生物活性 | |||
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描述 | ERR (Estrogen Related Receptor) is a group of nuclear receptors that is closely related to the estrogen receptor. The main isoforms of ERR are ERRα, ERRβ and ERRγ. ERRs act as a site-specific transcription regulator and have been also shown to interact with estrogen and the transcription factor TFIIB by direct protein-protein contact. The binding and regulatory activities of ERRs have been demonstrated in the regulation of a variety of genes[3]. Kaempferol is an inverse agonist of ERRα and ERRγ. Kaempferol dose-dependently inhibited ERRα and ERRγ activity at the concentrations of 5, 10, and 20 μM[4]. Human cholangiocarcinoma (CCA) cells HCCC9810 or QBC939 were exposed to 30, 60, 90, 120 or 150 μM kaempferol. Kaempferol significantly inhibited the viability of CCA cells in a time and dose dependent way[5]. Treatment to HepG2 cells by 10 μM kaempferol for 24h suppressed ERRα and ERRγ target genes PDK2 and PDK4[4]. In a CCA QBC939 xenograft model established in nude mice, kaempferol was i.p. administrated daily at the dose of 20 mg/kg for 3 weeks. Kaempferol significantly inhibited tumor growth and the number of Ki-67 positive tumor cells was lower in kaempferol-treated group than that in the control group[5]. In a BSA-challenged BALB/c mice model of asthma, oral administration of ≤20 mg/kg kaempferol blocked epithelial cell excrescence and smooth muscle hypertrophy[6]. | ||
作用机制 | Kaempferol directly binds the ligand binding domains (LBD) of ERRs. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
B16-4A5 cells | Function assay | Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs, IC50=20 μM | 19615910 | ||
HEK293 FS cells | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.2 μM | 20731357 | ||
human A549 cells | 5-40 μM | Cytotoxicity assay | 72 h | Cytotoxicity against human A549 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | 22871217 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.49mL 0.70mL 0.35mL |
17.47mL 3.49mL 1.75mL |
34.94mL 6.99mL 3.49mL |
参考文献 |
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