Indigo plant leaf extract inhibits the binding of SARS-CoV-2 spike protein to angiotensin-converting enzyme 2.
Indigo plant leaf extract inhibits the binding of SARS-CoV-2 spike protein to angiotensin-converting enzyme 2.
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DOI：
10.3892/etm.2022.11200
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发表时间：
2022-04
影响因子：
2.7
通讯作者：
Ito A
中科院分区：
文献类型：
--
作者：
Hagiyama M;Takeuchi F;Sugano A;Yoneshige A;Inoue T;Wada A;Kajiyama H;Takaoka Y;Sasaki K;Ito A
严重急性呼吸综合征冠状病毒2(SARS-CoV-2)在进入细胞的第一步利用其S1刺突蛋白与人类细胞上的血管紧张素转换酶2(ACE2)结合。色氰菊酯是用d-柠檬烯(17.3微克/毫升)从青黛植物的叶中提取的，被认为可以抑制ACE2介导的另一种冠状病毒HCoV-NL63的细胞进入。目前的研究检测了该提取物是否可以抑制SARS-CoV-2刺突蛋白与ACE2的结合。将高表达ACE2的犬肾MDCK细胞与荧光素标记的S1刺突蛋白孵育，在活细胞培养中结合定量为细胞结合荧光强度。当加入8,650倍和17,300倍稀释倍数的青黛提取物和S1蛋白时，荧光强度以剂量和S1提取物依赖的方式减弱，不影响细胞存活率。当加入4.0-NM色氨菊酯而不是青黛提取物时，荧光强度也有所降低，但幅度小于青黛提取物。对接模拟分析表明，色氨菊酯很容易与S1蛋白的受体结合域结合，并确定2-和7-氨基酸序列是首选结合部位。青黛提取物对S1-ACE2的结合有高稀释抑制作用，并明显含有其他抑制成分和色氰菊酯。该提取物可能对预防或治疗SARS-CoV-2感染有用。
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) uses its S1 spike protein to bind to angiotensin-converting enzyme 2 (ACE2) on human cells in the first step of cell entry. Tryptanthrin, extracted from leaves of the indigo plant, Polygonum tinctorium, using d-limonene (17.3 µg/ml), is considered to inhibit ACE2-mediated cell entry of another type of coronavirus, HCoV-NL63. The current study examined whether this extract could inhibit the binding of the SARS-CoV-2 spike protein to ACE2. Binding was quantified as cell-bound fluorescence intensity in live cell cultures in which canine kidney MDCK cells overexpressing ACE2 were incubated with fluorescein-labeled S1 spike protein. When indigo extract, together with S1 protein, was added at 8,650x and 17,300x dilutions, fluorescence intensity decreased in a dose- and S1 extract-dependent manner, without affecting cell viability. When 4.0-nM tryptanthrin was added instead of the indigo extract, fluorescence intensity also decreased, but to a lesser degree than with indigo extract. Docking simulation analyses revealed that tryptanthrin readily bound to the receptor-binding domain of the S1 protein, and identified 2- and 7-amino acid sequences as the preferred binding sites. The indigo extract appeared to inhibit S1-ACE2 binding at high dilutions, and evidently contained other inhibitory elements as well as tryptanthrin. This extract may be useful for the prevention or treatment of SARS-CoV-2 infection.
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