TY - JOUR
T1 - Synthesis and biological evaluation of chalcone, dihydrochalcone, and 1,3-diarylpropane analogs as anti-inflammatory agents
AU - Vijaya Bhaskar Reddy, Mopur
AU - Hung, Hsin Yi
AU - Kuo, Ping Chung
AU - Huang, Guan Jhong
AU - Chan, Yu Yi
AU - Huang, Shiow Chyn
AU - Wu, Shwu Jen
AU - Morris-Natschke, Susan L.
AU - Lee, Kuo Hsiung
AU - Wu, Tian Shung
N1 - Funding Information:
This work was supported by a grant (NSC 96-2628-M-006-002) from the National Science Council, Taiwan, and a grant (OUA 95-3-2-021) from National Cheng Kung University, Tainan, Taiwan, awarded to T. S. Wu. This study was also supported in part by the Taiwan Department of Health Clinical Trial and Research Center of Excellence (DOH100-TD-B-111-004).
Publisher Copyright:
© 2017 Elsevier Ltd
PY - 2017
Y1 - 2017
N2 - Twenty-one chalcones were prepared via aldol condensation and subsequent reduction of these compound led to the corresponding dihydrochalcone and 1,3-diphenylpropane derivatives. The synthetic products were examined for their effects on NO inhibition in LPS-activated mouse peritoneal macrophages. Among the tested compounds, a 1,3-diarylpropane analog, 2-(3-(3,4-dimethoxyphenyl)propyl)-5-methoxyphenol (3p), displayed the most significant inhibitory effects against NO production. To investigate the mechanism of action, the effects of 3p on iNOS and COX-2 protein expression were studied by immunoblot. The results concluded that 3p is capable of inhibiting iNOS expression in LPS-induced RAW264.7 cells via attenuation of NF-κB signaling by ERK, p38, and JNK.
AB - Twenty-one chalcones were prepared via aldol condensation and subsequent reduction of these compound led to the corresponding dihydrochalcone and 1,3-diphenylpropane derivatives. The synthetic products were examined for their effects on NO inhibition in LPS-activated mouse peritoneal macrophages. Among the tested compounds, a 1,3-diarylpropane analog, 2-(3-(3,4-dimethoxyphenyl)propyl)-5-methoxyphenol (3p), displayed the most significant inhibitory effects against NO production. To investigate the mechanism of action, the effects of 3p on iNOS and COX-2 protein expression were studied by immunoblot. The results concluded that 3p is capable of inhibiting iNOS expression in LPS-induced RAW264.7 cells via attenuation of NF-κB signaling by ERK, p38, and JNK.
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U2 - 10.1016/j.bmcl.2017.02.038
DO - 10.1016/j.bmcl.2017.02.038
M3 - Article
C2 - 28256373
AN - SCOPUS:85013911860
SN - 0960-894X
VL - 27
SP - 1547
EP - 1550
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 7
ER -