Quinolone alkaloids with inhibitory activity against nuclear factor of activated T cells from the fruits of Evodia rutaecarpa.
Nine quinolone alkaloids (1-9) from the fruits of Evodia rutaecarpa were investigated for their inhibitory activity on nuclear factor of activated T cells (NFAT)-dependent transcription in comparison with nuclear factor (NF)-kappa B-dependent transcription using a reporter gene assay. These alkaloids showed inhibitory effects against NFAT activity, with IC(50) values between 0.91 microM and 15.91 microM. Of the N-methylated quinolones, the longer aliphatic side chain at the quinolone ring showed stronger inhibition of NFAT activity. These N-methylated compounds showed comparable inhibitory effects against NF-kappa B activity. However, quinolone alkaloids without the N-methyl group showed a more selective inhibition of NFAT activity.
Jin
Hui Zi
HZ
Anticancer Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, Yuseong, Daejeon, Korea.
Lee
Jeong Hyung
JH
Lee
Dongho
D
Lee
Hyun Sun
HS
Hong
Young Soo
YS
Kim
Young Ho
YH
Lee
Jung Joon
JJ
D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000818:Animals; D004268:DNA-Binding Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D032086:Evodia; D005638:Fruit; D006801:Humans; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D019169:Jurkat Cells; D008213:Lymphocyte Activation; D051379:Mice; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016176:T-Lymphocyte Subsets / Q000378:metabolism; D014157:Transcription Factors / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000470:Alkaloids; D004268:DNA-Binding Proteins; D007166:Immunosuppressive Agents; D050778:NFATC Transcription Factors; D009687:Nuclear Proteins; D010936:Plant Extracts; D015363:Quinolones; D014157:Transcription Factors