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ABSTRACT: To observe the effect of Euphorbia kansui (E. KS) alcohol extracts on urination and kidney-related expressions of mice injected with normal saline and to discuss its impact on kidney.
Mice intraperitoneally injected with normal saline were observed for urination and changes in kidney-related histiocytic factors of after intragastrical administration of E. KS and compared with normal mice.
E. KS alcohol extracts can promote urination of mice injected with normal saline and enhance peripheral serum creatinine, with no obvious pathological change showed in tissue sections. It had a certain effect on reducing AQP2 expression and enhancing TNF-alpha expression.
Euphorbia kansui in large dose has a remarkable effect on kidney but may be accompanied with pathological reactions to some extent, especially the dose of 1.2 g x kg(-1). The pathological reactions may be related with increased serum creatinine and TNF-alpha expression.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 03/2012; 37(5):606-10.
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ABSTRACT: Berberine is a candidate clinical neuroprotective agent against ischemic stroke. In the present study, we examined the influence of the PI3K/Akt pathway in mediating the anti-apoptotic effects of berberine. Oxygen-glucose deprivation and reoxygenation of nerve growth factor-differentiated PC12 cells and primary neurons, and bilateral common carotid artery occlusion in mice were used as in vitro and in vivo ischemia models. We found that the anti-apoptotic effects of berberine against ischemia were indeed mediated by the increased phosphor-activation of Akt (higher p-Akt to total Akt), leading to the intensified phosphorylation of Bad and the decreased cleavage of the pro-apoptotic protease caspase-3. Berberine action is specific for PI3K, rather than the upstream receptor tyrosine kinase. The anti-apoptotic effect is maintained in the presence of tyrosine kinase inhibitor genistein and the epidermal growth factor receptor inhibitor PD153035, but is suppressed by the PI3K inhibitor Ly294002 and the Akt inhibitor Akti-1/2.The unique PI3K regulatory subunit p55γ was upregulated by berberine during ischemia-reperfusion and was not blocked by these inhibitors. We constructed a reporter plasmid to detect PI3K p55γ promoter activity and found that berberine enhanced PI3K p55γ promoter activity during cerebral ischemia-reperfusion.
European journal of pharmacology 11/2011; 674(2-3):132-42. · 2.59 Impact Factor
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ABSTRACT: Berberine (BBR) is an established natural DNA intercalator with numerous pharmacological functions. However, currently there are neither detailed reports concerning the distribution of this alkaloid in living cells nor reports concerning the relationship between BBR's association with DNA and the function of DNA. Here we report that the distribution of BBR within the nucleus can be observed 30 minutes after drug administration, and that the content of berberine in the nucleus peaks at around 4 µmol, which is twelve hours after drug administration. The spatial conformation of DNA and chromatin was altered immediately after their association with BBR. Moreover, this association can effectively suppress the transcription of DNA in living cell systems and cell-free systems. Electrophoretic mobility shift assays (EMSA) demonstrated further that BBR can inhibit the association between the TATA binding protein (TBP) and the TATA box in the promoter, and this finding was also attained in living cells by chromatin immunoprecipitation (ChIP). Based on results from this study, we hypothesize that berberine can suppress the transcription of DNA in living cell systems, especially suppressing the association between TBP and the TATA box by binding with DNA and, thus, inhibiting TATA box-dependent gene expression in a non-specific way. This novel study has significantly expanded the sphere of knowledge concerning berberine's pharmacological effects, beginning at its paramount initial interaction with the TATA box.
PLoS ONE 01/2011; 6(8):e23495. · 4.09 Impact Factor
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ABSTRACT: To investigate brazilein's role in energy metabolism of cerebral ischemia-reperfusion in mice.
Fourty mice were randomly divided into the sham group, ischemia group, brazilein 5 mg x kg(-1) group and brazilein 10 mg x kg(-1) group, each with ten cases. Cerebral ischemia model was the built. Mice were injected with brazilein three days before the operation, then they were killed. Cerebrum homogenate was prepared for the detecting of ATP, ADP, AMP and lactic acid by HPLC, expressions of MCT1 and MCT2 in mRNA level by RT-PCR.
The lactic acid in cerebrum increased sharply 20 minutes after cerebral ischemia and decreased 1 hour after reperfusion, then returned to the normal level 24 hours after reperfusion. The charge of energy decreased significantly at the beginning of the ischemia-reperfusion, and the charge restored 1 hour after reperfusion though it was still much lower than the normal level at the time point of 24 hours. Moreover, MCT1 and MCT2 upregulated accompanied with the increase of lactate, MCT2 mRNA enhanced in brazilein 5 mg x kg(-1) group (P < 0.05) while both the two factors increased in brazilein 10 mg x kg(-1) group (P < 0.01).
Brazilein might protect neurons by changing the charge of energy.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 09/2010; 35(18):2444-8.
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ABSTRACT: The aim of this study was to investigate the LD(50) (median lethal dosage) of berberine (BBR) through three different routes of injection in mice: intravenous (i.v.) injection, intraperitoneal (i.p.) injection, and intragastric (i.g.) oral administration. The concentration of BBR in blood from their i.g. doses (10.4, 20.8, 41.6, and 83.2 g/kg) and the content relationship of BBR among different injections were analyzed by high-performance liquid chromatography (HPLC). The LD(50) of BBR from i.v. and i.p. injections is 9.0386 and 57.6103 mg/kg, respectively; but no LD(50) was found in the i.g. group. A significant difference in bioavailability was observed between the different routes. Furthermore, the concentration of BBR in the blood from different i.g. doses was also significantly different. However, we discovered an interesting phenomenon indicating that the absorption of BBR by oral administration has a limit, therefore, explaining the difficulty in obtaining an LD(50) of BBR for i.g. injection. From the analysis of BBR content in blood after various administrations, we hypothesized that not only does the concentration of BBR in blood contribute to its acute toxicity, but also the routes of administration may be an important facet that affects this toxicity evaluation.
Food and chemical toxicology: an international journal published for the British Industrial Biological Research Association 02/2010; 48(4):1105-10. · 2.99 Impact Factor
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ABSTRACT: To screen the active component of Wuzhuyutang (WZYT, Evodiae prescription) and investigate the regulatory effects of the components in WZYT on the TPH2 promoter, and to explore the possible molecular mechanism of WZYT on migraine.
By transfecting a TPH2 promoter regulating Red Fluorescent Protein expressing plasmid into PC12 cell, the global fluorescence intensities and calculations of fluorescent cells after components treatment were statistically evaluated.
Different regulatory effects of different components in WZYT with different concentrations on TPH2 promoter were observed.
TPH2 promoter drove Red Fluorescent Protein expressing cell line can be used as system screening components targeting TPH2 promoter activity. The possible mechanism of WZYT on migraine may due to its stimulating effects on TPH2 promoter, and promote the synthesis and release of 5-HT in cerebral.
Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica 09/2009; 34(17):2261-4.
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ABSTRACT: Quantification of brazilein in rat plasma following intravenous administration was achieved by reversed-phase high-performance liquid chromatography using a mobile phase of acetonitrile-0.05 m potassium dihydrogen phosphate water (containing 0.5% triethylamine, pH 3.0; 20:80 v/v) and UV detection at 445 nm. The method was linear (determination coefficient, r(2) = 0.9992) within the tested range (0.313-5.0 microg/mL). Intra- and inter-day precision coefficients of variation and accuracy bias were acceptable (maximal CV value was 2.06% for intra-day and 1.71% for inter-day) over the entire range. The recoveries were 81.48, 84.61 and 82.83% for concentrations of 0.313, 1.25 and 5.0 microg/mL, respectively. The concentration-time curve of brazilein after intravenous administration was fitted to the two-compartment model. This is the first time that brazilein in rat plasma was detected by HPLC-UV method and its pharmacokinetic characteristic was comprehensively studied.
Biomedical Chromatography 11/2008; 22(11):1201-5. · 1.97 Impact Factor
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ABSTRACT: The aim of this study was to investigate the transport behavior and efflux of berberine through the primary culture cortical neurons. High-performance liquid chromatography coupled with an UV-vis detector at 347 nm was applied. The mobile phase was 0.05 m potassium dihydrogen phosphate solution (containing 0.5% triethylamine, pH 3.0)-acetonitrile (73:27, v/v). Neurons were incubated with Coptidis rhizoma extract 6.5 microg/mL (containing 1.91 microg/mL berberine) and verapamil, KCN or cimetidine for 2 h, and then lysed in methanol to extract intracellular berberine. A 20 microL aliquot of sample was injected into the HPLC system to determine berberine concentration. The results showed that metabolic inhibitor KCN and P-glycoprotein inhibitor verapamil could increase berberine concentration within the neurons, indicating that efflux of berberine was energy-dependent and P-glycoprotein was likely to be involved. Moreover, the organic cation transporter inhibitor cimetidine could decrease berberine concentration within the neurons, suggesting that the organic cation transporter might be involved in the berberine transport process.
Biomedical Chromatography 02/2008; 22(1):28-33. · 1.97 Impact Factor
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ABSTRACT: Antioxidant activities of the 95% ethanol extract from Caesalpinia sappan heartwood (ECS), protosappanin A, protosappanin B, and brazilein were studied in vitro. The inhibition of the formation of malondialdehyde (MDA) and the scavenging of superoxide anions, hydrogen peroxide, and hydroxyl radicals were assayed. The experimental results show that all four substances had antioxidant activity in vitro but their capabilities differed for the different indicators. ECS, protosappanin A, and protosappanin B show more inhibition of MDA and scavenging of hydrogen peroxide, while brazilein shows more scavenging of hydroxyl radicals. All the samples show little scavenging of superoxide anions.
Tsinghua Science & Technology.
