Yellow crystalline powder
Phellodendron amurense Rupr.; Coptis chinensis Franch.
1,3-Benzodioxolo[5,6-a]benzo[g]quinolizinium, 5,6-dihydro-9,10-dimethoxy-, hydrochloride (1:1)/berberine hydrochloride/BERBERINE HCL/5,6-dihydro-9,10-dimethoxy-1,3-benzodioxolo[5,6-a]benzo[g]quinolizinium chloride (1:1)/9,10-dimethoxy-5,6-dihydro[1,3]dioxolo[4,5-g]isoquino[3,2-a]isoquinolin-7-ium chloride/Berberine (chloride)
Berberine has shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells; MAPK and Wnt/β-catenin pathways affected by Berberine.IC50 value:Target: Anticancer agentThe plant-based alkaloid berberine has potential therapeutic applications for breast cancer, although a better understanding of the genes and cellular pathways regulated by this compound is needed to define the mechanism of its action in cancer treatment. In this review, the molecular targets of berberine in various cancers, particularly breast cancer, are discussed. Berberine was shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells. Some signaling pathways affected by berberine, including the MAP (mitogen-activated protein) kinase and Wnt/β-catenin pathways, are critical for reducing cellular migration and sensitivity to various growth factors . Treatment with BBR(Berberine) in rats on the atherogenic diet reduced plasma total cholesterol and nonHDL cholesterol levels by 29%-33% and 31%-41%, respectively, with no significant differences being observed among the three doses . Berberine induced both apoptotic and autophagic death of HepG2 cells, which was associated with a significant activation of AMPK and an increased expression of the inactive form of acetyl-CoA carboxylase (ACC) . Berberine did not show major effects on viability of HEK-293 embryonic kidney and HCT116 colon carcinoma cells and was not toxic in concentrations up to 20 μM. Berberine inhibited β-catenin transcriptional activity and attenuated anchorage-independent growth. As a result of berberine treatment, cellular levels of active β-catenin were reduced concomitant with an increase in the expression of E-cadherin .
Methanol; Ethanol; Water
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Berberine hydrochloride is one the effective compound among Rhizoma Coptidis, Cortex Phellodendri, and other plants. There are several clinical functions of berberine hydrochloride including anti-inflammation, antitumor and immunoregulatory. However, the anti-inflammatory of berberine hydrochloride in ulcerative colitis is barely understood. In this study, we aimed to explore the effects of berberine hydrochloride on dextran sulfate sodium (DSS)-induced rats model of ulcerative colitis.
The severity of colitis were measured by body weight, survial rate, colon length and disease activity index (DAI) score. The cytokines expression include IL-1, IL-1β, IL-4, IL-6, IL-10, IL-12, TNF-α, TGF-β and IFN-γ were performed by RT-PCR and ELISA. Signaling pathway proteins such as p-STAT3, STAT3, p-NF-κB p65 and NF-κB p65 were analyzed by western blot and immunofluorescence. The proteins expression of tight junction were explored using western blotting and immunohistochemistry.
Rats were administered berberine hydrochloride showed less weight loss and longer colon length than the DSS-induced group. The expression of IL-1, IL-1β, IL-6, IL-12, TNF-α, TGF-β and IFN-γ were suppressed, yet the expression of IL-4 and IL-10 were up-regulated by berberine hydrochloride and sulphasalazine treatment compared to the model group. Meanwhile, treatment with berberine hydrochloride effectively increased the expression of SIgA and decreased the expression of iNOS, MPO, MDA. In terms of the biochemical analyses, the results showed that the expression of p-STAT3 was signifcantly increased, while the expression of p-NF-κB (p65) was suppressed compared to the model group via western blot and immunofluorescence analysis.
Berberine hydrochloride has beneficial effects in UC. The possible mechanism of anti-inflammatory response by berberine hydrochloride may involve in the blocking of the IL-6/STAT3/NF-κB signaling pathway. Collectively, these fndings provide evidence that berberine hydrochloride might be a useful herb medicine and serve as a promising novel therapy in the treatment of UC in humans.
Copyright © 2018. Published by Elsevier B.V.
Berberine hydrochloride; IL-6/STAT3/NF-κB; Inflammation; Ulcerative colitis
Protective effects of berberine hydrochloride on DSS-induced ulcerative colitis in rats.
Zhu L1, Gu P1, Shen H2.
Berberine, also known as berberine hydrochloride and isoquinoline alkaloid, is a major alkaloid from Coptis chinensis. Berberine’s extensive biological properties have previously been studied, and it has been used clinically for the treatment of diarrhea, hypertension, diabetes and other diseases. The present study aimed to determine the possible anticancer effects of berberine hydrochloride treatment on human non-small cell lung cancer (NSCLC) cell proliferation and apoptosis via the matrix metalloproteinase 2 (MMP-2) and the B-cell lymphoma 2 (Bcl-2)/Bcl-2-associated X protein (Bax) signaling pathway. Human A549 lung carcinoma cells were exposed to various concentrations of berberine hydrochloride in order to analyze the possible anticancer effects on NSCLC cell proliferation and apoptosis, using a MTT assay and an Annexin V-fluorescein isothiocyanate/propidium iodide apoptosis kit. Subsequently, the present study detected the expression of MMP-2, Bcl-2, Bax and Janus kinase 2 (Jak2). Berberine hydrochloride treatment inhibited the expression of vascular endothelial growth factor (VEGF) and nuclear factor κB (NF-κB) and transcription factor AP-1 (AP-1) proteins, in A549 cells. Firstly, it was revealed that berberine hydrochloride treatment may inhibit proliferation, increase cytotoxicity and enhance apoptosis in A549 cells. Subsequently, treatment with berberine hydrochloride significantly downregulated MMP-2 protein expression, increased the activity of the Bcl-2/Bax signaling pathway and suppressed the Jak2/VEGF/NF-κB/AP-1signaling pathways. These results suggest that berberine hydrochloride may be a potential novel anticancer drug, since it inhibits cell proliferation and promotes the rate of apoptosis of NSCLC cells by the suppression of the MMP-2, Bcl-2/Bax and Jak2/VEGF/NF-κB/AP-1 signaling pathways.
B-cell lymphoma 2/B-cell lymphoma 2-associated X protein; berberine hydrochloride; matrix metalloproteinase 2; non-small cell lung cancer
Berberine hydrochloride inhibits cell proliferation and promotes apoptosis of non-small cell lung cancer via the suppression of the MMP2 and Bcl-2/Bax signaling pathways.
Li J1, Liu F2, Jiang S1, Liu J3, Chen X1, Zhang S1, Zhao H1.
Berberine hydrochloride is an isoquinoline type alkaloid extracted from Berberidaceae, Rutaceae, and other plants. Previous reports have shown that berberine hydrochloride has anti-inflammatory properties. However, the underlying molecular mechanisms remain unclear. In this study, a lipopolysaccharide- (LPS-) induced murine model of mastitis was established to explore the anti-inflammatory action of berberine hydrochloride. Sixty mice that had been lactating for 5-7 days were randomly divided into six groups, including control, LPS, three berberine hydrochloride treatment groups (5, 10, and 20 mg/kg), and a dexamethasone (DEX) (5 mg/kg) group. Berberine hydrochloride was administered intraperitoneally 1 h before and 12 h after LPS-induced mastitis, and all mice were sacrificed 24 h after LPS induction. The pathological and histopathological changes of the mammary glands were observed. The concentrations and mRNA expressions of TNF-α, IL-1β, and IL-6 were measured by ELISA and qRT-PCR. The activation of TLR4 and NF-κB signaling pathways was analyzed by Western blot. Results indicated that berberine hydrochloride significantly attenuated neutrophil infiltration and dose-dependently decreased the secretion and mRNA expressions of TNF-α, IL-1β, and IL-6 within a certain range. Furthermore, berberine hydrochloride suppressed LPS-induced TLR4 and NF-κB p65 activation and the phosphorylation of I-κB. Berberine hydrochloride can provide mice robust protection from LPS-induced mastitis, potentially via the TLR4 and NF-κB pathway.
Anti-Inflammatory Effects of Berberine Hydrochloride in an LPS-Induced Murine Model of Mastitis.
Wang X1, Feng S1, Ding N1, He Y1, Li C1, Li M1, Ding X1, Ding H1, Li J1, Wu J1, Li Y1.
2018 Apr 15