دورية أكاديمية
أعرض في EDS

Quercetin pentaacetate inhibits in vitro human respiratory syncytial virus adhesion.

التفاصيل البيبلوغرافية
العنوان: Quercetin pentaacetate inhibits in vitro human respiratory syncytial virus adhesion.
المؤلفون: Lopes BRP; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., da Costa MF; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., Genova Ribeiro A; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., da Silva TF; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil. Electronic address: titto.13.ax@gmail.com., Lima CS; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., Caruso IP; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil; Centro Multiusuário de Inovação Biomolecular (CMIB), Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., de Araujo GC; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil; Centro Multiusuário de Inovação Biomolecular (CMIB), Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., Kubo LH; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil., Iacovelli F; Department of Biology, University of Rome Tor Vergata, Via della Ricerca Scientifica 1, 00133, Rome, Italy., Falconi M; Department of Biology, University of Rome Tor Vergata, Via della Ricerca Scientifica 1, 00133, Rome, Italy., Desideri A; Department of Biology, University of Rome Tor Vergata, Via della Ricerca Scientifica 1, 00133, Rome, Italy., de Oliveira J; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil., Regasini LO; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., de Souza FP; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil; Centro Multiusuário de Inovação Biomolecular (CMIB), Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil., Toledo KA; Universidade Estadual Paulista, UNESP (FCLAssis), Brazil; Universidade Estadual Paulista, UNESP IBILCE, São José do Rio Preto, Brazil. Electronic address: karina.toledo@unesp.br.
المصدر: Virus research [Virus Res] 2020 Jan 15; Vol. 276, pp. 197805. Date of Electronic Publication: 2019 Nov 09.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: Elsevier Science Country of Publication: Netherlands NLM ID: 8410979 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1872-7492 (Electronic) Linking ISSN: 01681702 NLM ISO Abbreviation: Virus Res Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Amsterdam : Elsevier Science, c1984-
مواضيع طبية MeSH: Antiviral Agents/*pharmacology , Epithelial Cells/*drug effects , Quercetin/*analogs & derivatives , Respiratory Syncytial Virus, Human/*drug effects , Virus Attachment/*drug effects, Acetylation ; Cell Line ; Epithelial Cells/virology ; Humans ; Molecular Dynamics Simulation ; Quercetin/pharmacology ; Respiratory Syncytial Virus, Human/physiology ; Viral Fusion Proteins/metabolism ; Virus Replication/drug effects
مستخلص: Human respiratory syncytial virus (hRSV) is one of the main etiological agents of diseases of the lower respiratory tract and is often responsible for the hospitalization of children and the elderly. To date, treatments are only palliative and there is no vaccine available. Natural products show exceptional structural diversity and they have played a vital role in drug research. Several investigations focused on applied structural modification of natural products to improved metabolic stability, solubility and biological actions them. Quercetin is a flavonoid that presents several biological activities, including anti-hRSV role. Some works criticize the pharmacological use of Quercetin because it has low solubility and low specificity. In this sense, we acetylated Quercetin structure and we used in vitro and in silico assays to compare anti-hRSV function between Quercetin (Q0) and its derivative molecule (Q1). Q1 shows lower cytotoxic effect than Q0 on HEp-2 cells. In addition, Q1 was more efficient than Q0 to protect HEp-2 cells infected with different multiplicity of infection (0.1-1 MOI). The virucidal effects of Q0 and Q1 suggest interaction between these molecules and viral particle. Dynamic molecular results suggest that Q0 and Q1 may interact with F-protein on hRSV surface in an important region to adhesion and viral infection. Q1 interaction with F-protein showed ΔG= -14.22 kcal/mol and it was more stable than Q0. Additional, MTT and plate assays confirmed that virucidal Q1 effects occurs during adhesion step of cycle hRSV replication. In conclusion, acetylation improves anti-hRSV Quercetin effects because Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. These results show alternative anti-hRSV strategy and contribute to drug discovery and development.
(Copyright © 2019 Elsevier B.V. All rights reserved.)
فهرسة مساهمة: Keywords: Antiviral; Flavonoids; HEp-2 cells; In silico; In vitro; Respiratory virus
المشرفين على المادة: 0 (Antiviral Agents)
0 (F protein, human respiratory syncytial virus)
0 (Viral Fusion Proteins)
9IKM0I5T1E (Quercetin)
G0B9KJ0VKI (quercetin pentaacetate)
تواريخ الأحداث: Date Created: 20191113 Date Completed: 20210311 Latest Revision: 20210311
رمز التحديث: 20221213
DOI: 10.1016/j.virusres.2019.197805
PMID: 31712123
قاعدة البيانات: MEDLINE
الوصف
تدمد:1872-7492
DOI:10.1016/j.virusres.2019.197805