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目的:利用NMU2R稳定细胞株和阴性细胞株并通过siRNA干扰分析筛选柑橘类黄酮中对NMU2R有激活效应的物质。方法:利用NMU2R细胞考察9种柑橘黄酮对NMU2R的激活效应,然后针对激活效应较高的柑橘类黄酮,分别用阴性细胞和NMU2R的siRNA干扰分析来排除假阳性干扰。结果:柑橘类黄酮中的橙皮苷和川陈皮素能有效激活NMU2R,橙皮苷和川陈皮素的效能、半效浓度、效价强度分别为4.688,318.970μmol·L-1,200.933μmol·L-1和4.758,5.832μmol·L-1,3.124μmol·L-1。结论:柑橘类黄酮中的橙皮苷和川陈皮素都对NMU2R有激活效应。川陈皮素的半效浓度较低,具有药用开发价值。
OBJECTIVE: To screen the NMU2R-activating substances in citrus flavonoids by NMU2R stable cell lines and negative cell lines and through siRNA interference analysis. Methods: NMU2R cells were used to examine the activation of NMU2R by nine kinds of citrus flavonoids. Then, citrus flavonoids with higher activation were screened out by interference analysis of negative cells and NMU2R siRNA to eliminate false positives. Results: The hesperidin and nobiletin of citrus flavonoids could effectively activate the potency of NMU2R, hesperidin and nobiletin. The half-potency and potency of NMH2R, hesperidin and nobiletin were 4.688, 318.970μmol·L-1,200.933μmol·L- 1 and 4.758,5.832μmol·L-1, 1.124μmol·L-1. CONCLUSION: Both hesperidin and nobiletin in citrus flavonoids have an activating effect on NMU2R. Chuan Cineralin half-effect concentration is lower, with medicinal development value.