ArticleBiophysical journal2019
Molecular Mechanisms Responsible for Pharmacological Effects of Genipin on Mitochondrial Proteins.
Article in Biophysical journal, 2019. 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, 25 citations in OpenAlex.
- Reduced Cerebral Infarct Volume in Young UCP2Cells · 2026Article
- Dynamic changes in mitochondrial function in brain cortex synaptosomes during aging.Journal of bioenergetics and biomembranes · 2026Article
- Impact of polystyrene microplastic exposure at low doses on male fertility: an experimental study in rats.Scientific reports · 2026Article
- Mito-Genipin, a Novel Mitochondria-Targeted Genipin Derivative Modulates Oxidative Stress and Inflammation in Macrophages.Antioxidants (Basel, Switzerland) · 2025Article
- Epicatechin DecreasesInternational journal of molecular sciences · 2025Article
- Repurposed genipin targeting UCP2 exhibits antitumor activity through inducing ferroptosis in glioblastoma.Acta biochimica et biophysica Sinica · 2024Article
- Inhibition of Mitochondrial Uncoupling Proteins Arrests Human Spermatozoa Motility without Compromising Viability.Antioxidants (Basel, Switzerland) · 2023Article
- UCP2 as a Cancer Target through Energy Metabolism and Oxidative Stress Control.International journal of molecular sciences · 2022Review
- Genipin, an Inhibitor of UCP2 as a Promising New Anticancer Agent: A Review of the Literature.International journal of molecular sciences · 2022Review
- Novel Findings regarding the Bioactivity of the Natural Blue Pigment Genipin in Human Diseases.International journal of molecular sciences · 2022Review
- The Effects of Natural and Synthetic Blue Dyes on Human Health: A Review of Current Knowledge and Therapeutic Perspectives.Advances in nutrition (Bethesda, Md.) · 2021Review
- Mitochondrial Uncoupling Proteins (UCPs) as Key Modulators of ROS Homeostasis: A Crosstalk between Diabesity and Male Infertility?Antioxidants (Basel, Switzerland) · 2021Review
- Article
- Natural Products Targeting the Mitochondria in Cancers.Molecules (Basel, Switzerland) · 2020Review
- Assessment of Visual and Retinal Function Following In Vivo Genipin-Induced Scleral Crosslinking.Translational vision science & technology · 2020Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Genipin, a natural compound from Gardenia jasminoides, is a well-known compound in Chinese medicine that is used for the treatment of cancer, inflammation, and diabetes. The use of genipin in classical medicine is hindered because of its unknown molecular mechanisms of action apart from its strong cross-linking ability. Genipin is increasingly applied as a specific inhibitor of proton transport mediated by mitochondrial uncoupling protein 2 (UCP2). However, its specificity for UCP2 is questionable, and the underlying mechanism behind its action is unknown. Here, we investigated the effect of genipin in different systems, including neuroblastoma cells, isolated mitochondria, isolated mitochondrial proteins, and planar lipid bilayer membranes reconstituted with recombinant proteins. We revealed that genipin activated dicarboxylate carrier and decreased the activity of UCP1, UCP3, and complex III of the respiratory chain alongside with UCP2 inhibition. Based on competitive inhibition experiments, the use of amino acid blockers, and site-directed mutagenesis of UCP1, we propose a mechanism of genipin's action on UCPs. At low concentrations, genipin binds to arginine residues located in the UCP funnel, which leads to a decrease in UCP's proton transporting function in the presence of long chain fatty acids. At concentrations above 200 μM, the inhibitory action of genipin on UCPs is overlaid by increased nonspecific membrane conductance due to the formation of protein-genipin aggregates. Understanding the concentration-dependent mechanism of genipin action in cells will allow its targeted application as a drug in the above-mentioned diseases.
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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.