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[Activating effect of citrus flavonoids on neuromedin U2 receptor and analysis on siRNA interference]. | LitMetric

[Activating effect of citrus flavonoids on neuromedin U2 receptor and analysis on siRNA interference].

Zhongguo Zhong Yao Za Zhi

Research Center of Medicinal Chemistry and Chemical Biology, Chongqing Technology and Business University, Chongqing 400067, China.

Published: November 2012

AI Article Synopsis

Article Abstract

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.

Method: 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.

Result: 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(-).

Conclusion: Hesperidin and nobiletin contained in citrus flavonoids can activate NMU2R. Nobiletin shows such a low EC50 that it has medicinal value.

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