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Chemical Structure| 1447-88-7 Chemical Structure| 1447-88-7

Structure of Hispidulin
CAS No.: 1447-88-7

Chemical Structure| 1447-88-7

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Hispidulin, a natural product isolated and purified from the herbs of Ambrosia artemisiifolia Linn., is a Pim-1 inhibitor with an IC50 of 2.71 μM.

Synonyms: Dinatin; 6-Methoxyapigenin; NSC 122415

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Product Details of Hispidulin

CAS No. :1447-88-7
Formula : C16H12O6
M.W : 300.26
SMILES Code : O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(O)=C(OC)C(O)=C13
Synonyms :
Dinatin; 6-Methoxyapigenin; NSC 122415
MDL No. :MFCD00143504
InChI Key :IHFBPDAQLQOCBX-UHFFFAOYSA-N
Pubchem ID :5281628

Safety of Hispidulin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Hispidulin

epigenetics
JAK-STAT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293T cells 10 μM 24 hours Increased protein levels of α1(D219N) and α1(G251D) Pharmacol Res. 2024 Oct;208:107356
Mouse primary hepatocytes 1, 5, 10 μM 3 hours Hispidulin directly suppressed gluconeogenesis in hepatocytes, with the concentration as low as 1 μM already eliciting a significant effect Mol Nutr Food Res. 2020 Mar;64(6):e1900978
Mouse islets 1, 5, 10 μM 1 hour Hispidulin enhanced glucose-stimulated insulin secretion Mol Nutr Food Res. 2020 Mar;64(6):e1900978
INS832/13 cells 1, 5, 10 μM 1 hour Hispidulin dose-dependently augmented glucose-stimulated insulin secretion (GSIS), with the lowest effective concentration at 1 μM Mol Nutr Food Res. 2020 Mar;64(6):e1900978
Mouse ileum crypts 0.1, 1, 10, 50 μM 1 hour Hispidulin increased GLP-1 secretion from crypts, with 1 μM concentration eliciting 2.5-fold GLP-1 release over vehicle control Mol Nutr Food Res. 2020 Mar;64(6):e1900978
GluTag L-cells 0.1, 1, 10, 50 μM 1 hour Hispidulin promoted GLP-1 secretion from L-cells, with 1–50 μM concentrations inducing significant GLP-1 release Mol Nutr Food Res. 2020 Mar;64(6):e1900978
NCI-H460 cells 30 µM 10 hours TUDCA pretreatment effectively reversed the hispidulin-induced increase in CHOP protein expression. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 15 and 30 µM 10 hours Hispidulin significantly increased the protein expression level of CHOP. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 15 and 30 µM 4 hours Hispidulin increased the expression of p-eIF2α and ATF4 in a dose-dependent manner. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 30 µM 24 hours GSH pretreatment attenuated hispidulin-induced expression of apoptosis-related proteins in NCI-H460 cells. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 15 and 30 µM 3 hours Hispidulin significantly increased ROS levels in NCI-H460 cells in a concentration-dependent manner. Oncol Rep. 2020 Jun;43(6):1995-2003
A549 cells 15 and 30 µM 24 hours Hispidulin induced apoptosis in NCI-H460 and A549 cells in a concentration-dependent manner. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 15 and 30 µM 24 hours Hispidulin induced apoptosis in NCI-H460 and A549 cells in a concentration-dependent manner. Oncol Rep. 2020 Jun;43(6):1995-2003
A549 cells 5 and 10 µM 12 hours Hispidulin inhibited the colony formation ability of NCI-H460 and A549 cells. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 5 and 10 µM 12 hours Hispidulin inhibited the colony formation ability of NCI-H460 and A549 cells. Oncol Rep. 2020 Jun;43(6):1995-2003
A549 cells 4, 8, 15, 30, 60 µM 24 or 48 hours Hispidulin markedly decreased the viability of A549 and NCI-H460 cell lines in a time- and concentration-dependent manner. Oncol Rep. 2020 Jun;43(6):1995-2003
NCI-H460 cells 4, 8, 15, 30, 60 µM 24 or 48 hours Hispidulin markedly decreased the viability of A549 and NCI-H460 cell lines in a time- and concentration-dependent manner. Oncol Rep. 2020 Jun;43(6):1995-2003
Human keratinocytes (HaCaT and NHEK) 1, 3, 10, 30, 50 µM 24, 48, 72 hours Hispidulin did not significantly affect the viability of normal keratinocytes. Biomolecules. 2021 Jul 16;11(7):1039
Basal cell carcinoma cells (BCC) 10, 30, 50 µM 24, 48, 72 hours Hispidulin exhibited cytotoxic effects in BCC cells. Biomolecules. 2021 Jul 16;11(7):1039
A2058 human melanoma cells 1-50 µM 24, 48, 72 hours Hispidulin selectively decreased the cell viability of A2058 cells in a dose- and time-dependent manner, inducing apoptosis and cell cycle arrest. Biomolecules. 2021 Jul 16;11(7):1039
3T3-L1 preadipocytes 5, 10, 20, 40 μM 24 hours To evaluate the inhibitory effect of Hispidulin on the differentiation of 3T3-L1 preadipocytes. Results showed that 20 and 40 μM Hispidulin reduced the formation of red-labeled lipid droplets by 56.63% and 37.75%, respectively. Biomolecules. 2021 Nov 25;11(12):1764
human nasopharyngeal carcinoma CNE-2Z cells 6.25, 12.5, 25 μM 24 hours Hispidulin inhibited the migration and invasion of CNE-2Z cells Molecules. 2021 Mar 14;26(6):1604
human nasopharyngeal carcinoma CNE-2Z cells 25, 50, 100 μM 48 hours Hispidulin induced apoptosis in a dose-dependent manner Molecules. 2021 Mar 14;26(6):1604
human nasopharyngeal carcinoma CNE-2Z cells 0–200 μM 24, 48, 72 hours Hispidulin significantly inhibited CNE-2Z cell growth in a concentration and time-dependent manner Molecules. 2021 Mar 14;26(6):1604

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Streptozotocin (STZ)-induced diabetic mice Oral gavage 20 mg/kg/day Once daily for 6 weeks Hispidulin significantly improved glycemic control in diabetic mice, concomitant with improved insulin release and β-cell survival. Additionally, hispidulin decreased hepatic pyruvate carboxylase expression in diabetic mice and suppressed gluconeogenesis in hepatocytes. Mol Nutr Food Res. 2020 Mar;64(6):e1900978
BALB/c nude mice NCI-H460 xenograft model Intraperitoneal injection 20 and 40 mg/kg Once every 2 days for 20 days Hispidulin significantly inhibited the growth of NCI-H460 xenograft tumors and induced tumor cell apoptosis. Oncol Rep. 2020 Jun;43(6):1995-2003
Nude mice A2058 xenograft model Intraperitoneal injection 40 mg/kg Once daily for 19 consecutive days Hispidulin significantly inhibited tumor growth without affecting body weight in mice. Biomolecules. 2021 Jul 16;11(7):1039
Mice Chronic phencyclidine (PCP)-treated mice and isolated disrupted-in-schizophrenia-1 mutant (mutDISC1) mice Intraperitoneal injection 10 mg/kg Single administration, 15 minutes before Hispidulin attenuated social withdrawal by activating D1 receptors indirectly through elevated dopamine levels in the PFC by COMT inhibition. Br J Pharmacol. 2020 Jul;177(14):3210-3224
C57BL/6 mice Endotoxin-induced acute kidney injury model Intraperitoneal injection 50 mg/kg Single dose, lasted for 24 hours Hispidulin ameliorated endotoxin-induced acute kidney injury by suppressing inflammation, oxidative stress, and tubular cell apoptosis. Molecules. 2022 Mar 21;27(6):2019
BALB/c-nu mice CNE-2Z tumor xenograft model Intraperitoneal injection 20 mg/kg/day Once daily for 21 days Hispidulin significantly inhibited tumor growth with low toxicity Molecules. 2021 Mar 14;26(6):1604
ICR mice Passive cutaneous anaphylaxis model Intraperitoneal injection 1 and 10 mg/kg body weight Once, lasting 30 minutes Attenuated IgE-mediated passive cutaneous anaphylaxis Molecules. 2019 Jun 5;24(11):2131

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

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