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
Hispidulin/高车前素 动物实验
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
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