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从雄性花芽中分离出的一种抗疱疹化合物的鉴定。

Identification of an anti-herpetic compound isolated from male floral buds.

作者信息

Chhoud Rihab, Bouslama Lamjed, Gharbi Dorra, Nouira Fatma, Papetti Adele, Majdoub Hatem

机构信息

Laboratory of Interfaces and Advanced Materials (LR11ES55), Faculty of Sciences of Monastir, University of Monastir, Bd. of the Environment, 5019 Monastir, Tunisia.

Laboratory of Bioactive Substances - LR15CBBC03, Center of Biotechnology of Borj Cedria, University of Tunis El Manar, BP 901, 2050 Hammam Lif, Tunisia.

出版信息

3 Biotech. 2022 Dec;12(12):336. doi: 10.1007/s13205-022-03393-y. Epub 2022 Nov 2.

Abstract

Due to the numerous side effects of conventional drugs against herpetic infections and the growing phenomenon of resistance, the researchers turned to natural compounds as a source of new drugs because they are less toxic than the synthetic molecules. This study aimed to analyse the activity of male floral bud extracts, against the replication of herpes simplex virus type 2, as well as to investigate their mode of action, isolate, and identify the active compound. Cell viability and anti-herpes virus activity were performed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and the plaque reduction assay, respectively. Three extracts (ethanolic, aqueous and polysaccharide extracts) were tested, only aqueous and polysaccharide extracts had anti-herpetic activity with a selectivity index of 29.12 and 20.25, respectively. Investigation about the mechanism of action indicated that the two active extracts inhibited the virus replication by direct contact with virucidal selectivity indexes of 39.15 and 32.09, respectively. An active compound was isolated from the aqueous extract using TLC bio-guided assay: it was identified as gallic acid by high-performance liquid chromatography-diode array detection coupled with electrospray ionization mass spectrometry (HPLC-DAD-ESI-MSn). The antiviral activity of has been previously shown. The selectivity index of gallic acid is much lower than that of the active extract from which it has been isolated. Therefore, we can consider the aqueous extract prepared from male floral buds as a promising natural product for treating herpetic diseases.

摘要

由于传统抗疱疹感染药物存在众多副作用以及耐药现象日益严重,研究人员转向天然化合物作为新药来源,因为它们的毒性低于合成分子。本研究旨在分析雄花芽提取物对单纯疱疹病毒2型复制的活性,以及研究其作用方式、分离和鉴定活性化合物。分别使用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐和蚀斑减少试验来检测细胞活力和抗疱疹病毒活性。测试了三种提取物(乙醇提取物、水提取物和多糖提取物),只有水提取物和多糖提取物具有抗疱疹活性,选择性指数分别为29.12和20.25。对作用机制的研究表明,这两种活性提取物通过与病毒直接接触抑制病毒复制,杀病毒选择性指数分别为39.15和32.09。使用薄层色谱生物导向分析法从水提取物中分离出一种活性化合物:通过高效液相色谱-二极管阵列检测结合电喷雾电离质谱(HPLC-DAD-ESI-MSn)将其鉴定为没食子酸。没食子酸的抗病毒活性此前已有报道。没食子酸的选择性指数远低于从中分离出它的活性提取物。因此,我们可以认为从雄花芽制备的水提取物是一种有前景的治疗疱疹疾病的天然产物。

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本文引用的文献

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Anti-Herpes Simplex Virus Type 1 Activity of Specially Selected Groups of Tannins.
Drug Res (Stuttg). 2019 Jul;69(7):374-373. doi: 10.1055/a-0640-2557. Epub 2018 Aug 22.
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Gallic acid: molecular rival of cancer.没食子酸:癌症的分子对手。
Environ Toxicol Pharmacol. 2013 May;35(3):473-85. doi: 10.1016/j.etap.2013.02.011. Epub 2013 Feb 20.

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