ArticleFrontiers in pharmacology2018
Gambogic Acid and Its Analogs Inhibit Gap Junctional Intercellular Communication.
Article in Frontiers in pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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6 citing papers in PubMed, 16 citations in OpenAlex.
- Chemical Profiling and Vascular Effects of a Hydroalcoholic Extract ofPlants (Basel, Switzerland) · 2026Article
- Evaluation of Cx43 Gap Junction Inhibitors Using a Quantitative Structure-Activity Relationship Model.Biomedicines · 2023Article
- Perspectives and controversies regarding the use of natural products for the treatment of lung cancer.Cancer medicine · 2021Review
- Identification of Cx45 as a Major Component of GJs in HeLa Cells.Biomolecules · 2020Article
- Endothelial Cell Inflammation and Barriers Are Regulated by the Rab26-Mediated Balance betweenMediators of inflammation · 2019Article
- Inhibition of gap junctional intercellular communication by an anti-migraine agent, flunarizine.PloS one · 2019Article
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4 authors at 1 institution in 1 country.
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Abstract
Gap junctions (GJs) are intercellular channels composed of connexins. Cellular molecules smaller than 1 kDa can diffuse through GJs by a process termed gap junctional intercellular communication (GJIC), which plays essential roles in various pathological and physiological conditions. Gambogic acid (GA), a major component of a natural yellow dye, has been used as traditional medicine and has been reported to have various therapeutic effects, including an anti-cancer effect. In this study, two different GJ assay methods showed that GA and its analogs inhibited GJIC. The inhibition was rapidly reversible and was not mediated by changes in surface expression or S368 phosphorylation of Cx43, cellular calcium concentration, or redox state. We also developed an assay system to measure the intercellular communication induced by Cx40, Cx30, and Cx43. Dihydrogambogic acid (D-GA) potently inhibited GJIC by Cx40 (IC50 = 5.1 μM), whereas the IC50 value of carbenoxolone, which is known as a broad spectrum GJIC inhibitor, was 105.2 μM. Thus, D-GA can act as a pharmacological tool for the inhibition of Cx40.
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