Homoisoflavonoids from Caesalpinia sappan displaying viral neuraminidases inhibition.
In this study, twelve neuraminidase (NA) inhibitory compounds 1-12 were isolated from heartwood of Caesalpinia sappan on the basis of their biological activities against three types of viral NAs. Of isolated homoisoflavonoids, sappanone A (2) showed the most potent NAs inhibitory activities with IC(50) values of 0.7 µM [H1N1], 1.1 µM [H3N2], and 1.0 µM [H9N2], respectively, whereas saturated homoisoflavonoid (3) did not show significantly inhibition. This result revealed that α,β-unsaturated carbonyl group in A-ring was the key requirements for viral NAs inhibitory activity. In our enzyme kinetic study, all NA inhibitors screened were found to be reversible noncompetitive types.
Infection Control Material Research Center, Korea Research Institute of Bioscience and Biotechnology, Jeongeup, Republic of Korea.
Hyung Jae
HJ
Jeong
Young Min
YM
Kim
Jang Hoon
JH
Kim
Ji Young
JY
Kim
Ji-Young
JY
Park
Su-Jin
SJ
Park
Young Bae
YB
Ryu
Woo Song
WS
Lee
D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D029911:Caesalpinia / Q000737:chemistry*; D002460:Cell Line; D004285:Dogs; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects / Q000201:enzymology; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects / Q000201:enzymology; D053127:Influenza A Virus, H9N2 Subtype / Q000187:drug effects / Q000201:enzymology; D009980:Influenza A virus / Q000187:drug effects* / Q000201:enzymology; D020128:Inhibitory Concentration 50; D009439:Neuraminidase / Q000037:antagonists & inhibitors*; D009976:Orthomyxoviridae Infections / Q000188:drug therapy / Q000821:virology; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D014764:Viral Proteins / Q000037:antagonists & inhibitors*; D014934:Wood
D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D005419:Flavonoids; D010936:Plant Extracts; D014764:Viral Proteins; D009439:Neuraminidase