Dihydroberberine |
Catalog No.GC38223
One-Click Copy Product Info
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Dihydroberberine is a potent haematopoietic prostaglandin D2 synthase (H-PGDS), with an IC50 value of 3.7µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 483-15-8
Sample solution is provided at 25 µL, 10mM.
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Dihydroberberine is a potent haematopoietic prostaglandin D2 synthase (H-PGDS), with an IC50 value of 3.7µM [1]. Dihydroberberine inhibits respiration in L6 myotubes and muscle mitochondria, through a specific effect on respiratory complex I, and activates AMP-activated protein kinase [2]. Dihydroberberine has been widely used in various animal models to lower blood sugar and improve glucose tolerance[3].
In vitro, Dihydroberberine treatment for 48h significantly inhibited the growth of A549, NCI-H460, and NCI-H1299 cells with IC50 values of 11.17, 46.33 and 37.91μM, respectively[4]. The perfusion of 10μM Dihydroberberine into HEK293 cells for 10 minutes significantly inhibited the expression of the human ether-a-go-go-related gene (hERG) potassium channel and reduced the transport of hERG protein[5].
In vivo, Dihydroberberine treatment via oral administration at a dose of 50mg/kg/day for one week significantly alleviated renal damage in mice with hyperuricemia, as evidenced by a significant decrease in serum creatinine and blood urea nitrogen levels and a reduction in inflammatory cytokine levels (TNF-α, IL-1β, IL-6, and IL-18)[6]. Administering Dihydroberberine (40mg/kg/day) by intragastric administration daily for 7 consecutive days could significantly reduce the swelling degree of paw edema, tissue damage extent, and inflammatory cell infiltration in mice treated with carrageenan[7]. Daily intragastric administration of Dihydroberberine (50mg/kg/day) for 8 days alleviated the symptoms of ulcerative colitis induced by dextran sulfate sodium (DSS) in mice and significantly improved the intestinal barrier function[8].
References:
[1] Li C H, Tung M C, Tsai C K, et al. Discovery and characterization of novel hematopoietic prostaglandin D synthase inhibitors from traditional Chinese medicine: the bioactive potential of dihydroberberine in treatments of Duchenne muscular dystrophy and inflammation-related diseases[J]. Journal of Enzyme Inhibition and Medicinal Chemistry, 2025, 40(1): 2555624.
[2] Turner N, Li J Y, Gosby A, et al. Berberine and its more biologically available derivative, dihydroberberine, inhibit mitochondrial respiratory complex I: a mechanism for the action of berberine to activate AMP-activated protein kinase and improve insulin action[J]. Diabetes, 2008, 57(5): 1414-1418.
[3] Purwaningsih I, Maksum I P, Sumiarsa D, et al. A review of Fibraurea tinctoria and its component, berberine, as an antidiabetic and antioxidant[J]. Molecules, 2023, 28(3): 1294.
[4] Dai B, Ma Y, Wang W, et al. Dihydroberberine exhibits synergistic effects with sunitinib on NSCLC NCI‐H460 cells by repressing MAP kinase pathways and inflammatory mediators[J]. Journal of Cellular and Molecular Medicine, 2017, 21(10): 2573-2585.
[5] Yu D, Lv L, Fang L, et al. Inhibitory effects and mechanism of dihydroberberine on hERG channels expressed in HEK293 cells[J]. PLoS One, 2017, 12(8): e0181823.
[6] Xu L, Lin G, Yu Q, et al. Anti-hyperuricemic and nephroprotective effects of dihydroberberine in potassium oxonate-and hypoxanthine-induced hyperuricemic mice[J]. Frontiers in Pharmacology, 2021, 12: 645879.
[7] Tan L, Wang Y, Ai G, et al. Dihydroberberine, a hydrogenated derivative of berberine firstly identified in Phellodendri Chinese Cortex, exerts anti-inflammatory effect via dual modulation of NF-κB and MAPK signaling pathways[J]. International Immunopharmacology, 2019, 75: 105802.
[8] Li C, Dong N, Wu B, et al. Dihydroberberine, an isoquinoline alkaloid, exhibits protective effect against dextran sulfate sodium-induced ulcerative colitis in mice[J]. Phytomedicine, 2021, 90: 153631.
| Cell experiment [1]: | |
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Cell lines |
A549 cells |
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Preparation Method |
A549 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). A549 cells (5×103 cells) were plated in 96-well plates and subjected to incubation for 24h in a 5% CO2 incubator. Incubation was followed by treatment with different doses of Dihydroberberine (0.39, 0.78, 1.56, 3.12, 6.25, 12.5, 25 and 50μM) for 48h and cell viability was measured. |
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Reaction Conditions |
0.39, 0.78, 1.56, 3.12, 6.25, 12.5, 25 and 50μM; 48h |
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Applications |
Dihydroberberine treatment inhibited the cell viability of A549 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Male KM mice |
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Preparation Method |
Male KM mice (4 weeks old, weighing 24±2g) were housed in an SPF animal facility with 12/12h light/dark cycle (25±1℃, humidity 60±10%), and fed with laboratory regular diet and sterilized water ad libitum. The hyperuricemic mouse model was induced by intraperitoneal injection of potassium oxonate (300mg/kg) combined with intragastric administration of hypoxanthine (300mg/kg) for 7 days. One hour after modeling, mice orally received Dihydroberberine (50mg/kg) once daily for 1 week. Collect the kidney tissues of mice for histopathological assessment. |
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Dosage form |
50mg/kg/day for 1 week; p.o. |
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Applications |
Dihydroberberine treatment significantly alleviated renal damage in mice with hyperuricemia. |
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References: |
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| Cas No. | 483-15-8 | SDF | |
| Canonical SMILES | COC1=CC=C(C=C23)C(CN2CCC(C3=C4)=CC5=C4OCO5)=C1OC | ||
| Formula | C20H19NO4 | M.Wt | 337.37 |
| Solubility | DMSO : 20 mg/mL (59.28 mM; Need ultrasonic (<70°C)) | Storage | Store at -20°C,sealed storage, away from moisture and light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
| 5 mM | 592.8 μL | 2.9641 mL | 5.9282 mL |
| 10 mM | 296.4 μL | 1.4821 mL | 2.9641 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)