Potent inhibition of Western Equine Encephalitis virus by a fraction rich in flavonoids and phenolic acids obtained from Achyrocline satureioides

Revista Brasileira de Farmacognosia

Escobar, Franco Matías¹  Sereno, José¹  Sabini, Liliana Inés¹  Comini, Laura¹  Cariddi, Laura Noelia¹  Larrauri, Mariana¹  Mañas, Fernando¹  Universidad Nacional de Río Cuarto, Río Cuarto, Argentina¹  Sabini, María Carola¹  Universidad Nacional de Córdoba, Córdoba, Argentina¹  Cantero, Juan José¹  Contigiani, Marta Silvia¹  Iglesias, Delvis¹  Montoya, Susana Núñez¹ 

关键词:  Achyrocline satureioides;    Antiviral activity;    Cytotoxicity;    Genotoxicity;    Western Equine Encephalitis virus;   

DOI  :  10.1016/j.bjp.2016.05.004

来源: Sociedade Brasileira de Farmacognosia

【 摘 要 】

Achyrocline satureioides (Lam.) DC. Asteraceae, ‘marcela del campo', possess several pharmacological properties. Previously we reported antiviral activity of an aqueous extract of A. satureioides against an alphavirus, Western Equine Encephalitis virus. Alphaviruses are highly virulent pathogens which cause encephalitis in humans and equines. There are no effective antiviral to treat its infections. The aim of this study was to evaluate in vitro cytotoxic and antiviral activities against Western Equine Encephalitis virus of five water extract chromatographic fractions from A. satureioides and identify the main compounds of the bioactive fraction. Also, it was to assess in vivo cytogenotoxic ability of the active fraction. Cytotoxicity studies revealed low toxicity of the most of fractions in Vero and in equine peripheral blood mononuclear cells. Antiviral studies showed that the water crude extract – Sephadex LH 20 – fraction 3 MeOH–H2O (Fraction 3) was active against Western Equine Encephalitis virus with Effective Concentration 50% = 5 µg/ml. Selectivity Indices were 126.0 on Vero and 133.6 on peripheral blood mononuclear cells, four times higher than aqueous extract selectivity index. Regarding the mechanism of action we demonstrated that F3 exerted its action in intracellular replication stages. Further, fraction 3 showed important virucidal action. Fraction 3 contains, in order of highest to lowest: chlorogenic acid, luteolin, 5,7,8-trimethoxyflavone, 3-O-methylquercetin and caffeic acid. Fraction 3 did not induce in vivo toxic nor mutagenic effect. Therefore, it is safe its application as antiviral potential. Further studies of antiviral activity in vivo will be developed using a murine model.

【 授权许可】

Unknown