Sorry if you misunderstood I mean it is used as decoction not as seasoning!
Is is very mild so you can use it to skin, mouth, tonsils, eyes, vaginal etc, it has soothing action, tastes like mixed sage - rooibos tea!
link1: J Ethnopharmacol. 2002 Feb;79(2):237-48. Links
Berberis crataegina DC. root exhibits potent anti-inflammatory, analgesic and febrifuge effects in mice and rats.Yeşilada E, Küpeli E.
Gazi University, Faculty of Pharmacy, Etiler 06330, Ankara, Turkey. yesilada@pharmacy.gazi.edu.tr
Extracts obtained from the roots and barks of various Berberis species are used as folk remedy worldwide for the treatment of various inflammatory ailments including lumbago, rheumatism and to reduce fever. Effects of the extracts and fractions from the roots of Berberis crataegina DC. (Berberidaceae) were studied using various in vivo models of inflammation in mice and rats and observed potent inhibitory activity against carrageenan- and serotonin-induced hind paw oedema, acetic acid-induced increased vascular permeability, castor oil-induced diarrhoea, and Freund's complete adjuvant-induced (FCA) arthritis models. Through bioassay-guided fractionation berberine was isolated as the main active ingredient. Moreover, a dose-dependent analgesic activity was determined, which assessed by using the model based on the inhibition of acetic acid-induced writhing reflexes, as well as antipyretic activity on FCA-induced increased body temperature. Acute and subchronic toxicity studies were also performed.
PMID: 11801387 [PubMed - indexed for MEDLINE]
link1: Pharmacol Toxicol. 2001 May;88(5):232-7.Links
Protective effect of berberine on cyclophosphamide-induced haemorrhagic cystitis in rats.Xu X, Malavé A.
Department of Pharmaceutical Sciences, College of Pharmacy, Nova Southeastern University, Fort Lauderdale, Florida 33328, USA.
The urotoxicity of cyclophosphamide and the protective effect of the herb berberine were investigated in this study. Administration of 150 mg/kg cyclophosphamide intraperitoneally caused a serious haemorrhagic cystitis in rats after 12 hr, including bladder oedema, haemorrhage, and dramatic elevation of nitric oxide metabolites (nitrite+nitrate) in urine and in plasma. To explore whether cyclophosphamide-induced cystitis could be prevented by berberine, rats were pretreated with a single dose or two doses of berberine at 50, 100, or 200 mg/kg intraperitoneally then challenged with cyclophosphamide (150 mg/kg, intraperitoneally). The results indicated that pretreatment of rats with berberine could reduce cyclophosphamide-induced cystitis in a dose-dependent manner. Furthermore, we found that two doses of berberine showed greater protection against cyclophosphamide urotoxicity than when given a single dose. In addition, our data shows that a single dose of 200 mg/kg berberine, or two doses of 100, and 200 mg/kg berberine could completely block cyclophosphamide-induced bladder oedema and haemorrhage, as well as nitric oxide metabolites increase in rat urine and plasma. In conclusion, our findings suggest that berberine could be a potential effective drug in the treatment of cyclophosphamide-induced cystitis, and provides us with the bright hope in the prevention and treatment of cyclophosphamide urotoxicity.
PMID: 11393582 [PubMed - indexed for MEDLINE]
link1: Int J Immunopharmacol. 1996 Oct;18(10):553-61. Links
Study on the anti-inflammatory action of Berberis vulgaris root extract, alkaloid fractions and pure alkaloids.Ivanovska N, Philipov S.
Institute of Microbiology, Bulgarian Academy of Sciences, Sofia, Bulgaria.
Extracts obtained from the roots of Berberidaceae species have been used in Eastern and Bulgarian folk medicine in rheumatic and other chronic inflammatory disorders. The investigations of the chemical composition and immunological properties show that their activity is mainly due to the alkaloid constituents. In the present study the anti-inflammatory properties of total ethanol extract (TEE), three alkaloid fractions, a major alkaloid berberine and oxyacanthine isolated from Berberis vulgaris roots were compared. All these were applied in acute inflammation (carrageenan- and zymosan-induced paw oedema), as the TEE showed the highest reducing effect. Their ability to alter in vivo and in vitro complement activity was determined. Also, the TEE was most effective in a chronic inflammatory model of adjuvant arthritis. The protoberberine fractions Bv2, Bv3 and berberine suppressed a delayed type hypersensitivity (DTH) reaction. Fraction Bv1 and berberine diminished antibody response against SRBC in vivo. The in vitro treatment of splenocytes with berberine showed that the anti-SRBC antibody synthesis was influenced in a different manner depending on the time course of its application. Oxyacanthine was less effective than berberine in the tests used.
PMID: 9080249 [PubMed - indexed for MEDLINE]
[cilor=blue]link[/color]1: Antimicrob Agents Chemother. 2002 Oct;46(10):3133-41. Links
Multidrug pump inhibitors uncover remarkable activity of plant antimicrobials.Tegos G, Stermitz FR, Lomovskaya O, Lewis K.
Department of Biology, Northeastern University, Boston, Massachusetts 02115, USA.
Plant antimicrobials are not used as systemic antibiotics at present. The main reason for this is their low level of activity, especially against gram-negative bacteria. The reported MIC is often in the range of 100 to 1,000 micro g/ml, orders of magnitude higher than those of common broad-spectrum antibiotics from bacteria or fungi. Major plant pathogens belong to the gram-negative bacteria, which makes the low level of activity of plant antimicrobials against this group of microorganisms puzzling. Gram-negative bacteria have an effective permeability barrier, comprised of the outer membrane, which restricts the penetration of amphipathic compounds, and multidrug resistance pumps (MDRs), which extrude toxins across this barrier. It is possible that the apparent ineffectiveness of plant antimicrobials is largely due to the permeability barrier. We tested this hypothesis in the present study by applying a combination of MDR mutants and MDR inhibitors. A panel of plant antimicrobials was tested by using a set of bacteria representing the main groups of plant pathogens. The human pathogens Pseudomonas aeruginosa, Escherichia coli, and Salmonella enterica serovar Typhimurium were also tested. The results show that the activities of the majority of plant antimicrobials were considerably greater against the gram-positive bacteria Staphylococcus aureus and Bacillus megaterium and that disabling of the MDRs in gram-negative species leads to a striking increase in antimicrobial activity. Thus, the activity of rhein, the principal antimicrobial from rhubarb, was potentiated 100- to 2,000-fold (depending on the bacterial species) by disabling the MDRs. Comparable potentiation of activity was observed with plumbagin, resveratrol, gossypol, coumestrol, and berberine. Direct measurement of the uptake of berberine, a model plant antimicrobial, confirmed that disabling of the MDRs strongly increases the level of penetration of berberine into the cells of gram-negative bacteria. These results suggest that plants might have developed means of delivering their antimicrobials into bacterial cells. These findings also suggest that plant antimicrobials might be developed into effective, broad-spectrum antibiotics in combination with inhibitors of MDRs.
PMID: 12234835 [PubMed - indexed for MEDLINE]
linkZhang MF, Shen YQ.
Berberine sulfate (Ber) 40 and 80 mg/kg ig reduced the purging effects of castor oil or Cassia angustifolia leaf in mice, but did not affect the gastrointestinal transport function of Chinese ink in normal mice. Ber 60 mg/kg ig significantly inhibited the increased vascular permeability induced by ip 0.7% acetic acid in mice. Ber 20 and 50 mg/kg sc markedly inhibited the increased vascular permeability induced by histamine 100 micrograms/0.1 ml ic in rats. Ber 4 and 8 mg/kg sc produced obvious inhibition in the xylene-induced swelling of mouse ear. The anti-inflammatory effects were enhanced in a dose-dependent manner. It is suggested that the antidiarrheal effect of Ber is relative to its restriction against exudative inflammation to a certain extent.
PMID: 2816420 [PubMed - indexed for MEDLINE
link1: Cardiovasc Res. 2009 Mar 19. [Epub ahead of print] Links
Berberine prevents hyperglycemia-induced endothelial injury and enhances vasodilatation via adenosine monophosphate-activated protein kinase and endothelial nitric oxide synthase.Wang Y, Huang Y, Lam KS, Li Y, Wong WT, Ye H, Lau CW, Vanhoutte PM, Xu A.
Department of Medicine, University of Hong Kong, L8-40, New Laboratory Block, 21 Sassoon Road, Hong Kong.
AIMS: Endothelial dysfunction is a key event that links obesity, diabetes, hypertension, and cardiovascular diseases. The aim of the present study was to examine the protective effect of the alkaloid drug berberine against hyperglycemia-induced cellular injury and endothelial dysfunction. METHODS AND RESULTS: In both cultured endothelial cells and blood vessels isolated from rat aorta, berberine concentration dependently enhanced phosphorylation of endothelial nitric oxide synthase (eNOS) at Ser(1177) and promoted the association of eNOS with heat shock protein 90 (HSP90), leading to an increased production of nitric oxide. Furthermore, berberine attenuated high glucose-induced generation of reactive oxygen species, cellular apoptosis, nuclear factor-kappaB activation, and expression of adhesion molecules, thus suppressing monocyte attachment to endothelial cells. In mouse aortic rings, berberine elicited endothelium-dependent vasodilatations and alleviated high glucose-mediated endothelial dysfunction. All these beneficial effects of berberine on the endothelium were abolished by either pharmacological inhibition of adenosine monophosphate-activated protein kinase (AMPK) or adenovirus-mediated overexpression of a dominant negative version of AMPK. CONCLUSION: Berberine protects against endothelial injury and enhances the endothelium-dependent vasodilatation, which is mediated in part through activation of the AMPK signalling cascade. Berberine or its derivatives may be useful for the treatment and/or prevention of endothelial dysfunction associated with diabetes and cardiovascular disease.
PMID: 19251722 [PubMed - as supplied by publisher]
link1: Atherosclerosis. 2006 May;186(1):29-37. Epub 2005 Aug 10. Links
Berberine inhibits rat vascular smooth muscle cell proliferation and migration in vitro and improves neointima formation after balloon injury in vivo. Berberine improves neointima formation in a rat model.Lee S, Lim HJ, Park HY, Lee KS, Park JH, Jang Y.
BK21 project of Medical Science, Yonsei University College of Medicine, Seoul, Republic of Korea..
Berberine, an alkaloid isolated from Chinese medicinal herbs, long been known for its anti-microbial activity and used to treat various infectious disorders in traditional Chinese medicine. In the present study, we have tested the hypothesis that berberine could inhibit vascular smooth muscle cell (VSMC) proliferation as it did in endothelial cells or cancer cells. Our results show that berberine significantly inhibits growth factor, mainly angiotensin II (AngII) and heparin binding epidermal growth factor (HB-EGF), induced VSMC proliferation and migration in vitro, and this effect is achieved by delaying or partially suppressing activation of Akt pathway rather than ERK pathway. Furthermore, we have examined its effect in vivo using a rat carotid artery injury model. A 28 days of chronic berberine treatment using an osmotic pump (100 microg kg(-1)d(-1), 2 weeks before and 2 weeks after the injury) improved neointima formation. The Neointima/Media ratio for control group and berberine treated group were 1.14+/-0.11 and 0.85+/-0.06 (p<0.05), respectively, and the reduction was approximately 25%. The result of the present study suggests a possibility of berberine being a potent agent to control restenosis after balloon angioplasty and warrants further study to gain a more complete understanding of its underlying mechanisms at a cellular level.
PMID: 16098530 [PubMed - indexed for MEDLINE]
link1: J Mol Cell Cardiol. 2009 Feb;46(2):234-40. Epub 2008 Oct 30. Links
Berberine, a natural lipid-lowering drug, exerts prothrombotic effects on vascular cells.Holy EW, Akhmedov A, Lüscher TF, Tanner FC.
Cardiovascular Research, Physiology Institute, University of Zürich, Switzerland.
Berberine (BBR) is a novel natural hypolipidemic agent. This study investigates whether BBR, similar to statins, exerts pleiotropic effects on endothelial tissue factor (TF) expression. BBR enhanced tumor necrosis factor-alpha (TNF-alpha) and thrombin induced TF expression in human endothelial cells by 3.5-fold. These effects were paralleled by an enhanced TF surface activity. In contrast, expression of TF pathway inhibitor was impaired. BBR enhanced TNF-alpha induced TF mRNA expression; however, TF promoter activity was inhibited. Activation of ERK and p38 remained unaffected, while c-Jun terminal NH(2) kinase was inhibited. BBR reduced TF mRNA degradation rates, prolonging its half-life from 1.1 to 4.3 h. The HMG-CoA reductase inhibitor simvastatin impaired thrombin induced TF expression, and BBR blunted this inhibition. Simvastatin did not affect TNF-alpha induced TF expression, and BBR enhanced TF under these conditions. Administration of BBR (100 mg/kg/d) increased TF activity and impaired TFPI expression in carotid artery of ApoE(-/-) mice. BBR enhances TF via mRNA stabilization at clinically relevant concentrations. Clinical application of BBR, either as an alternative to or in combination with statins, should be considered with caution.
PMID: 19014947 [PubMed - in process]
link1: Thromb Res. 2002 May 15;106(4-5):223-7. Links
Effect of berberine on arachidonic acid metabolism in rabbit platelets and endothelial cells.Huang CG, Chu ZL, Wei SJ, Jiang H, Jiao BH.
Department of Biochemistry and Molecular Biology, Second Military Medical University, 800 Xiang Yin Road, Shanghai 200433, PR China. xuyue500@lol365.com
The antiplatelet effect of berberine has been demonstrated in both laboratory research and clinical trials. In the present study, we show ex vivo that berberine significantly inhibited rabbit platelet aggregation induced by adenosine diphosphate, arachidonic acid, collagen or calcium ionophore A23187. The most potent inhibition was observed in collagen-induced platelet aggregation. Using radioimmunoassay, we show in vitro that berberine significantly inhibited synthesis of thromboxane A(2) in rabbit platelets induced by adenosine diphosphate, arachidonic acid or collagen in which collagen-induced thromboxane A(2) synthesis was also most potently inhibited. In our in vivo study using radioimmunoassay, the plasma prostacyclin level was reduced by 34.6% during a 30-min period after intravenous administration of 50 mg/kg of berberine. These results suggest that berberine might inhibit arachidonic acid metabolism in rabbit platelets and endothelial cells at two or more sites: cyclooxygenase in the arachidonic acid cascade and possibly the enzyme(s) for arachidonic acid liberation from membrane phospholipid(s).
PMID: 12297129 [PubMed - indexed for MEDLINE]
no pubmed reference1: Vascul Pharmacol. 2002 Dec;39(6):281-6.Links
Effects of berberine on angiotensin-converting enzyme and NO/cGMP system in vessels.Kang DG, Sohn EJ, Kwon EK, Han JH, Oh H, Lee HS.
Department of Herbal Resources, Professional Graduate School of Oriental Medicine and Medicinal Resources Research Center (MRRC), Wonkwang University, Iksan, Chonbuk, 570-749, Republic of Korea.
The present study was designed to examine the relaxant and anticonstrictive effects of berberine in the isolated thoracic aorta in rats. Intravenous injection of berberine lowered the mean arterial pressure (MAP) of anesthesized rats in a dose-dependent manner. The angiotensin-converting enzyme (ACE) activities were inhibited significantly by the addition of berberine in a dose-dependent manner of which the IC50 value of berberine for ACE was 42 micrograms/ml (125 microM). In the endothelium-intact rings, angiotensin I-induced contraction was markedly attenuated by prior exposure of aortic rings to berberine. Treatment of the intact aortic rings with berberine (10 micrograms/ml) increased the NOx and cGMP productions relative to the vehicle-treated group. Berberine induced a dose-dependent relaxation in phenylephrine-precontracted aortic rings, but NG-nitro-L-arginine methyl ester (L-NAME)-pretreated intact aortic rings or functional removal of the endothelium attenuated the berberine-induced relaxation without an effect on maximum response. These results suggest that berberine has a hypotensive effect, at least in part, via the inhibition of ACE and direct release of NO/cGMP in the vascular tissues.
PMID: 14567065 [PubMed - indexed for MEDLINE]
link1: Mult Scler. 2009 Feb;15(2):262-5. Epub 2009 Jan 9. Links
Angiotensin-converting enzyme (ACE) and ACE2 levels in the cerebrospinal fluid of patients with multiple sclerosis.Kawajiri M, Mogi M, Higaki N, Matsuoka T, Ohyagi Y, Tsukuda K, Kohara K, Horiuchi M, Miki T, Kira JI.
Department of Geriatric Medicine, Graduate School of Medicine, Ehime University, Ehime, Japan. mz1965kawajj@khc.biglobe.ne.jp
BACKGROUND: We reported a reduction in the levels of angiotensin II in cerebrospinal fluid (CSF) from patients with multiple sclerosis (MS). OBJECTIVE AND METHODS: To clarify the mechanism underlying this reduction, we assayed angiotensin-converting enzyme (ACE) and ACE2 concentrations along with angiotensin II concentrations in CSF samples from 20 patients with MS and 17 controls with non-neurological diseases. RESULTS: ACE levels were significantly elevated in patients with MS compared with controls (48.42 +/- 4.84 vs 44.71 +/- 3.9 pg/mL), whereas ACE2 levels were significantly reduced (2.56 +/- 0.26 vs 2.78 +/- 0.24 pg/mL), acting toward a normalization of angiotensin II levels. CONCLUSION: These results further indicate an alteration of the intrathecal renin-angiotensin system in patients with MS.
PMID: 19136547 [PubMed - in process
link1: J Hum Hypertens. 2008 Jun;22(6):389-93. Epub 2007 Dec 13. Links
Berberine-induced mobilization of circulating endothelial progenitor cells improves human small artery elasticity.Xu MG, Wang JM, Chen L, Wang Y, Yang Z, Tao J.
Department of Hypertension and Vascular Disease, The First Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China.
Berberine (BR) has been proved to promote endothelial function. However, the exact mechanisms underlying the effect of BR on endothelial function are not completely clear. It has been demonstrated that endothelial progenitor cells (EPCs) contribute to improvement of endothelial function and C2 small artery elasticity index is a surrogate parameter for the clinical evaluation of endothelial function. We hypothesized that BR-induced mobilization of circulating EPCs is associated with BR-related improvement of endothelial function. To address this assumption, 15 healthy volunteers were recruited and received BR 0.4 g three times per day for 30 days. The number of circulating CD34/KDR double-positive cells as well as C1 large and C2 small artery elasticity indices were evaluated before and after BR therapy. The number of CD34/KDR double-positive EPCs increased significantly after BR treatment (0.030+/-0.020% vs 0.017+/-0.010%, P<0.01). After 30-day BR therapy C2 increased significantly (6.21+/-2.80 ml per mm Hg x 100 vs 4.06+/-2.67 ml per mm Hg x 100, P<0.01) and C1 remained unchanged (10.79+/-3.27 ml per mm Hg x 10 vs 10.06+/-2.08 ml per mm Hg x 10, P>0.05). The increment of CD34/KDR double-positive EPCs was positively correlated with the increment of C2 (r=0.68, P<0.01). We concluded that BR-induced mobilization of circulating EPCs contributes to improvement of small artery elasticity in healthy persons.
PMID: 18075521 [PubMed - indexed for MEDLINE]
link1: Vascul Pharmacol. 2007 Aug-Sep;47(2-3):189-96. Epub 2007 Jun 19. Links
Inhibitory effects of Zoagumhwan water extract and berberine on angiotensin II-induced monocyte chemoattractant protein (MCP)-1 expression and monocyte adhesion to endothelial cells.Ko YJ, Lee JS, Park BC, Shin HM, Kim JA.
College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
Angiotensin II (Ang II), a potent vasoconstrictor, has been implicated in vascular inflammation through induction of reactive oxygen species (ROS) and pro-inflammatory genes. Among the chemokines, monocyte chemoattractant protein (MCP)-1 induced by Ang II acts as a central mediator of the inflammatory responses. In the present study, we found that the water extract of ZoaGumHwan (ZGH), a Korean herbal remedy, dose-dependently inhibited Ang II-induced U937 monocyte adhesion to human umbilical vein endothelial cells (HUVECs) and mRNA expression of MCP-1 in HUVECs and C-C chemokine receptor 2 (CCR-2) in U937 cells. In addition, ZGH water extract inhibited Ang II-induced generation of reactive oxygen species in HUVECs in a dose-dependent manner. Berberine, a major component of Coptis chinensis Franch, also showed similar effects on ROS production and MCP-1 expression induced by Ang II. These results suggest that Korean herbal remedy, ZGH, effectively protects against Ang II-induced endothelial inflammation.
PMID: 17631057 [PubMed - indexed for MEDLINE]
link1: Phytomedicine. 2006 May;13(5):334-42. Epub 2005 Sep 23. Links
Selective inhibition of vascular smooth muscle cell proliferation by coptisine isolated from Coptis rhizoma, one of the crude drugs composing Kampo medicines Unsei-in.Tanabe H, Suzuki H, Nagatsu A, Mizukami H, Ogihara Y, Inoue M.
Laboratory of Pharmacognosy, Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya 467-8603, Japan.
Acceleration of vascular smooth muscle cell (VSMC) proliferation is closely linked to the pathogenesis of vascular diseases. We, therefore, focused on traditional Japanese herbal medicines (Kampo medicines) used to ameliorate the impairment of microcirculation or blood stasis and screened them for their ability to inhibit rat VSMC proliferation. Among them, Unsei-in was found to effectively suppress VSMC proliferation, and Coptis rhizome was the responsible constituent crude drug. The extract of Coptis rhizome inhibited VSMC proliferation with the GI(50) value of 4.4 microg/ml, which was much lower than those against the proliferation of 3Y1, dRLh-84, B16, and HeLa cells. The Coptis rhizome extract inhibited the progression of VSMC arrested at G(0)/G(1) phase from G(0)/G(1) to S phase, but not that of 3Y1 cells. Biological assay-guided fractionation revealed that an alkaloid of Coptis rhizome, coptisine, was the active ingredient in selectively preventing VSMC proliferation with GI(50) of 3.3 microM (1.2 microg/ml). When the structurally-related isoquinoline alkaloids of protoberberine class were studied for their inhibitory activities, berberine decreased the VSMC proliferation with GI(50) of 95.1 microM (35.4 microg/ml), about 30 times higher concentration than coptisine, while palmatine failed to show any activity. This study provides evidence that coptisine, an ingredient of Unsei-in, prevents VSMC proliferation selectively at lower concentrations compared with various cells or other structurally related alkaloids.
PMID: 16635741 [PubMed - indexed for MEDLINE]
Coptis (Gold Thread or Goldenthread) is a genus of between 10–15 species of flowering plants in the family Ranunculaceae, native to Asia and North America.
Among other active compounds that Coptis chinensis contains is berberine[3] and coptisine
Berberine is a quaternary ammonium salt from the group of isoquinoline alkaloids. It is found in such plants as Berberis, goldenseal (Hydrastis canadensis), and Coptis chinensis, usually in the roots, rhizomes, stems, and bark. Berberine is strongly yellow colored, which is why in earlier times berberis species were used to dye wool, leather and wood. Wool is still today dyed with berberine in Northern India. Under ultraviolet light, berberine shows a strong yellow fluorescence.[1] Because of this it is used in histology for staining heparin in mast cells.[2] As a natural dye berberin has a Colour Index (CI) of 75160.
As a drug, berberine has showed some activity against fungal infections, candida, yeast, parasites, and bacterial/viral infections.[3][4] Some research has been undertaken into possible use against MRSA infection.[5] Although berberine has been tested and used in diabetes, prostate cancer cell lines,[6] liver and leukaemia cancers,[7] cardiac arrhythmia,[8] and leukemia,[9] it has not been researched thoroughly with humans. Berberine is considered an ineffective antibiotic, but a minority claim that when not tested in isolation but in conjunction with the other biochemical substances from the barberry plant, berberine might then be effective.[10]
Berberine is a component of some eye drops formulations[11]. There is some evidence that it is useful in the treatment of trachoma, [12] and it has been a standard treatment for leishmaniasis [13].
Goldenseal contains the isoquinoline alkaloids: hydrastine, berberine, berberastine, hydrastinine, tetrahydroberberastine, canadine, and canalidine.[11] A related compound, 8-oxotetrahydrothalifendine was identified in one study.[12] Berberine and hydrastine act as quaternary bases and are poorly soluble in water but freely soluble in alcohol.
Multiple bacteria and fungi, along with selected protozoa and chlamydia are susceptible to berberine in vitro[13]. Berberine alone has weak antibiotic activity in vitro since many microorganisms actively export it from the cell (although a whole herb is likely to work on the immune system as well as on attacking the microbes and hence have a stronger clinical effect than the antibiotic activity alone would suggest). Interestingly, there is some evidence for other berberine-containing species synthesizing an efflux pump inhibitor that tends to prevent antibiotic resistance, a case of solid scientific evidence that the herb is superior to the isolated active principle.[14] However, it is not yet known whether goldenseal contains a drug resistance efflux pump inhibitor, although many antimicrobial herbs do.
link1: Biochem Pharmacol. 2006 Mar 14;71(6):806-17. Epub 2006 Jan 31. Links
Berberine suppresses MEK/ERK-dependent Egr-1 signaling pathway and inhibits vascular smooth muscle cell regrowth after in vitro mechanical injury.Liang KW, Ting CT, Yin SC, Chen YT, Lin SJ, Liao JK, Hsu SL.
Institute of Clinical Medicine and Department of Medicine, National Yang-Ming University, Taipei, Taiwan.
Vascular smooth muscle cell (SMC) proliferation plays an important role in the pathogenesis of atherosclerosis and post-angioplasty restenosis. Berberine is a well-known component of the Chinese herb medicine Huanglian (Coptis chinensis), and is capable of inhibiting SMC contraction and proliferation, yet the exact mechanism is unknown. We therefore investigated the effect of berberine on SMC growth after mechanic injury in vitro. DNA synthesis and cell proliferation assay were performed to show that berberine inhibited serum-stimulated rat aortic SMC growth in a concentration-dependent manner. Mechanical injury with sterile pipette tip stimulated the regrowth of SMCs. Treatment with berberine prevented the regrowth and migration of SMCs into the denuded trauma zone. Western blot analysis showed that activation of the MEK1/2 (mitogen-activated protein kinase kinase 1/2), extracellular signal-regulated kinase (ERK), and up-regulation of early growth response gene (Egr-1), c-Fos and Cyclin D1 were observed sequentially after mechanic injury in vitro. Semi-quantitative reverse-transcription PCR assay further confirmed the increase of Egr-1, c-Fos, platelet-derived growth factor (PDGF) and Cyclin D1 expression in a transcriptional level. However, berberine significantly attenuated MEK/ERK activation and downstream target (Egr-1, c-Fos, Cyclin D1 and PDGF-A) expression after mechanic injury in vitro. Our study showed that berberine blocked injury-induced SMC regrowth by inactivation of ERK/Egr-1 signaling pathway thereby preventing early signaling induced by injury in vitro. The anti-proliferative properties of berberine may be useful in treating disorders due to inappropriate SMC growth.
PMID: 16448624 [PubMed - indexed for MEDLINE]
link1: Eur J Pharmacol. 2000 Jul 7;399(2-3):187-96. Links
Vasorelaxant and antiproliferative effects of berberine.Ko WH, Yao XQ, Lau CW, Law WI, Chen ZY, Kwok W, Ho K, Huang Y.
Department of Physiology, Faculty of Medicine, Chinese University of Hong Kong, Shatin, Hong Kong, People's Republic of China.
The present study was intended to examine the relaxant effects of berberine in rat isolated mesenteric arteries. Berberine produced a rightward shift of the concentration-response curve to phenylephrine and significantly reduced the maximal contractile response to phenylephrine. Berberine (10(-7)-3x10(-5) M) also relaxed the phenylephrine- and 9,11-dideoxy-11alpha, 9alpha-epoxy-methanoprostaglandin F(2alpha)-precontracted arteries with respective IC(50) values of 1.48+/-0.16x10(-6) and 2.23+/-0. 22x10(-6) M. Removal of a functional endothelium significantly attenuated the berberine-induced relaxation (IC(50): 4.73+/-0. 32x10(-6) M) without affecting the maximum relaxant response. Pretreatment with N(G)-nitro-L-arginine methyl ester (L-NAME) or methylene blue reduced the relaxant effect of berberine, and L-arginine (10(-3) M) partially antagonized the effect of L-NAME. In contrast, pretreatment with 10(-6) M glibenclamide or 10(-5) M indomethacin had no effect. Berberine (10(-5) M) reduced over by 50% the transient contraction induced by caffeine or phenylephrine in endothelium-denuded rings bathed in Ca(2+)-free Krebs solution. Pretreatment with putative K(+) channel blockers, such as tetrapentylammonium ions (1-3x10(-6) M), 4-aminopyridine (10(-3) M), or Ba(2+) (3x10(-4) M), significantly attenuated the berberine-induced relaxation in endothelium-denuded arteries. In contrast, tetraethylammonium ions (3x10(-3) M), charybdotoxin (10(-7) M) or glibenclamide (10(-6) M) were without effect. Berberine reduced the high-K(+)-induced sustained contraction and the relaxant response to berberine was greater in rings with endothelium (IC(50): 4.41+/-0.47x10(-6) M) than in those without endothelium (IC(50): 8.73+/-0.74x10(-6) M). However, berberine (10(-6)-10(-4) M) did not affect the high-K(+)-induced increase of intracellular [Ca(2+)] in cultured aortic smooth muscle cells. Berberine did not affect active phorbol ester-induced contraction in Ca(2+)-free Krebs solution. In addition, berberine inhibited proliferation of cultured rat aortic smooth muscle cells with an IC(50) of 2.3+/-0.43x10(-5) M. These findings suggest that berberine could act at both endothelium and the underlying vascular smooth muscle to induce relaxation. Nitric oxide from endothelium may account primarily for the berberine-induced endothelium-dependent relaxation, while activation of tetrapentylammonium-, 4-aminopyridine- and Ba(2+)-sensitive K(+) channels, inhibition of intracellular Ca(2+) release from caffeine-sensitive pools, or a direct relaxant effect, is likely responsible for the berberine-induced endothelium-independent relaxation. Mechanisms related to either Ca(2+) influx or protein kinase C activation may not be involved. Both vasorelaxant and antiproliferative effects may contribute to a long-term benefit of berberine in the vascular system.
PMID: 10884519 [PubMed - indexed for MEDLINE]
link1: Zhongguo Yao Li Xue Bao. 1989 Mar;10(2):174-6.Links
[Antidiarrheal and anti-inflammatory effects of berberine][Article in Chinese]
Zhang MF, Shen YQ.
Berberine sulfate (Ber) 40 and 80 mg/kg ig reduced the purging effects of castor oil or Cassia angustifolia leaf in mice, but did not affect the gastrointestinal transport function of Chinese ink in normal mice. Ber 60 mg/kg ig significantly inhibited the increased vascular permeability induced by ip 0.7% acetic acid in mice. Ber 20 and 50 mg/kg sc markedly inhibited the increased vascular permeability induced by histamine 100 micrograms/0.1 ml ic in rats. Ber 4 and 8 mg/kg sc produced obvious inhibition in the xylene-induced swelling of mouse ear. The anti-inflammatory effects were enhanced in a dose-dependent manner. It is suggested that the antidiarrheal effect of Ber is relative to its restriction against exudative inflammation to a certain extent.
PMID: 2816420 [PubMed - indexed for
link1: Eur J Cancer. 2008 Nov;44(16):2425-32. Epub 2008 Sep 11. Links
Protective effects of berberine on radiation-induced lung injury via intercellular adhesion molecular-1 and transforming growth factor-beta-1 in patients with lung cancer.Liu Y, Yu H, Zhang C, Cheng Y, Hu L, Meng X, Zhao Y.
The Key Laboratory of Cardiovascular Remodeling and Function Research, Shandong University, Qilu Hospital, Jinan, Shandong Province, China. liuyf@sdu.edu.cn
PURPOSE: To investigate the protective effects of berberine on radiation-induced lung injury (RILI) in non-small cell lung cancer (NSCLC) patients treated with radiotherapy. PATIENTS AND METHODS: In this randomised, double-blind study, 90 patients with NSCLC were divided into two groups. The trial group received radiation therapy plus berberine, and the control group received radiation therapy plus a placebo for 6 weeks. Soluble intercellular adhesion molecular-1 (sICAM-1) and transforming growth factor-beta-1 (TGF-beta1) were measured. RILI and pulmonary function were evaluated at 6 weeks and 6 months after treatment, respectively. RESULTS: Of the 90 patients enroled, 43 in the control group and 42 in the trial group completed the study. The incidence of RILI was significantly lower in the trial group at 6 weeks and 6 months than that in the control group (45.2% versus 72.1% and 35.7% versus 65.1%, respectively, both P<0.05). sICAM-1 levels in the trial group were significantly lower at weeks 6 and 12 (373.64+/-89.33 versus 459.53+/-123.59 and 447.83+/-111.21 versus 513.91+/-150.46, both P<0.01), and plasma TGF-beta1 levels were lower at week 3 and 6 (5.43+/-1.47 versus 6.22+/-1.78 and 5.93+/-2.39 versus 7.67+/-2.74, P<0.05 and 0.01, respectively) in comparison with the control group. Significant differences were observed in FEV1 (P=0.033) and DLCO (P=0.003) between patients receiving berberine and those receiving placebo. Independent-samples T-test showed reductions from baseline FVC at week 6 (P<0.05), and FEV1 and DLCO at month 6 (P<0.05 and 0.01, respectively) in the trial group were significantly smaller than that in the control group. CONCLUSION: Berberine significantly reduced the incidence of RILI, improved PF and decreased the levels of sICAM-1 and TGF-beta1. The exact mechanisms remain to be further explored.
PMID: 18789680 [PubMed - indexed for MEDLINE]
link1: Clin Exp Pharmacol Physiol. 2008 Mar;35(3):303-9. Epub 2007 Oct 30. Links
Protection by and anti-oxidant mechanism of berberine against rat liver fibrosis induced by multiple hepatotoxic factors.Zhang BJ, Xu D, Guo Y, Ping J, Chen LB, Wang H.
Department of Pharmacology, Basic Medical School of Wuhan University, Wuhan, China.
1. The aim of the present study was to investigate the effect and mechanism of berberine, an alkaloid extracted from the traditional Chinese medicine coptis, on rat liver fibrosis induced by multiple hepatotoxic factors. 2. Male Wistar rats were separated into five groups, a normal control group, a fibrotic control group and fibrotic groups treated with three different doses of berberine. The fibrotic models were established by introduction of multiple hepatotoxic factors, including CCl(4), ethanol and high cholesterol. Rats in the treatment groups were administered 50, 100 or 200 mg/kg berberine, intragastrically, daily for 4 weeks. Serum levels of alanine aminotransferase (ALT) and serum aspartate aminotransferase (AST), hepatic activity of superoxide dismutase (SOD) and hepatic malondialdehyde (MDA) and hepatic hydroxyproline (Hyp) content were determined. Liver biopsies were obtained for histological and immunohistochemical studies to detect the expressions of alpha-smooth muscle actin (SMA) and transforming growth factor (TGF)-beta1. 3. The results showed that, compared with the fibrotic control group, serum levels of ALT and AST and hepatic content of MDA and Hyp were markedly decreased, but the activity of hepatic SOD was significantly increased in berberine-treated groups in a dose-dependent manner. In addition, histopathological changes, such as steatosis, necrosis and myofibroblast proliferation, were reduced and the expression of a-SMA and TGF-b1 was significantly downregulated in the berberine-treated groups (P < 0.01). 4. These results suggest that berberine could be used to prevent experimental liver fibrosis through regulation of the anti-oxidant system and lipid peroxidation.
PMID: 17973934 [PubMed - indexed for MEDLINE]
http://www.ncbi.nlm.nih.gov/pubmed/11577981Bromelain is a crude extract from the pineapple that contains, among other components, various closely related proteinases, demonstrating, in vitro and in vivo, antiedematous, antiinflammatory, antithrombotic and fibrinolytic activities. The active factors involved are biochemically characterized only in part. Due to its efficacy after oral administration, its safety and lack of undesired side effects, bromelain has earned growing acceptance and compliance among patients as a phytotherapeutical drug. A wide range of therapeutic benefits has been claimed for bromelain, such as reversible inhibition of platelet aggregation, angina pectoris, bronchitis, sinusitis, surgical traumas, thrombophlebitis, pyelonephritis and enhanced absorption of drugs, particularly of antibiotics. Biochemical experiments indicate that these pharmacological properties depend on the proteolytic activity only partly, suggesting the presence of nonprotein factors in bromelain.
How is the EGCG trial going, Ursula? Hope you're well-Quercetin-Bromelain Forté™ provides a mixture of proteolytic enzymes and specific bioflavonoids that help regulate the immune response during inflammation as may occur during exposure to allergenic substances or irritants. Quercetin is a potent bioflavonoid compound that protects cells and tissues against free radical damage. Bromelain, papain, and pancreatin provide a mixture of protein-specific and other enzymes that help ensure proper breakdown of protein molecules that may otherwise cause tissue irritation and allergic responses.
