Dihydroberberine是一种强效的haematopoietic prostaglandin D2 synthase (H-PGDS)抑制剂，IC50值为3.7µM。
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.
Dihydroberberine是一种强效的haematopoietic prostaglandin D2 synthase (H-PGDS)抑制剂，IC50值为3.7µM[1]。Dihydroberberine通过特异性作用于呼吸复合物I，抑制L6肌管和肌肉线粒体的呼吸作用，并激活AMP活化蛋白激酶[2]。Dihydroberberine已被广泛用于多种动物模型，以降低血糖并改善葡萄糖耐量[3]。
在体外，Dihydroberberine处理48小时显著抑制了A549、NCI-H460和NCI-H1299细胞的生长，IC50值分别为11.17、46.33和37.91µM[4]。向HEK293细胞灌注10µM的Dihydroberberine 10分钟，显著抑制了human ether-a-go-go related gene（hERG）钾通道的表达，并减少了hERG蛋白的转运[5]。
在体内，每日口服给予50mg/kg剂量的Dihydroberberine一周，显著减轻了高尿酸血症小鼠的肾脏损伤，表现为血清肌酐和血尿素氮水平显著下降，以及炎症细胞因子（TNF-α、IL-1β、IL-6和IL-18）水平降低[6]。连续7天每日灌胃给予Dihydroberberine（40mg/kg/day），可显著减轻carrageenan处理后的小鼠爪子肿胀程度、组织损伤范围和炎症细胞浸润[7]。连续8天每日灌胃给予Dihydroberberine（50mg/kg/day），缓解了葡聚糖硫酸钠（DSS）诱导的小鼠溃疡性结肠炎症状，并显著改善了肠道屏障功能[8]。
| 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. |
|
Reaction Conditions |
0.39, 0.78, 1.56, 3.12, 6.25, 12.5, 25 and 50μM; 48h |
|
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. |
|
Dosage form |
50mg/kg/day for 1 week; p.o. |
|
Applications |
Dihydroberberine treatment significantly alleviated renal damage in mice with hyperuricemia. |
|
References: |
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| Cas No. | 483-15-8 | SDF | |
| 别名 | 二氢小檗碱 | ||
| Canonical SMILES | COC1=CC=C(C=C23)C(CN2CCC(C3=C4)=CC5=C4OCO5)=C1OC | ||
| 分子式 | C20H19NO4 | 分子量 | 337.37 |
| 溶解度 | DMSO : 20 mg/mL (59.28 mM; Need ultrasonic (<70°C)) | 储存条件 | Store at -20°C,sealed storage, away from moisture and light |
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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 |
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动物数量 | 只 |
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