Gambogic acid and its analogs inhibit gap junctional intercellular communication

Eun J. Choi, Joo H. Yeo, Sei M. Yoon, Jinu Lee

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

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.

Original languageEnglish
Article number814
JournalFrontiers in Pharmacology
Volume9
DOIs
Publication statusPublished - 2018

Bibliographical note

Funding Information:
This research was supported by the Basic Science Research Program through the National Research Foundation of Korea

Funding Information:
his research was supported by the Basic Science Research Program through the National Research Foundation of Korea NRF) funded by the Ministry of Education (2011-0023701, 2016R1D1A1A02937397, and 2018R1A6A1A03023718).

Publisher Copyright:
© 2018 Frontiers in Neurology. All Rights Reserved.

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

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