iridoids and palmatine

HuanglianJiedu decoction (HJD) is a classic prescription for heat-clearing away and detoxifying, which is used for the clinical treatment of sepsis, due to sepsis refers to the systemic inflammatory response induced by infection in western medicine, and infection belongs to the category of poison-heat syndrome in traditional Chinese medicine.. Previous study had elucidated the effective components from HJD with high affinity to lipid A, which can generate the release of pro-inflammatory-cytokines, resulting in sepsis. Now the anti-sepsis activities of these compounds were evaluated.. Immunofluorescence, immunohistochemical staining, ELISA and MTT methods were used to evaluated these compounds.. Immunofluorescence analysis evaluated the effects of compounds on the binding of FITC-LPS to RAW264.7 cells, and showed the fluorescence intensity was significant attenuated in geniposides, palmatine, baicalin and berberine groups (64 and 128 μg/mL) compared with model group (p < 0.05), which showed these compounds inhibit the combination of LPS with receptor of cells; immunohistochemical staining and ELISA method showed the TLR4 receptor expression, IL-6 and TNF-α levels were significant decreased in the groups treated with compounds, indicating that geniposides, baicalin, palmatine and berberine can play the role of anti-sepsis by inhibiting the expression of TLR4, the releasing of IL-6 and TNF-α; MTT assay showed that palmatine and berberine had a weak effect on cell viability, while others not, indicating that the compounds have protective activity.. It could be concluded the high affinity binding between these compounds and lipid A may be an important basis for its anti-LPS activity in vitro.

Topics: Animals; Berberine; Berberine Alkaloids; Cell Line; Drugs, Chinese Herbal; Flavonoids; Interleukin-6; Iridoids; Lipid A; Lipopolysaccharides; Mice; RAW 264.7 Cells; Sepsis; Toll-Like Receptor 4; Tumor Necrosis Factor-alpha

Hwangryunhaedok-tang (HHT) is a traditional herbal medicine that is used for the treatment of fever, inflammation, gastritis, and hypertension. In this study, we performed simultaneous determination of the five components, geniposide (1), baicalin (2), coptisine (3), palmatine (4), and berberine (5) in HHT by using a high-performance liquid chromatography-photodiode array (HPLC-PDA) analysis. We also evaluated the antioxidative activity of HHT and compounds 1-5 by measuring their effects on low-density lipoprotein (LDL) oxidation and antiproliferative abilities in vascular smooth muscle cells (VSMCs).. Five compounds were separated within 40 min by using a Gemini C18 column (temp. 35°C; two-component gradient elution; flow rate 1.0 mL/min; detector 240 and 277 nm). The activities of HHT and compounds 1-5 were tested with the radical scavengers 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt and 2,2-diphenyl-1-picrylhydrazyl, in thiobarbituric acid reactive substance assays, and in relative electrophoretic mobility assays using CuSO4-induced LDL oxidation systems. The antiproliferative effects of samples on platelet-derived growth factor (PDGF)-induced VSMC proliferation were studied by using a cell proliferation assay.. Regression analysis of the five major compounds showed good linearity (r (2) ≥ 0.9997) in different concentration ranges. The recoveries of the five compounds were in the range 86.31-110.78%, with relative standard deviations below 2.1%; those of intra- and interday precision were 0.04-3.78% and 0.04-1.69%, respectively. HHT reduced the oxidation properties of LDL induced by CuSO4 and inhibited cell proliferation in PDGF-treated VSMCs. Among the five components, compound 2 could effectively suppress LDL oxidation and PDGF-induced VSMC proliferation.. The established HPLC-PDA method will help to improve quality control of HHT. The results demonstrate that HHT has antiatherosclerotic activity and that it functions by modulating LDL oxidation and VSMC proliferation. The effects of HHT may be attributed, at least I part, to compound 2.

Topics: Animals; Antioxidants; Atherosclerosis; Berberine; Berberine Alkaloids; Biphenyl Compounds; Cell Proliferation; Chromatography, High Pressure Liquid; Coptis; Drugs, Chinese Herbal; Flavonoids; Gardenia; Iridoids; Lipoproteins, LDL; Medicine, Korean Traditional; Muscle, Smooth, Vascular; Phellodendron; Phytotherapy; Picrates; Platelet-Derived Growth Factor; Rats; Regression Analysis; Scutellaria

To observe the protective effect of active fractions of Huanglian Jiedu Decoction (HJD) on primary cortical neuron injury after oxygen-glucose deprivation (OGD)/reperfusion (R) injury. Methods Using macroporous resin method, HJDFE30, HJDFE50, HJDFE75, and HJDFE95 with 30%, 50%, 75%, and 95% alcohol were respectively prepared. Then the content of active components in different HJD fractions was determined with reverse phase high-performance liquid chromatography (RP-HPLC). The OGD/R injury model was induced by sodium dithionite on primary cortical neurons in neonate rats. MTT assay was used to observe the effect of four fractions (HJDFE30, HJDFE50, HJDFE75, and HJDFE95) and seven index components of HJD on the neuron viability.. RP-HPLC showed active component(s) contained in HJDFE30 was geniposide; baicalin, palmatine, berberine, and wogonside contained in HJDFE50; baicalin, berberine, baicalein, and wogonin contained in HJDFE75. The neuron viability was decreased after OGD for 20 min and reperfusion for 1 h, (P <0. 01), and significantly increased after administered with HJD, HJDFE30, HJDFE50, and HJDFE75 (P <0. 05, P <0. 01). Geniposide, baicalin, baicalein, palmatine, wogonside, and wogonin could increase the cortical neuron viability (P <0. 05, P <0. 01).. HJDFE30, HJDFE50, and HJDFE75, as active fractions of HJD, had protective effect on primary cortical neuron injury after OGD/R. Furthermore, geniposide, baicalin, and baicalein were main active components of HJD.

Topics: Animals; Berberine; Berberine Alkaloids; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavanones; Flavonoids; Glucose; Iridoids; Models, Animal; Neurons; Oxygen; Rats; Reperfusion Injury

Pharmacochemistry and integrated pharmacokinetics of six alkaloids (groenlandicine, berberine, palmatine, epiberberine, jatrorrhizine, and columbamine) after oral administration of Huang-Lian-Jie-Du-Tang (HLJDT) decoction were investigated in this paper. The method of plasma pharmacochemistry was applied to predict the potential bioactive components in HLJDT decoction. Based on the accurate molecular weight, 10 components including 2 flavonoids (baicalin and wogonoside), 1 iridoid glycoside (geniposide), and 7 alkaloids (above-mentioned 6 alkaloids and coptisine) were structurally identified. Then, integrated pharmacokinetics of the alkaloids in Sprague-Dawley rats after oral administration of HLJDT decoction was investigated by HPLC method. The results showed that the pharmacokinetic behaviors of the alkaloids were different although their chemical structures were similar. This study developed a method to predict the potential bioactive components in HLJDT decoction and research the pharmacokinetic behaviors of the potential bioactive components.

Topics: Administration, Oral; Alkaloids; Animals; Berberine; Berberine Alkaloids; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavanones; Flavonoids; Glucosides; Iridoids; Molecular Structure; Rats; Rats, Sprague-Dawley

Our previous studies showed that after oral administration of an Huang-Lian-Jie-Du-Tang (HLJDT) decoction, there is a higher concentration of the pure components, berberine, baicalin and gardenoside in the plasma of Middle cerebral artery occlusion (MCAO) rats than in sham-operated rats, The aim of the present study was to determine whether these components could be reliably measured in MCAO rat tissues. First, the plasma concentration-time profiles of berberine, palmatine, baicalin, baicalein and gardenoside were characterised in MCAO rats after oral administration of the aqueous extract of HLJDT. Subsequently, liver, lung and kidney tissues were obtained from sudden death MCAO rats in the absorption phase (0.25 h), the distribution phase (1.0 h) and the elimination phase (8.0 h) after administration of the HLJDT aqueous extract. An HPLC method was developed and validated for the determination of the distribution characteristics of berberine, palmatine, baicalin, baicalein and gardenoside simultaneously from the above-mentioned rat tissues. The results indicated that berberine, palmatine, baicalin and baicalein distributed rapidly and accumulated at high levels in the lung, while gardenoside distributed widely in the lung and the kidney. To the best of our knowledge, this is the first report to describe the distribution of the active ingredients derived from HLJDT in MCAO rat tissues. The tissue distribution results provide a biopharmaceutical basis for the design of the clinic application of HLJDT in cerebrovascular disease.

Topics: Animals; Berberine; Berberine Alkaloids; Drugs, Chinese Herbal; Flavanones; Flavonoids; Infarction, Middle Cerebral Artery; Iridoids; Male; Rats; Rats, Sprague-Dawley; Tissue Distribution

To study the phenomenon of subsidence emergence in the process of Huanglian Jiedu Tang decoction extraction, and the mechanism of subsidence emergence.. UV was applied to determine the concentration of total alkaloids and total flavones; Simultaneous determination of berberine, jatrorrhizine, palmatine, baicalin and geniposide were carried out by HPLC; The solid holdup and precipitation rate were calculated by the formula. The relativity among these parameters was analyzed by the SPSS software program.. The contains of berberine, jatrorrhizine, palmatine in total alkaloids showed a good correlation with total alkaloids. The correlation between baicalin and total flavones was lower than that between geniposide and total flavones. Compared to precipitation rate, solided hold up shows a larger relevance with index component. With the change of time, the total alkaloids represented by berberine alkaloids and baicalin at a certain concentration can be regarded as the equilibrium point, or one generated by the critical point of precipitation, the reaction can generate "sediments"; because "precipitation objects" generated, reducing the concentration of the above-mentioned components, destroy the" balance". The relevant components of herbal medicine increased dissolution rate, at the same time might partly dissolved sediment, reaching a new equilibrium state.

Topics: Alkaloids; Berberine; Berberine Alkaloids; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavones; Flavonoids; Fractional Precipitation; Iridoids; Plants, Medicinal

To determinate 3 kinds of effective components (5 compounds) in Huanglian Jiedu decoction at the same time, namely berberine, palmtine, jatrorrhizine, baicalin and geniposide.. A HPLC method detected by 3 different UV wavelengths 345 nm for berberine, palmtine and jatrorrhizine, 280 nm for baicalin, 238 nm for geniposide. Diamonsil C18 (4.6 mm x 250 mm, 5 microm) column was used, the mixture of H2O (A) , CH3OH (B) and 0.05% H3PO4 solution (C) as mobile phase in gradient mode. The column temperature was 35 degrees C and the flow rate was 1 mL x min(-1).. This method was applied to determined 5 compounds in Huanglian Jiedu decoction rapidly and accurately.. The quality control method is convenient, reasonable and credible for Huanglian Jiedu decoction.

Topics: Berberine; Berberine Alkaloids; Chromatography, High Pressure Liquid; Drug Combinations; Drugs, Chinese Herbal; Flavonoids; Iridoids; Plants, Medicinal; Pyrans; Quality Control; Ultraviolet Rays

High-performance liquid chromatography was employed to determine the contents of several marker substances such as gentiopicroside, mangiferin, palmatine, berberine, baicalin, wogonin and glycyrrhizin in Sann-Joong-Kuey-Jian-Tang. The separation was performed on a Cosmosil 5C18-AR column by gradient elution with 0.03% (v/v) phosphoric acid-acetonitrile (0 min, 90:10; 10 min, 87:13; 17-27 min, 77:23; 40 min, 62:38; 50 min, 55:45) as the mobile phase at a flow-rate of 1.0 ml/min, with detection at 254 nm. n-Propylparaben was used as the internal standard and seven regression equations revealed linear relationships between the peak-area ratios (marker substances/internal standard) and concentrations. The repeatability and reproducibility (relative standard deviation) of the method were in the ranges 0.02-1.78% and 1.44-4.95%, respectively.

Topics: Berberine; Berberine Alkaloids; Chromatography, High Pressure Liquid; Drugs, Chinese Herbal; Flavanones; Flavonoids; Glucosides; Glycyrrhetinic Acid; Glycyrrhizic Acid; Iridoid Glucosides; Iridoids; Pyrans; Reproducibility of Results; Xanthenes; Xanthones