BerberineCAS# 2086-83-1 |
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 2086-83-1 | SDF | Download SDF |
PubChem ID | 2353 | Appearance | Yellow powder |
Formula | C20H18NO4 | M.Wt | 336.4 |
Type of Compound | Alkaloids | Storage | Desiccate at -20°C |
Solubility | Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | ||
SMILES | COC1=C(C2=C[N+]3=C(C=C2C=C1)C4=CC5=C(C=C4CC3)OCO5)OC | ||
Standard InChIKey | YBHILYKTIRIUTE-UHFFFAOYSA-N | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | Berberine has neuroprotective, antidepressant, antineoplastic, and anti- fibrosis activities; it is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism, it may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS; it also may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states.Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 75160. |
Targets | ROS | COX | AMPK | Bcl-2/Bax | Caspase | TGF-β/Smad | ROS | GLUT | Akt | GSK-3 | Beta Amyloid |
In vitro | Berberine induces apoptosis and DNA damage in MG‑63 human osteosarcoma cells.[Pubmed: 25050485]Mol Med Rep. 2014 Oct;10(4):1734-8.Berberine, an isoquinoline alkaloid extracted from the dry root of Coptidis Rhizoma, has been found to exhibit marked anticancer effects on a panel of established cancer cells. Among the human osteosarcoma lines treated, MG‑63 cells were found to be the most sensitive.
The present study investigated the potential genotoxic effect of Berberine on MG‑63 human osteosarcoma cells. |
In vivo | Berberine improves endothelial function by inhibiting endoplasmic reticulum stress in the carotid arteries of spontaneously hypertensive rats.[Pubmed: 25686503]Biochem Biophys Res Commun. 2015 Mar 20;458(4):796-801.Activation of endoplasmic reticulum (ER) stress in endothelial cells leads to increased oxidative stress and often results in cell death, which has been implicated in hypertension.
The present study investigated the effects of Berberine, a botanical alkaloid purified from Coptidis rhizoma, on ER stress in spontaneously hypertensive rats (SHRs) and the underling mechanism. Berberine, a natural plant product, activates AMP-activated protein kinase with beneficial metabolic effects in diabetic and insulin-resistant states.[Pubmed: 16873688 ]Diabetes. 2006 Aug;55(8):2256-64.Berberine has been shown to have antidiabetic properties, although its mode of action is not known. Here, we have investigated the metabolic effects of Berberine in two animal models of insulin resistance and in insulin-responsive cell lines. Berberine ameliorates β-amyloid pathology, gliosis, and cognitive impairment in an Alzheimer's disease transgenic mouse model.[Pubmed: 22459600 ]Neurobiol Aging. 2012 Dec;33(12):2903-19.The accumulation of β-amyloid (Aβ) peptide derived from abnormal processing of amyloid precursor protein (APP) is a common pathological hallmark of Alzheimer's disease (AD) brains.
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Cell Research | Synergistic inhibitory effect of berberine and d-limonene on human gastric carcinoma cell line MGC803.[Pubmed: 25045784]J Med Food. 2014 Sep;17(9):955-62.This study aims at evaluating the anticancer effects of Berberine hydrochloride (Berberine) and d-limonene, alone and in combination, on human gastric carcinoma cell line MGC803 to determine whether Berberine and d-limonene work synergistically and elucidate their mechanisms. MGC803 cells were treated with Berberine and d-limonene, alone and in combination, for 24-48 h.
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Animal Research | Berberine reverses epithelial-to-mesenchymal transition and inhibits metastasis and tumor-induced angiogenesis in human cervical cancer cells.[Pubmed: 25217495]Berberine ameliorates renal interstitial fibrosis induced by unilateral ureteral obstruction in rats.[Pubmed: 24754438]Nephrology (Carlton). 2014 Sep;19(9):542-51.To investigate the potential effects of Berberine on renal interstitial fibrosis (RIF) of obstructed kidneys in a unilateral ureteral obstruction (UUO) rat model.
Mol Pharmacol. 2014 Dec;86(6):609-23.Metastasis is the most common cause of cancer-related death in patients, and epithelial-to-mesenchymal transition (EMT) is essential for cancer metastasis, which is a multistep complicated process that includes local invasion, intravasation, extravasation, and proliferation at distant sites.
When cancer cells metastasize, angiogenesis is also required for metastatic dissemination, given that an increase in vascular density will allow easier access of tumor cells to circulation, and represents a rational target for therapeutic intervention. Berberine has several anti-inflammation and anticancer biologic effects. |
Berberine Dilution Calculator
Berberine Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.9727 mL | 14.8633 mL | 29.7265 mL | 59.453 mL | 74.3163 mL |
5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL | 11.8906 mL | 14.8633 mL |
10 mM | 0.2973 mL | 1.4863 mL | 2.9727 mL | 5.9453 mL | 7.4316 mL |
50 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.1891 mL | 1.4863 mL |
100 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.5945 mL | 0.7432 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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Berberine, a natural plant product, activates AMP-activated protein kinase with beneficial metabolic effects in diabetic and insulin-resistant states.[Pubmed:16873688]
Diabetes. 2006 Aug;55(8):2256-64.
Berberine has been shown to have antidiabetic properties, although its mode of action is not known. Here, we have investigated the metabolic effects of Berberine in two animal models of insulin resistance and in insulin-responsive cell lines. Berberine reduced body weight and caused a significant improvement in glucose tolerance without altering food intake in db/db mice. Similarly, Berberine reduced body weight and plasma triglycerides and improved insulin action in high-fat-fed Wistar rats. Berberine downregulated the expression of genes involved in lipogenesis and upregulated those involved in energy expenditure in adipose tissue and muscle. Berberine treatment resulted in increased AMP-activated protein kinase (AMPK) activity in 3T3-L1 adipocytes and L6 myotubes, increased GLUT4 translocation in L6 cells in a phosphatidylinositol 3' kinase-independent manner, and reduced lipid accumulation in 3T3-L1 adipocytes. These findings suggest that Berberine displays beneficial effects in the treatment of diabetes and obesity at least in part via stimulation of AMPK activity.
Berberine ameliorates beta-amyloid pathology, gliosis, and cognitive impairment in an Alzheimer's disease transgenic mouse model.[Pubmed:22459600]
Neurobiol Aging. 2012 Dec;33(12):2903-19.
The accumulation of beta-amyloid (Abeta) peptide derived from abnormal processing of amyloid precursor protein (APP) is a common pathological hallmark of Alzheimer's disease (AD) brains. In this study, we evaluated the therapeutic effect of Berberine (BBR) extracted from Coptis chinensis Franch, a Chinese medicinal herb, on the neuropathology and cognitive impairment in TgCRND8 mice, a well established transgenic mouse model of AD. Two-month-old TgCRND8 mice received a low (25 mg/kg per day) or a high dose of BBR (100 mg/kg per day) by oral gavage until 6 months old. BBR treatment significantly ameliorated learning deficits, long-term spatial memory retention, as well as plaque load compared with vehicle control treatment. In addition, enzyme-linked immunosorbent assay (ELISA) measurement showed that there was a profound reduction in levels of detergent-soluble and -insoluble beta-amyloid in brain homogenates of BBR-treated mice. Glycogen synthase kinase (GSK)3, a major kinase involved in APP and tau phosphorylation, was significantly inhibited by BBR treatment. We also found that BBR significantly decreased the levels of C-terminal fragments of APP and the hyperphosphorylation of APP and tau via the Akt/glycogen synthase kinase 3 signaling pathway in N2a mouse neuroblastoma cells stably expressing human Swedish mutant APP695 (N2a-SwedAPP). Our results suggest that BBR provides neuroprotective effects in TgCRND8 mice through regulating APP processing and that further investigation of the BBR for therapeutic use in treating AD is warranted.
Berberine induces apoptosis and DNA damage in MG63 human osteosarcoma cells.[Pubmed:25050485]
Mol Med Rep. 2014 Oct;10(4):1734-8.
Berberine, an isoquinoline alkaloid extracted from the dry root of Coptidis Rhizoma, has been found to exhibit marked anticancer effects on a panel of established cancer cells. Among the human osteosarcoma lines treated, MG63 cells were found to be the most sensitive. The present study investigated the potential genotoxic effect of Berberine on MG63 human osteosarcoma cells. The effect of Berberine on cell viability was determined using a 3-(4,5-dimethylthiazol-2-yl)-2,5diphenyltetrazolium bromide assay and cell apoptosis was analyzed by flow cytometry and a DNA ladder assay. gammaH2AX focus formation was used to detect DNA damage in MG-63 cells. Berberine induced a significant increase in apoptosis in MG-63 cells in a concentration- and time-dependent manner, as determined by DNA fragmentation analysis and flow cytometry. Furthermore, Berberine induced significant concentration- and time-dependent increases in DNA damage compared with that in the negative control. In conclusion, these observations indicated that Berberine induced apoptosis and DNA damage in MG63 cells.
Berberine ameliorates renal interstitial fibrosis induced by unilateral ureteral obstruction in rats.[Pubmed:24754438]
Nephrology (Carlton). 2014 Sep;19(9):542-51.
AIM: To investigate the potential effects of Berberine on renal interstitial fibrosis (RIF) of obstructed kidneys in a unilateral ureteral obstruction (UUO) rat model. METHODS: Forty-eight rats were randomly divided into three groups: sham-operated, vehicle-treated UUO, and Berberine-treated UUO. Rats were gavaged with Berberine (200 mg/kg per day) or vehicle. Eight randomly chosen rats in each group were kiled and specimens were collected at day 14 after UUO. Physiological parameters and histological changes were assessed, RIF was evaluated using Masson's trichrome and Sirius red staining, oxidative stress and inflammation markers were determined, transforming growth factor beta1 (TGF-beta1), phosphorylated Smad3 (pSmad3) and alpha-smooth muscle actin (alpha-SMA) were measured using immunohistochemistry or western blotting analysis. The obstruction was relieved at day 14 by percutaneous nephrostomy in the remaining UUO rats. The resistive index of left kidneys was undertaken by coloured Doppler flow imaging at day 14 before nephrostomy and day 7 after the relief. RESULTS: Berberine treatment significantly attenuated RIF induced by UUO. The UUO-induced reduction in kidney superoxide dismutase and catalase activities increased, whereas elevated kidney malondialdehyde level markedly decreased. Berberine treatment significantly ameliorated UUO-induced inflammation, and decreased TGF-beta1, pSmad3 and alpha-SMA expression of UUO kidneys. Moreover, Berberine treatment significantly suppressed the increase of resistive index compared with UUO group at day 14 after UUO as well as day 7 after the relief of obstruction. CONCLUSION: Berberine treatment ameliorates RIF in a UUO rat model by inhibition of oxidative stress, inflammatory responses, and TGF-beta1/pSmad3 signalling.
Synergistic inhibitory effect of berberine and d-limonene on human gastric carcinoma cell line MGC803.[Pubmed:25045784]
J Med Food. 2014 Sep;17(9):955-62.
This study aims at evaluating the anticancer effects of Berberine hydrochloride (Berberine) and d-limonene, alone and in combination, on human gastric carcinoma cell line MGC803 to determine whether Berberine and d-limonene work synergistically and elucidate their mechanisms. MGC803 cells were treated with Berberine and d-limonene, alone and in combination, for 24-48 h. The inhibitory effects of these drugs on growth were determined by MTT assay. The combination index and drug reduction index were calculated with the Chou-Talalay method based on the median-effect principle. Flow cytometry and laser scanning confocal microscopy were employed to evaluate the effects of both drugs on cell-cycle perturbation and apoptosis, generation of reactive oxygen species (ROS), mitochondrial membrane potential, and expression of Bcl-2 and caspase-3 in MGC803 cells. Berberine or d-limonene alone can inhibit the growth of MGC803 cells in a dose- and time-dependent manner. Berberine and d-limonene at a combination ratio of 1:4 exhibited a synergistic effect on anti-MGC803 cells. The two drugs distinctly induced intracellular ROS generation, reduced the mitochondrial transmembrane potential (DeltaPsim), enhanced the expression of caspase-3, and decreased the expression of Bcl-2. The combination of Berberine and d-limonene showed more remarkable effects compared with drugs used singly in MGC803 cells. The combination of Berberine and d-limonene exerted synergistic anticancer effects on MGC803 cells by cell-cycle arrest, ROS production, and apoptosis induction through the mitochondria-mediated intrinsic pathway.
Berberine improves endothelial function by inhibiting endoplasmic reticulum stress in the carotid arteries of spontaneously hypertensive rats.[Pubmed:25686503]
Biochem Biophys Res Commun. 2015 Mar 20;458(4):796-801.
Activation of endoplasmic reticulum (ER) stress in endothelial cells leads to increased oxidative stress and often results in cell death, which has been implicated in hypertension. The present study investigated the effects of Berberine, a botanical alkaloid purified from Coptidis rhizoma, on ER stress in spontaneously hypertensive rats (SHRs) and the underling mechanism. Isolated carotid arteries from normotensive WKYs and SHRs were suspended in myograph for isometric force measurement. Protein phosphorylations and expressions were determined by Western blotting. Reactive oxygen species (ROS) level was measured by DHE staining. SHR carotid arteries exhibited exaggerated acetylcholine-triggered endothelium-dependent contractions (EDCs) and elevated ROS accumulation compared with WKY arteries. Moreover, Western blot analysis revealed the reduced AMPK phosphorylation, increased eIF2alpha phosphorylation, and elevated levels of ATF3, ATF6, XBP1 and COX-2 in SHR carotid arteries while these pathological alterations were reversed by 12 h-incubation with Berberine. Furthermore, AMPK inhibitor compound C or dominant negative AMPK adenovirus inhibited the effects of Berberine on above-mentioned marker proteins and EDCs. More importantly, ROS scavengers, tempol and tiron plus DETCA, or ER stress inhibitors, 4-PBA and TUCDA normalized the elevated levels of ROS and COX-2 expression, and attenuated EDCs in SHR arteries. Taken together, the present results suggest that Berberine reduces EDCs likely through activating AMPK, thus inhibiting ER stress and subsequently scavenging ROS leading to COX-2 down-regulation in SHR carotid arteries. The present study thus provides additional insights into the vascular beneficial effects of Berberine in hypertension.
Berberine reverses epithelial-to-mesenchymal transition and inhibits metastasis and tumor-induced angiogenesis in human cervical cancer cells.[Pubmed:25217495]
Mol Pharmacol. 2014 Dec;86(6):609-23.
Metastasis is the most common cause of cancer-related death in patients, and epithelial-to-mesenchymal transition (EMT) is essential for cancer metastasis, which is a multistep complicated process that includes local invasion, intravasation, extravasation, and proliferation at distant sites. When cancer cells metastasize, angiogenesis is also required for metastatic dissemination, given that an increase in vascular density will allow easier access of tumor cells to circulation, and represents a rational target for therapeutic intervention. Berberine has several anti-inflammation and anticancer biologic effects. In this study, we provided molecular evidence that is associated with the antimetastatic effect of Berberine by showing a nearly complete inhibition on invasion (P < 0.001) of highly metastatic SiHa cells via reduced transcriptional activities of matrix metalloproteinase-2 and urokinase-type plasminogen activator. Berberine reversed transforming growth factor-beta1-induced EMT and caused upregulation of epithelial markers such as E-cadherin and inhibited mesenchymal markers such as N-cadherin and snail-1. Selective snail-1 inhibition by snail-1-specific small interfering RNA also showed increased E-cadherin expression in SiHa cells. Berberine also reduced tumor-induced angiogenesis in vitro and in vivo. Importantly, an in vivo BALB/c nude mice xenograft model and tail vein injection model showed that Berberine treatment reduced tumor growth and lung metastasis by oral gavage, respectively. Taken together, these findings suggested that Berberine could reduce metastasis and angiogenesis of cervical cancer cells, thereby constituting an adjuvant treatment of metastasis control.