Kaempferol

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Chemical Structure| 520-18-3 同义名 : 山柰酚 ;Kempferol; Robigenin; Pelargidenolon; Indigo Yellow; Campherol; 3,4',5,7-Tetrahydroxyflavone; Trifolitin; Swartziol; Rhamnolutein; Pelargidenon; NSC 656277; Nimbecetin; NSC 407289
CAS号 : 520-18-3
货号 : A272671
分子式 : C15H10O6
纯度 : 98%
分子量 : 286.24
MDL号 : MFCD00016938
存储条件:

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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
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

[1]Wang J, Fang F, et al. Kaempferol is an estrogen-related receptor alpha and gamma inverse agonist. FEBS Lett. 2009 Feb 18;583(4):643-7.

[2]Luo H, Jiang B, et al. Kaempferol nanoparticles achieve strong and selective inhibition of ovarian cancer cell viability. Int J Nanomedicine. 2012;7:3951-9.

[3]Sladek R, Bader JA, Giguère V. The orphan nuclear receptor estrogen-related receptor alpha is a transcriptional regulator of the human medium-chain acyl coenzyme A dehydrogenase gene. Mol Cell Biol. 1997 Sep;17(9):5400-9. doi: 10.1128/MCB.17.9.5400. PMID: 9271417; PMCID: PMC232390.

[4]Wang J, Fang F, Huang Z, Wang Y, Wong C. Kaempferol is an estrogen-related receptor alpha and gamma inverse agonist. FEBS Lett. 2009 Feb 18;583(4):643-7. doi: 10.1016/j.febslet.2009.01.030. Epub 2009 Jan 24. PMID: 19171140.

[5]Qin Y, Cui W, Yang X, Tong B. Kaempferol inhibits the growth and metastasis of cholangiocarcinoma in vitro and in vivo. Acta Biochim Biophys Sin (Shanghai). 2016 Mar;48(3):238-45. doi: 10.1093/abbs/gmv133. Epub 2016 Feb 15. PMID: 26883800; PMCID: PMC4885126.

[6]Shin D, Park SH, Choi YJ, Kim YH, Antika LD, Habibah NU, Kang MK, Kang YH. Dietary Compound Kaempferol Inhibits Airway Thickening Induced by Allergic Reaction in a Bovine Serum Albumin-Induced Model of Asthma. Int J Mol Sci. 2015 Dec 16;16(12):29980-95. doi: 10.3390/ijms161226218. PMID: 26694364; PMCID: PMC4691161.