PDF(Pubmed)
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.
摘要：
钙信号在各种细胞过程的调节中起着至关重要的作用，包括激活,扩散,和T淋巴细胞的分化，由ORAI1和钾（K+）通道介导。这些通道也已被确定为免疫相关疾病的极具吸引力的治疗靶标。LicochalconeA是一种甘草衍生的查耳酮，以其在药物治疗中的多方面有益作用而闻名。包括它的消炎药,抗哮喘,抗氧化剂，抗菌，和抗肿瘤特性。然而,其涉及淋巴细胞离子通道的抗炎作用尚不清楚.因此，本研究旨在研究甘草查尔酮A是否抑制T淋巴细胞的ORAI1和K+通道。我们的结果表明，甘草查尔酮A在浓度依赖性物质中抑制了所有三个通道（ORAI1，Kv1.3和KCa3.1），IC50值为2.97±1.217µM，0.83±1.222µM，和11.21±1.07µM，分别。值得注意的是，LichochalconeA对CD3和CD28抗体诱导的T细胞中IL-2的分泌和增殖具有抑制作用。这些结果表明，甘草查尔酮A的使用可能为炎症相关的免疫疾病提供有效的治疗策略。
