Berberine Sulfate Research Articles

Ornamental Barberry Twigs as an Underexploited Source of Berberine-Rich Extracts-Preliminary Research.

Berberine is a natural substance obtained from the roots of common barberry which, due to its strong pharmacological activity, is a commonly tested ingredient of dietary supplements. However, ornamental barberries, which are widely available, have not been considered as a source of berberine so far. The research aimed to check whether the ornamental barberry leaves and twigs could be used as an easily accessible raw material for obtaining natural berberine-rich extract with biological activity. Twigs and leaves of seven cultivars of ornamental barberry extracts were assessed for their polyphenol content, antioxidant potential (FRAP and DPPH), and berberine content using high-performance thin layer chromatography (HPTLC). As a reference, commercially available roots of Berberis vulgaris were used. For the next step, selected extracts (two with high and two with low berberine content) were tested on three cell lines (HaCaT, A375, Caco-2) using neutral red assay, and pure berberine sulfate (1-100 μg mL-1) was used as a control. Although the antioxidant potential of aqueous-methanol extracts of tested barberry was higher for the leaves than for the twigs, the berberine content was determined only in the twig extracts (from 42 to 676 mg 100 g-1). Studies on cell lines have shown the general toxicity of barberry extracts, but the observed effect was not directly correlated with the content of the alkaloid. However, the extract showed greater activity compared to an analogous dose of pure berberine, suggesting a significant effect of the matrix composition. For the first time, it was shown that the twigs of selected cultivars of ornamental barberry can be considered as a promising berberine source for the pharmaceutical industry to develop new effective formulations. However, these findings require further studies.

Construction of organ of Corti organoid to study the effects of berberine sulfate on damaged auditory cells.

Sensorineural hearing loss (SNHL) is mainly caused by injury or loss of hair cells (HCs) and associated spiral ganglion neurons (SGNs) in the inner ear. At present, there is still no effective treatment for SNHL in clinic. Recently, advances in organoid bring a promising prospect for research and treatment of SNHL. Meanwhile, three-dimensional (3D) printing provides a tremendous opportunity to construct versatile organoids for tissue engineering and regenerative medicine. In this study, gelatin (Gel), sodium alginate (SA), and polyvinyl alcohol (PVA) were used to fabricate biomimetic scaffold through 3D printing. The organ of Corti derived from neonatal mice inner ear was seeded on the PVA/Gel/SA scaffold to construct organ of Corti organoid. Then, the organ of Corti organoid was used to study the potential protective effects of berberine sulfate on neomycin-juried auditory HCs and SGNs. The results showed that the PVA/Gel/SA biomimetic 3D scaffolds had good cytocompatibilities and mechanical properties. The constructed organoid could maintain organ of Corti activity well in vitro. In addition, the injury intervention results showed that berberine sulfate could significantly inhibit neomycin-induced HC and SGN damage. This study suggests that the fabricated organoid is highly biomimetic to the organ of Corti, which may provide an effective model for drug development, cell and gene therapy for SNHL.

The in Vitro Effect of Berberine Sulfate and Berberine Chloride on the Growth and Aflatoxin Production by Aspergillus flavus and Aspergillus parasiticus

Background: Aflatoxins are harmful mycotoxins that can contaminate animal and human food products. To prevent toxigenic fungi growth and aflatoxin production, researchers have long investigated plant compounds as potential inhibitory agents. Objectives: This study aimed to evaluate the in vitro effect of berberine sulfate and berberine chloride on the growth and aflatoxin production of Aspergillus flavus and Aspergillus parasiticus. Methods: The antifungal activity of berberine salts was determined according to the Clinical and Laboratory Standards Institute (CLSI) document M38-A3. The aflatoxin levels were measured using high-performance liquid chromatography (HPLC) method. Results: The berberine sulfate and berberine chloride showed inhibitory effects against both Aspergillus species, with minimum inhibitory concentration (MIC) ranging from 125 to 500 µg/mL. Berberine sulfate at 2000 μg/mL and berberine chloride at 1000 μg/mL completely inhibited the mycelial growth of A. flavus, while berberine chloride at 1000 μg/mL also completely inhibited the mycelial growth of A. parasiticus. Berberine sulfate at 2000 µg/mL reduced the mycelial growth of A. parasiticus by 96.7%. Conclusion: Berberine salts significantly decreased the total aflatoxin production of Aspergillus species at MIC/2 and MIC/4 concentrations (P˂0.05). The results suggest that berberine salts could be used as potential antifungal and anti-aflatoxigenic agents against toxigenic Aspergillus isolates.

Separation and determination of the group-type composition of modern base and lubricating oils with a wide range of polarity, especially emitted to the environment

Lubricating oils are composed of base oils (>85% v/v) and enriching additives (<15% v/v). Three types of base oils may be distinguished: 1) traditional bases (obtained by low-volatile fractions from crude oil distillation refining), 2) synthetic bases (mainly poly-alpha-olefins, sometimes esters, especially succinic acid esters), 3) bases of natural origin (especially obtained from refined plant oils). The bases of natural origin are the only ones recommended for application when lubricating oil may be emitted to the environment (e.g. when the machine with an open cutting system is used). Group-type separation and analysis of group-type composition of base and lubricating oils are of significant importance in quality control and environmental monitoring. Due to the potentially wide range of polarity of the components of base and lubricating oils, group- type separation becomes a difficult separation problem. It is also a serious analytical problem due to the considerable diversity of physicochemical properties. The authors propose a new procedure for the separation and determination of the group-type composition of base and lubricating oils using thin-layer liquid chromatography in normal phase systems (abr. NP-TLC) on silica gel plates impregnated with berberine salt/in the coupling of thin-layer chromatography with flame ionization detection (abr. TLC-FID). A new, effective procedure of TLC plates impregnation with berberine sulphate was presented. The proposed procedure ensures the visualization of all groups of base oils. Extensive experimental research showed that a 2-step development procedure with application of n-hexane up to 100% height of development +15 min and further n-hexane: isopropanol: tri-fluoroacetic acid 96.25: 3: 0.75 (v: v: v) up to 75% height of development is advantageous for the group-type separation, both in TLC-FID and TLC.

Identification and Determination of Berberine from Arcangelisia Flava, East Borneo

Berberine is a compound that has various benefits but also has dangerous toxic effects. In Indonesia, the Regulation of the Head of the Food and Drug Supervisory Agency No. 10 of 2014 concerning the Prohibition of Producing and Circulating Traditional Medicines and Health Supplements Containing Coptis Sp, Berberis Sp, Mahonia Sp, Chelidonium Majus, Phellodendron Sp, Arcangelica Flava, Tinosporae Radix, and Catharanthus Roseus. Regulation No. 7 of 2018 (BPOM, 2018) also prohibits the presence of berberine in processed food. This research was conducted to determine the content of berberine compounds from the extract and stem fraction of Arcangelisia flava. The research was conducted by identifying the content of berberine by TLC method compared with Rf Berberine sulfate and determination of berberine content by HPLC method (High-Performance Liquid Chromatography) using column C-18 (ODS). Berberine content of methanol extract, n-hexane fraction, ethyl acetate fraction and Arcangelisia Flava methanol-water fraction were 0.0040, respectively; 0.0010; 0.0041, 0.0044%.

A novel high-performance thin layer chromatography method for quantification of long chain aliphatic hydrocarbons from Cissus quadrangularis

Context: A high-performance thin layer chromatography (HPTLC) is an analytical technique, which can be used for the determination of constituents or marker components in various parts of the plants. Earlier studies have estimated phytoconstituents from the stem and other aerial plant parts of Cissus quadrangularis Linn. Estimation of hydrocarbons can also be successfully done using HPTLC technique using suitable derivatization. Aims: To develop and validate a simple and rapid method for the estimation of long chain aliphatic hydrocarbons from the leaves of C. quadrangularis using HPTLC technique. Methods: Precoated silica gel 60 F254 plates were used as stationary phase. The mobile phase used was hexane (100 %). The detection of spots was carried out using berberine sulphate as detecting reagent. Results: The method was validated in terms of linearity, sensitivity, accuracy, and precision. Linearity range was found to be 2-10 µg/mL, limit of detection 0.127 µg/mL, and limit of quantification 0.384 µg/mL. Conclusions: A novel, simple, accurate, precise and sensitive HPTLC method has been developed and validated for the estimation of long chain aliphatic hydrocarbons obtained from the leaves of C. quadrangularis Linn.

Berberine Sulfate Attenuates Osteoclast Differentiation through RANKL Induced NF-κB and NFAT Pathways.

Osteoporosis, a metabolic bone disease, is characterized by an excessive formation and activation of osteoclasts. Anti-catabolic treatment using natural compounds has been proposed as a potential therapeutic strategy against the osteoclast related osteolytic diseases. In this study, the activity of berberine sulfate (an orally available form of berberine) on osteoclast differentiation and its underlying molecular mechanisms of action were investigated. Using bone marrow macrophages (BMMs) derived osteoclast culture system, we showed that berberine sulfate at the dose of 0.25, 0.5 and 1 μM significantly inhibited the formation of osteoclasts. Notably, berberine sulfate at these doses did not affect the BMM viability. In addition, we observed that berberine sulfate inhibited the expression of osteoclast marker genes, including cathepsin K (Ctsk), nuclear factor of activated T cells cytoplasmic 1 (NFATc1), tartrate resistant acid phosphatase (TRAcP, Acp5) and Vacuolar-type H+-ATPase V0 subunit D2 (V-ATPase d2). Luciferase reporter gene assay and Western blot analysis further revealed that berberine sulfate inhibits receptor for activation of nuclear factor ligand (RANKL)-induced NF-κB and NFAT activity. Taken together, our results suggest that berberine sulfate is a natural compound potentially useful for the treatment of osteoporosis.

Nano-cellulose 3D-networks as controlled-release drug carriers.

Bacterial cellulose (BC) membranes are used as the carrier for berberine hydrochloride and berberine sulphate to produce a new controlled release system. Release studies and transdermal experiments were carried out in vitro. Carrier BC can significantly extend the drug release time, in contrast to existing commercial carriers. Freeze-dried BC membranes 10 mm thick were optimized for drug delivery. The lowest release rate was in simulated gastric fluid (SGF) or in H2SO4 solution, the highest in simulated intestinal fluid (SIF) and an intermediate rate was found in alkaline conditions. The release curves closely followed the Ritger-Peppas model with free diffusion the most prominent mechanism. Scanning electron microscopy (SEM) analysis demonstrated that BC fibers were swollen in acid and base conditions. 1H high-resolution magic angle spinning nuclear magnetic resonance (1H HRMAS NMR) diffusion-ordered spectroscopy (DOSY) analysis showed that there was an interaction between the drugs and BC. The structure of BC, the media and the solubility of the drug all influenced the sustained-release behavior. The results from the release studies, the electron micrographs, and the transdermal experiments were in good agreement.

Nutritional supplementation of hop rho iso-alpha acids, berberine, vitamin D3, and vitamin K1 produces a favorable bone biomarker profile supporting healthy bone metabolism in postmenopausal women with metabolic syndrome

Metabolic syndrome poses additional risk for postmenopausal women who are already at risk for osteoporosis. We hypothesized that a nutritional supplement containing anti-inflammatory phytochemicals and essential bone nutrients would produce a favorable bone biomarker profile in postmenopausal women with metabolic syndrome. In this 14-week, randomized trial, 51 women were instructed to consume a modified Mediterranean-style, low-glycemic-load diet and to engage in aerobic exercise. Those in the intervention arm (n = 25) additionally received 200 mg hop rho iso-alpha acids, 100 mg berberine sulfate trihydrate, 500 IU vitamin D₃, and 500 μg vitamin K₁ twice daily. Forty-five women completed the study. Baseline nutrient intake did not differ between arms. Compared with baseline, the intervention arm exhibited an approximate 25% mean decrease (P < .001) in serum osteocalcin (indicative of bone turnover), whereas the placebo arm exhibited a 21% increase (P = .003). Serum 25-hydroxyvitamin D increased 23% (P = .001) in the intervention arm and decreased 12% (P = .03) in the placebo arm. The between-arm differences for osteocalcin and 25-hydroxyvitamin D were statistically significant. Serum insulin-like growth factor I was statistically increased in both arms, but the between-arm differences were not statistically significant. Subanalysis showed that among those in the highest tertile of baseline insulin-like growth factor I, the intervention arm exhibited a significant increase in amino-terminal propeptide of type I collagen, whereas the placebo arm showed a significant decrease at 14 weeks. Treatment with rho iso-alpha acids, berberine, vitamin D₃, and vitamin K₁ produced a more favorable bone biomarker profile indicative of healthy bone metabolism in postmenopausal women with metabolic syndrome.

Coptis Rhizome and Phellodendron Bark Extracts and Berberine Inhibit the Development of Mouse Embryos

After screening 269 crude drugs for their ability to inhibit the development of mouse zygotes, we found Coptis rhizome and Phellodendron bark to have inhibitory effects. We examined the effects of both extracts and of berberine, a major component of these plants, on in vitro development of zygotes and on fullterm fetal development in the mouse. Mouse zygotes were cultured in medium containing water-soluble extracts of Coptis rhizome or Phellodendron bark, or berberine at various concentrations for 5 days and the potential of zygotes to develop to blastocysts was examined. In addition, superovulated mice were intramuscularly injected with berberine and mated, and examined for the in vivo development of fertilized eggs to blastocysts and full-term fetuses. In vitro development of zygotes to blastocysts was almost completely inhibited when they were cultured in medium containing more than 0.1 µg/ml Coptis rhizome, 10 µg/ml Phellodendron bark, or 0.01 µg/ml berberine chloride or berberine sulfate. When superovulated and mated females received 100 µg berberine chloride once a day for 2 to 14 days, the proportions of recovered blastocysts and full-term fetuses were significantly decreased. The present study indicates the potential use of berberine as a contraceptive for animals.

Distribution, density and histochemical profiles of the lung mast cells during the post-hatching period of Japanese quails ( Coturnix coturnix japonica)

The distribution, density and histochemical characteristics of mast cells in the lungs of the Japanese quail were investigated during the post-hatching period. In the period starting from the first to the 60th day post-hatching, based on proteoglycan content, three types of mast cells, which were alcian blue-positive, safranin O-positive and alcian blue/safranin O-positive, were found to exist in the lungs. The application of staining with berberine sulphate demonstrated that, similar to the distribution of safranin O-positive cells, the heparin-containing cells were located in the periphery of large blood vessels. The percentages of mast cells in different localization sites of the lungs were found to vary with age in the post-hatching period with toluidine blue staining. The lack of any statistically significant increase/decrease in the number of mast cells per unit area of the right and left lung lobes is partially in favour of the proposal that the mast cell number increases with the growth of the lung volume in the post-hatching period.

Histochemical method for demonstrating quail mast cell types simultaneously

The development and application of selective staining methods for routine detection of mast cells are of considerable interest, because these cells play an important role in health and disease. The composition of cytoplasmic mast cell granules depends on the species and type of mast cell. The study reported here was conducted to investigate the combined use of aldehyde fuchsin (AF) and the Alcian blue-critical electrolyte concentration (AB-CEC) (pH 5.8, 0.3 M MgCl2) techniques for differentiating avian mast cell subtypes. Tissue samples from skin, intestines, and lungs of six healthy adult quail and two control rats were fixed in Carnoy's solution and 10% formolin for routine histological processing. To determine the staining properties of sulfated glycosaminoglycans (GAGs), a three-step staining technique was applied using berberine sulfate, AF, and AB-CEC. In quail, AF positivity following application of the AB-CEC technique was found only in the lungs, mostly in cells that gave a berberine sulfate-positive reaction, and this positivity was determined to be localized particularly in the nucleus and perinuclear cytoplasm. In other regions, the pale AF staining of cells that did not emit fluorescence when stained with berberine sulfate was determined to be replaced by a blue color after application of AB-CEC. The AF/AB-CEC (pH 5.8, 0.3 M MgCl2) technique demonstrated that rat and quail mast cells varied in both GAG types and their distribution within the cell. Especially in avian species, this technique can be applied to distinguish mast cells according to their GAG content. It can be used as an alternative to the AB/safranin O staining procedure for differentiating mast cells that contain and lack heparin.

Hop rho iso-alpha acids, berberine, vitamin D3 and vitamin K1 favorably impact biomarkers of bone turnover in postmenopausal women in a 14-week trial

Osteoporosis is a major health issue facing postmenopausal women. Increased production of pro-inflammatory cytokines resulting from declining estrogen leads to increased bone resorption. Nutrition can have a positive impact on osteoporosis prevention and amelioration. The objective of this study was to investigate the impact of targeted phytochemicals and nutrients essential for bone health on bone turnover markers in healthy postmenopausal women. In this 14-week, single-blinded, 2-arm placebo-controlled pilot study, all women were instructed to consume a modified Mediterranean-style low-glycemic-load diet and to engage in limited aerobic exercise; 17 randomized to the placebo and 16 to the treatment arm (receiving 200 mg hop rho iso-alpha acids, 100 mg berberine sulfate trihydrate, 500 IU vitamin D(3) and 500 microg vitamin K(1), twice daily). Thirty-two women completed the study. Baseline nutrient intake did not differ between arms. At 14 weeks, the treatment arm exhibited an estimated 31% mean reduction (P = 0.02) in serum osteocalcin (a marker of bone turnover), whereas the placebo arm exhibited a 19% increase (P = 0.03) compared to baseline. Serum 25-hydroxyvitamin D (25(OH)D) increased by 13% (P = 0.24) in the treatment arm and decreased by 25% (P < 0.01) in the placebo arm. The between-arm differences for OC and 25(OH)D were statistically significant. Serum IGF-I was increased in both arms, but the increase was more significant in the treatment arm at 14 weeks (P < 0.01). Treatment with hop rho iso-alpha acids, berberine sulfate trihydrate, vitamin D(3) and vitamin K(1) produced a more favorable bone biomarker profile that supports a healthy bone metabolism.

Desenvolvimento e validação de metodologia para quantificação de alcalóides totais como berberina em fitoterápico contendo Berberis vulgaris L.

A Robusterina® é um produto fitoterápico, com eficácia no tratamento de disfunções do ciclo menstrual. Em sua composição encontram-se Berberis vulgaris L., de ação sedativa e antiespasmódica; Gossypium herbaceum L., enemagoga, hemostática e ocitócica; Viburnum opulus L., antiespasmódico nas cólicas menstruais. De acordo com a Resolução RDC N° 48, de 16 de março de 2004, observa-se que o produto adequa-se na definição de Fitoterápico. A presença de alcalóides em Berberis vulgaris e a ausência de metodologias analíticas de quantificação para o produto, nos incentivaram a propor e validar um método apoiando-nos na Resolução RE N° 899, de 29 de Maio de 2003. Tal metodologia fundamenta-se na determinação espectrofotométrica de alcalóides utilizando-se Dragendorff como reagente precipitante, e o sulfato de berberina MerckÒ, como substância química de referência. A curva de calibração foi determinada com seis concentrações entre 40 e 200 mg/mL. A equação da reta é y = 0,0038x + 0,0092 com R² de 0,9996. Os parâmetros robustez, precisão, especificidade, limite de detecção e quantificação e exatidão foram avaliados estatisticamente com intervalo de confiança de 95% (teste t de Student, ANOVA).

A Taste Receptor Required for the Caffeine Response In Vivo

Caffeine is a methylxanthine present in the coffee tree, tea plant, and other naturally occurring sources and is among the most commonly consumed drugs worldwide. Whereas the pharmacological action of caffeine has been studied extensively, relatively little is known concerning the molecular mechanism through which this substance is detected as a bitter compound. Unlike most tastants, which are detected through cell-surface G protein-coupled receptors, it has been proposed that caffeine and related methylxanthines activate taste-receptor cells through inhibition of a cyclic nucleotide phosphodiesterase (PDE) . Here, we show that the gustatory receptor Gr66a is expressed in the dendrites of Drosophila gustatory receptor neurons and is essential for the caffeine response. In a behavioral assay, the aversion to caffeine was specifically disrupted in flies missing Gr66a. Caffeine-induced action potentials were also eliminated, as was the response to theophylline, the methylxanthine in tea. The Gr66a mutant exhibited normal tastant-induced action potentials upon presentation of theobromine, a methylxanthine in cocoa. Given that theobromine and caffeine inhibit PDEs with equal potencies , these data further support the role of Gr66a rather than a PDE in mediating the caffeine response. Gr66a is the first gustatory receptor shown to be essential for caffeine-induced behavior and activity of gustatory receptor cells in vivo.

Characterization of aqueous pores in plant cuticles and permeation of ionic solutes

Plant cuticles are lipid membranes with separate diffusion paths for lipophilic non-electrolytes and hydrated ionic compounds. Ions are lipid insoluble and require an aqueous pathway across cuticles. Based on experimental data, the aqueous pathway in cuticles has been characterized. Aqueous pores arise by hydration of permanent dipoles and ionic functional groups. They can be localized using ionic fluorescent dyes, silver nitrate, and mercuric chloride. Aqueous pores preferentially occur in cuticular ledges, at the base of trichomes, and in cuticles over anticlinal walls. Average pore radii ranged from 0.45 to 1.18 nm. Penetration of ions was a first order process as the fraction of the salt remaining on the cuticle surface decreased exponentially with time. Permeability of cuticles to ions depended on humidity and was highest at 100% humidity. Wetting agents increased rate constants by factors of up to 12, which indicates that the pore openings are surrounded by waxes. The pores in cuticular ledges of Helxine soleirolii allowed passage of berberine sulphate, which has a molecular weight of 769 g mol(-1). Increasing the molecular weight of solutes from 100 to 500 g mol(-1) decreased the rate constants of penetration by factors of 7 (Vicia faba) and 13 (Populus canescens), respectively. Half-times of penetration of inorganic salts and organic ions across Populus cuticles and Vicia leaf surfaces varied between 1 and 12 h. This shows that penetration of ionic compounds can be fairly rapid, and ions with molecular weights of up to 800 g mol(-1) can penetrate cuticles that possess aqueous pores.

Ectomycorrhizal impacts on nutrient uptake pathways in woody roots

Ectomycorrhizae are a common symbiosis between the roots of woody plants and fungi common to the soil. That ectomycorrhizae can assist the plant partner in absorbing mineral nutrients has long been established. However, the impact of mycorrhizae on pathways available for soil nutrients to enter the root system is not clear. In particular, the impact of the fungal mantle, which surrounds the root tips, is most critical. In the present study, we assessed the permeability of the Pinus banksiana/Hebeloma cylindrosporum fungal mantle to both berberine and radioactive sulfate ions. It was found that the fungal mantle was completely impermeable to tracer dye. To test the permeability to sulfate ions, a novel technique called the internal perfusion technique was employed. By this method, permeability can be assessed. The fungal mantle proved to be impermeable to sulfate over a 24-hour exposure period. Based on recent findings pertaining to root anatomy, this result suggests that the plant may be highly dependent on the fungus to supply mineral nutrients as there is little plant tissue capable of nutrient absorption outside the fungal mantle.

Distribution, histochemical and enzyme histochemical characterization of mast cells in dogs.

This study describes the distribution, proteoglycan properties and protease activity of mast cells from 15 different dog organs. In beagles and mixed breed dogs, staining with Alcian Blue-Safranin O revealed mast cells in all the organs examined. However, their numbers varied and they demonstrated unique localization patterns within some of these organs. Berberine sulphate fluorescence-positive mast cells were observed in the submucosa, muscularis and serosa of the intestines, as well as the tongue and liver (within the connective tissue). Mast cells within the intestinal mucosa were negative for, or demonstrated weak, berberine sulphate staining. Heterogeneity of mast cells in terms of the proteoglycans contained within their granules was further confirmed by determination of critical electrolyte concentrations (CECs). The CECs of mast cells within the connective tissue of several organs, including the intestines (submucosal and muscularis-serosal layers) were all greater than 1.0 M. The results from CEC experiments together with berberine staining indicate that heparin was contained within their granules. Relative to the CECs of mast cells in other organs, mast cells in the intestinal mucosa exhibited lower CECs, suggesting that the proteoglycans within their granules were of lower charge density and/or molecular weight. Although mast cells were classified into two groups by proteoglycans within the granules, enzyme histochemical analysis in beagles revealed three subtypes of mast cells: chymase (MC(C)), tryptase (MC(T)) and dual positive (MC(TC)) cells. There was no correlation between the proteoglycan content and enzyme properties of the mast cell granules.

Calorimetric study and thermal analysis of berberine sulphate

Abstract The heat capacities of berberine sulphate [(C20H18NO4)2SO43H2O] were measured from 80 to 390 K by means of an automated adiabatic calorimeter. Smoothed heat capacities, H T-H 298.15 and S T-S 298.15 were calculated. The loss of crystalline water started at about 339.30.2 K, and its peak temperature was 365.80.6 K. The peak temperature of decomposition for berberine sulphate was at about 391.40.4 K by DSC curve. TG-DTG analysis of this material was carried out in temperature range from 310 to 970 K. TG and DSC curves show that there is no melting in the whole heating process.

Rat lens aldose reductase inhibitory activities of Coptis japonica root-derived isoquinoline alkaloids.

The inhibitory activity of Coptis japonica root-derived materials was evaluated against lens aldose reductase isolated from male Sprague-Dawley rats and compared to that of three commercially available isoquinoline alkaloids (berberine sulfate, berberine iodide, and palmatine chloride), as well as quercitrin as aldose reductase inhibitor. The biologically active constituents of C. japonica extract were characterized as the isoquinoline alkaloids, berberine chloride and palmatine iodide, by spectral analysis. The inhibitory effects varied with both chemical and concentration used. The IC(50) values of berberine chloride and palmatine iodide are 13.98 and 13.45 nM, respectively. Among three berberines and two palmatines, the inhibitory activity was much greater for the choridated and sulfated analogues than for those with iodide. Quercitrin was a much more potent inhibitor than berberines and palmatines. Nonetheless, berberines and palmatines may be useful as lead compounds and new agents for aldose reductase inhibition.