Kaempferol (Synonyms: Nimbecetin, NSC 407289, NSC 656277, Pelargidenon, Rhamnolutein, Swartziol, Trifolitin)

Kaempferol is a flavonoid that acts as an inverse agonist of ERRα and ERRγ and possesses antioxidant, anti-inflammatory and antitumor activities^[1-2].

Kaempferol significantly inhibited the activity of HCCC9810 and QBC939 cells in a time- and dose-dependent manner. The IC₅₀ values of Kaempferol-treated cells for 72 h were 58.99 μM and 74.91 μM respectively. Kaempferol inhibits the migration and invasion of HCCC9810 and QBC939 cells in a dose-dependent manner and induces apoptosis^[1]. In A2780 OC cells, Kaempferol promoted cell apoptosis (158%), inhibited cell viability (53.17%) and cell proliferation (49.17%). Kaempferol increased the protein levels of GRP78, PERK, ATF6, IRE-1, LC3II, beclin 1 and caspase 4, and activated cytotoxic autophagy^[3].

Kaempferol (20 mg/kg) inhibited the growth of mouse tumors in a QBC939 cell xenograft model. In a lung metastasis model simulated by injecting QBC939 cells into nude mice, Kaempferol (20 mg/kg) significantly reduced the number and volume of lung metastatic nodules^[1]. Kaempferol can reduce plasma glucose levels and increase insulin levels in diabetic rats. Compared with 50 and 200 mg/kg, 100 mg/kg of Kaempferol showed the greatest hypoglycemic effect. After Kaempferol was administered to diabetic rats, lipid peroxidation products, enzymes, and non-enzyme antioxidants all returned to near normal levels^[4].

References:
[1] Youyou Qin, Wu Cui, Xuewei Yang, Baifeng Tong, Kaempferol inhibits the growth and metastasis of cholangiocarcinoma in vitro and in vivo, Acta Biochimica et Biophysica Sinica, Volume 48, Issue 3, March 2016, Pages 238–245.
[2] Wang J, Fang F, Huang Z, et al. Kaempferol is an estrogen-related receptor α and γ inverse agonist[J]. FEBS letters, 2009, 583(4): 643-647.
[3] El-Kott A F, Shati A A, Al-Kahtani M A, et al. Kaempferol Induces Cell Death in A2780 Ovarian Cancer Cells and Increases Their Sensitivity to Cisplatin by Activation of Cytotoxic Endoplasmic Reticulum-Mediated Autophagy and Inhibition of Protein Kinase B[J]. Folia Biologica (00155500), 2020, 66(1).
[4] Al-Numair K S, Chandramohan G, Veeramani C, et al. Ameliorative effect of kaempferol, a flavonoid, on oxidative stress in streptozotocin-induced diabetic rats[J]. Redox Report, 2015, 20(5): 198-209.