Ro 09-0179 and its orally active derivative Ro 09-0298 selectively inhibited human picornavirus replication in tissue culture and prevented coxsackievirus infection in mice.
Ro 09-0179 and its oral derivative Ro 09-0298 demonstrate specific antiviral activity against picornaviruses by inhibiting viral replication before RNA synthesis initiation.
Ro 09-0179 (4',5-dihydroxy-3,3',7-trimethoxyflavone), isolated from a Chinese medicinal herb, was found to have potent antiviral activity. It selectively inhibited the replication of human picornaviruses, such as rhinoviruses and coxsackieviruses in tissue culture, but not other DNA and RNA viruses. Ro 09-0298 (4',5-diacetyloxy-3,3',7-trimethoxyflavone), an orally active derivative of Ro 09-0179, prevented coxsackievirus (B1) infection in mice. The critical time for the inhibition of rhinovirus replication by Ro 09-0179 was 2 to 4 h after virus adsorption, i.e., in the early stages of virus replication. It markedly inhibited coxsackievirus and rhinovirus RNA synthesis in infected HeLa cells, but not in a cell-free system using the RNA polymerase complex isolated from the infected cells. In the infected cells, the RNA polymerase complex was not formed in the presence of Ro 09-0179. Therefore, it is suggested that Ro 09-0179 interferes with some process of viral replication which occurs between viral uncoating and the initiation of viral RNA synthesis.
Ishitsuka et al. (Fri,) conducted a other in Picornavirus infection. Ro 09-0179 and Ro 09-0298 was evaluated on Viral replication and RNA synthesis. Ro 09-0179 and its orally active derivative Ro 09-0298 selectively inhibited human picornavirus replication in tissue culture and prevented coxsackievirus infection in mice.
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