5TH International Congress on Technology - Engineering & Science - Kuala Lumpur - Malaysia (2018-02-01)

The Novel Compound Shows Potent Anti-human Cytomegalovirus Activity

It has been reported that treatment with tricin (4’,5,7-trihydroxy-3’,5’-dimethoxyflavone) after human cytomegalovirus (HCMV) infection significantly suppressed HCMV replication in the Human embryonic lung fibroblast cells. The strength of anti-HCMV activities of tricin was similar degree to that of GCV, but it could not exceed the anti-HCMV effect of GCV. Therefore, we decided to try to discover novel compounds with much stronger anti-HCMV activity than tricin and GCV. The novel compound, ①F-tricin strongly suppressed HCMV replication in a dose-dependent manner than the potently of GCV and tricin. ①F-tricin showed anti-HCMV effect at very low concentration of 1 nM or less (IC50=0.126 nM), and it was revealed that the same effect was obtained at a concentration of about 1/200 of GCV (IC50=27.47 nM) and about 1/400 of tricin (IC50=54.25 nM). We also examined the toxicity of ①F-tricin. In the cytotoxicity test on HEL cells, no toxicity was observed at concentrations up to 10 μM. Furthermore, no direct inactivating effect (virucidal effect) on cell-free HCMV was observed at concentrations up to 10 μM. These results suggest that ①F-tricin is a promising novel compound with potential anti-HCMV activity.
Tsugiya Murayama, Kazuhiro J. Fujimoto, Mamoru Koketsu, Masaya Takemoto, Hidetaka Sadanari, Tohru Daitoku