首页> 美国卫生研究院文献>Molecules >Hibiscus sabdariffa L. and Its Bioactive Constituents Exhibit Antiviral Activity against HSV-2 and Anti-Enzymatic Properties against Urease by an ESI-MS Based Assay
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Hibiscus sabdariffa L. and Its Bioactive Constituents Exhibit Antiviral Activity against HSV-2 and Anti-Enzymatic Properties against Urease by an ESI-MS Based Assay

机译:通过基于ESI-MS的方法芙蓉及其生物活性成分具有针对HSV-2的抗病毒活性和针对脲酶的抗酶特性

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摘要

For decades, Hibiscus sabdariffa L. and its phytochemicals have been shown to possess a wide range of pharmacologic properties. In this study, aqueous extract of Hibiscus sabdariffa (AEHS) and its bioactive constituent protocatechuic acid (PCA), have been evaluated in vitro for their antiviral activity against HSV-2 clinical isolates and anti-enzymatic activity against urease. Antiherpetic activity was evaluated by the titer reduction assay in infected Vero cells, and cytotoxicity was evaluated by the neutral red dye-uptake method. Anti-urease activity was determined by a developed Electrospray Ionization-Mass Spectrometry (ESI-MS)-based assay. PCA showed potent anti-HSV-2 activity compared with that of acyclovir, with EC50 values of 0.92 and 1.43 µg∙mL−1, respectively, and selectivity indices > 217 and > 140, respectively. For the first time, AEHS was shown to exert anti-urease inhibition activity, with an IC50 value of 82.4 µg∙mL−1. This, combined with its safety, could facilitate its use in practical applications as a natural urease inhibitor. Our results present Hibiscus sabdariffa L. and its bioactive compound PCA as potential therapeutic agents in the treatment of HSV-2 infection and the treatment of diseases caused by urease-producing bacteria.
机译:数十年来,已证明芙蓉及其植物化学物质具有广泛的药理特性。在这项研究中,已评估了芙蓉水提取物(AEHS)及其生物活性成分原儿茶酸(PCA)在体外对HSV-2临床分离株的抗病毒活性和对脲酶的抗酶活性。通过减少感染的Vero细胞中的滴度测定法评估抗疱疹活性,并通过中性红色染料吸收法评估细胞毒性。通过开发的基于电喷雾电离质谱(ESI-MS)的测定法测定抗脲酶活性。与阿昔洛韦相比,PCA具有较强的抗HSV-2活性,EC50值分别为0.92和1.43 µg∙mL -1 ,选择性指数分别为> 217和> 140。 AEHS首次显示出抗尿素酶抑制活性,IC50值为82.4 µg∙mL -1 。结合其安全性,可以促进其在实际应用中作为天然脲酶抑制剂的用途。我们的结果表明,芙蓉及其生物活性化合物PCA在治疗HSV-2感染和治疗由产生脲酶的细菌引起的疾病方面具有潜在的治疗作用。

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