Activating effect of citrus flavonoids on neuromedin U2 receptor and analysis on siRNA interference.
- Author:
Dao-Qing WANG
1
;
Xu-Xu ZHENG
;
Zhong-Yi YIN
;
Li-Xia GUO
;
Xiao-Hong DENG
;
Gang CHEN
Author Information
- Publication Type:Journal Article
- MeSH: Cell Line; Citrus; chemistry; Flavonoids; pharmacology; Gene Expression; drug effects; Humans; Plant Extracts; pharmacology; RNA Interference; drug effects; RNA, Small Interfering; genetics; metabolism; Receptors, Neurotransmitter; genetics; metabolism
- From: China Journal of Chinese Materia Medica 2012;37(22):3462-3466
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVETo screen out active substances on Neuromedin U2 receptor (NMU2R) by using stable NMU2R cell lines and negative cell lines and analyzing siRNA interference.
METHODNMU2R 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.
RESULTHesperidin 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(-).
CONCLUSIONHesperidin and nobiletin contained in citrus flavonoids can activate NMU2R. Nobiletin shows such a low EC50 that it has medicinal value.
