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3,4',5,7-tetrahydroxyflavone, kaempferol, kempferol

No.	Title	Href
1	Synergistic effect of kaempferol and 5‑fluorouracil on the growth of colorectal cancer cells by regulating the PI3K/Akt signaling pathway. Mol Med Rep. 2019 Jul;20(1):728-734. doi: 10.3892/mmr.2019.10296.	`Click`
2	Kaempferol potentiates the sensitivity of pancreatic cancer cells to erlotinib via inhibition of the PI3K/AKT signaling pathway and epidermal growth factor receptor. Inflammopharmacology. 2021 Oct;29(5):1587-1601. doi: 10.1007/s10787-021-00848-1.	`Click`
3	Deregulation of the CD44-NANOG-MDR1 associated chemoresistance pathways of breast cancer stem cells potentiates the anti-cancer effect of Kaempferol in synergism with Verapamil. Toxicol Appl Pharmacol. 2022 Feb 15;437:115887. doi: 10.1016/j.taap.2022.115887.	`Click`
4	Kaempferol sensitizes tumor necrosis factor-related apoptosis-inducing ligand-resistance chronic myelogenous leukemia cells to apoptosis. Mol Biol Rep. 2022 Jan;49(1):19-29. doi: 10.1007/s11033-021-06778-z.	`Click`
5	Kaempferol suppresses glioma progression and synergistically enhances the antitumor activity of gefitinib by inhibiting the EGFR/SRC/STAT3 signaling pathway. Drug Dev Res. 2023 May;84(3):592-610. doi: 10.1002/ddr.22048.	`Click`
6	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. Folia Biol (Praha). 2020;66(1):36-46.	`Click`
7	Kaempferol enhances cisplatin's effect on ovarian cancer cells through promoting apoptosis caused by down regulation of cMyc. Cancer Cell Int. 2010 May 11;10:16. doi: 10.1186/1475-2867-10-16.	`Click`
8	Combination of Kaempferol and Docetaxel Induces Autophagy in Prostate Cancer Cells In Vitro and In Vivo. Int J Mol Sci. 2023 Sep 25;24(19):14519. doi: 10.3390/ijms241914519.	`Click`
9	Kaempferol-Mediated Sensitization Enhances Chemotherapeutic Efficacy of Sorafenib Against Hepatocellular Carcinoma: An In Silico and In Vitro Approach. Adv Pharm Bull. 2020 Jul;10(3):472-476. doi: 10.34172/apb.2020.058.	`Click`
10	Kaempferol sensitizes colon cancer cells to TRAIL-induced apoptosis. Biochem Biophys Res Commun. 2008 Oct 10;375(1):129-33. doi: 10.1016/j.bbrc.2008.07.131.	`Click`
11	Kaempferol with Verapamil impeded panoramic chemoevasion pathways in breast cancer through ROS overproduction and disruption of lysosomal biogenesis. Phytomedicine. 2023 May;113:154689. doi: 10.1016/j.phymed.2023.154689.	`Click`
12	Kaempferol Can Reverse the 5-Fu Resistance of Colorectal Cancer Cells by Inhibiting PKM2-Mediated Glycolysis. Int J Mol Sci. 2022 Mar 24;23(7):3544. doi: 10.3390/ijms23073544.	`Click`
13	The Phenolic compound Kaempferol overcomes 5-fluorouracil resistance in human resistant LS174 colon cancer cells. Sci Rep. 2019 Jan 17;9(1):195. doi: 10.1038/s41598-018-36808-z.	`Click`

No.

Title

Href

Synergistic effect of kaempferol and 5‑fluorouracil on the growth of colorectal cancer cells by regulating the PI3K/Akt signaling pathway. Mol Med Rep. 2019 Jul;20(1):728-734. doi: 10.3892/mmr.2019.10296.

Click

Kaempferol potentiates the sensitivity of pancreatic cancer cells to erlotinib via inhibition of the PI3K/AKT signaling pathway and epidermal growth factor receptor. Inflammopharmacology. 2021 Oct;29(5):1587-1601. doi: 10.1007/s10787-021-00848-1.

Click

Deregulation of the CD44-NANOG-MDR1 associated chemoresistance pathways of breast cancer stem cells potentiates the anti-cancer effect of Kaempferol in synergism with Verapamil. Toxicol Appl Pharmacol. 2022 Feb 15;437:115887. doi: 10.1016/j.taap.2022.115887.

Click

Kaempferol sensitizes tumor necrosis factor-related apoptosis-inducing ligand-resistance chronic myelogenous leukemia cells to apoptosis. Mol Biol Rep. 2022 Jan;49(1):19-29. doi: 10.1007/s11033-021-06778-z.

Click

Kaempferol suppresses glioma progression and synergistically enhances the antitumor activity of gefitinib by inhibiting the EGFR/SRC/STAT3 signaling pathway. Drug Dev Res. 2023 May;84(3):592-610. doi: 10.1002/ddr.22048.

Click

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. Folia Biol (Praha). 2020;66(1):36-46.

Click

Kaempferol enhances cisplatin's effect on ovarian cancer cells through promoting apoptosis caused by down regulation of cMyc. Cancer Cell Int. 2010 May 11;10:16. doi: 10.1186/1475-2867-10-16.

Click

Combination of Kaempferol and Docetaxel Induces Autophagy in Prostate Cancer Cells In Vitro and In Vivo. Int J Mol Sci. 2023 Sep 25;24(19):14519. doi: 10.3390/ijms241914519.

Click

Kaempferol-Mediated Sensitization Enhances Chemotherapeutic Efficacy of Sorafenib Against Hepatocellular Carcinoma: An In Silico and In Vitro Approach. Adv Pharm Bull. 2020 Jul;10(3):472-476. doi: 10.34172/apb.2020.058.

Click

Kaempferol sensitizes colon cancer cells to TRAIL-induced apoptosis. Biochem Biophys Res Commun. 2008 Oct 10;375(1):129-33. doi: 10.1016/j.bbrc.2008.07.131.

Click

Kaempferol with Verapamil impeded panoramic chemoevasion pathways in breast cancer through ROS overproduction and disruption of lysosomal biogenesis. Phytomedicine. 2023 May;113:154689. doi: 10.1016/j.phymed.2023.154689.

Click

Kaempferol Can Reverse the 5-Fu Resistance of Colorectal Cancer Cells by Inhibiting PKM2-Mediated Glycolysis. Int J Mol Sci. 2022 Mar 24;23(7):3544. doi: 10.3390/ijms23073544.

Click

The Phenolic compound Kaempferol overcomes 5-fluorouracil resistance in human resistant LS174 colon cancer cells. Sci Rep. 2019 Jan 17;9(1):195. doi: 10.1038/s41598-018-36808-z.

Click

Name	Kaempferol
PubChem CID	5280863
Molecular Weight	286.24g/mol
Synonyms	3,4',5,7-tetrahydroxyflavone, kaempferol, kempferol
Formula	C₁₅H₁₀O₆
SMILES	C1=CC(=CC=C1C2=C(C(=O)C3=C(C=C(C=C3O2)O)O)O)O
InChI	1S/C15H10O6/c16-8-3-1-7(2-4-8)15-14(20)13(19)12-10(18)5-9(17)6-11(12)21-15/h1-6,16-18,20H
InChIKey	IYRMWMYZSQPJKC-UHFFFAOYSA-N
CAS Number	520-18-3
ChEMBL ID	CHEMBL150
ChEBI ID	CHEBI:28499
Herb ID	HBIN031753
Drug Bank ID	DB01852
KEGG ID	C05903
Toxicity	Organism	Test Type	Route(Dose)
	rat	LD50	intraperitoneal(165 mg/kg)
	mouse	LD50	intraperitoneal(254 mg/kg)
	rat	LD50	oral(322 mg/kg)
Structure			Download 2D MOL 3D MOL

Chineses Pinyin	MuZei
Use Part	Aerial parts
Habitat	HeiLongJiang, JiLin, LiaoNing, HeBei, Shaanxi, GanSu, XinJiang, SiChuan
Flavor	Bitter; Sweet
Meridian Tropism	Lung; Liver
Species	>Kingdom: Viridiplantae 　-->Phylum: Streptophyta 　　-->Class: Equisetopsida 　　　-->Order: Equisetales 　　　　-->Family: Equisetaceae 　　　　　-->Genus: Equisetum 　　　　　　-->Species: Equisetum hyemale

Pair Name	Kaempferol, Fluorouracil
Partner Name	Fluorouracil
Disease Info	[ICD-11: 2B91]	Colorectal cancer		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Phosphorylation	AKT1	hsa207
	Up-regulation	Expression	BAX	hsa581
	Down-regulation	Expression	BCL2	hsa596
	Down-regulation	Activity	PIK3CA	hsa5290
	Down-regulation	Expression	TYMS	hsa7298
In Vitro Model	HCT 8	Colon adenocarcinoma	Homo sapiens (Human)	CVCL_2478
In Vitro Model	HCT 116	Colon carcinoma	Homo sapiens (Human)	CVCL_0291
In Vivo Model	To generate HCT116 xenografts in BALB/c nude mice, 3 × 106 HCT116 cells were subcutaneously injected into the left and right flanks of each mouse.
Result	The present study demonstrated that kaempferol has a synergistic effect with 5‑FU by inhibiting cell proliferation and inducing apoptosis in colorectal cancer cells via suppression of TS or attenuation of p‑Akt activation. The combination of kaempferol and 5‑FU may be used as an effective therapeutic strategy for colorectal cancer.

Pair Name	Kaempferol, Erlotinib
Partner Name	Erlotinib
Disease Info	[ICD-11: 2C10]	Pancreatic cancer		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Phosphorylation	AKT1	hsa207
	Up-regulation	Expression	BAX	hsa581
	Down-regulation	Expression	BCL2	hsa596
	Up-regulation	Cleavage	CASP9	hsa842
	Down-regulation	Phosphorylation	EGFR	hsa1956
	Down-regulation	Phosphorylation	MAPK1	hsa5594
	Up-regulation	Cleavage	PARP1	hsa142
	Down-regulation	Expression	PIK3CA	hsa5290
In Vitro Model	PANC-1	Pancreatic ductal adenocarcinoma	Homo sapiens (Human)	CVCL_0480
In Vitro Model	BxPC-3	Pancreatic ductal adenocarcinoma	Homo sapiens (Human)	CVCL_0186
In Vivo Model	The in vivo results revealed that treatment combination of KAE and ERL further reduced the volume and weight of subcutaneous grafted tumors.
Result	These data imply that KAE may be a valid therapeutic candidate to potentiate PC cell sensitivity to ERL via inhibiting PI3K/AKT and EGFR signaling.

Pair Name	Kaempferol, Verapamil
Partner Name	Verapamil
Disease Info	[ICD-11: 2C60]	Breast cancer		Investigative
Biological Phenomena	Induction-->Blockade of cell cycle in G2/M phase
Gene Regulation	Down-regulation	Expression	ABCB1	hsa5243
	Down-regulation	Expression	CD44	hsa960
	Down-regulation	Expression	NANOG	hsa79923
	Down-regulation	Expression	POU5F1	hsa5460
	Down-regulation	Expression	SOX2	hsa6657
In Vitro Model	MDA-MB-231	Breast adenocarcinoma	Homo sapiens (Human)	CVCL_0062
Result	Deregulation of the CD44-NANOG-MDR1 associated chemoresistance pathways of breast cancer stem cells potentiates the anti-cancer effect of Kaempferol in synergism with Verapamil

Pair Name	Kaempferol, TNF-related apoptosis inducing ligand
Partner Name	TNF-related apoptosis inducing ligand
Disease Info	[ICD-11: 2A20.1]	Chronic myelogenous leukemia		Investigative
Biological Phenomena	Induction-->Apoptosis
Gene Regulation	Down-regulation	Expression	BIRC2	hsa329
	Down-regulation	Expression	BIRC3	hsa330
	Down-regulation	Expression	CFLAR	hsa8837
	Up-regulation	Expression	TNFRSF10A	hsa8797
	Up-regulation	Expression	TNFRSF10B	hsa8795
In Vitro Model	K-562	Blast phase chronic myelogenous leukemia	Homo sapiens (Human)	CVCL_0004
Result	It is reasonable to conclude that sensitization of chronic leukemia cells to TRAIL by kaempferol in vitro should be considered as a way of focusing clinical attention on leukemia therapy.

Pair Name	Kaempferol, Gefitinib
Partner Name	Gefitinib
Disease Info	[ICD-11: 2F7Z]	Glioma		Investigative
Biological Phenomena	Induction-->Blockade of cell cycle in G2/M phase
Gene Regulation	Down-regulation	Phosphorylation	EGFR	hsa1956
	Down-regulation	Phosphorylation	SRC	hsa6714
	Down-regulation	Phosphorylation	STAT3	hsa6774
In Vitro Model	U-251MG	Astrocytoma	Homo sapiens (Human)	CVCL_0021
In Vivo Model	U251 cells at a count of 1×10⁷cells per 200 μl weresubcutaneously injected into the right armpit and mice wererandomly divided into six groups of six each.
Result	Kaempferol suppresses glioma progression and synergistically enhances the antitumor activity of gefitinib by inhibiting the EGFR/SRC/STAT3 signaling pathway

Pair Name	Kaempferol, Cisplatin
Partner Name	Cisplatin
Disease Info	[ICD-11: 2C73]	Ovarian cancer		Investigative
Biological Phenomena	Induction-->Endoplasmic reticulum stress and autophagy
Gene Regulation	Down-regulation	Expression	AKT1	hsa207
	Up-regulation	Expression	ATF6	hsa22926
	Up-regulation	Expression	BECN1	hsa8678
	Up-regulation	Expression	CASP4	hsa837
	Up-regulation	Expression	EIF2AK3	hsa9451
	Up-regulation	Expression	HSPA5	hsa3309
	Up-regulation	Expression	MAP1LC3A	hsa84557
In Vitro Model	A2780	Ovarian endometrioid adenocarcinoma	Homo sapiens (Human)	CVCL_0134
Result	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

Pair Name	Kaempferol, Docetaxel
Partner Name	Docetaxel
Disease Info	[ICD-11: 2C82]	Prostate cancer		Investigative
Biological Phenomena	Induction-->Autophagy
Gene Regulation	Up-regulation	Expression	BECN1	hsa8678
	Up-regulation	Expression	GABPA	hsa2551
	Down-regulation	Expression	MAP1LC3A	hsa84557
	Up-regulation	Expression	MAP1LC3B	hsa81631
	Up-regulation	Expression	SQSTM1	hsa8878
In Vitro Model	DU145	Prostate carcinoma	Homo sapiens (Human)	CVCL_0105
In Vitro Model	PC-3	Prostate carcinoma	Homo sapiens (Human)	CVCL_0035
In Vivo Model	Mouse was subcutaneously inoculated with 5×10⁵ androgen-independent PC-3 human prostate cancer cells
Result	The above cellular and animal data suggest that docetaxel in combination with kaempferol has significant anti-prostate cancer effects and that it works by inducing autophagy in cells.

Pair Name	Kaempferol, Sorafenib
Partner Name	Sorafenib
Disease Info	[ICD-11: 2C12]	Hepatocellular carcinoma		Investigative
Gene Regulation	Down-regulation	Expression	ABCB1	hsa5243
In Vitro Model	Hep-G2	Hepatoblastoma	Homo sapiens (Human)	CVCL_0027
Result	Kaempferol is able to sensitize the HepG2 and N1S1 against the sub-toxic concentration of sorafenib. Hence, we consider that the efficacy of sorafenib chemotherapy can be enhanced by the significant approach of combining the sub-toxic concentrations of sorafenib with kaempferol. Thus, kaempferol can be used as a better candidate molecule along with sorafenib for enhancing its efficacy, if validated through preclinical studies.