[Activating effect of citrus flavonoids on neuromedin U2 receptor and analysis on siRNA interference].
OBJECTIVE
To screen out active substances on Neuromedin U2 receptor (NMU2R) by using stable NMU2R cell lines and negative cell lines and analyzing siRNA interference.


METHODS
NMU2R cells were used to observe the activating effect of nine nine citrus flavonoids on NMU2R cell. Afterwards, false-positive interference of citrus flavonoids that showed higher activating effect was eliminated by using negative cells and analyzing the efficiency of siRNA interference.


RESULTS
Hesperidin and nobiletin contained in citrus flavonoids were found to effectively activate NMU2R. The efficacy, EC50 and potency values of hesperidin were 4.688, 318.970 micromol x L(-1) and 200.933 micromol x L(-1), while the efficacy, EC50 and potency values of nobiletin were 4.758, 5.832 micromol x L(-1) and 3.124 micromol x L(-).


CONCLUSIONS
Hesperidin and nobiletin contained in citrus flavonoids can activate NMU2R. Nobiletin shows such a low EC50 that it has medicinal value.
Research Center of Medicinal Chemistry and Chemical Biology, Chongqing Technology and Business University, Chongqing 400067, China.
Dao-Qing
DQ
Wang
Xu-Xu
XX
Zheng
Zhong-Yi
ZY
Yin
Li-Xia
LX
Guo
Xiao-Hong
XH
Deng
Gang
G
Chen
D002460:Cell Line; D002957:Citrus / Q000737:chemistry*; D005419:Flavonoids / Q000494:pharmacology*; D015870:Gene Expression / Q000187:drug effects; D006801:Humans; D010936:Plant Extracts / Q000494:pharmacology*; D034622:RNA Interference / Q000187:drug effects*; D034741:RNA, Small Interfering / Q000235:genetics* / Q000378:metabolism; D017981:Receptors, Neurotransmitter / Q000235:genetics* / Q000378:metabolism
D005419:Flavonoids; D010936:Plant Extracts; D034741:RNA, Small Interfering; D017981:Receptors, Neurotransmitter; C082444:neuromedin U receptor