Anti-Inflammatory Effect of Licochalcone A via Regulation of ORAI1 and K+ Channels in T-Lymphocytes
07 Oct 2021-International Journal of Molecular Sciences (Multidisciplinary Digital Publishing Institute)-Vol. 22, Iss: 19, pp 10847
TL;DR: Zhang et al. as discussed by the authors investigated whether licochalcone A inhibits ORAI1 and K+ channels in T-lymphocytes and found that it suppressed all three channels (ORAI1, Kv1.3, and KCa3) in a concentration-dependent matter.
Abstract: Calcium signaling plays a vital role in the regulation of various cellular processes, including activation, proliferation, and differentiation of T-lymphocytes, which is mediated by ORAI1 and potassium (K+) channels. These channels have also been identified as highly attractive therapeutic targets for immune-related diseases. Licochalcone A is a licorice-derived chalconoid known for its multifaceted beneficial effects in pharmacological treatments, including its anti-inflammatory, anti-asthmatic, antioxidant, antimicrobial, and antitumorigenic properties. However, its anti-inflammatory effects involving ion channels in lymphocytes remain unclear. Thus, the present study aimed to investigate whether licochalcone A inhibits ORAI1 and K+ channels in T-lymphocytes. Our results indicated that licochalcone A suppressed all three channels (ORAI1, Kv1.3, and KCa3.1) in a concentration-dependent matter, with IC50 values of 2.97 ± 1.217 µM, 0.83 ± 1.222 µM, and 11.21 ± 1.07 µM, respectively. Of note, licochalcone A exerted its suppressive effects on the IL-2 secretion and proliferation in CD3 and CD28 antibody-induced T-cells. These results indicate that the use of licochalcone A may provide an effective treatment strategy for inflammation-related immune diseases.
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6 citations
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TL;DR: In this article , the potential of modulation of particular types of potassium channels by different flavonoids is discussed, and the biological meaning of the flavonoid-mediated changes in the activity of K+ channels is outlined.
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