Anti-influenza virus activities of flavonoids from the medicinal plant Elsholtzia rugulosa.
ELSHOLTZIA RUGULOSA (Lamiaceae), a common Chinese herb, is widely used in the treatment of cold and fever. In order to elucidate the action mechanism and the active principles from the plant against anti-influenza virus, the influenza virus neuraminidase (NA) activity assay and IN VITRO antiviral activity assay were established, and the isolation of the active principles was guided by NA activity. Finally, 5 active constituents were obtained, namely apigenin ( 1), luteolin ( 2), apiin ( 3), galuteolin ( 4) and luteolin 3'-glucuronyl acid methyl ester ( 5), respectively. They all belong to the flavonoids. The IN VITRO antiviral assay using a cytopathic effect (CPE) reduction method showed that they all possessed anti-influenza virus activity. Among them, apigenin and luteolin exhibited the highest activities against influenza virus (H3N2) with IC (50) values of 1.43 microg/mL and 2.06 microg/mL, respectively. The structure-activity relationship (SAR) of these flavonoids with different chemical structures and their anti-influenza virus activities was addressed in this study.
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, People's Republic of China.
Ai-Lin
AL
Liu
Bo
B
Liu
Hai-Lin
HL
Qin
Simon Mingyuen
SM
Lee
Yi-Tao
YT
Wang
Guan-Hua
GH
Du
D000818:Animals; D000998:Antiviral Agents / Q000302:isolation & purification*; D002460:Cell Line; D004285:Dogs; D005419:Flavonoids / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects* / Q000201:enzymology; D019686:Lamiaceae / Q000737:chemistry*; D009439:Neuraminidase / Q000037:antagonists & inhibitors*
D000998:Antiviral Agents; D005419:Flavonoids; D009439:Neuraminidase