Antiviral Activity of Vitis vinifera Leaf Extract against SARS-CoV-2 and HSV-1.

Carla Zannella,Donatella De Pascale,Carmine Buonocore,Giovanni Andrea Vitale,Angela Nebbioso,Pasquale Termolino,Rosa Giugliano,Lucia Altucci,Annalisa Chianese,Giuseppina Sanna,Gianluigi Franci,Aldo Manzin,Federica Sarno,Massimiliano Galdiero

doi:10.3390/v13071263

Abstract

Vitis vinifera represents an important and renowned source of compounds with significant biological activity. Wines and winery bioproducts, such as grape pomace, skins, and seeds, are rich in bioactive compounds against a wide range of human pathogens, including bacteria, fungi, and viruses. However, little is known about the biological properties of vine leaves. The aim of this study was the evaluation of phenolic composition and antiviral activity of Vitis vinifera leaf extract against two human viruses: the Herpes simplex virus type 1 (HSV-1) and the pandemic and currently widespread severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). About 40 phenolic compounds were identified in the extract by HPLC-MS/MS analysis: most of them were quercetin derivatives, others included derivatives of luteolin, kaempferol, apigenin, isorhamnetin, myricetin, chrysoeriol, biochanin, isookanin, and scutellarein. Leaf extract was able to inhibit both HSV-1 and SARS-CoV-2 replication in the early stages of infection by directly blocking the proteins enriched on the viral surface, at a very low concentration of 10 μg/mL. These results are very promising and highlight how natural extracts could be used in the design of antiviral drugs and the development of future vaccines.

Highlights

Grapevine is one of the major fruit crops worldwide, in terms of economic value and cultivated area
Identification of Kaempferol and Luteolin Derivatives is present in traces and compound 39 represents 3% of the cluster
This study focuses on the high anti-inflammatory ability of quercetin, effective in COVID-19 treatment, and its dosage depends on the type of treatment: 500 mg for prophylactic use Cytotoxicity Evaluation and 1000 mg for curative treatment

Summary

Introduction

Grapevine is one of the major fruit crops worldwide, in terms of economic value and cultivated area. Grape seed extract inhibits the expression of the epidermal growth factor receptor (EGFR) in head and neck cutaneous squamous cell carcinoma [18], and of MEPK/ERK1-2 and MAPK/p38 in breast cancer, counteracting tumor invasiveness and progression. Some phenolic compounds, such as quercetin and catechins, given their similarity to estrogenic hormones, determine a pro- and anti-estrogenic receptor response in breast cancer [19]. Sharma et al demonstrated the apoptotic activity of proanthocyanidins blocking COX-2 and the prostaglandin receptor (PGE2) [20] In this context, two stilbenoids of wine, trans-astringin and trans-piceatannol, show a cancer-chemiopreventive action by inhibiting cyclooxigenases and precancerous lesions [21].

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