP-Sensitive KMolecules (Basel, Switzerland) · 2020Article
- Cardamonin as a potential treatment for melanoma induces human melanoma cell apoptosis.Oncology letters · 2020Article
- Real-time cell analysis system in cytotoxicity applications: Usefulness and comparison with tetrazolium salt assays.Toxicology reports · 2020Review
- Usnic Acid Potassium Salt: Evaluation of the Acute Toxicity and Antinociceptive Effect in Murine Model.Molecules (Basel, Switzerland) · 2019Article
- Recent development in antihyperalgesic effect of phytochemicals: anti-inflammatory and neuro-modulatory actions.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2018Review
- Cardamonin reduces chemotherapy resistance of colon cancer cells via the TSP50/NF-κB pathwayOncology letters · 2018Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The increasing demand for safe and effective treatments of chronic pain has promoted the investigation of novel analgesic drugs. Some herbals have been known to be able to relieve pain, while the chemical basis and target involved in this process remained to be clarified. The current study aimed to find anti-nociceptive candidates targeting transient receptor potential ankyrin 1 (TRPA1), a receptor that implicates in hyperalgesia and neurogenic inflammation. In the current study, 156 chemicals were tested for blocking HEK293/TRPA1 ion channel by calcium-influx assay. Docking study was conducted to predict the binding modes of hit compound with TRPA1 using Discovery Studio. Cytotoxicity in HEK293 was conducted by Cell Titer-Glo assay. Additionally, cardiotoxicity was assessed via xCELLigence RTCA system. We uncovered that cardamonin selectively blocked TRPA1 activation while did not interact with TRPV1 nor TRPV4 channel. A concentration-dependent inhibitory effect was observed with IC50 of 454 nM. Docking analysis of cardamonin demonstrated a compatible interaction with A-967079-binding site of TRPA1. Meanwhile, cardamonin did not significantly reduce HEK293 cell viability, nor did it impair cardiomyocyte constriction. Our data suggest that cardamonin is a selective TRPA1 antagonist, providing novel insight into the target of its anti-nociceptive activity.
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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.