柑橘类黄酮对Neuromedin U2受体的激活效应及siRNA干扰分析(4)
Activating effect of citrus flavonoids on Neuromedin U2 receptor
and analysis on siRNA interference
WANG Dao-qing2， ZHENG Xu-xu1，2*， YIN Zhong-yi1， GUO Li-xia1， DENG Xiao-hong1， CHEN Gang1
(1. Research Center of Medicinal Chemistry and Chemical Biology， Chongqing Technology and
Business University， Chongqing 400067， China；
2. Environmental and Biological College， Chongqing Technology and Business University， Chongqing 400067， China)
[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 μmol·L-1 and 200.933 μmol·L-1， while the efficacy， EC50 and potency values of nobiletin were 4.758， 5.832 μmol·L-1 and 3.124 μmol·L-1. Conclusion： Hesperidin and nobiletin contained in citrus flavonoids can activate NMU2R. Nobiletin shows such a low EC50 that it has medicinal value.
[Key words] NMU2R； agonist； hesperidin； nobiletin； siRNA
doi：10.4268/cjcmm20122224
[责任编辑 张宁宁], http://www.100md.com(王道庆 郑旭煦 殷钟意 郭莉霞 邓小红 陈刚)
and analysis on siRNA interference
WANG Dao-qing2， ZHENG Xu-xu1，2*， YIN Zhong-yi1， GUO Li-xia1， DENG Xiao-hong1， CHEN Gang1
(1. Research Center of Medicinal Chemistry and Chemical Biology， Chongqing Technology and
Business University， Chongqing 400067， China；
2. Environmental and Biological College， Chongqing Technology and Business University， Chongqing 400067， China)
[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 μmol·L-1 and 200.933 μmol·L-1， while the efficacy， EC50 and potency values of nobiletin were 4.758， 5.832 μmol·L-1 and 3.124 μmol·L-1. Conclusion： Hesperidin and nobiletin contained in citrus flavonoids can activate NMU2R. Nobiletin shows such a low EC50 that it has medicinal value.
[Key words] NMU2R； agonist； hesperidin； nobiletin； siRNA
doi：10.4268/cjcmm20122224
[责任编辑 张宁宁], http://www.100md.com(王道庆 郑旭煦 殷钟意 郭莉霞 邓小红 陈刚)