Lu Jing, Zhang Ying, Qi Dan, Yan Chunyan, Wu Benhao, Huang Jason H, Yao Jianwen, Wu Erxi, Zhang Guoying
Key Laboratory of Molecular Pharmacology and Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, School of Pharmacy, Yantai University, Yantai, Shandong, 264005, China.
Shandong YingdongYinghao Biotechnology Inc., Yantai, Shandong, 264670, China.
Heliyon. 2022 Jun;8(6):e09660. doi: 10.1016/j.heliyon.2022.e09660. Epub 2022 Jun 9.
Recent research efforts have shown that tea has activities against SARS-CoV-2. However, the active compounds and the action mechanisms are largely unknown. Here we study the inhibitory potential of L-theanine from tea and its semi-synthesized derivative, a small-molecule fluorescent compound, ethyl 6-bromocoumarin-3-carboxylyl L-theanine (TBrC) against infection and replication of SARS-CoV-2 and the underlying mechanisms of action. We reveal that TBrC has potential activities against SARS-CoV-2 in addition to its activity against lung cancer. TBrC showed extracellular inhibition of SARS-CoV-2 M/3CL and the host cell receptor ACE2 while interacting with the viral spike glycoproteins (wild-type, Delta, and Omicron mutants). Moreover, TBrC and L-theanine significantly suppressed growth and TNFα-induced nuclear transcriptional activation of NF-κB in human lung cancer cells without affecting the viability of normal lung cells, suggesting a potential protection of TBrC and L-theanine from pulmonary damages in SARS-CoV-2 infected patients, especially for lung cancer patients with SARS-CoV-2 infection.
最近的研究表明，茶具有抗新型冠状病毒（SARS-CoV-2）的活性。然而，其活性成分和作用机制在很大程度上尚不清楚。在此，我们研究了茶叶中的L-茶氨酸及其半合成衍生物——一种小分子荧光化合物6-溴香豆素-3-羧基-L-茶氨酸乙酯（TBrC）对SARS-CoV-2感染和复制的抑制潜力及其潜在作用机制。我们发现，TBrC除了对肺癌有活性外，还具有抗SARS-CoV-2的潜在活性。TBrC在与病毒刺突糖蛋白（野生型、Delta和Omicron突变体）相互作用时，对SARS-CoV-2 M/3CL和宿主细胞受体ACE2表现出细胞外抑制作用。此外，TBrC和L-茶氨酸显著抑制人肺癌细胞的生长以及TNFα诱导的NF-κB核转录激活，而不影响正常肺细胞的活力，这表明TBrC和L-茶氨酸可能对SARS-CoV-2感染患者的肺部损伤具有潜在保护作用，尤其是对于合并SARS-CoV-2感染的肺癌患者。
