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Chemical Structure| 20243-59-8 Chemical Structure| 20243-59-8

Structure of Hydroxygenkwanin
CAS No.: 20243-59-8

Chemical Structure| 20243-59-8

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Hydroxygenkwanin, a natural product isolated and purified from the herbs of Lobelia chinensis, has cytotoxicity, may be an effective natural product to treat glioma, and the combination with apigenin may be a promising method for glioma chemotherapy.

Synonyms: 7-O-Methylluteolin; 3'-Hydroxygenkwanin; Luteolin 7-methyl ether

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Product Details of Hydroxygenkwanin

CAS No. :20243-59-8
Formula : C16H12O6
M.W : 300.26
SMILES Code : O=C1C=C(C2=CC=C(O)C(O)=C2)OC3=C1C(O)=CC(OC)=C3
Synonyms :
7-O-Methylluteolin; 3'-Hydroxygenkwanin; Luteolin 7-methyl ether
MDL No. :MFCD11046350

Safety of Hydroxygenkwanin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H1975 18.3 ± 0.3 µM (IC50) 24 hours HGK displayed selective cytotoxicity against H1975 cells with an IC50 of 18.3 ± 0.3 μM Molecules. 2020 Feb 19;25(4):941.
PC9 18.3 ± 3.1 µM (IC50) 24 hours HGK displayed selective cytotoxicity against PC9 cells with an IC50 of 18.3 ± 3.1 μM Molecules. 2020 Feb 19;25(4):941.
A549 22.0 ± 0.9 µM (IC50) 24 hours HGK displayed selective cytotoxicity against A549 cells with an IC50 of 22.0 ± 0.9 μM Molecules. 2020 Feb 19;25(4):941.
OECM1 cells 25-75 µM 24 hours HGK inhibited cell growth and colony formation in OECM1 cells Front Oncol. 2019 Sep 18;9:911.
SAS cells 25-75 µM 24 hours HGK inhibited cell growth and colony formation in SAS cells Front Oncol. 2019 Sep 18;9:911.
HepG2 cells 0, 20, 40 µM 4 hours To evaluate the effect of HGK on DNA damage repair ability in HepG2 cells, results showed that HGK significantly inhibited DNA damage repair. Int J Mol Sci. 2021 Sep 9;22(18):9766.
Huh7 cells 0, 20, 40 µM 4 hours To evaluate the effect of HGK on DNA damage repair ability in Huh7 cells, results showed that HGK significantly inhibited DNA damage repair. Int J Mol Sci. 2021 Sep 9;22(18):9766.
HepG2 cells 30 µM, 40 µM 48 hours HGK significantly inhibited the proliferation, migration, and invasion of HepG2 cells Biomolecules. 2019 Dec 21;10(1):20.
HepG2 cells 30 µM 48 hours HGK inhibited the proliferation, migration, and invasion of HepG2 cells and induced apoptosis. Front Oncol. 2020 Feb 25;10:216.
Huh7 cells 40 µM 48 hours HGK inhibited the proliferation, migration, and invasion of Huh7 cells and induced apoptosis. Front Oncol. 2020 Feb 25;10:216.
U2OS cells 10, 20, 40, 60 µM 48 hours HGK decreased the viability of U2OS cells in a concentration-dependent manner, inhibiting cell proliferation, migration, and invasion Mol Med Rep. 2022 Oct;26(4):299.
MG-63 cells 10, 20, 40, 60 µM 48 hours HGK decreased the viability of MG-63 cells in a concentration-dependent manner, inhibiting cell proliferation, migration, and invasion Mol Med Rep. 2022 Oct;26(4):299.
HFOB 1.19 cells 0, 10, 20, 40, 60 µM 48 hours To test the safety of HGK, results showed HGK had no significant toxicity on hFOB 1.19 cells Mol Med Rep. 2022 Oct;26(4):299.
R482-HEK293 5.07 µM 72 hours Evaluate the cytotoxicity of Hydroxygenkwanin in ABCG2-transfected cells, showing an IC50 of 5.07 μM Int J Mol Sci. 2022 Oct 23;23(21):12763.
MDR19-HEK293 6.10 µM 72 hours Evaluate the cytotoxicity of Hydroxygenkwanin in ABCB1-transfected cells, showing an IC50 of 6.10 μM Int J Mol Sci. 2022 Oct 23;23(21):12763.
A549-Bec150 5.93 µM 72 hours Evaluate the cytotoxicity of Hydroxygenkwanin in ABCG2-overexpressing cells, showing an IC50 of 5.93 μM Int J Mol Sci. 2022 Oct 23;23(21):12763.
NCI-H460/MX20 5.20 µM 72 hours Evaluate the cytotoxicity of Hydroxygenkwanin in ABCG2-overexpressing cells, showing an IC50 of 5.20 μM Int J Mol Sci. 2022 Oct 23;23(21):12763.
NCI-ADR-RES 7.31 µM 72 hours Evaluate the cytotoxicity of Hydroxygenkwanin in ABCB1-overexpressing cells, showing an IC50 of 7.31 μM Int J Mol Sci. 2022 Oct 23;23(21):12763.
KB-V1 7.94 µM 72 hours Evaluate the cytotoxicity of Hydroxygenkwanin in ABCB1-overexpressing cells, showing an IC50 of 7.94 μM Int J Mol Sci. 2022 Oct 23;23(21):12763.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Huh7 xenograft model Intraperitoneal injection 1 mg/kg 3 times per week for 4 weeks HGK significantly inhibited tumor growth without significant toxicity Biomolecules. 2019 Dec 21;10(1):20.
BALB/c nude mice Huh7 xenograft model Intraperitoneal injection 1 mg/kg 3 times per week for 21 days HGK significantly inhibited the growth of Huh7 xenograft tumors and showed synergistic effects when combined with sorafenib. Front Oncol. 2020 Feb 25;10:216.
BALB/c nude mice H1975 xenograft model Intraperitoneal injection 1.0 mg/kg Every two days for 7 days HGK significantly inhibited the growth of H1975 xenograft tumors without observable toxicity Molecules. 2020 Feb 19;25(4):941.
BALB/c nude mice Osteosarcoma model by subcutaneous inoculation of MG-63 cells Intraperitoneal injection 1.0 mg/kg Every two days for 4 weeks HGK inhibited the growth of osteosarcoma tumors in nude mice, reducing tumor volume and weight Mol Med Rep. 2022 Oct;26(4):299.
BALB/c mice Liver cancer xenograft model Intraperitoneal injection 1.5 mg/kg Three times a week for 15 days To evaluate the effect of HGK on the sensitivity of liver cancer cells to doxorubicin in vivo, results showed that HGK significantly enhanced the antitumor effect of doxorubicin without physiological toxicity. Int J Mol Sci. 2021 Sep 9;22(18):9766.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.33mL

0.67mL

0.33mL

16.65mL

3.33mL

1.67mL

33.30mL

6.66mL

3.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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