Antiviral Action of Tryptanthrin Isolated from Strobilanthes cusia Leaf against Human Coronavirus NL63
Antiviral Action of Tryptanthrin Isolated from Strobilanthes cusia Leaf against Human Coronavirus NL63
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DOI：
10.3390/biom10030366
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发表时间：
2020-03-01
期刊：
影响因子：
5.5
通讯作者：
Lin, Cheng-Wen
中科院分区：
文献类型：
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作者：
Tsai, Yu-Chi;Lee, Chia-Lin;Lin, Cheng-Wen
Strobilanthes cusia（Nees）Kuntze是用于治疗呼吸道病毒感染的中草药。S.苦碟子叶含有具有多种生物活性的化学成分，如β-谷甾醇、靛玉红、色胺酮、桦木醇、靛豆素A和靛豆素B。然而，S.番木鳖叶及其抗人类冠状病毒的成分仍有待阐明。人类冠状病毒NL 63感染在免疫功能低下的个体、幼儿和老年人中很常见。本研究探讨了S.大叶黄杨叶及其主要成分。S.在HCoV-NL 63感染的细胞中，番荔枝叶有效地抑制细胞病变效应（CPE）和病毒产量（IC 50 = 0.64 μ g/mL）。此外，该提取物以浓度依赖性方式有效抑制HCoV-NL 63感染。在S. Cusia叶、色胺酮和靛酚B（5 aR-乙基色胺酮）在降低CPE和子代病毒产生方面表现出有效的抗病毒活性。色胺酮和靛酚B对病毒产量的IC 50值分别为1.52 μ M和2.60 μ M。不同模式的添加/去除时间测定表明，色胺酮阻止HCoV-NL 63复制的早期和晚期阶段，特别是通过阻断病毒RNA基因组合成和木瓜蛋白酶样蛋白酶2活性。值得注意的是，色胺酮（IC 50 = 0.06 μ M）和靛果素B（IC 50 = 2.09 μ M）也表现出强的杀病毒活性。本研究确定色胺酮为S.以不依赖细胞类型的方式对抗HCoV-NL 63的番荔枝叶甲醇提取物。结果表明色胺酮对HCoV-NL 63感染具有抗病毒潜力。
Strobilanthes cusia (Nees) Kuntze is a Chinese herbal medicine used in the treatment of respiratory virus infections. The methanol extract of S. cusia leaf contains chemical components such as beta-sitosterol, indirubin, tryptanthrin, betulin, indigodole A, and indigodole B that have diverse biological activities. However, the antiviral action of S. cusia leaf and its components against human coronavirus remains to be elucidated. Human coronavirus NL63 infection is frequent among immunocompromised individuals, young children, and in the elderly. This study investigated the anti-Human coronavirus NL63 (HCoV-NL63) activity of the methanol extract of S. cusia leaf and its major components. The methanol extract of S. cusia leaf effectively inhibited the cytopathic effect (CPE) and virus yield (IC50 = 0.64 mu g/mL) in HCoV-NL63-infected cells. Moreover, this extract potently inhibited the HCoV-NL63 infection in a concentration-dependent manner. Among the six components identified in the methanol extract of S. cusia leaf, tryptanthrin and indigodole B (5aR-ethyltryptanthrin) exhibited potent antiviral activity in reducing the CPE and progeny virus production. The IC50 values against virus yield were 1.52 mu M and 2.60 mu M for tryptanthrin and indigodole B, respectively. Different modes of time-of-addition/removal assay indicated that tryptanthrin prevented the early and late stages of HCoV-NL63 replication, particularly by blocking viral RNA genome synthesis and papain-like protease 2 activity. Notably, tryptanthrin (IC50 = 0.06 mu M) and indigodole B (IC50 = 2.09 mu M) exhibited strong virucidal activity as well. This study identified tryptanthrin as the key active component of S. cusia leaf methanol extract that acted against HCoV-NL63 in a cell-type independent manner. The results specify that tryptanthrin possesses antiviral potential against HCoV-NL63 infection.