Study on metabolism of Pulsatilla saponin in normal and ulcerative colitis model rats by UPLC-Q-TOF-MSE technology / 药学学报

In this study, ultra performance liquid chromatography-quadrupole-time of flight mass spectrometer-MSE (UPLC-Q-TOF-MSE) combined with UNIFI analysis platform was used to rapidly analyze and identify the metabolites of hederagenins 3-O-α-L-rhamnosyl-(1→2)-[β-D-glucopyranosyl-(1→4)]-α-L-arabopyranoside (Pulsatilla saponin D) and oleanolic acid 3-O-α-L-rhamnosyl-(1→2)-[β-D-glucopyranosyl-(1→4)]-α-L-arabopyranoside (Pulsatilla saponin B7) and hederagenins 3-O-α-L-rhamnosyl-(1→2)-α-L-arabopyranoside (Pulsatilla saponin BD) in plasma and colonic tissue of normal and ulcerative colitis (UC) rats. The database and analysis methods were established based on the precise molecular weight of compounds, retention time, neutral loss and reported data, and then the final data were obtained by comparing with the blank control group, combining with the deviation and the cracking rule of the compound. The results showed that the glucoses, hydroxylation and dehydroxylation, methylation and demethylation, dehydrogenation, decarboxylation and hydrolysis of saponin D, B7 and BD occurred in the plasma and colon tissues of normal and UC model rats. This study will clarify the metabolic transformation of Pulsatilla saponins D, B7 and BD in rats, determine the prototype components and their metabolites that enter the body, and whether colon injury will affect their metabolism in vivo, so as to explore the possible anti-colitis effective components in the prototype or metabolites of Pulsatilla saponins D, B7 and BD. This experiment was approved by Animal Ethics Committee of Jiangxi Science and Technology Normal University (approval number: Y202227).

Warming acupuncture combined with "three steps and seven methods" of tuina for chronic nonspecific low back pain of yang deficiency and cold-dampness blockage: a randomized controlled trial / 中国针灸

OBJECTIVE@#To compare the clinical efficacy and possible mechanism of warming acupuncture combined with "three steps and seven methods" of tuina and simple "three steps and seven methods" of tuina in treatment of chronic nonspecific low back pain (NLBP) of yang deficiency and cold-dampness blockage.@*METHODS@#A total of 138 patients were randomized into an observation group (69 cases, 5 cases dropped off) and a control group (69 cases, 7 cases dropped off). In the control group, "three steps and seven methods" of tuina was applied. On the basis of the treatment in the control group, warming acupuncture was applied at Shenshu (BL 23), Yaoyangguan (GV 3), Mingmen (GV 4), Weizhong (BL 40) and ashi points. The treatment was given once a day, 6 times a week for 3 weeks in both groups. Before and after treatment, the short form of McGill pain questionnaire (SF-MPQ) score, Oswestry disability index (ODI) score, finger-to-floor distance (FFD), Schober test distance, fear-avoidance beliefs questionnaire (FABQ) score and yang deficiency and cold-dampness blockage score were observed, the serum levels of tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6 and thromboxane B2 (TXB2) were detected in both groups. The recurrence rate was evaluated in follow-up of 6 months after treatment.@*RESULTS@#After treatment, the scores of PRI, PPI, VAS, ODI, FABQ and FFD, yang deficiency and cold-dampness blockage scores were decreased compared before treatment in both groups (P<0.01), and those in the observation group were lower than the control group (P<0.01); the Schober test distances were increased compared before treatment in both groups (P<0.01), and that in the observation group was larger than the control group (P<0.01). After treatment, the serum levels of TNF-α, IL-1β, IL-6 and TXB2 were decreased compared before treatment in both groups (P<0.01), and those in the observation group were lower than the control group (P<0.01). In follow-up, the recurrence rate was 12.8% (6/47) in the observation group, which was lower than 34.3% (12/35) in the control group (P<0.05).@*CONCLUSION@#Warming acupuncture combined with "three steps and seven methods" of tuina can effectively alleviate pain in patients with chronic NLBP of yang deficiency and cold-dampness blockage, improve activity and dysfunction of waist, the clinical efficacy is superior to simple "three steps and seven methods" of tuina, its mechanism may be relate to the inhibition of inflammatory reaction.

Predictive significance of exhaled breath temperature for airway inflammation changes in children with asthma / 中国当代儿科杂志

OBJECTIVE@#To explore the predictive significance of exhaled breath temperature (EBT) for airway inflammation changes in children with asthma.@*METHODS@#A total of 60 children with asthma who met the inclusion criteria at the first visit were chosen as the asthma group, and 60 healthy children were selected as the control group. The EBT level was measured by the latest third-generation product (X-halo). The Childhood Asthma Control Test (C-ACT) score was recorded. EBT level and C-ACT score were compared between the asthma and control groups. At the subsequent visit one month later, the children were divided into well-controlled, partially-controlled, and uncontrolled groups according to their C-ACT scores. The EBT level and the FeNO level of the three groups were measured. EBT level and C-ACT score were compared among the three groups. The correlation between EBT and FeNO was analyzed. The data of initial diagnosis were reviewed, the EBT level and C-ACT score at the first visit were compared among the three groups, and the differences in EBT level and C-ACT score among the three groups at the second and first visits were evaluated.@*RESULTS@#At the first visit, the asthma group had a significantly higher EBT and a significantly lower C-ACT score compared with the control group (P partially-controlled group > well-controlled group (P partially-controlled group > uncontrolled group (P<0.05). There were no significant differences in EBT level and C-ACT score at the first visit between the three groups. From the first visit to the subsequent visit, EBT level was significantly decreased in the well-controlled group (P<0.05), but significantly increased in both partially-controlled group uncontrolled groups (P<0.05); C-ACT score was significantly increased in the well-controlled and partially-controlled groups (P<0.05), but significantly decreased in the uncontrolled group (P<0.05). EBT and FeNO levels at the subsequent visit were positively correlated with each other in the uncontrolled group (P<0.05).@*CONCLUSIONS@#EBT has predictive significance for the changes in airway inflammation in children with asthma.

Intestinal absorption of pulchinenosides from Pulsatilla chinensis in rats / 中国中药杂志

HPLC-ELSD was applied to explore the absorption mechanism of pulchinenosides (B3, BD, B7, B10, B11) in rats. The experimental results showed that the absorption rate constant, Ka value (B3, BD) and Permeability coefficient, Peff value (B3, B7) displayed significant difference (P <0.05) in various intestinal segments, The Ka value and Peff value of PRS was different from each other with the highest absorption in duodenum (duodenum > jejunum > colon > ileum); The PRS displayed excessive satuation as the concentration increased over 0.05-2.5 g · L(-1). There were no obvious linear correlations between Peff values and concentrations in duodenum (0.6007 ≤ R2 ≤ 0.7727); Ka and Peff value declined when the PRS was perfused with P-glycoprotein promoter digoxin, on the other hand, inclined when perfused with P-glycoprotein inhibitor verapamil with significant difference among PRS B3, BD, B7, B11 (P <0.05). All the above results demonstrated that B3, BD, B7 were greatly influenced by absorption sites, duodenum was the main absorption site; PRS didn't entirely transported in a concentration dependent manner, and the transporter-protein involved the transportation, so the intestinal absorption of the five pulchinenosides was not entirely passive diffusion; and PRS might be the substrates of P-glycoprotein.

Study on solubilization effect of solid dispersion technology and inclusion technology on pulsatillae total saponins / 中国中药杂志

<p><b>OBJECTIVE</b>To study the effect of solid dispersion technology and inclusion technology on dissolution performance of Pulsatillae total saponins, and preliminarily investigate its mechanism.</p><p><b>METHOD</b>The solid dispersion of Pulsatillae total saponins-PEG 4000 was prepared by the melting method. The inclusion compound of Pulsatillae total saponins-hydroxypropyl-beta-cyclodextrin ( HP-beta-CD) was prepared by the freeze-drying method. The properties of solid dispersion and inclusion compound were identified by using IR, DSC and NMR. And the dissolution of solid dispersion and inclusion compound were also determined by the small glass method.</p><p><b>RESULT</b>IR, DSC and NMR results showed the formation of solid dispersion and inclusion compound. In terms of the dissolution, the inclusion compound ranked first, which was followed by solid dispersion and bulk pharmaceutical chemicals.</p><p><b>CONCLUSION</b>The inclusion technology could significantly increase the dissolution of Pulsatillae total saponins, whereas the solid dispersion showed no notable solubilization effect.</p>

Preparation of colon target pellets of Pulsatilla total saponins-hydroxypropyl-beta-cyclodextrin inclusion / 中国中药杂志

<p><b>OBJECTIVE</b>To prepare colon target pellets of Pulsatilla total saponins.</p><p><b>METHOD</b>Pulsatilla total saponins-hydroxypropyl-beta-cyclodextrin inclusion was prepared by the water solution-mixing method. Then plain pills of inclusion were prepared by the granulation-spheronization method, and coated by Glatt fluid bed.</p><p><b>RESULT</b>The dissolution of plain pills of Pulsatilla total saponins at 2 h was 16.0%, while that of plain pills of inclusion at 0.5 h was 91.9%. With Eudragit S100 as the coating material, TEC as the plasticizer and talcum power as the anti-adherent, when the coating weight was 12%, the coating efficiency was high, with almost no bonding and drug release of coated pellets in artificial gastric juice for 2 h. The accumulated drug release in artificial intestinal fluid for 4 h was less than 15%, and that in artificial colon fluid for 4 h was more than 90%.</p><p><b>CONCLUSION</b>Coated pellets of Pulsatilla total saponins-hydroxypropyl-beta-cyclodextrin inclusion showed a good colon targeted drug release in vitro, thus could be further developed to be oral colon targeted preparations.</p>

Broncho-alveolar lavage in the severe toxic pulmonary edema caused by irritative gas / 中国基层医药

Objective To discuss the feasibility and curative effect of broncho-alveolar lavage(BAL)through bronchofiberscope in the treatment of severe toxic pulmonary edema caused by irritative gas.Methods 16 cases se- vere toxic pulmonary edema caused by irritative gas were performed BAL through bronchofiberseope.The index of oxygen in arterial blood,clinical and radiological changes before,during and 2 hours after BAL were observed.Results 2 hours after BAL through bronchofiberscope,the partial pressure of oxygen in arterial blood(PaO2)obviously in- creased,the partial pressure of carbon dioxide in arterial blood(PaCO_2)did not change much.PaO_2 and PaCO_2 had no obvious change before and during BAL.The shadow area in the X-ray film of chest obviously decreased 24 hours af- ter BAL.In all 16 cases,13 cases were cured,1 case got improvement,and 2 cases died.The curative rate was 81%. Conclusion BAL through bronchofiberscope could clear the noxious substance in airway and improve the ventilation function.It was safe and had confirmed curative effect.

Establishment of a reporter gene-based cell screening model for discovering new agonists of estrogen receptor beta subtype / 药学学报

<p><b>AIM</b>To establish a sensitive and efficient reporter gene-based screening model for finding agonists of estrogen receptor beta subtype.</p><p><b>METHODS</b>A recombinant vector pTAL-ERE-SEAP was constructed by inserting a synthetic sequence composed of five estrogen responsive elements in front of promoter of pTAL-SEAP vector. pTAL-ERE-SEAP was then transfected into human embryonic kidney (HEK293) cells. G418 (200 microg x mL(-1)) was added to select positive clones that can be induced by E2 to express reporter gene SEAP. The speciality was tested by several ligands of relative nuclear receptors of the same family. The stability of the model, the time-effect relationship, the dose-response relationship, and the immunocytochemistry staining of ERbeta expression after transfection were observed. 2 622 compounds were screened by using this model.</p><p><b>RESULTS</b>Stably transfected clones were obtained. The expression levels of reporter gene SEAP of positive clones was induced by E2 in a dose-response and time-effect relationship manners. The Z' factor value was 0.7. The expression levels of dexamethasone and other ligands were low. The result of immunocytochemistry staining showed the expression of ERbeta. E2 had no proliferating effects on stably transfected clones.</p><p><b>CONCLUSION</b>Stably transfected positive clones transfected with recombinant vector pTAL-ERE-SEAP were obtained. The positive clones may be used to screen for agonists of estrogen receptor beta subtype by measurement of luminescent value of expressed SEAP in wells of microlitre plate.</p>

Study of the curative effect of modified tracheal in acute respiratory failure caused by central airway stenosis / 中华全科医师杂志

Objective To investigate the curative effect of modified tracheal catheter in acute respiratory failure caused by central airway stenosis.Methods 16 cases inpatient with acute respiratory failure caused by central airway stenosis were involved.Found out the position and range of stenosis of central airway by X-ray and CT of chest and fiberbronchoscope,chose the suitable silicon suction tube and cut it to make a tracheal catheter,then guided the catheter through the stenosis by fiberbronchoscope to construct artificial airway.Results The dyspnea of all 16 cases of acute respiratory failure caused by central airway stenosis could by relieved in short time,the PaO_2 raised from(39?12)mm Hg to(72?10)mm Hg,SaO_2 raised from(75?13)% to(93?3)%,PaCO_2 dropped from(102?21)mm Hg to(62?13)mm Hg after therapy.The effective rate is 100%.There was no other serious complication except for 2 cases of little amount of bleeding in trachea.15 cases survived and one died of serious muhisystem organ failure.Conclusions The use of modified tracheal catheter in treatment of acute respiratory failure caused by central airway stenosis can relieve the acute dyspnea in short time,it also can dilate central airway,save the cost of tracheal balloon dilatation for the follow-up therapy.