Antiviral activity against HSV-1 of triterpene saponins from Anagallis arvensis is related tothe fusion-inhibitory activity of desglucoanagalloside B

IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL
Nica Classen , Jandirk Sendker , Diana Ulrich , Michael Schöfbänker , Eike R. Hrincius , Stephan Ludwig , Alexander Weng , Matthias Melzig , Joachim Kühn , Andreas Hensel
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Abstract

The identification of antiviral natural products as new lead structures has become a major task in medical science. Especially saponins have gained high interest for their antiviral activity. Antiviral effects of the saponin-containing plant Anagallis arvensis, widely used in traditional medicine, have been described, while mode of action or detailed phytochemical and functional investigations are still missing. A saponin enriched extract (AAS) from the aerial material of A. arvensis was characterized in detail by LC-HRMS, indicating the presence of a complex mixture of triterpene saponins and flavonoid glycosides. Plaque assays with Herpes simplex virus 1 (HSV-1) on Vero cells indicated strong inhibition of viral spread after infection of the host cells, resulting in reduced plaque size. The strongest effect was achieved by treating host cells post infection, which points towards an interference with the viral post-entry step. Using a specific HSV-1 fusion assay, AAS was shown to inhibit HSV-1 glycoprotein-mediated cell fusion at >2 μg/mL. Bioassay-guided fractionation of AAS yielded one active subfraction, which significantly reduced HSV-1 plaque size on Vero cells. The membrane-fusion inhibiting effect was correlated to the presence of desglucoanagalloside B 9. Interestingly, this compound was also detected in relevant amounts in herbal preparations from traditional medicine, which again could rationalize the use of A. arvensis as antiviral remedy in folk medicine. Relevant antiviral activity against SARS-CoV-2 was not detected.
穿山甲三萜皂苷对HSV-1的抗病毒活性与去糖穿山甲苷B的融合抑制活性有关
作为新型先导结构的抗病毒天然产物的鉴定已成为医学领域的重要课题。特别是皂苷因其抗病毒活性而受到广泛关注。传统医学中广泛应用的含皂苷植物阿那马(Anagallis arvensis)的抗病毒作用已被描述,但其作用方式或详细的植物化学和功能研究仍缺乏。利用液相色谱-质谱联用技术(LC-HRMS)对一种富含三萜皂苷和黄酮类苷的化合物进行了表征。单纯疱疹病毒1型(HSV-1)在Vero细胞上的空斑试验表明,感染宿主细胞后,病毒传播受到强烈抑制,导致空斑大小减小。最强的效果是通过治疗感染后的宿主细胞实现的,这指向了对病毒进入后步骤的干扰。通过特异性HSV-1融合实验,AAS在2 μg/mL时抑制HSV-1糖蛋白介导的细胞融合。生物测定引导的AAS分离得到一个活性亚组分,显著减少了Vero细胞上HSV-1斑块的大小。抑制膜融合的作用与去糖苷b9的存在有关。有趣的是,该化合物在传统医学中草药制剂中也检测到相应的量,这再次证明了民间医学中使用刺蒺藜作为抗病毒药物的合理性。未检测到对SARS-CoV-2的相关抗病毒活性。
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来源期刊
Fitoterapia
Fitoterapia 医学-药学
CiteScore
5.80
自引率
2.90%
发文量
198
审稿时长
1.5 months
期刊介绍: Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.
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