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Berberine
Selected AbstractsPROTECTION BY AND ANTI-OXIDANT MECHANISM OF BERBERINE AGAINST RAT LIVER FIBROSIS INDUCED BY MULTIPLE HEPATOTOXIC FACTORSCLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, Issue 3 2008Ben-Jian Zhang SUMMARY 1The 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. 2Male 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 CCl4, 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 a-smooth muscle actin (SMA) and transforming growth factor (TGF)-b1. 3The 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). 4These results suggest that berberine could be used to prevent experimental liver fibrosis through regulation of the anti-oxidant system and lipid peroxidation. [source] , -Cyclodextrin as Inhibitor of the Precipitation Reaction between Berberine and Glycyrrhizin in Decoctions of Natural Medicines: Interaction Studies of Cyclodextrins with Glycyrrhizin and Glycyrrhetic Acid by 1H-NMR Spectroscopy and Molecular-Dynamics CalculationHELVETICA CHIMICA ACTA, Issue 9 2008Miyoko Kamigauchi Abstract To prevent the precipitation reaction between glycyrrhizin (1) and berberine (3) in the decoctions of Glycyrrhiza/Coptis rhizome or Glycyrrhiza/Phellodendron bark, the presence of cyclodextrin (CD) in the mixture was proven to be effective. The preventing effect decreased in the order , -CD>, -CD, and no effect was observed for , -CD. On the other hand, the extraction degree of 1 from the natural medicine Glycyrrhia was considerably increased in the presence of , -CD, , -CD being much more effective than , - or , -CD. Thus, the blocking effect of CD on the precipitate formation between 1 and 3 is suggested to be primarily dependent on the stability of the inclusion complex of the CD with 1. To establish the structure of such a preferred inclusion complex, the interactions of 1 with , - and , -CDs were investigated by 1H-NMR spectroscopy and molecular-dynamics (MD) calculations. The 1H-NMR measurements showed that the increase in solubility of 1 in H2O is dependent on the degree of its inclusion into the CD, which depends on the molecular size of the CD. The MD calculations suggested that the H-bond interactions are sufficiently strong to form a stable [1/, -CD] complex, in which the lipophilic rings C, D, and E of 1 are fully inserted into the molecular cavity of , -CD, thus forming a kind of structure covered by a hydrophilic molecular capsule, while such an interaction mode is impossible for , - or , -CD. [source] Berberine inhibits Staphylococcus Epidermidis adhesion and biofilm formation on the surface of titanium alloyJOURNAL OF ORTHOPAEDIC RESEARCH, Issue 11 2009Xiaoqing Wang Abstract Biofilm formed by Staphylococcus epidermidis (S. epidermidis) is a common cause of periprosthetic infection. Recently, we have discovered that berberine is bacteriostatic for S. epidermidis. The purpose of the present study was to examine the effect of berberine on S. epidermidis adhesion and biofilm formation on the surface of titanium alloy, which is a popular material for orthopedic joint prostheses. Three strains of S. epidermidis (ATCC 35984, ATCC 12228, and SE 243) were used for in vitro experiment. Direct colony counting showed that berberine significantly inhibited S. epidermidis adhesion on the titanium alloy disk in 2 h at the concentration of 45 µg/mL. When examined with crystal violet staining, confocal laser scanning microscopy, and scanning electron microscopy, we found that higher concentrations (>30 µg/mL) of berberine effectively prevented the formation of S. epidermidis biofilm on the surface of the titanium disk in 24 h. These findings suggest that berberine is a potential agent for the treatment of periprosthetic infection. © 2009 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 27:1487,1492, 2009 [source] Process-induced phase transformation of berberine chloride hydratesJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 4 2010Henry H.Y. Tong Abstract Berberine is a natural quaternary ammonium alkaloid used clinically in the chloride salt form for the treatment of diarrhea in many Asian countries. Although the hydrate formation of berberine chloride (BCl) is well documented, the associated mechanism and implications in pharmaceutical formulation have not been studied in detail. In this study, pure BCl dihydrate and BCl tetrahydrate were recrystallized from water and their phase transformation behaviors under defined conditions were investigated. Additionally, pharmacopoeial grade BCl material consisting predominantly of the dihydrate form was examined for potential phase changes when being subjected to a conventional wet granulation procedure for tablet production. Results from solubility measurements, thermal analysis, variable temperature-powder X-ray diffraction (VT-PXRD), and variable temperature-Fourier transform infrared spectroscopy (VT-FTIR) confirmed the solid-state interconversions between the tetrahydrate and dihydrate at 30,49°C and between the dihydrate and anhydrate at 70,87°C. Consistent with the observed phase changes of the two pure hydrates, wet massing of the pharmacopoeial grade BCl sample led to a thermodynamics-driven transition to the tetrahydrate form at room temperature while subsequent tray drying at 50°C caused a reversion back to the dihydrate form. The rate and extent of such hydrate conversion depended largely on the water activity of the granulated powder matrix, which in turn was governed by the particular excipients employed. The present findings have important implications in the regulation of the hydrate forms of BCl in the finished products using specific excipients. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 1942,1954, 2010 [source] Neuropharmacological and pharmacokinetic properties of berberine: a review of recent researchJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 7 2009Minzhong Ye Abstract Objectives This review summarizes recent research on the neuropharmacological and pharmacokinetic properties of berberine, an isoquinoline alkaloid extracted from Coptidis rhizoma. Key findings Berberine has multiple neuropharmacological properties, such as neuroprection, anti-neuronal apoptosis, improvement of cerebral microcirculation and anti-Alzheimer's disease, and so on. The pharmacokinetic characteristics of berberine are that it is not easily absorbed and it is not stable in the gastrointestinal tract of animals or humans. Summary Further studies need to be carried out to develop berberine as a drug for nervous system diseases, such as brain ischaemia and Alzheimer's disease, that has favorable pharmacokinetic properties. [source] Effect of berberine on proliferation, cell cycle and apoptosis in HeLa and L1210 cellsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2003a Jantová Previous studies on the anticancer activity of protoberberine alkaloids against a variety of cancer cell lines were extended to human tumour HeLa and murine leukemia L1210 cell lines. An attempt was also made to investigate the relationship between the cytotoxic activity of berberine and its molecular mechanism of action. Cytotoxicity was measured in-vitro using a primary biochemical screening according to Oyama and Eagle, and the growth inhibition assay. The in-vitro cytotoxic techniques were complemented by cell cycle analysis and determination of apoptotic DNA fragmentation in L1210 cells. Berberine acted cytotoxically on both tumour cell lines. The sensitivity of leukemia L1210 cells to the berberine was higher than that of HeLa cells. The IC100 was below 100 ,g mL,1 for HeLa cells and approached a 10 , mL,1 limit for the leukemia L1210 cells. For both cell lines the IC50 was found to be less than 4 ,g mL,1, a limit put forward by the National Cancer Institute (NCI) for classification of the compound as a potential anticancer drug. In L1210 cells treated with 10,50 , mL,1 berberine, G0/G1 cell cycle arrest was observed. Futhermore, a concentration-dependent decrease of cells in S phase and increase in G2/M phase was detected. In addition, apoptosis detected as sub-G0 cell population in cell cycle measurement was proved in 25,100 ,g mL,1 berberine-treated cells by monitoring the apoptotic DNA fragmentation (DNA ladder) using agarose gel electrophoresis. [source] p53 cooperates berberine-induced growth inhibition and apoptosis of non-small cell human lung cancer cells in vitro and tumor xenograft growth in vivoMOLECULAR CARCINOGENESIS, Issue 1 2009Santosh K. Katiyar Abstract Berberine has been shown to have anti-carcinogenic effects. Since p53 is the most commonly mutated tumor suppressor gene, and a lack of functional p53 is associated with an increased risk of cancer development, we examined the effects of berberine on p53-positive and p53-deficient non-small cell human lung cancer cells in vitro and in vivo. Treatment of A549, which express wild-type p53, and H1299, which are p53-deficient, human lung cancer cells with berberine resulted in inhibition of cell proliferation and an increase in apoptotic cell death; however, A549 cells were more sensitive to the berberine-induced cytotoxic effects than H1299 cells. Further, the treatment of A549 cells with pifithrin-,, a specific inhibitor of p53, or transfection of A549 cells with a p53 antisense oligodeoxynucleotide resulted in a reduction in the berberine-induced inhibition of cell proliferation and apoptosis. The berberine-induced apoptosis of both the A549 and H1299 human lung cancer cells was associated with the disruption of mitochondrial membrane potential, reduction in the levels of Bcl-2, Bcl-xl while increase in Bax, Bak, and activation of caspase-3. Treatment of the cells with pan-caspase inhibitor (z-VAD-fmk) or caspase-3 inhibitor (z-DEVD-fmk) inhibited berberine-induced apoptosis, thus suggesting the role of caspase-3. Further, the administration of berberine by oral gavage inhibited the growth of s.c. A549 and H1299 lung tumor xenografts in athymic nude mice, however, the growth of tumor xenograft of H1299 cells was faster than A549 cells in mice and the chemotherapeutic effect of berberine was more pronounced in the p53-positive-A549 tumor xenograft than p53-deficient-H1299 tumor xenograft. © 2008 Wiley-Liss, Inc. [source] Photochemistry and Photocytotoxicity of Alkaloids from Goldenseal (Hydrastis canadensis L.) 3: Effect on Human Lens and Retinal Pigment Epithelial CellsPHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 4 2007Colin F. Chignell ABSTRACT The dried root or rhizome of Goldenseal (Hydrastis canadensis L.) contains several alkaloids including berberine, hydrastine, palmatine and lesser amounts of canadine and hydrastinine. Preparations derived from Goldenseal have been used to treat skin and eye ailments. Berberine, the major alkaloid in Goldenseal root powder, has been used in eye drops to treat trachoma, a disease characterized by keratoconjunctivitis. Berberine and palmatine are also present in extracts from Berberis amurensis Ruprecht (Berberidaceae) which are used to treat ocular disorders. We have previously shown that Goldenseal alkaloids are phototoxic to keratinocytes (Chem Res Toxicol. 14, 1529, 2001; ibid 19, 739, 2006) and now report their effect on human lens and retinal pigment epithelial cells. Human lens epithelial cells (HLE-B3) were severely damaged when incubated with berberine (25 ,M) and exposed to UVA (5 J cm,2). Under the same conditions, palmatine was less phototoxic and hydrastine, canadine and hydrastinine were inactive. Moderate protection against berberine phototoxicity was afforded by the antioxidants ascorbate (2 mM) and N -acetylcysteine (5 mM). When exposed to UVA (5 J cm,2) both berberine (10 ,M) and palmatine (10 ,M) caused mild DNA damage as determined by the alkaline comet assay which measures single strand breaks. Berberine and palmatine are the only Goldenseal alkaloids with appreciable absorption above 400 nm. Because light at wavelengths below 400 nm is cut off by the anterior portion of the adult human eye only berberine and palmatine were tested for phototoxicity to human retinal pigment epithelial (hRPE) cells. Although berberine did damage hRPE cells when irradiated with visible light (, > 400 nm) approximately 10 times higher concentrations were required to produce the same amount of damage as seen in lens cells. Palmatine was not phototoxic to hRPE cells. Neither berberine nor palmatine photodamaged DNA in hRPE. Infusions of Goldenseal are estimated to contain ,1 mM berberine, while in tinctures the alkaloid concentration may be more than 10 times higher. Our findings show that eyewashes and lotions derived from Goldenseal or containing berberine must be used with caution when the eyes are exposed to bright sunlight but that oral preparations are not likely to cause ocular phototoxicity. [source] Pharmacological and therapeutic effects of Berberis vulgaris and its active constituent, berberinePHYTOTHERAPY RESEARCH, Issue 8 2008Mohsen Imanshahidi Abstract Barberry (Berberis vulgaris L. family Berberidaceae) is well known in Iran and various parts of this plant including its root, bark, leaf and fruit have been used as folk medicine. The two decades of research has demonstrated different pharmacological and therapeutic effects of B. vulgaris and its isoquinoline alkaloids (particularly berberine). Studies carried out on the chemical composition of the plant show that the most important constituents of this plant are isoquinoline alkaloids such as berberine, berbamine and palmatine. Berberine represents one of the most studied among the naturally occurring protoberberine alkaloids. In addition to B. vulgaris (barberry), berberine is present in many other plants and is used for the treatment of different diseases. This article reviews the traditional uses and pharmacological effects of total extract and the most active ingredient of B. vulgaris (berberine). Copyright © 2008 John Wiley & Sons, Ltd. [source] In vitro antibacterial effect of berberine hydrochloride and enrofloxacin to fish pathogenic bacteriaAQUACULTURE RESEARCH, Issue 7 2010Defeng Zhang Abstract Berberine the main antibacterial substance in the rhizome of Coptis chinensis Franch, is used as an antimicrobial agent for a long time. This study was carried out to investigate the potential of berberine alone or in combination with enrofloxacin against six common fish pathogens for use in fish disease management in aquaculture. The minimum inhibitory concentrations (MICs) of berberine hydrochloride against Aeromonas hydrophila, Pseudomonas fluorescens, Vibrio vulnificus, Edwardsiella ictaluri, Escherichia coli and Streptococcus agalactiae were determined and to be >500, >500, >500, 300, 400 and 100 ,g mL,1 respectively. The minimal bactericidal concentrations (MBCs) of berberine hydrochloride to E. coli, E. ictaluri and S. agalactiae were 300,500 ,g mL,1. In combination with enrofloxacin, the MICs and MBCs of berberine hydrochloride significantly decreased against E. coli and E. ictaluri but not against Streptococcus dysgalactiae. These results demonstrated that the berberine hydrochloride enhanced the bactericidal effect of enrofloxacin and vice versa. The synergistic bactericidal effect of berberine hydrochloride and enrofloxacin suggest its potential use in fish disease management in aquaculture. This is the first study on the inhibitory effect of berberine hydrochloride against fish pathogenic bacteria. [source] Protective Effect of Berberine on Cyclophosphamide-Induced Haemorrhagic Cystitis in RatsBASIC AND CLINICAL PHARMACOLOGY & TOXICOLOGY, Issue 5 2001Xinyun Xu 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. [source] Analysis of major alkaloids in Rhizoma coptidis by capillary electrophoresis-electrospray-time of flight mass spectrometry with different background electrolytesELECTROPHORESIS, Issue 10 2008Junhui Chen Abstract CE-based techniques with DAD and detection ESI-TOF-MS have been developed for the analysis of seven protoberberine alkaloids and one aporphinoid alkaloid in Huanglian (Rhizoma coptidis), a well-known traditional Chinese herbal medicine. One aqueous BGE and one nonaqueous BGE were developed for CE-DAD and CE-MS analyses, and the CE-ESI-TOF-MS conditions including nebulizer gas pressure, the sheath-liquid composition, its flow rate, etc. were optimized. Eight main alkaloids in R. coptidis could be separated with baseline resolution by CE-DAD with these two different BGEs, and identified by TOF-MS analysis. Moreover, three major alkaloids (berberine, palmatine, and jatrorrhizine) could be quantified accurately by CE-DAD and CE-MS with the BGE system consisting of 50:50 v/v water and ACN containing 50,mM ammonium acetate at pH,6.8. Both techniques provided similar LODs and could be applied with confidence within similar linear dynamic range. However, reproducibility and speed of analysis were better using CE-DAD. When the CE technique was compared with the RP-HPLC method, the CE-DAD and CE-MS methods provided greater efficiency and faster analysis speed, i.e., achieving baseline resolution for all the eight main basic compounds in less than 14,min. The CE method, as a viable alternative to HPLC, is suitable for use as a routine procedure for the rapid identification and quantification of basic compounds in herbal or natural product applications. [source] Study of the mechanism of microwave-assisted extraction of Mahonia bealei (Fort.) leaves and Chrysanthemum morifolium (Ramat.) petalsFLAVOUR AND FRAGRANCE JOURNAL, Issue 3 2004Shan Gao Abstract A study of microwave-assisted extraction (MAE) for berberine in Mahonia bealei (Fort.) was carried out with batch equipment, in order to investigate the mechanism of the extraction related to structural changes in the glands. The extracts were analysed by ultraviolet-visible spectrophotometry at 347 nm. The parameters investigated were solvent types, the intensity of microwave energy and the process ratio (g/ml) of materials to solvent volume. The microwave-assisted extraction of different moisture content of materials was developed and optimized by means of three-factor and three-level orthogonal designs. Electron and optical micrographs of M. bealei (Fort.) leaves and Chrysanthemum morifolium (Ramat.) petals showed that the mechanism of the extractions was related to structural changes in the plant cells. Copyright © 2004 John Wiley & Sons, Ltd. [source] Identification of Major Alkaloids in Rat Urine by HPLC/DAD/ESI-MS/MS Method Following Oral Administration of Cortex Phellodendri DecoctionHELVETICA CHIMICA ACTA, Issue 2 2009Chun-Hui Ma Abstract A rapid, sensitive, and specific high-performance liquid chromatography (HPLC), diode-array detection, and mass-spectrometry techniques were developed for an identification of the constituents of Cortex Phellodendri and their metabolites in rat urine. The dose of 10,ml/kg of Cortex Phellodendri decoction was used for rats' oral administration. 0,24-h Urine was purified using a C18 solid-phase extraction cartridge, and then analyzed by an on-line MS detector. A total of 13,characteristic HPLC peaks were detected in the urine samples. Nine of them, including five alkaloids and four of their metabolites, were tentatively elucidated as magnoflorine (1), the glucuronide conjugate of demethyleneberberine (2), menisperine (3), jatrorrhizine 3- O -glucuronide (4), berberubine 9- O -glucuronide (5), jatrorrhizine (6), the monomethyl and monohydroxy catabolite of berberubine (7), palmatine (8), and berberine (9). Identification and structural elucidation of the metabolites were performed by comparing their MSn spectra data with those reported. [source] , -Cyclodextrin as Inhibitor of the Precipitation Reaction between Berberine and Glycyrrhizin in Decoctions of Natural Medicines: Interaction Studies of Cyclodextrins with Glycyrrhizin and Glycyrrhetic Acid by 1H-NMR Spectroscopy and Molecular-Dynamics CalculationHELVETICA CHIMICA ACTA, Issue 9 2008Miyoko Kamigauchi Abstract To prevent the precipitation reaction between glycyrrhizin (1) and berberine (3) in the decoctions of Glycyrrhiza/Coptis rhizome or Glycyrrhiza/Phellodendron bark, the presence of cyclodextrin (CD) in the mixture was proven to be effective. The preventing effect decreased in the order , -CD>, -CD, and no effect was observed for , -CD. On the other hand, the extraction degree of 1 from the natural medicine Glycyrrhia was considerably increased in the presence of , -CD, , -CD being much more effective than , - or , -CD. Thus, the blocking effect of CD on the precipitate formation between 1 and 3 is suggested to be primarily dependent on the stability of the inclusion complex of the CD with 1. To establish the structure of such a preferred inclusion complex, the interactions of 1 with , - and , -CDs were investigated by 1H-NMR spectroscopy and molecular-dynamics (MD) calculations. The 1H-NMR measurements showed that the increase in solubility of 1 in H2O is dependent on the degree of its inclusion into the CD, which depends on the molecular size of the CD. The MD calculations suggested that the H-bond interactions are sufficiently strong to form a stable [1/, -CD] complex, in which the lipophilic rings C, D, and E of 1 are fully inserted into the molecular cavity of , -CD, thus forming a kind of structure covered by a hydrophilic molecular capsule, while such an interaction mode is impossible for , - or , -CD. [source] Abstracts: The effects of Coptis japonica root extract and its key component, berberine, on human subcutaneous adipocytesINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 5 2010Keiko Yashiki(Tohi) pp.274,280 An increase of subcutaneous fat presses lymph vessels and blood vessels in skin tissues, and results in not only causing skin troubles such as skin sagging and swelling but also forming cellulite that makes bodylines worse. To expand further application of plant extracts to cosmetics, we focused on inhibitory effects of subcutaneous preadipocytes differentiation and facilitating lipolysis in adipocytes. In this study, in a screening test of a number of plant extracts, Coptis japonica root extract and its key component, berberine, showed potent inhibition of triglyceride accumulation and subcutaneous preadipocytes differentiation. Furthermore, Coptis japonica root extract and berberine down-regulated the mRNA expression level of several differentiation factors derived from subcutaneous preadipocytes. Coptis japonica root extract and berberine in subcutaneous adipocytes facilitated lipolysis in mature adipocytes. Our study suggested that Coptis japonica root extract and its key component, berberine, is expected to be useful for slimming and related skin troubles such as skin sagging, swelling, cellulite, and so on. [source] Berberine inhibits Staphylococcus Epidermidis adhesion and biofilm formation on the surface of titanium alloyJOURNAL OF ORTHOPAEDIC RESEARCH, Issue 11 2009Xiaoqing Wang Abstract Biofilm formed by Staphylococcus epidermidis (S. epidermidis) is a common cause of periprosthetic infection. Recently, we have discovered that berberine is bacteriostatic for S. epidermidis. The purpose of the present study was to examine the effect of berberine on S. epidermidis adhesion and biofilm formation on the surface of titanium alloy, which is a popular material for orthopedic joint prostheses. Three strains of S. epidermidis (ATCC 35984, ATCC 12228, and SE 243) were used for in vitro experiment. Direct colony counting showed that berberine significantly inhibited S. epidermidis adhesion on the titanium alloy disk in 2 h at the concentration of 45 µg/mL. When examined with crystal violet staining, confocal laser scanning microscopy, and scanning electron microscopy, we found that higher concentrations (>30 µg/mL) of berberine effectively prevented the formation of S. epidermidis biofilm on the surface of the titanium disk in 24 h. These findings suggest that berberine is a potential agent for the treatment of periprosthetic infection. © 2009 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 27:1487,1492, 2009 [source] High-performance liquid chromatography determination of hydrastine and berberine in dietary supplements containing goldensealJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 7 2001Ehab A. Abourashed Abstract Goldenseal (Hydrastis canadensis L., Ranunculaceae) is an ingredient of various dietary supplements intended for enhancing general body immunity. Many goldenseal products are currently available in the United States, either alone or in combination with echinacea. In most products, the content of the main active alkaloids of goldenseal, hydrastine and berberine, is not indicated on the label. A high-performance liquid chromatography (HPLC) method has been developed for the detection and quantification of hydrastine and berberine in a number of products obtained from the United States market. The method uses a Phenomenex® Luna C18 column, a mobile phase consisting of solvent A (100 mM sodium acetate/acetic acid, pH 4.0) and solvent B (acetonitrile/methanol; 90/10, v/v). Elution was run at a flow rate of 1.0 mL/min, with a linear gradient of 80, 40% A in B over 20 min and ultraviolet detection at 290 nm. A wide range of content variation was observed for both alkaloids in the tested samples. © 2001 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 90:817,822, 2001 [source] Neuropharmacological and pharmacokinetic properties of berberine: a review of recent researchJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 7 2009Minzhong Ye Abstract Objectives This review summarizes recent research on the neuropharmacological and pharmacokinetic properties of berberine, an isoquinoline alkaloid extracted from Coptidis rhizoma. Key findings Berberine has multiple neuropharmacological properties, such as neuroprection, anti-neuronal apoptosis, improvement of cerebral microcirculation and anti-Alzheimer's disease, and so on. The pharmacokinetic characteristics of berberine are that it is not easily absorbed and it is not stable in the gastrointestinal tract of animals or humans. Summary Further studies need to be carried out to develop berberine as a drug for nervous system diseases, such as brain ischaemia and Alzheimer's disease, that has favorable pharmacokinetic properties. [source] Acetylcholinesterase inhibitors from Stephania venosa tuberJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 5 2006Kornkanok Ingkaninan Acetylcholinesterase (AChE) inhibitors have lately gained interest as potential drugs in the treatment of Alzheimer's disease. Three AChE inhibitors were isolated from tubers of a Thai medicinal plant, Stephania venosa (Bl) Spreng. They were identified as quaternary protoberberine alkaloids, stepharanine, cyclanoline and N -methyl stepholidine. They expressed inhibitory activity on AChE with IC50 values (concentration that caused 50% inhibition of activity) of 14.1K ± 0.81, 9.23 ± 3.47 and 31.30 ± 3.67 ,M, respectively. The AChE inhibitory activity of these compounds was compared with those of the related compounds, palmatine, jatrorrhizine and berberine, as well as tertiary protoberberine alkaloids isolated from the same plant, stepholidine and corydalmine. The results suggest that the positive charge at the nitrogen of the tetrahydroisoquinoline portion, steric substitution at the nitrogen, planarity of the molecule or substitutions at C-2, ,3, ,9, and ,10 affect the AChE inhibitory activity of protoberberine alkaloids. [source] Effect of berberine on proliferation, cell cycle and apoptosis in HeLa and L1210 cellsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2003a Jantová Previous studies on the anticancer activity of protoberberine alkaloids against a variety of cancer cell lines were extended to human tumour HeLa and murine leukemia L1210 cell lines. An attempt was also made to investigate the relationship between the cytotoxic activity of berberine and its molecular mechanism of action. Cytotoxicity was measured in-vitro using a primary biochemical screening according to Oyama and Eagle, and the growth inhibition assay. The in-vitro cytotoxic techniques were complemented by cell cycle analysis and determination of apoptotic DNA fragmentation in L1210 cells. Berberine acted cytotoxically on both tumour cell lines. The sensitivity of leukemia L1210 cells to the berberine was higher than that of HeLa cells. The IC100 was below 100 ,g mL,1 for HeLa cells and approached a 10 , mL,1 limit for the leukemia L1210 cells. For both cell lines the IC50 was found to be less than 4 ,g mL,1, a limit put forward by the National Cancer Institute (NCI) for classification of the compound as a potential anticancer drug. In L1210 cells treated with 10,50 , mL,1 berberine, G0/G1 cell cycle arrest was observed. Futhermore, a concentration-dependent decrease of cells in S phase and increase in G2/M phase was detected. In addition, apoptosis detected as sub-G0 cell population in cell cycle measurement was proved in 25,100 ,g mL,1 berberine-treated cells by monitoring the apoptotic DNA fragmentation (DNA ladder) using agarose gel electrophoresis. [source] Simultaneous analysis of nine active components in Gegen Qinlian preparations by high-performance liquid chromatography with diode array detectionJOURNAL OF SEPARATION SCIENCE, JSS, Issue 14 2006Lihong Chen Abstract HPLC with diode array detection (HPLC/DAD) was employed to determine the quantities of puerarin, daidzin, daidzein, berberine, palmatine, coptisine, baicalin, baicalein, and glycyrrhizin in Gegen Qinlian preparations of three different pharmaceutical forms including decoction, dispensing granule and pill. The calibration curves for the nine bioactive components were linear in the given concentration ranges. The precision of the method was in the range of 0.2,5.0% (RSD), and the recoveries of this method were between 96.5 and 104.1%. The proposed method was applicable to analyze Gegen Qinlian preparations. [source] Analysis of protoberberine alkaloids in several herbal drugs and related medicinal preparations by non-aqueous capillary electrophoresisJOURNAL OF SEPARATION SCIENCE, JSS, Issue 1 2005Wen Hua Gao Abstract A simple, rapid, reproducible, and universal non-aqueous capillary electrophoresis method has been developed for the separation and determination of three major active protoberberine alkaloids including berberine, palmatine, and jatrorrhizine within 7 min. The effects of the concentrations of acetic acid and electrolyte, the ratio of organic solvent, and the applied voltage on the separation were investigated. The optimum running buffer was composed of 50 mM ammonium acetate, 0.5% (v/v) acetic acid, and 10% (v/v) acetonitrile in methanol. The applied voltage was 18 kV. The analytes were detected by UV at 214 nm. The linearities between peak areas and the concentrations of the analytes were also investigated, and they exhibit excellent linear behavior over the concentration ranges (correlation coefficients: 0.9975,0.9986). The method was successfully applied to determine the three alkaloids in several families of herbal drugs (Rhizoma Coptidis, Cortex Berberidis, Cortex Phellodendri, Herba Chelidonii,Caulis Mahoniae) and their relevant medicinal preparations for the first time, and the recoveries of the three constituents ranged between 95.6,103.2% for berberine, 97.5,103.3% for palmatine, and 96.1,103.6% for jatrorrhizine. [source] Molecular aspects on the interaction of protoberberine, benzophenanthridine, and aristolochia group of alkaloids with nucleic acid structures and biological perspectivesMEDICINAL RESEARCH REVIEWS, Issue 5 2007Motilal Maiti Abstract Alkaloids occupy an important position in chemistry and pharmacology. Among the various alkaloids, berberine and coralyne of the protoberberine group, sanguinarine of the benzophenanthridine group, and aristololactam-,- d -glucoside of the aristolochia group have potential to form molecular complexes with nucleic acid structures and have attracted recent attention for their prospective clinical and pharmacological utility. This review highlights (i) the physicochemical properties of these alkaloids under various environmental conditions, (ii) the structure and functional aspects of various forms of deoxyribonucleic acid (DNA) (B-form, Z-form, HL -form, protonated form, and triple helical form) and ribonucleic acid (RNA) (A-form, protonated form, and triple helical form), and (iii) the interaction of these alkaloids with various polymorphic DNA and RNA structures reported by several research groups employing various analytical techniques like absorbance, fluorescence, circular dichroism, and NMR spectroscopy; electrospray ionization mass spectrometry, thermal melting, viscosity, and DNase footprinting as well as molecular modeling and thermodynamic studies to provide detailed binding mechanism at the molecular level for structure,activity relationship. Nucleic acids binding properties of these alkaloids are interpreted in relation to their biological activity. © 2006 Wiley Periodicals, Inc. Med Res Rev, 27, No. 5, 649,695, 2007 [source] p53 cooperates berberine-induced growth inhibition and apoptosis of non-small cell human lung cancer cells in vitro and tumor xenograft growth in vivoMOLECULAR CARCINOGENESIS, Issue 1 2009Santosh K. Katiyar Abstract Berberine has been shown to have anti-carcinogenic effects. Since p53 is the most commonly mutated tumor suppressor gene, and a lack of functional p53 is associated with an increased risk of cancer development, we examined the effects of berberine on p53-positive and p53-deficient non-small cell human lung cancer cells in vitro and in vivo. Treatment of A549, which express wild-type p53, and H1299, which are p53-deficient, human lung cancer cells with berberine resulted in inhibition of cell proliferation and an increase in apoptotic cell death; however, A549 cells were more sensitive to the berberine-induced cytotoxic effects than H1299 cells. Further, the treatment of A549 cells with pifithrin-,, a specific inhibitor of p53, or transfection of A549 cells with a p53 antisense oligodeoxynucleotide resulted in a reduction in the berberine-induced inhibition of cell proliferation and apoptosis. The berberine-induced apoptosis of both the A549 and H1299 human lung cancer cells was associated with the disruption of mitochondrial membrane potential, reduction in the levels of Bcl-2, Bcl-xl while increase in Bax, Bak, and activation of caspase-3. Treatment of the cells with pan-caspase inhibitor (z-VAD-fmk) or caspase-3 inhibitor (z-DEVD-fmk) inhibited berberine-induced apoptosis, thus suggesting the role of caspase-3. Further, the administration of berberine by oral gavage inhibited the growth of s.c. A549 and H1299 lung tumor xenografts in athymic nude mice, however, the growth of tumor xenograft of H1299 cells was faster than A549 cells in mice and the chemotherapeutic effect of berberine was more pronounced in the p53-positive-A549 tumor xenograft than p53-deficient-H1299 tumor xenograft. © 2008 Wiley-Liss, Inc. [source] Photochemistry and Photocytotoxicity of Alkaloids from Goldenseal (Hydrastis canadensis L.) 3: Effect on Human Lens and Retinal Pigment Epithelial CellsPHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 4 2007Colin F. Chignell ABSTRACT The dried root or rhizome of Goldenseal (Hydrastis canadensis L.) contains several alkaloids including berberine, hydrastine, palmatine and lesser amounts of canadine and hydrastinine. Preparations derived from Goldenseal have been used to treat skin and eye ailments. Berberine, the major alkaloid in Goldenseal root powder, has been used in eye drops to treat trachoma, a disease characterized by keratoconjunctivitis. Berberine and palmatine are also present in extracts from Berberis amurensis Ruprecht (Berberidaceae) which are used to treat ocular disorders. We have previously shown that Goldenseal alkaloids are phototoxic to keratinocytes (Chem Res Toxicol. 14, 1529, 2001; ibid 19, 739, 2006) and now report their effect on human lens and retinal pigment epithelial cells. Human lens epithelial cells (HLE-B3) were severely damaged when incubated with berberine (25 ,M) and exposed to UVA (5 J cm,2). Under the same conditions, palmatine was less phototoxic and hydrastine, canadine and hydrastinine were inactive. Moderate protection against berberine phototoxicity was afforded by the antioxidants ascorbate (2 mM) and N -acetylcysteine (5 mM). When exposed to UVA (5 J cm,2) both berberine (10 ,M) and palmatine (10 ,M) caused mild DNA damage as determined by the alkaline comet assay which measures single strand breaks. Berberine and palmatine are the only Goldenseal alkaloids with appreciable absorption above 400 nm. Because light at wavelengths below 400 nm is cut off by the anterior portion of the adult human eye only berberine and palmatine were tested for phototoxicity to human retinal pigment epithelial (hRPE) cells. Although berberine did damage hRPE cells when irradiated with visible light (, > 400 nm) approximately 10 times higher concentrations were required to produce the same amount of damage as seen in lens cells. Palmatine was not phototoxic to hRPE cells. Neither berberine nor palmatine photodamaged DNA in hRPE. Infusions of Goldenseal are estimated to contain ,1 mM berberine, while in tinctures the alkaloid concentration may be more than 10 times higher. Our findings show that eyewashes and lotions derived from Goldenseal or containing berberine must be used with caution when the eyes are exposed to bright sunlight but that oral preparations are not likely to cause ocular phototoxicity. [source] Photostabilization of an Entomopathogenic Fungus Using Composite Clay Matrices,PHOTOCHEMISTRY & PHOTOBIOLOGY, Issue 2 2003Ephraim Cohen ABSTRACT To provide photostabilization for entomopathogenic fungi by anionic dyes, composite matrices based on clay,biopolymer combinations were prepared. In the first step, the negative surface charge of various clays (montmorillonite, attapulgite, bentonite and kaolinite) was reversed to positive by adsorption to the polycationic biopolymer chitosan. The second step involved adsorption of the toxicologically safe anionic dyes fast green (FG) and naphthol yellow S (NYS) to the clay complexes. Compared with cytotoxic photoprotectants like berberine, palmatine and acriflavine, the anionic dyes have no adverse effects up to a concentration of 1 M. In assays using various clay,chitosan,dye matrices and UV irradiation from a lamp source, it was evident that both FG and NYS provided considerable photostabilization for conidia of the entomopathogenic fungus Aschersonia spp. that served as a model biocontrol agent. Apparently, because of the light-dispersing property, bentonite and attapulgite per se provided significant photoprotection. All clay matrices containing FG provided a substantial photostabilization effect. [source] Pharmacological and therapeutic effects of Berberis vulgaris and its active constituent, berberinePHYTOTHERAPY RESEARCH, Issue 8 2008Mohsen Imanshahidi Abstract Barberry (Berberis vulgaris L. family Berberidaceae) is well known in Iran and various parts of this plant including its root, bark, leaf and fruit have been used as folk medicine. The two decades of research has demonstrated different pharmacological and therapeutic effects of B. vulgaris and its isoquinoline alkaloids (particularly berberine). Studies carried out on the chemical composition of the plant show that the most important constituents of this plant are isoquinoline alkaloids such as berberine, berbamine and palmatine. Berberine represents one of the most studied among the naturally occurring protoberberine alkaloids. In addition to B. vulgaris (barberry), berberine is present in many other plants and is used for the treatment of different diseases. This article reviews the traditional uses and pharmacological effects of total extract and the most active ingredient of B. vulgaris (berberine). Copyright © 2008 John Wiley & Sons, Ltd. [source] Antifungal activity of Mahonia aquifolium extract and its major protoberberine alkaloidsPHYTOTHERAPY RESEARCH, Issue 7 2003Anna Volleková Abstract The crude extract of Mahonia aquifolium (Berberidaceae) stem bark and its components berberine, palmatine and jatrorrhizine were screened for their inhibitory activity against a variety of dermatophytes and two Candida species of human origin using the in vitro dilution agar plate method. Jatrorrhizine was found to be the most effective against all fungal species tested (MIC ranges from 62.5 to 125 µg/mL), while the crude extract, berberine, and palmatine exhibited only marginal activity (MIC 500 to , 1000 µg/mL). Dermatophytes were more susceptible to jatrorrhizine than yeasts, and Scopulariopsis brevicaulis appeared the least sensitive species to all the compounds tested. The effects of the alkaloids were compared with those of .uconazole and bifonazole for which the MIC ranges were 12.5 to >100 µg/mL. Our results suggest that jatrorrhizine may serve as a leading compound for further studies to develop new antifungal agents with highly potent antifungal activity and low host toxicity. Copyright © 2003 John Wiley & Sons, Ltd. [source] Synthesis of the hydrophobic,hydrophilic macroporous poly divinylbenzene/poly(sodium acrylate) IPN resin and adsorption performance for berberinePOLYMERS FOR ADVANCED TECHNOLOGIES, Issue 12 2009Guqing Xiao Abstract The macroporous polydivinylbenzene/poly(methyl acrylate) interpenetrating polymer network (PDVB/PMA IPN) was prepared by the sequential suspension polymerization method, and was modified to be hydrophobic,hydrophilic macroporous polydivinylbenzene/poly (sodium acrylate) IPN (PDVB/PNaA IPN) by converting the PMA to PNaA under the condition of base. The effects of different mass ratio of the two networks and different cross-linking degree of the second network on the pore structure and adsorption capacity of PDVB/PNaA IPN resin were studied. The PDVB/PNaA IPN resin whose adsorption quantity is the biggest was chosen to study further. The pore structure, the weak acid exchange capacity, the water retention capacity, and the swelling ability of PDVB/PNaA IPN resin were measured. The study focused on the adsorption isotherms of berberine at different temperatures. Isosteric adsorption enthalpy, adsorption Gibbs free energies can be calculated according to thermodynamic functions. The results show that the saturated adsorption quantity of berberine is up to 109.4,mg,ml,1 (wet resin) by the way of dynamic adsorption and desorption experiment. The resin could be reused by the mixture with 0.5% sodium chloride and 80% ethanol. On the one hand the hydrophobic PDVB in the PDVB/PNaA IPN resin has the ability of adsorption using ,,, interaction, and on the other hand the hydrophilic PNaA in the PDVB/PNaA IPN resin has the ability of adsorption using ion exchange interaction. An important conclusion can be drawn that the PDVB/PNaA IPN resin has a promising application prospect in extracting and separating quaternary ammonium type alkaloids such as berberine. Copyright © 2009 John Wiley & Sons, Ltd. [source] | |||||||||||||||||||