Study on improvement mechanism of caudatin on liver injury in rats / 中国药房

OBJECTIVE To investigate the improvement mechanism of caudatin on liver injury of rats. METHODS SD rats were randomly divided into blank group， model group， caudatin low-dose and high-dose groups （25， 50 mg/kg）， with 6 rats in each group. Diethylnitrosamine （DEN） was injected intraperitoneally three times per week for eight weeks to establish liver injury model of rats. At 5th week of modeling， the rats received relevant medicine or 0.5% sodium carboxymethylcellulose intragastrically for 4 weeks. The levels of liver function indexes [alanine transaminase （ALT）， aspartate transaminase （AST）， total protein （TP） and total bilirubin （TBI）] and inflammatory factors [interleukin （IL-6）， tumor necrosis factor α （TNF-α）， IL-1β] in serum were detected； the histopathological morphological changes of rat liver were observed； the positive protein expressions of nuclear factor κB （NF-κB） and 78 kDa glucose regulatory protein （Grp78） in liver tissue were also determined； the expressions of endoplasmic reticulum stress-related protein Grp78， C/EBP homologous protein （CHOP）， activating transcription factor 6 （ATF6） and inositol requiring enzyme 1α （IRE1α） and the level of protein kinase R-like endoplasmic reticulum kinase robertluoyi@126.com （PERK） in liver tissue were detected. RESULTS Compared with blank group， serum levels of ALT， AST， TBI， IL-6， TNF-α and IL-1β and positive expressions of NF-κB and Grp78 in liver tissue as well as protein expressions of Grp78， CHOP， ATF6 and IRE1α， PERK protein phosphorylation level were all increased significantly in model group （P＜0.05）， while the serum level of TP was decreased significantly （P＜0.05）. The disordered structure of liver lobule， swollen liver cells， unclear intercellular boundary were observed and accompanied by inflammatory cell infiltration. Compared with model group， most of the above indexes were significantly reversed in caudatin groups （P＜0.05）； the structure of hepatic lobule was relatively complete and clear， the cells were arranged orderly， and the infiltration of inflammatory cells was also reduced. CONCLUSIONS Caudatin has a significant improvement effect against DEN-induced liver injury in rats， the mechanism of which may be associated with inhibiting endoplasmic reticulum stress and inflammatory reaction.

Impact of saikosaponin on absorption and transport of paeoniflorin in Caco-2 cell model / 中国中药杂志

<p><b>OBJECTIVE</b>To study the impact of saikosaponin on absorption and transport of paeoniflorin in Caco-2 cell model.</p><p><b>METHOD</b>The concentration of paeoniflorin in cell culture medium was measured by UPLC and the apparent permeability coefficients (P(app)) was calculated to study differences in bi-direction transport of paeoniflorin solutions of different concentrations and its compatibility with saikosaponin a, and saikosaponin d in Caco-2 cell model. Meanwhile, the electric resistance of Caco-2 cell was determined before and after the experiment.</p><p><b>RESULT</b>The amount of paeoniflorin increased linearly with the transport of Caco-2 cell monolayer in 4 h, with a lower absorptive permeability, which was (0.98 +/- 0.10) x 10(-6), (0.92 +/- 0.09) x 10(-6), (0.89 +/- 0.04) x 10(-6) cm x s(-1) at the concentration of 20, 50, 100 micromol x L(-1), respectively. After compatibility with saikosaponin a and saikosaponin d, the absorptive permeability of paeoniflorin increased by 2.37 times and 2.54 times, respectively, while the electric resistance of Caco-2 cell was decreased significantly after the experiment.</p><p><b>CONCLUSION</b>Saikosaponin a, d can enhance the absorption of paeoniflorin in Caco-2 cell monolayer, which may be related to saikosaponin's ability to open up intercellular tight junctions among Caco-2 cells.</p>

Protective effect and mechanism of Ecliptae Herba on cigarette smoke extract-induced cytotoxicity of NHBE cells / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the protective effect and mechanism of Ecliptae Herba extract on cigarette smoke extract-induced cytotoxicity.</p><p><b>METHOD</b>The effect of Ecliptae Herba extract on CSE-induced NHBE cell proliferation was detected by MTT assay. GSH content was determined by DTNB colorimetry. GST activity was measured by CDNB colorimetric assay. NQO1 activity was detected by NADPH and DCIP. The protein expression was determined by Western blot assay.</p><p><b>RESULT</b>Ecliptae Herba extract reduced CSE's inhibitory effect on NHBE cells, recover the decrease in intracellular GSH caused by CSE and reduce the CSE-induced activity of GST and NQO1 and NQO1 protein expression.</p><p><b>CONCLUSION</b>Ecliptae Herba extract can reduce CSE-induced injury on NHBE cells, which may be related to phase II detoxification enzymes.</p>

Ideas and methods of fresh herb basic research based on constituent structure theory / 中国中药杂志

Application of fresh herbs is a kind of special forms of traditional Chinese medicine. In China, there is a long and rich experience in clinical application of fresh herbs. Many studies showed that the efficacy of fresh herbs was better than that of dried herbs, but the further study about the difference of their chemical composition, effective components and the overall material basis were few. In this paper, the ideas and methods to study on material basis of the fresh herbs by comparing the difference of the fresh and dry herbs in medicine chemical composition and pharmacological activity of effective components with modern advanced separation, analysis and screening technology under the "Constituent structure theory" were proposed. It was an effectual method for studying on the reasonable development of Chinese medicine and fresh herbs resources.

Intestinal absorption properties of flavones and extract of fructus aurantii immaturus in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the intestinal absorption of naringin, hesperidin, neohesperidin and the extract of Fructus Aurantii Immaturus in rats.</p><p><b>METHOD</b>The rat intestinal perfusion and enzymes incubation models were used, together with the determination of the n-octanol/water partition coefficient of the components (P).</p><p><b>RESULT</b>In perfusion model, the P(eff) of all components were low, and the P(eff) of naringin, hesperidin and neohesperidin were 0.140-0.252, 0.156-0.268 and 0.154-0.285, respectively. In four different regions of intestine of rat and with different concentration, the P(eff) of the components both had no significant difference, whereas the P(eff) of the extract were higher than the P(eff) of the single component. The metabolite of components was not detected in intestine. The P of naringin, hesperidin and neohesperidin were 0.36, 0.40 and 0.48, respectively, and the pH of buffer solution had no influence to its distribution coefficient.</p><p><b>CONCLUSION</b>Poor permeation contributed to the poor intestinal absorption of naringin, hesperidin and neohesperidin. The absorption of components in extract were increased, and the results suggest that the extract may enhance the intestinal absorption of the components.</p>

Study on preparation of CIT microemulsion and its absorption in intestine / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare CIT microemulsion and to investigate its properities and the absorption character in rat intestine in situ.</p><p><b>METHOD</b>The optimum formulation of the blank microemulsion was selected by pseudo tertiary phase diagrams and the CIT microemulsion was prepared based on the blank microemulsion. The appearance, particle diameter distribution and Zeta potential were investigated by electron microscopy and grainsize analyzer. The entrapment efficiency was determined by sephadex column chromatography. An in situ single pass intestine perfusion method was used to investigate the intestinal absorption of CIT microemulsion. HPLC method for determination of CIT in the intestinal flux was established.</p><p><b>RESULT</b>The formulation was OP-glycerol-water-ethylis oleas (3:3:4:2). CIT microemulsion in electron microscopy was consisted of small spherical drop. The mean diameter was 61.7 nm, Zeta potential was -46.3 mV. The Entrapment efficiency was (92.1 +/- 1.74)% (n=3). Both CIT and CIT microemulsion had been absorbed in general intestinal tract,and the absorption of CIT microemulsion was significantly high compared with CIT in duodenum, colon, jejunum and ileum (P < 0.01).</p><p><b>CONCLUSION</b>The preparation technology of CIT microemulsion was feasible,and the microemulsion system might improve the absorption of CIT in the intestinal tract.</p>

Absorption and metabolism of flavonoids in Herba Epimedii via rat intestinal perfusion model / 中国中药杂志

<p><b>OBJECTIVE</b>To study the absorption and metabolism of five flavonoids of Herba Epimedii (icariin, epimedin A, epi-medin B, epimedin C and baohuoside I) in rat intestine.</p><p><b>METHOD</b>Using the rat intestinal perfusion model, the contents of the five flavonoids in perfusates were measured by HPLC and the permeability coefficients in different intestines were calculated.</p><p><b>RESULT</b>The permeabilities of five flavonoids in duodenum, jejunum, ileum, colon according to the sequence were as: icariin: 6.365, 5.349, 1.004, 0.601, epimedinA: 4.120, 3.397, 0.401, 0.257, epimedin B: 3.645, 3.135, 0.990 7, 0.434, epimedin C: 3.114, 2.882, 0.688, 0.470, baohuoside I: 2.324, 2.398, 1.529, 1.045, respectively. The analysis of the perfusates showed that icariin, epimedin A, epimedin B, epimedin C could be hydrolyzed in intestine. Icariin had two hydrolytic metabolites, whereas epimedin A, B, C only had one hydrolytic metabolite, respectively.</p><p><b>CONCLUSION</b>The results indicated that the absorption of all the five flavonoids was significantly different in different intestinal segments, and the permeability in ileum and colon was significantly lower than that of the duodenum and jejunum. The metabolites of icariin, epimedin A, epimedin B, epimedin C were related with their structures and enzymes in intestine, and the metabolites were more in duodenum, jejunum, whereas were less in ileum and colon.</p>

Evaluation on fi ngerprint characteristic of Prunella Species with cluster analysis method / 中华中医药杂志

Objective:To establish the HPLC fingerprint of Prunella Species from different places and evaluate it by cluster analysis.Methods:The analysis method of HPLC ngerprint was established.Alltima C18(4.6mm?250mm,5?m) was utilized for separation.The mobile phase consisted of methanol(A) and 0.5% glacial acetic acid(B) with a ow-rate of 1.0ml/min.The detection wavelength was 280nm and the injection volume was 20?l.The column temperature was 30℃.The HPLC ngerprints of Prunella Species from three di erent places were determined and analyzed by SPSS.Results:There is a big di erence among ngerprints of Prunella from di erent places.Prunella from Hubei,Anhui,Jiangxi,Guizhou,Guangxi,Sichuan were divided into a class;Henan,Jiangsu,Zhejiang were divided into another class.Conclusion:the eatsblished ngerprint showed characteristics of Prunella Species from di erent places obviously,and the attribute of Prunella Species can be distinguished e ectively by cluster analysis method.

Pharmacodynamic Optimization of Purification Technique for Acanthopanax Senticosus Harms / 中国药房

OBJECTIVE: To optimize the purification technique for the extract of Acanthopanax senticosus Harms. METHODS: The techniques of D- 101 macroporous resin adsorption, polyamide adsorption and n- butanol extraction were separately applied to purify the aqueous extract of Acanthopanax senticosus Harms. Syringin was detected by HPLC and total flavone was detected by UV. The anti- cerebral ischemia effects of three purified samples were compared using rat MCAO model and mouse decapitation gape model. RESULTS: The three purified samples all showed anti- cerebral ischemia effects, with the sample purified via D- 101 macroporous resin adsorption having stronger effects than the other two. The content of Syringin was correlated with anti- cerebral ischemia effects. CONCLUSIONS: D- 101 macroporous resin adsorption is a be-tter technique for purifying the aqueous extract of Acanthopanax senticosus Harms.

Purification of Acanthopanax root extract with anticerebral ischemia / 中成药

AIM:To optimize the purification of Acanthopanax senticosus Harms root extract based on the rodent with anticerebral ischemia. METHODS:We identified the effect of D-101 macroporous resin adsorption,polyamide adsorption and n-butanol extraction on cerebral ischemia-reperfusion injure model rat and behead-mouth(opening) model mouse in the treatment of aqueous acanthopanax root extract. RESULTS:Aqueous acanthopanax root extract,which was purfied by using D-101 macroporous resin,had advantage over that were treated with polyamide adsorption and n-butanol extraction.Eleutheroside content in the root extract showed the positive correlation with anticerebral ischemia. CONCLUSION:D-101 macroporous resin adsorption is a good purification method for acanthopanax root extract.

Absorptive property of eleutheroside B in rat intestine / 中成药

AIM:To observe the absorption characteristics,absorption sites,and mechanism of eleutheroside B from Radix acathopanacis senticosi in various intestinal segments in rat and provide theoretical evidences for designing its preparation. METHODS: In situ perfusion method in rats.The absorption characteristics and absorption sites of eleutheroside B in intestine were applied. RESULTS: Absorbed dose and intestinal surface permeation rate of various intestinal segments decreased in turns in duodenum,jejunum,ileum,and colon;The concentration of eleutheroside B degraded through intestinal enzyme declined in turns in same manner. CONCLUSION: The poor bioavailability of eleutheroside B is not only due to absorption but also due to enzymolysis.