OBJECTIVETo observe the impact on absorption of berberine and palmatine in different compatibilities of Wuji pill by the perfused rat intestine-liver preparation.

METHODUse L9 (3(4)) orthogonal design table, establish the perfused rat intestine-liver preparation, the twelve Wuji pill compatibilities duodenal administrated, collect the perfusate at different times points for LC-MS detection, calculate the absorbed score, Ka.

RESULTEvodiae Fructus and the absorption score, Ka of berberine and palmatine are inverse correlated. The most superior portion which promote the absorption is Coptidis Rhizoma-Evodiae Fructus-Paeoniae Radix Alba 3:1:3.

CONCLUSIONEvodiae Fructus suppressed the absorption of berberine and palmatine. With the different portion the absorption also have big different.

Animals ; Berberine ; metabolism ; pharmacokinetics ; Berberine Alkaloids ; metabolism ; pharmacokinetics ; Drugs, Chinese Herbal ; pharmacology ; Evodia ; chemistry ; Intestinal Absorption ; drug effects ; Male ; Rats

OBJECTIVETo observe the effects of tetrahydropalmatine, dehydrocorydaline, berberine and palmatine on anoxia and peroxidation injuries in cardiomyocytes, and study the marterial basis of the anti-ischemia effect on myocardium of Rhizoma Corydalis.

METHODNeonatal rat cardiomyocytes were cultured in vitro, and subjected to an anoxia-reoxia and the hydrogen peroxide injury models. The four compounds were added into the culture medium. The cell viability was measured by MTT method to determine the safe concentrations and the anti-hydrogen peroxide injury effects of the compounds. The LDH activity in culture mediums was measured with the enzyme reaction dynamics-monitoring method to value the anti-anoxia injury effects of the compounds.

RESULTAt most up to 500 mg x L(-1), tetrahydropalmatine showed no sinificant effect on the cell viability, while dehydrocorydaline, berberine and palmatine significantly decreased the cell viability, exceeding 6.3, 0.6 and 6.3 mg x L(-1), respectively (P < 0.05 or P < 0.01). Tetrahydropalmatine, dehydrocorydaline, berberine and palmatine significantly inhibited LDH leakage induced by anoxia-reoxia injury, at concentrations of 50-100, 1.25-5, 4 and 30 mg x L(-1), respectively (P < 0.05 or P < 0.01). None of the four compounds showed significant effect on the hydrogen peroxide injury.

CONCLUSIONThe anti-ischemia effect in myocardium of Rhizoma Corydalis is related to the direct protective effects on cardiomyocytes of its components, tetrahydropalmatine, dehydrocorydaline, berberine and palmatine, amomg which tetrahydropalmatine and dehydrocorydaline are the most important, the former with high safety and low efficacy, while the latter with low safety and high efficacy. And the direct protective effects on cardiomyocytes of these four components may be attained through mechanisms other than anti-peroxidation.

Alkaloids ; pharmacology ; Animals ; Animals, Newborn ; Berberine ; pharmacology ; Berberine Alkaloids ; pharmacology ; Cell Hypoxia ; drug effects ; Cells, Cultured ; Hydrogen Peroxide ; pharmacology ; Myocytes, Cardiac ; drug effects ; metabolism ; Rats

OBJECTIVETo reveal the response of content berberine in root of Coptis chinensis to different intensity of UV-B radiation, and provide the theory basis for promoting the content of berberine.

METHODFour groups of UV-B radiation were set in the experiment which included: natural light control (0 W x m(-2)), UL (0.05 W x m(-2)), UM (0.10 W x m(-2)), UH (0.20 W x m(-2)). The special photosynthesis character, PPP pathway in the primary metabolism and lyrosinase activity, the changes of berberine in the root of C. chinensis were measured under different UV-B radiation.

RESULTPhotosynthetic pigment, qN, Fo, ETR, activity of glucose-6-phosphate dehydrogenase and the content of berberine in the root of C. chinensis, all of these parameters were lower than other groups under the UH radiation. However, under the UM radiation, C. chinensis protected itself from the light UV-B radiation by promoting the power of photosynthesis and PPP pathway in order to produce more NADPH and secondary metabolites.

CONCLUSIONC. chinensis increases its photosynthetic ability and PPP pathway which can furnish more precursor of secondary metabolites and NADPH that are needed in the secondary metabolism. Furthermore, the content of berberine increases correspondingly. The research provide the example for increasing the content of berberine in C. chinensis cultivation.

Berberine ; analysis ; Coptis ; chemistry ; drug effects ; metabolism ; Glucosephosphate Dehydrogenase ; metabolism ; NADP ; metabolism ; Photosynthesis ; radiation effects ; Ultraviolet Rays

A new MS-titration method for the non-covalent binding of protein-ligand based on the research of berberine and alpha1-acid glycoprotein was established. The major presumption of new method is that the total concentration of protein-ligand complex is approximately the same as the total concentration of acting protein if a certain extent of affinity is existed between protein and ligand, in addition, the mole amount of acting ligand is more than that of acting protein. The non-covalent binding behaviours between berberine and alpha1-acid glycoprotein was studied by using electrospray ionization ion trap mass spectrometry (ESI-ITMS) , and the results were verified by fluorescence quenching method. The results showed that the binding behaviours between berberine and alpha1-acid glycoprotein, for example, stability constant, number of binding site, type of the main binding force, were almost the same by using the new MS-titration method and fluorescence quenching method. Comparing with the reported MS-titration method, the presented MS-titration method in this paper is more simple and applicable, does not demand much for the devices, and can lead to reliable results in same cases.
Berberine ; metabolism ; Ligands ; Orosomucoid ; metabolism ; Protein Binding ; Protein Interaction Mapping ; methods ; Proteins ; metabolism ; Spectrometry, Mass, Electrospray Ionization

The present study was designed to construct the structurally diverse library of tetrahydroprotoberberines (THPBs) by combining the methods of chemical nonselective demethylation and microbial glycosylation. HPLC-MS/MS analyses tentatively identified 12 de-methylated and 9 glycosylated derivates of THPBs and 5 rarely oxidized glycosides of THPBs in the library. Through this effort, we achieved not only a variety of the THPBs and their glycosides but also tested the catalytic characteristics and capabilities of G. deliquescens NRRL 1086.
Berberine Alkaloids ; chemical synthesis ; chemistry ; metabolism ; Biotransformation ; Catalysis ; Gliocladium ; metabolism ; Glycosides ; chemical synthesis ; chemistry ; metabolism ; Glycosylation ; Molecular Structure

OBJECTIVEUsing in vitro everted gut seas to research the intestinal absorption of the extractive Rhizoma Coptidis at the different intestinal section and the different density.

METHODBerberine (BER) and palmatine (PAL) which are representative compositions of the extractive Rhizoma Coptidis in everted gut seas are detected by HPLC, and calculated the absorption parameter to describe the character of absorption.

RESULTThe absorption of BER and PAL is linearity in different intestine and different dose, and the square of coefficient correlation exceed 0.9, which consistent with zero order rate process. The K(a) of BER and PAL increases along with the raised dosage of the extractive Rhizoma Coptidis (P < 0.05), indicated it is the passive absorption. The absorption of BER and PAL in the jejunum is the most quick, the ileum and colon are slower.

CONCLUSIONIn the different dosage of extractive Rhizoma Coptidis, the absorption of BER and PAL Conforms to the zero order rate process at the different intestine, and is the passive absorption.

Animals ; Berberine ; pharmacokinetics ; Berberine Alkaloids ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Cicatrix ; metabolism ; Colon ; metabolism ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Gastrointestinal Tract ; metabolism ; Ileum ; metabolism ; Jejunum ; metabolism ; Male ; Rats ; Rats, Wistar

OBJECTIVETo study the metabolism of berberine and palmatine in prescription compatibility of Wuji Wan in human intestinal flora.

METHODThe L9 (3(4)) orthogonal design was adopted to compare prescription compatibility of nine groups of Wuji Wan composed of Coptis chinensis, Evodiae and fried Radix paeoniae alba into and single ingredient of C. chinensis. They were cultivated with fresh human excrements under anaerobic conditions for 24 h. A HPLC-UV method was adopted for determining berberine and palmatine in bacteria culture medium, in order to compare the metabolism of the two components in different prescription compatibility.

RESULTMetabolism of berberine was positively correlated with doses, whereas metabolism of palmatine was negatively correlated with doses in extracts from C. chinensis. Compound compatibility speeded up the metabolism of berberine in low dose, which was positively related to the doses of Evodiae and fried Paeoniae Alba Radix; meanwhile Compound compatibility slowed down the metabolism of berberine in high dose, which was negatively related to the dose of Evodiae. Compound compatibility speeded up the metabolism of palmatine in high dose, which was negatively related to the doses of Evodiae and fried Paeoniae Alba Radix.

CONCLUSIONThe metabolism of the compatibility of Wuji Wan speeds up, when Coptis chinensis components metabolite rapidly in intestinal flora; while the metabolism of the compatibility of Wuji Wan slows down, when C. chinensis components metabolite slowly in intestinal flora. Therefore, they show a balanced effect. Additionally, different proportion of C. chinensis, Evodiae and fried Paeoniae Alba Radix cause difference in metabolism speed of berberine and palmatine to some extent.

Anaerobiosis ; Bacteria ; metabolism ; Berberine ; metabolism ; pharmacokinetics ; Berberine Alkaloids ; metabolism ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Coptis ; chemistry ; Drugs, Chinese Herbal ; metabolism ; pharmacokinetics ; Evodia ; chemistry ; Feces ; microbiology ; Intestinal Absorption ; Intestines ; metabolism ; microbiology ; Paeonia ; chemistry ; Time Factors

The correlations between soil nutrition and yield as well as active compound contents of Coptis teeta were analyzed. The contents of 13 soil factors, rhizome biomass and the content of berberine, jatrorrhizine, and palmatine in rhizome of C. teeta were determined, and analyzed by factor analysis (FA) and correlation analysis (CA). FA showed that the first three factors accounted for 86.9% of the total variance. The contents of Ca, Mg, Fe, Mn, and Zn correlated with the first factor. The content of organic matter, N, available N, available P, and available K correlated with the second factor. CA showed that yield of C. teeta had a significant positive correlation with available P (r = 0.931) at 0.01 level, and available N (r = 0.703) at 0.05 level. The content of berberine of C. teeta had a significant positive correlation with available P (r = 0.680) at 0.05 level. The yield and berberine content of C. teeta were high in the soil with high contents of available N and available P.
Berberine ; analysis ; metabolism ; China ; Coptis ; chemistry ; metabolism ; Drugs, Chinese Herbal ; analysis ; metabolism ; Nitrogen ; analysis ; metabolism ; Phosphates ; analysis ; metabolism ; Potassium ; analysis ; metabolism ; Rhizome ; chemistry ; metabolism ; Soil ; chemistry

OBJECTIVETo study the absorption kinetics of dehydrocavidine in rats' stomachs and intestines.

METHODThe absorption kinetics was investigated by the in situ perfusion in rats and the concentrations of drug perfusion solutions were determined by HPLC.

RESULTThe hourly absorption percentages of dehydrocavidine in stomach, small intestine were 8.88%, 2.08%, respectively. Although the absorption rate constants of dehydrocavidine in duodenum and jejunum are more than that in ileum and colon, there is no significance difference between them. The absorption rate constants kept at the same level when the concentrations of drug perfusion solution are at middle and high level. The increase of the pH of perfusion solution didnt significantly affect the absorption rate constants of the drug.

CONCLUSIONDehydrocavidine was absorbed poorly at stomach and all segments of intestine in rats, but the absorptions in stomach are better than intestine. Dehydrocavidine was absorbed mainly via passive transport mechanism between middle and high concentration levels.

Animals ; Berberine Alkaloids ; pharmacokinetics ; Colon ; metabolism ; Duodenum ; metabolism ; Hydrogen-Ion Concentration ; Ileum ; metabolism ; Intestines ; metabolism ; Jejunum ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley ; Stomach ; metabolism

OBJECTIVETo 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.

RESULTSRP-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).

CONCLUSIONSHJDFE30, 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.

Animals ; Berberine ; Berberine Alkaloids ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Flavanones ; Flavonoids ; Glucose ; metabolism ; Iridoids ; Models, Animal ; Neurons ; Oxygen ; metabolism ; Rats ; Reperfusion Injury ; drug therapy