Guijarro-Real Carla, Plazas Mariola, Rodríguez-Burruezo Adrián, Prohens Jaime, Fita Ana
Instituto de Conservación y Mejora de la Agrodiversidad Valenciana, Universitat Politècnica de València, 46022 Valencia, Spain.
Foods. 2021 Jun 29;10(7):1503. doi: 10.3390/foods10071503.
Antiviral treatments inhibiting Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) replication may represent a strategy complementary to vaccination to fight the ongoing Coronavirus disease 19 (COVID-19) pandemic. Molecules or extracts inhibiting the SARS-CoV-2 chymotripsin-like protease (3CL) could contribute to reducing or suppressing SARS-CoV-2 replication. Using a targeted approach, we identified 17 plant products that are included in current and traditional cuisines as promising inhibitors of SARS-CoV-2 3CL activity. Methanolic extracts were evaluated in vitro for inhibition of SARS-CoV-2 3CL activity using a quenched fluorescence resonance energy transfer (FRET) assay. Extracts from turmeric () rhizomes, mustard () seeds, and wall rocket subsp. ) at 500 µg mL displayed significant inhibition of the 3CL activity, resulting in residual protease activities of 0.0%, 9.4%, and 14.9%, respectively. Using different extract concentrations, an IC value of 15.74 µg mL was calculated for turmeric extract. Commercial curcumin inhibited the 3CL activity, but did not fully account for the inhibitory effect of turmeric rhizomes extracts, suggesting that other components of the turmeric extract must also play a main role in inhibiting the 3CL activity. Sinigrin, a major glucosinolate present in mustard seeds and wall rocket, did not have relevant 3CL inhibitory activity; however, its hydrolysis product allyl isothiocyanate had an IC value of 41.43 µg mL. The current study identifies plant extracts and molecules that can be of interest in the search for treatments against COVID-19, acting as a basis for future chemical, in vivo, and clinical trials.
抑制严重急性呼吸综合征冠状病毒2(SARS-CoV-2)复制的抗病毒治疗可能是一种与疫苗接种互补的策略,以对抗当前的冠状病毒病19(COVID-19)大流行。抑制SARS-CoV-2类胰凝乳蛋白酶样蛋白酶(3CL)的分子或提取物可能有助于减少或抑制SARS-CoV-2复制。通过靶向方法,我们鉴定出17种植物产品,它们存在于当前和传统菜肴中,有望成为SARS-CoV-2 3CL活性的抑制剂。使用淬灭荧光共振能量转移(FRET)分析体外评估甲醇提取物对SARS-CoV-2 3CL活性的抑制作用。姜黄根茎、芥菜种子和野芝麻提取物在500μg/mL时对3CL活性表现出显著抑制,导致残余蛋白酶活性分别为0.0%、9.4%和14.9%。使用不同的提取物浓度,计算出姜黄提取物的IC值为15.74μg/mL。商业姜黄素抑制3CL活性,但不能完全解释姜黄根茎提取物的抑制作用,这表明姜黄提取物的其他成分在抑制3CL活性中也必须发挥主要作用。黑芥子硫苷酸钾是芥菜种子和野芝麻中存在的一种主要硫代葡萄糖苷,没有相关的3CL抑制活性;然而,其水解产物异硫氰酸烯丙酯的IC值为41.43μg/mL。本研究鉴定出了在寻找COVID-19治疗方法中可能有意义的植物提取物和分子,为未来的化学、体内和临床试验奠定了基础。