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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Genipin is an effective cross-linking reagent derived from Gardenia jasminoides Ellis fruits. Genipin at a concentration of 50μM inhibited superoxide-activated, uncoupling protein 2-mediated mitochondrial proton leak in the mitochondria isolated from mouse kidney.[4] Genipin increased glucose uptake in C2C12 myotubes in a dose-dependent (1 – 10μM) and time-dependent (0.5 – 2 hours) manner. Also in C2C12 myotubes, 10 μM of genipin increased the cellular concentrations of adenosine triphosphate and reactive oxygen species within 30 min of incubation.[5] Intraperitoneal administration of genipin at a dose of 25mg/kg/day for 7 days attenuated depression-like behaviors and normalized reduced hippocampal Bdnf expression in young adult PRS mice.[3]
作用机制
Genipin is a monoterpenoid compound with multiple bioactive properties, such as anti-inflammatory, anti-angiogenic, and anti-depressive activities.[3]
Genipin/京尼平 细胞实验
Cell Line
Concentration
Treated Time
Description
References
SCC-9 cells
10, 30, 60 µM
72 hours
Inhibited cell growth and induced apoptosis
Drug Des Devel Ther. 2020 Jan 29;14:395-405.
SCC-25 cells
10, 30, 60 µM
72 hours
Inhibited cell growth and induced apoptosis
Drug Des Devel Ther. 2020 Jan 29;14:395-405.
GLUTag L-cells
0.1 µM, 1 µM, 10 µM, 100 µM
1 hour
To evaluate the effect of Genipin on GLP-1 secretion, results showed Genipin significantly stimulated GLP-1 secretion
Int J Mol Sci. 2023 Jan 21;24(3):2131.
RAW264.7 cells
1, 10, 50, 100 µM
24 hours
To evaluate the effect of Genipin on inflammatory responses in Pam3CSK4 or LPS-stimulated RAW264.7 cells. Genipin significantly suppressed Pam3CSK4 or LPS-induced production of nitrites, TNF-α, IL-1β, IL-6, and HMGB1.
Mol Med. 2012 May 9;18(1):455-65.
ARPE-19 cells
30 µM
24 hours
To investigate the protective effects of Genipin on H2O2-induced oxidative damage in ARPE-19 cells. Results showed that Genipin reversed the inhibitory effects of H2O2 by promoting cell viability, attenuating ROS accumulation and cell apoptosis, and increased the expression of Nrf2, HO-1, and NQO1.
Int J Mol Med. 2019 Feb;43(2):936-944.
Mouse mesenchymal stromal cells
0, 0.01, 0.05, 0.1, 0.5, 1, or 10 mM
24 hours
Evaluate differentiation potential, results showed that cells on 10 mM Genipin-mixed collagen gels differentiated into vascular smooth muscle cells, while cells on 0 mM Genipin-mixed collagen gels differentiated into visceral smooth muscle cells.
Gels. 2023 Feb 10;9(2):148.
H1299 human lung cancer cells
0, 0.01, 0.05, 0.1, 0.5, 1, or 10 mM
24 hours
Evaluate cell morphology changes, results showed that cells on 10 mM Genipin-mixed collagen gels exhibited spreading morphology, while cells on 0 mM Genipin-mixed collagen gels maintained a round shape.
Gels. 2023 Feb 10;9(2):148.
Mouse Leydig tumor MLTC-1 cells
20 µM
24 hours
To assess the effect of genipin on steroidogenesis, results showed that genipin significantly increased progesterone secretion and upregulated mRNA and protein expression of StAR and CYP11A1 in MLTC-1 cells
Reprod Biol Endocrinol. 2020 Dec 11;18(1):122.
HMC3 cells
5 µM, 10 µM, 20 µM
4 hours pretreatment followed by 12 hours stimulation
To evaluate the inhibitory effect of Genipin on inflammation and lipid accumulation in LPS/HG/PA-induced HMC3 cells. Results showed that Genipin significantly reduced the expressions of M1 phenotype biomarkers (TNF-α, IL-6, iNOS mRNA, CCL2 mRNA) and increased the expressions of M2 phenotype biomarkers (IL-4, IL-10, ARG1 mRNA, YM1 mRNA), inhibited CD68 expression and increased CD206 expression.
Antioxidants (Basel). 2022 Dec 29;12(1):74.
AML-12 cells
40 µM
48 hours
Genipin suppressed CCL2/CCR2 axis via PPARγ-mediated p65 degradation.
Int J Biol Sci. 2023 Oct 16;19(16):5257-5274.
Bone marrow-derived mononuclear cells (BMDMs)
80 µM
48 hours
Genipin promoted phagocytosis and differentiation of BMDMs.
Int J Biol Sci. 2023 Oct 16;19(16):5257-5274.
NHOK cells
0 to 400 µM
48 hours
No significant effect at concentrations below 100 μM
Drug Des Devel Ther. 2020 Jan 29;14:395-405.
Yeast cells
10 µM
6 hours
Genipin reduced αSyn-GFP aggregation and toxicity, decreasing cell death and inclusion formation.
Nat Commun. 2023 Apr 6;14(1):1918.
Human retinal microvascular endothelial cells (hRMECs)
0.4 µM
7 days
Genipin promoted cell viability in high glucose-induced hRMECs, reduced apoptosis, inhibited the increase in ATP, ROS, MMP, and 2-NBDG levels, and decreased the expression of inflammatory cytokines TNF-α, IL-1β, IL-18, and NLRP3.
World J Diabetes. 2023 Sep 15;14(9):1349-1368.
M2 macrophages
150 µM/ml
72 hours
To evaluate the effect of Genipin on the polarization of M2 macrophages, results showed that Genipin maintained and enhanced the expression of arginase 1 and Ym-1 in M2 macrophages.
Acta Biomater. 2021 Sep 1;131:198-210.
M1 macrophages
150 µM/ml
72 hours
To evaluate the effect of Genipin on the polarization of M1 macrophages, results showed that Genipin reduced the expression of iNOS and IL-1β in M1 macrophages.
Acta Biomater. 2021 Sep 1;131:198-210.
M0 macrophages
150 µM/ml
72 hours
To evaluate the effect of Genipin on the polarization of M0 macrophages, results showed that Genipin induced M0 macrophages to polarize towards the M2 subtype, as evidenced by increased expression of arginase 1 and Ym-1.
Acta Biomater. 2021 Sep 1;131:198-210.
Genipin/京尼平 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Corneal stromal injury model
Topical application
0.1% , 0.125 % or 0.25% for 2 mins or 0.5% for 5 mins
Single application
To evaluate the effects of genipin on corneal stromal healing, higher concentrations of genipin were found to result in denser stromal scarring
Ocul Surf. 2023 Apr;28:115-123
Drosophila melanogaster
PD model overexpressing αSyn-GFP
Food feeding
1 mM
Food changed every 2 days, observing lifespan and motor performance
Genipin significantly increased lifespan and motor performance in flies, reducing insoluble αSyn-GFP aggregates.
Nat Commun. 2023 Apr 6;14(1):1918.
ICR mice
Cecal ligation and puncture (CLP)-induced sepsis model and LPS-induced endotoxemia model
Intravenous injection (CLP model) and intraperitoneal injection (LPS model)
1, 2.5, 5 mg/kg
Single or double administration (24-hour interval), observed for 10 days
To evaluate the protective effect of Genipin on sepsis and endotoxemia. Genipin significantly improved the survival rate of septic mice induced by CLP and LPS, attenuated multiple organ dysfunction, inhibited the activation of TLR2 and TLR4 signaling pathways, and reduced the release of proinflammatory cytokines and HMGB1.
Mol Med. 2012 May 9;18(1):455-65.
Mice
Sepsis model induced by caecal ligation and puncture (CLP)
Intravenous injection
1, 2.5, 5 mg/kg
Single dose, observation up to 10 days
Genipin protects against septic liver injury by restoring impaired autophagic flux, improving survival rate, and reducing serum aminotransferases and pro-inflammatory cytokine levels.
Br J Pharmacol. 2016 Mar;173(6):980-91
ICR mice
STZ/HFD-induced diabetic cognitive impairment model
Intragastric administration and brain stereotaxic injection
10 mg/kg, 20 mg/kg, 40 mg/kg
Intragastric administration four times a week for 4 weeks; brain stereotaxic injection once at the 7th and 9th weeks
To evaluate the ameliorative effect of Genipin on diabetic cognitive impairment. Results showed that Genipin reduced blood glucose levels, improved glucose and insulin tolerance in OGTT and ITT, increased the discrimination index in novel object recognition, decreased escape latency, increased platform crossing times and time in target quadrant in Morris water maze, and reduced error number in passive avoidance test.
Antioxidants (Basel). 2022 Dec 29;12(1):74.
C57/BL6 mice
Streptozotocin (STZ)-induced diabetic mice model
Intraocular injection
10 mM
After 3 months of STZ administration, body weight and fasting blood glucose were assessed every 2 weeks for 1 month.
Genipin via intraocular injection reduced ROS levels and glucose uptake in the retina of STZ mice, decreased the expression of inflammatory cytokines and pathway proteins, maintained retinal structure, and reduced oxidative stress and inflammation levels.
World J Diabetes. 2023 Sep 15;14(9):1349-1368.
ICR mice
Circadian disruption model
Oral gavage
25 mg/kg
Once daily for 5 or 10 weeks
To evaluate the ameliorative effect of genipin on reproductive health problems caused by circadian disruption, results showed that genipin treatment restored testis size and morphology, improved sperm concentration and motility, and normalized serum levels of testosterone, dihydrotestosterone, and androstenedione
Reprod Biol Endocrinol. 2020 Dec 11;18(1):122.
C57BL/6 mice
Orthotopic HCC recurrence model
Oral
25 mg/kg and 50 mg/kg
Every other day until the end of the experiment
Genipin significantly delayed postoperative HCC recurrence by inhibiting macrophage infiltration and CCL2/CCR2 axis.
Int J Biol Sci. 2023 Oct 16;19(16):5257-5274.
BALB/c nude mice
OSCC xenograft model
Intraperitoneal injection
30 mg/kg
One week
Significantly reduced tumor size and weight
Drug Des Devel Ther. 2020 Jan 29;14:395-405.
Mice
High-fat-diet-induced obese mouse model
Oral gavage
50 mg/kg/day
Once daily for 6 weeks
To evaluate the effect of Genipin on blood glucose and insulin resistance, results showed Genipin improved hyperglycemia and insulin resistance
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