Network pharmacology and molecular docking strategies reveal the mechanism of Shengmai powder in the treatment of diabetes and its complications.Screened the active ingredients and targets in Shengmai powder through the TCMSP,BATMAN-TCM,SwissTarge-tPrediction,Pubchem databases and combined literature search.Uniprot database was used to uniformly standardize target names and find the genes corresponding to the targets.Searched for diabetes-related targets through OMIM,Genecards,and Drugbank databases.Venny 2.1 obtained the core targets of Shengmai powder and diabetes,and the core targets were imported into the STRING database for Protein-Protein interaction(PPI)analysis.The component-target network of Shengmai powder was established in Cytoscape 3.7.2.Then the David database was used for GO and KEGG enrichment analysis.Finally,AutoDock Toolsl.5.6 and AutoDock vinal.1.2 software were used to verify the results of molecular docking results.48 active ingredients and 352 predictive targets of Shengmai powder were screened,and 1 269 diabetes targets were selected.Venn diagram gets 97 common targets of Shengmai powder and diabetes.4 key targets and 3 potential pathways have been obtained.The core active ingredients of Shengmai powder in treating diabetes are stigmasterol,β-sitosterol,uridine,kaempferol,and the core targets are AKT1,TNF,CASP3,and PTGS2.The biological pathways of Shengmai powder in the treatment of diabetes mainly act on the TNF signaling pathway,HIF-1 signaling pathway,and apoptosis signaling pathway.The molecular docking results showed that the core components of Shengmai powder,stigmasterol,β-sitosterol,uridine and Kaempferol,etc.,have a strong binding activity to the main targets(AKT1,JUN,TNF and CASP3).Thus,this study systematically demonstrated Shengmai powder has played an important role in the molecular mechanism of Shengmai powder in the treatment of diabetes through multiple components,multiple targets and multiple path-ways,It could provide a thearetical basis and new direction for further exploring the treatment of diabetes with Shengmai powder.
以教学内容为载体,开展药剂学课程思政探索.深入挖掘药剂学课程蕴含的思政元素及两者间的融合点,建立有助于培养学生爱岗敬业、科学精神、科学思维、职业道德和工匠精神的思政案例库,使学生掌握药剂学基本知识和基本技能,引导学生形成良好的职业素养.
Heart failure (HF), with a high fatality rate, is seriously harmful to human health. Ginsenoside Rg5 (Rg5) is the major active component in black ginseng. The effect and mechanism of Rg5 on HF were investigated for the first time. Firstly, the in vitro angiotensin-converting enzyme (ACE) inhibitory activity was evaluated. Then, the verapamil-induced zebrafish HF model was used to assay the effect of Rg5. Finally, the untargeted metabolomics based on UPLC-QTOF-MS was applied to explore the latent mechanism by analyzing the metabolic perturbation. The results showed that Rg5 had a similar ACE-inhibitory activity (IC50 = 0.124 μM) to the reference drug enalapril. Rg5 could dramatically improve cardiac function in a dose-dependent manner. A total of 22 differentiated metabolites and 8 perturbed metabolic pathways were identified. In summary, this study indicated that Rg5 could be a potential agent for protecting heart function in the clinical treatment of heart failure.
采用星点设计法(Central composite design,CCD)优化灯盏乙素水解制备野黄芩素的反应条件.选取反应温度及介质固液比为主要考察因素,归一化法合并产品收率及反应时间为评价指标,采用Statistica 6.0及SAS软件进行试验设计并分析试验结果.反应温度及介质固液比对试验结果影响显著,并确定酸水解法制备野黄芩素的最优反应条件为固液比(g/L) 15(0.15g灯盏乙素加入10mL95%乙醇)、反应温度80℃,在此条件下可通过较短时间得到较为理想的产物收率.CCD优化野黄芩素制备工艺直观、高效,值得推广应用.
为全面了解中药大品种血栓心脉宁片(XXT)化学成分,采用超高效液相色谱-四极杆飞行时间串联质谱联用技术(UPLC-Q-TOF MS)测定该复方制剂的小分子成分(100~1500 u),通过UNIFI天然产物分析平台,比对各成分的精确分子质量、保留时间及质谱碎片离子信息,分析鉴定各化合物结构.结果表明,在XXT中共鉴定出187种化学成分,包括三萜皂苷类、菲醌类、蟾蜍甾二烯类和甾体类及其他结构类型的化合物.血栓心脉宁片富含小分子化学成分且结构类型多样,是其发挥抗血瘀活性及多靶点作用机制的物质基础.该研究可为阐明XX T的药效物质基础和提升质量控制标准提供数据参考.
以体外释放度作为评价指标,制备并筛选人参皂苷Rd结肠定位包衣片处方.采用高效液相色谱法测定释放度,分别考察崩解剂的种类及用量、壳聚糖用量(20%、30%、40%)、增塑剂种类(PEG6 000、TEC、DEP)、时滞层包衣增重(8%、10%、12%)及pH层包衣增重(8%、10%、12%)对包衣片体外释放度的影响.结果表明,以崩解剂(10%羧甲基纤维素钠∶羧甲基淀粉钠=1∶1)用量10%、壳聚糖用量30%、PEG6 000作为增塑剂、时滞层包衣增重及pH层包衣增重用量均为10%时可获得较为理想的包衣片,达到较好结肠定位效果.
Ginsenoside Rd,which has wide pharmacological effects,is one of the key active component of ginseng.Studies show that Ginsenoside Rd could improve cardiovascular system,protect nervous system,treat ulcerative colitis,inhibit angiogenesis and tumor cells,delay senilly and so on.This text summarized the analytic methods,pharmacokinetics and dosage form of Ginsenoside Rd by researching relative literature at home and abroad in recent years,which provides a theoretical reference for the clinical application,further development and utilization of Ginsenoside Rd.
通过查阅近年来国内、外相关文献,对野黄芩素的药物代谢动力学性质、药物剂型的研究情况进行综述.
This experiment was established for the simultaneous determination of five kinds of free anthraquinone methods of Qiming tablets.Chromatographic column is DiamonsiL C18 (4.6mm×250mm,5μm),acetonitrile-0.1% phosphoric acid solution as mobile phase,gradient elution (0min-20min,40 ∶ 60;20min-30min,60;40;30min-50min,90 ∶ 10),the detection wavelength of 284nm 1.0mL/min,flow rate,column temperature of 25℃.The linear ranges were in concentration of 0.001 36 mg/mL-0.00 680mg/mL for ehrysophanol,in concentration of 0.000 65mg/mL-0.003 25mg/mL for emodin,in concentration of 0.000 13mg/mL-0.000 65mg/mL for physcion,in concentration of 0.000 96mg/mL-0.004 80mg/mL for obtusifolin,in concentration of 0.000 54 mg/mL-0.002 70mg/mL for aurantio-ob-tusin,in precision and stability;repeat the test,RSD < 1%;the average recovery rate was 99.73%,99.53%,99.31%,99.69%,99.33%.the method is simple and feasible,of good reproducibility and high accuracy,which can be used as a method for simultaneous determination of five kinds of anthraquinone in the Qiming tablets.
To study the chemical constituents ofFilipendula intermedia (Glehn) Juzep.The constituents were separated and purified by column chromatography and their structures were identified on the basis of physico-chemical and spectral data.Eight compounds were isolated and identified as Kaempferol(compound 1),Kaempferol-3-O-α-L-rhamnoside (compound 2),Kaempferitrin(compound 3),Kaempferol-3-O-rutinoside (compound 4),Quercetin(compound 5),Isoquercitrin(eompound 6),β-sitosterol (compound 7),Daucosterol (compound 8).Compound 3 and 4 were isolated from this genus for the first time,Compound 1,2,5,6,7 and 8 were isolated from this plant for the first time.
The text summarized the chemical components and pharmacological effects of Rumex japonicus by researching relative literature at home and abroad in recent years .
In the present study, effects of floroquinone on anaplastic thyroid cancer cell lines and mouse tumor xenografts were investigated. Increase in the concentration of floroquinone from 10 to 100 µM reduced the cell growth from 98 to 17% after 48 hours in HOTHC cells. Similarly, in FRO cells growth rate was found to be 96 and 21%, respectively at 10 and 100 µM concentra-tions of floroquinone. Western blot analysis showed a marked reduction in Bcl-2 expression and increased in Bax, caspase-3 and cleaved PARP expre-ssion in HOTHC cell lines on treatment with floroquinone. Floroquinone treatment of the HOTHC cells led to inhibition of the cobalt chloride-induced increase in the hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor expression. In HOTHC cells, floroquinone treatment inhibited the tube formation and migration potential significantly compared to control cells. Treatment of the mouse bearing HOTHC tumor xenograft with 50 and 100 mg/kg doses of floroquinone alternatively for one month reduced the tumor volume to 48 and 17%, respectively compared to the control. Thus, floroquinone effectively inhibits growth of thyroid cancer and can be used for its treatment. Video Clip: Migration assay: 1 min 09 sec
用气相色谱-质谱法对樱桃番茄茎的挥发油进行化学成分分析.采用水蒸气蒸馏法从樱桃番茄茎中提取挥发油.用归一化法测定其百分含量,并用气相色谱-质谱法对化学成分进行鉴定.共鉴定了14个成分,占挥发油总量的60.59%.该结果为樱桃番茄茎的开发和利用提供了实验数据.
对人参皂苷Rd-羟丙基-β-环糊精包合物的制备和表征进行研究.采用溶剂-搅拌法制备包合物,然后用差示扫描量热法、红外光谱法以及显微镜法对得到的产物进行表征,3种表征方法均表明包合物已经形成.用高效液相色谱法测定包合物中人参皂苷Rd的含量为7.53%,包合物在25℃下的溶解度比人参皂苷Rd增大了24.3倍,在37℃下的溶解度增大了219倍.包合物水溶性良好,说明羟丙基-β-环糊精作为药物载体可以提高药物溶解度.
目的:探讨临床护理路径在糖尿病健康教育中的应用效果。方法选取2013年1月~2013年12月于本院治疗的糖尿病患者121例为研究对象,将其随机分为对照组(普通护理组)58例和观察组(常规护理组)63例,然后对2组患者血糖达标率、低血糖反应发生率、患者满意度、住院总费用、住院天数进行统计及比较。结果观察组血糖达标率:29例(46.03%)、低血糖反应发生率:8例(12.70%)、患者满意度100%,住院总费用(元):2657±215.36,住院天数(天):10.58±2.76;对照组血糖达标率:15例(25.86%)、低血糖反应发生率:16例(27.59%)、患者满意度84.5%,住院总费用(元):3246±365.67,住院天数(天):14.78±3.85。与对照组相比(均P<0.05)。结论临床护理路径在糖尿病健康教育中的应用效果良好。
Objective To optimize the formulation of sinomenine hydrochloride colon-targeted tablets by the central composite design-response surface method.Methods The coating weight gain of enteric coating layer(X1) and the proportion of EUDRAGIT S100 and L100(X2) were taken as the independent variables,and the synthesized estimated value(Y) was taken as the dependent variable,the synthesized estimated value(Y) was calculated by the cumulative release at 6,8,12 h of sinomenine hydrochloride.Statistica 6.0 software was used to fit multilinear model and quadratic multinomial model for experimental data,obtained optimum mathematical model by comparing the fitting results,delineated 3D surface plot and contour plot,selected optimum prescription and verified.Results The correlation coefficient of quadratic multinomial model(r = 0.994 7) was better than multilinear model(r = 0.168 5),so the quadratic multinomial model was the optimum mathematical model,optimum prescription was confirmed that coating weight gain of enteric coating layer was 4.5% and the proportion of S100 and L100 was 3:1,verified the optimum prescription and it was according with drug release requirement of colon-targeted tablets.Conclusions Central composite design-response surface method is simple and reliable,and the mathematical model has high predictability.So the method could be applied in the optimization of the formulation of sinomenine hydrochloride colon-targeted tablets.
Objective To study the effect of hemostasis and healing of basic fibroblast growth factor(bFGF) chitosan paint.Methods The 1.8 cm diameter round wounds were created in the back skin of 24 SD rats.The rats were randomly classified into four groups,one group were not administered as control group,the other three groups were treated with blank chitosan paint,bFGF solution and bFGF chitosan paint,respectively.The hemostasis time and amount of hemorrhage were recorded,the residual wound area was measured in the fifth day,tenth day and fifteenth day,scabs and decrustation healing time were recorded.Results The bleeding time and bleeding volume of blank chitosan paint and bFGF chitosan paint treated groups had significant differences(P 0.01) compared with that of control group.The wound healing rate of blank chitosan paint,bFGF solution and bFGF chitosan paint treated groups were significantly higher than that of the control group(P 0.01),but only the wound scab and decrustation healing time of bFGF chitosan paint group were significantly shortened(P 0.05) compared with that of control group.Conclusion The bFGF chitosan paint can promote hemostasis and wound healing.
Objective:To develop an effective HPLC method based on a reaction of phenylisothiocyanate(PITC) with glucosamine(GL) in alkaline media for the determination of glucosamine hydrochloride in dosage forms.Method:Reverse phase chromatography using pre-column derivatization with phenylisothiocyanate,and ultraviolet detection(254 nm) was used to quantify the eluate.The reaction produces a phenylthiocarbamyl-glucosamine(PTC-GL) adduct which was separated on a reverse-phase(RP) column packed with Agilent TC C18(4.6 mm×250 mm,5 μm).The mobile phase consisted of pH 5.8 phosphate buffered saline acetonitrile(90︰10) and was pumped at a flow rate of 0.8 mL·min-1,and the column temperature was maintained at 30 ℃.Galactosamine hydrochloride(Gal-HCl) was used as an internal standard.Result:The standard curves for GL-HCl showed linearity(r=0.999 1) over the selected concentration range from 350 to 550 mg·L-1 for dosage forms.The average recoveriy of glucosamine hydrochloride was 98.3%(RSD 2.3%).Conclusion:The method was found to be specific and with excellent linearity,accuracy and precision and is well suited for the quantitation of GL-HCl in dosage forms.
目的:建立盛添谷元片中淫羊藿苷的含量测定方法.方法:采用高效液相色谱法,样品处理后,由Agilent TC C18(250mm×4.6mm,5μm)色谱柱分离,流动相为乙腈-水(32∶68),检测波长为270nm,流速为1.0mL·min-1,柱温为30℃.结果:样品中杂质不干扰淫羊藿苷的分离测定,淫羊藿苷浓度在5~20mg·L-1范围内与峰面积有良好的线性关系(r=0.9999);平均加样回收率为100.2%,RSD=1.43%.结论:本方法简便、可行、重现性好,可用于盛添谷元片中淫羊藿苷有效成分的质量控制.
Objective:To establish an RP-HPLC method for determination of metoclopramide (MCL) concentration in dog plasma.Methods:Metoclopramide was extracted with ether under the alkaline condition.Hypersil-C_(18) (4.6 mm×200 mm,5 μm)column was employed and the mobile phase consisted of a mixture of methanol-acetonitrile -acetate buffer(pH 4.0)-triethylamine (7:18:75:0.1) with a flow rate of 1.0 mL·min~(-1).Tramadol hydrochlo- ride was used as an internal standard.Results:A linear calibration curve of MCL in plasma was obtained in the con- centration from 5.0 ng·mL~(-1)to 100.0 ng·mL~(-1)(r=0.9993).The minimal detectable drug plasma concentration was 1 ng·mL~(-1).Intra-day and inter-day RSD were 2.4%-6.8% and 3.6%-8.6%,respectively.The ex- tracted recoveries were 81.5%,84.6%,80.4%,and method recovery were 96.6%,98.5%,101.2% at low,mid- dle and high concentrations,respectively.Conclusion:A simple,sensitive and selective HPLC method for determi- nation of metoclopramide concentration in plasma was established.