Antiviral activity and mode of action of caffeoylquinic acids from Schefflera heptaphylla (L.) Frodin.

Abstract:

:Schefflera heptaphylla is a popular medicinal plant in southern China. Three caffeoylquinic acid derivatives, namely 3,4-di-O-caffeoylquinic acid, 3,5-di-O-caffeoylquinic acid, and 3-O-caffeoylquinic acid, were isolated from this plant and investigated for their antiviral activity against respiratory syncytial virus (RSV). 3,4-Di-O-caffeoylquinic acid and 3,5-di-O-caffeoylquinic acid possessed potent anti-RSV activity. The median inhibitory concentrations (IC50) of 3,4-di-O-caffeoylquinic acid and 3,5-di-O-caffeoylquinic acid against RSV were 2.33 microM (1.2 microg/ml) and 1.16 microM (0.6 microg/ml), respectively, in a plaque reduction assay. The dicaffeoylquinic acids exhibited minimal cytotoxicity against HEp-2 cells with median cytotoxic concentration (CC50) higher than 1000 microM. The maximal non-cytotoxic concentration (MNCC) of the two dicaffeoylquinic acids were about 96.7 microM, which suggested their anti-RSV effect was not due to cytotoxicity. The antiviral action of 3,4-di-O-caffeoylquinic acid and 3,5-di-O-caffeoylquinic acid was specific against RSV, as they had no obvious antiviral activity against influenza A (Flu A), Coxsackie B3 (Cox B3), and Herpes simplex type one (HSV-1) viruses. Studies were performed that indicated that the dicaffeoylquinic acids could inhibit RSV directly, extracellularly, but only at much higher concentrations than seen in standard assays. Moreover, they could not inhibit RSV attachment to host cells, and could not protect HEp-2 cells from RSV infection at lower concentrations. The data suggest that the compounds exerted their anti-RSV effects via the inhibition of virus-cell fusion in the early stage, and the inhibition of cell-cell fusion at the end of the RSV replication cycle.

journal_name

Antiviral Res

journal_title

Antiviral research

authors

Li Y,But PP,Ooi VE

doi

10.1016/j.antiviral.2005.06.004

subject

Has Abstract

pub_date

2005-10-01 00:00:00

pages

1-9

issue

1

eissn

0166-3542

issn

1872-9096

pii

S0166-3542(05)00120-8

journal_volume

68

pub_type

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