Analysis of chemical components of Changtong oral liquid by UHPLC-Orbitrap HRMS / 中国药房

OBJECTIVE To identify the chemical components of Changtong oral liquid （CTOL），and to provide reference for the basic research and secondary development of its pharmacological substances. METHODS UHPLC-Orbitrap HRMS technique was adopted. CTOL sample was separated on a Hypersil Gold column with mobile phase consisted of 0.1% formic acid （containing 5 mmol/L ammonium formate）-acetonitrile （gradient elution）. The eluent was detected in positive and negative ion modes using an electrospray ionization source. The data was processed by Xcalibur 4.3 and Compound Discoverer 3.3 software. The primary and secondary mass spectra data of each compound were collected. The unknown compounds were identified according to the mass spectrometry library of the instrument and the network databases mzCloud，mzVault，etc. Through matching with the pharmacology database and analysis platform of the traditional Chinese medicine system，the chemical components could be attributed to the traditional Chinese medicine. RESULTS Fifty-three chemical components were identified and analyzed from CTOL，such as 24 flavonoids，8 quinones，5 phenylpropanoids，4 sugars and glycosides，5 organic acids，3 amino acids，1 alkaloid，1 phenolic and 2 other compounds. Among them，12 components were derived from Salvia miltiorrhiza，9 from Citrus aurantium，7 from Rheum palmatum，4 from Angelica sinensis，1 from Magnolia officinalis，16 from Glycyrrhiza uralensis，and 4 from many kinds of medicinal materials. CONCLUSIONS CTOL mainly contains flavonoids，quinones and phenylpropanoid compounds，and its chemical components mainly come from G. uralensis，S. miltiorrhiza and C. aurantium.

Investigation on the Mechanism of Salvia miltiorrhiza in the Treatment of Postoperative Abdominal Adhesion Based on Network Pharmacology and Molecular Docking / 中国药房

OBJECTIVE：To investigate the potential mechanism of Salvia miltiorrhiza in the treatment of postoperative abdominal adhesion （PAA）. METHODS ：Active components and target genes of S. miltiorrhiza were retrieved from TCMSP database，SwissADME database ，Perl database ，UniProt database and other databases. GeneCards ，OMIM and PubMed database were used to retrieve target genes related to PAA. Venn diagram was drawn by using mapping tool of bioinformatic online database so as to screen the intersecting targets of active component-PAA. STRING platform was adopted to establish target network related to active component-PAA and protein-protein interaction （PPI）network of intersecting targets ，etc.，and to screen hub genes. Gene ontology（GO）and Kyoto Encyclopedia of Genes and Genom es（KEGG）pathway enrichment were carried out by using R 3.6.1 software. Using the protein encoded by hub gene as receptor and tanshinone Ⅱ A as ligand ，the molecular docking was carried out with AutoDock 1.5.6 tool. RESULTS ：A total of 38 active components of S. miltiorrhiza with high gastrointestinal absorption and their corresponding 72 targets，755 PAA-related target genes were identified. Results of Venn diagram showed that there were 33 intersecting targets of active components of chuqi90@163.com S. miltiorrhiza with PAA. Tanshinone ⅡA，dihydrotanshinolac- tone and other components may be important nodes of the target network related to active component-PAA. FOS，APP，ACHE， CASP3 and PTGS2 may be the hub genes in PPI network of intersecting targets. Results of GO enrichment showed that the intersecting targets were mainly concentrated in adrenergic receptor activity ，catecholamine binding ，G protein-coupled amine receptor activity and so on ；KEGG pathway enrichment analysis showed that the intersecting targets were mainly enriched in neuroactive ligand-receptor interaction ，cGMP-PKG signaling pathway ，endocrine resistance ，EGFR-tyrosine kinase inhibitor resistance and calcium signaling pathway.Molecular docking analysis showed that tanshinone ⅡA could form hydrogen bonds with many amino acid residues such as VAL- 580 of proto oncogenes c-Fos ，amyloid precursor protein ，acetylcholinesterase，caspase 3 and prostaglandin G/H synthase 2. CONCLUSIONS ：The active components of S. miltiorrhiza play a role in the treatment of PAA by directly or indirectly acting on neuroactive ligand-receptor interaction ，cGMP-PKG signaling pathway ，endocrine resistance ， EGFR-tyrosine kinase inhibitor resistance resistance and calcium signaling pathway.

Quantitative Estimation of Blood Concentration of Lamotrigine in Chinese Han Pediatric Patients with Epi-lepsy Based on UGT1A4142T>G Polymorphism and Blood Concentration of Valproic Acid / 中国药房

OBJECTIVE:To investigate the effects of UGT1A4142T>G polymorphism and blood concentration of valproic ac-id(VPA)on blood concentration of lamotrigine(LTG)in southern Chinese Han children with epilepsy,and to establish the predic-tion equation for quantitatively estimating blood concentration of LTG. METHODS:A total of 72 southern Chinese Han children with epilepsy selected from Guangzhou Women and Children's Medical Center during Jan. 2010-Sept. 2016 were given LTG+VPA. LC-MS/MS and enzyme amplified immunoassay were adopted to determine the blood concentration of LTG and VPA. RFLP-PCR was adopted to determine UGT1A4142T>G polymorphism. The relationships of age, gender, blood concentration of VPA, UGT1A4142T>G polymorphism and LTG concentration-to-dose-ratio (CDR) were also investigate. The prediction equation for blood concentration of LTG was established by multiple linear regression analysis. RESULTS:Age and blood concentration of VPA were positively related to CDR of LTG(r=0.225,0.300,P0.05). UGT1A4 TT,TG and GG genotypes were detected in 39,29,and 4 cases respectively;the frequencies of each genotype were in line with the Har-dy-Weinberg balance(P>0.05). CDR of LTG of TT genotype was significantly lower than those of TG and GG genotype,with sta-tistical significance(PG polymorphism(x4)were all related to blood concentration of LTG(PG polymorphism may associated with blood concentration of LTG. Established prediction equation can provide reference for precise medication in south-ern Chinese Han children with epilepsy.

Status and Control Strategy of TCM-induced Diseases / 中国药师

In recent years, Chinese medicine preparations have been applied in clinic increasingly with the development of tradi-tional Chinese medicine ( TCM) . Meanwhile, TCM-induced diseases and adverse reactions have attracted more and more attention. In the study, the main symptoms and etiological factors of TCM-induced diseases were summarized, and relative control methods and strat-egies were suggested. The summarization can provide theoretical support for clinical rational drug use, which shows clinical significance and scientific value for preventing TCM-induced diseases and reducing the frequency and severity of the diseases.

Screening of the Different Concentrations of Ethanol Extracts from Smilax China for Its Antiinflammatory Activity / 医药导报

Objective To study the effects of the different concentrations of ethanol extracts of Smilax China on ear edema in mice and granuloma in rats,and to provide an evidence for optimizing the extraction process. Methods Effects of different concentrations of ethanol extracts of Smilax China on the xylene-induced ear edema in mice and the cotton ball-induced granuloma hyperplasia in rats were tested . Results Compared with the model controls,70% ethanol extracts of Smilax China at high,medium and low doses significantly inhibited ear edema in mice (t=2. 58,P<0. 05;t=2. 28,P<0. 05;t=2. 17,P<0. 05) and reduced the granuloma hyperplasia in rats(t=5. 28,P<0. 01;t=5. 24,P<0. 01;t=5. 17,P<0. 01). Conclusion The 70% ethanol extracts of Smilax China at three doses present the most active antiinflammatory effect,confirmed in both mice ear edema and rats granuloma models.

Effect of Smilax china bioactive fraction on tumor necrosis factor-α and interleukin-4 contents in uterine tissue of rats with chronic pelvic inflammatory disease / 南方医科大学学报

<p><b>OBJECTIVE</b>To study the mechanism that mediates the therapeutic effect of the bioactive fraction of Baqia (Smilax china) on chronic pelvic inflammatory disease (CPID).</p><p><b>METHODS</b>Seventy rats were randomized into CPID model group, sham-operated group, normal control group, Jingangteng capsule group, and high-, medium-, and low-dose Baqia groups. Rat models of CPID were established by inducing chemical burns of the uterus and corresponding treatments were administered. After 14 days of treatment, the rat uterus was observed for swelling and inhibition rate, and the expressions of tumor necrosis factor-α (TNF-α) and interleukin-4 (IL-4) in the uterine tissues were determined using enzyme-linked immunosorbent assay.</p><p><b>RESULTS</b>The bioactive fraction of Baqia at the 3 doses obviously reduced the inflammatory cells in the endometrium, promoted epithelial cell proliferation, and ameliorated congestion and edema of the serosa. High and medium doses of Baqia bioactive fraction significantly decreased uterus swelling rate of the rats (P<0.01). All the 3 doses of the Baqia bioactive fraction obviously decreased uterine TNF-α content (P<0.01) and significantly increased uterine IL-4 expression level (P<0.05), and IL-4 up-regulation was especially obvious in high and medium dose groups (P<0.01).</p><p><b>CONCLUSION</b>Baqia bioactive fraction can ameliorate uterine swelling, lower uterine TNF-α and increase IL-4 expressions in rats with CPID, which may be a pharmacological mechanism underlying its therapeutic effect on CPID and cervical adhesion.</p>

Pharmaceutical screening of the effective fraction from Smilax for treatment of chronic pelvic inflammatory disease / 南方医科大学学报

<p><b>OBJECTIVE</b>To determine the effective fraction of Smilax for treatment of chronic pelvic inflammatory disease (CPID) by pharmacodynamic screening as the basis for further development of sarsaparilla preparations.</p><p><b>METHODS</b>The chemical fractions of Smilax were administered intragastrically in rat models of CPID induced by injecting phenol mucilage into the uterus to observe the therapeutic effects. The anti-inflammatory effects of different extract fractions from Smilax were tested in mice with xylene-induced ear edema and in rats with cotton-ball-induced granuloma.</p><p><b>RESULTS</b>High-dose ethyl acetate extract of Smilax could obviously inhibit uterus inflammation in rats with CPID, showing also strong anti-inflammatory effects against ear edema in mice and granuloma in rats (P<0.01). The moderate dose of ethyl acetate extract also obviously ameliorated the inflammation. Both the ethyl acetate extract fraction and the total extract fraction of Smilax showed anti-inflammatory effects, while the former produced strong effects while the latter has only weak actions.</p><p><b>CONCLUSION</b>The ethyl acetate extract fraction of Smilax is the effective fraction to produce anti-inflammatory and anti-CPID effects.</p>

Prevention Action of Changtong Oral Liquid on Postoperative Intestinal Adhesions in Rabbits / 中华中医药杂志

Objective: To observe the Prevention Action of Changtong Oral Liquid (CTOL) on the postoperative intestinal adhesions in rabbits. Method: Thirty-six male New Zealand rabbits were randomly divided into six equal groups (n=6): Normal control (group 1); model control (group 2); Simo Decoction (group 3); and CTOL minimal, medium and maximal dosages (group 4,5,6). Except group 1, the other rabbits were created as intestinal adhesive models. Group 1 and group 2 were orally fed with distilled water (20ml/kg), and group 3 to 6 with Simo Decoction 10ml/kg and CTOL in doses of 2.15g/kg, 4.30g/kg and 8.60g/kg respectively. On day 3 after surgery, the blood samples were collected to determine the fibrinolytic activity, and on day 9 the adhesion was graded. Result: CTOL could evidently reduce the severity of postoperative adhesions and increase plasma tPA activity and inhibit plasma PAI-1 activity. Conclusion: CTOL could prevent postoperative intestinal adhesion formation.

Determination of Microelement Manganese in Changtong Oral Liquid by Atomic Absorption Spectrometry / 中国药房

OBJECTIVE:To establish atomic absorption spectrometry for the assaying of the microelement manganese in Changtong oral liquid.METHODS:The light source was hollow-cathode lamp with wavelength at 279.5nm,the electric current of the light was 3.0mA,the slit-width was 1.2nm,the air flow rate was 5.0L/min and the flow rate of acetylene was 1.0L/min.RESULTS:The calibration curves was in linear correlation with adsorption when the detection concentration range of manganese was 0.5～2.5?g/ml(r=0.9 997),the average recovery was 99.24%(RSD=2.06%,n=5).CONCLUSION:This method is simple,fast,accurate,sensitive and precise.

Effect of ChangTong oral liquid on the cell cycle of cultured fibroblasts from normal peritoneum and adhesion / 中华中医药杂志

Objective:To explore the effect of ChangTong oral liquid(CTOL) on cell cycle of cultured fibroblasts from normal peritoneum(NF) and adhesion(AF).Methods:15 SD male rats were randomly divided into 3 groups:normal serum group,2 CTOL groups(medium and high doses).After administration of medication at the different dosages for 7 days,serums were obtained from the abdominal arteries;the prepared tissues were cultured until outgrowth of fibroblasts.In our study,the passage 3-8 cells were used in order to maintain comparability;The fibroblasts in desired condition were plated in 10% FBS,then divided into three groups:rat serum normal group,CTOL groups(medium and high dose).Cells were cultured respectively for 12,24 and 48 h,and analyzed by flow cytometer.Results:Compared with serum normal group of NF,CTOL medium dosage could increase the proportion of NF in the G1 stage at 12,24 and 48h,but only CTOL high dosage had significance(P

Effect of Shenshuaining Dispersible Tablets on Serum NO,NOS,SOD and MDA Levels in Rats with Chronic Renal Failure / 中国药房

OBJECTIVE: To observe the effect of Shenshuaining dispersible tablets on renal function of rats with chronic renal failure (CRF) induced by adenine and explore its action mechanism. METHODS: Seventy-two Sprague-Dawley rats (the ratio of male to female was 1∶1) were randomly divided into 6 groups: normal control group, model control group, Niaoduqing group, Shenshuaining dispersible tablets groups (high, middle and low doses). All groups except the normal control were fed with feed containing 0.5% adenine to estabish CRF model. After giving corresponding drugs for 7 weeks, the levels of nitric oxide (NO), total nitric oxide synthase (T-NOS), inducing nitric oxide synthase (iNOS), configuration nitric oxide synthase (cNOS), total superoxide dismutase (SOD), Cu/Zn-SOD and malonaldehyde (MDA) were detected. RESULTS: Compared with normal control group, the levels of NO,T-NOS, cNOS, T-SOD and Cu/Zn-SOD markedly decreased, and the iNOS and MDA contents were significantly increased in adenine-induced CRF rats. Shenshuaining dispersible tablets could markedly ameliorate the above indexes. CONCLUSION: Shenshuaining dispersible tablets could effectively ameliorate renal function. The mechanism might be related to the enhanced body's antioxidation abiliy, reduced damage of free radical and increased synthesis of cNOS and NO which possess protective effect on renal function.

Diagnosis of acute tubular necrosis in renal allograft with contrast ultrasound: an experimental study / 中华超声影像学杂志

Objective To investigate the diagnostic feasibility of acute tubular necrosis(ATN) in renal allograft using time intensity curves by intravenous contrast ultrasound.Methods The canine models of acute tubular necrosis in renal allograft were established,and examined subsequently with intravenous contrast ultrasound using auto control,and also the parameters of time intensity curves were analyzed,tracking the renal biopsies simultaniously.Results After ATN occured, the curve peak was ante displaced.And parameters of TIC (except peak intensity,PI),area under the curve(AUC),half time of descent(HT),mean transit time(MTT),the ratio of AUC were decreased dramatically.Conclusions Contrast ultrasound combined with TIC quantitative analysis could reflect the variation of blood perfusion objectively,and it is a potential new method for diagnosis of ATN in renal allograft.

Study on the effect of myeloperioxidase in rat colitis by oral administration of HPMCP-coated chitosan capsule filled with dexamethasone liposome lyophilized powder / 中国药理学通报

Aim To observe the inhibition of myeloperioxidase(MPO) activity in rat colitis by oral administration of HPMCP-coated chitosan capsule filled with dexamethasone(DSP) liposome lyophilized powder.Method The rat colitis was induced with the coloclysis of 2,4,6-trinitrobenzene sulfonic acid(TNBS),and then methods were established for quantifying MPO in colon tissue and the ratio of rat colon weight/rat body weight(C/B),which were chosen as the index of colitis degree.These indexes were used to evaluate the inhibiting action of various DSP dosage forms on MPO in colon tissue after their oral administration.Results The observed MPO in colon tissue reached the max on the fifth day with the coloclysis of TNBS.All the experimented DSP preparations could effectively inhibit MPO activity,while DSP lyophilized liposome capsule had the most effectiveness.Conclusion DSP lyophilized liposome chitosan capsule may be more helpful in treating colitis than DSP powder chitosan capsule and its other dosage forms.Hence,it is worth studying further.

Effect of skin condition on the permeability of theophylline via rat skin / 中国药理学通报

Aim To investigate the influence of skin layers ( st ratum corneum and viable layer) on the percutaneous absorption of drug with or w ithout isopropyl myristate (IPM). Methods We chose theophylline (TP ) as a model drug. Patches containing saturated concentration of TP were prepare d. The in vitrotransdermal permeation experiment via different rat skin lay ers was carried out. Results The Kp of TP via stripped skin was 2.1 times larger than that via intact skin. The permea bility was en hanced when coexisted with IPM either via intact skin or via stripped skin. Conclusion IPM can significantly enhance the percutaneous absorption of TP via different skin layers. And these data and methods represent a novel appr oach to evaluate the effects of skin damage and skin disease on drug percutaneou s absorption.

Experimental study on blood perfusion of acute rejection in renal allograft with ultraharmonic contrast imaging / 中华超声影像学杂志

Objective To evaluate the value of using ultraharmonic contrast imaging(UHCI) and acoustic densitometry(AD) technique to quantify cortex blood perfusion of acute rejection in renal allograft.Methods The canine models with acute renal allograft rejection were established. The examinations of renal allograft were performed by intravenous contrast ultrasound and AD technique on the days 1,3,5,7,9,11 after transplantation,some parameters related to perfusion such as peak intensity(PI),the area under the curve(AUC),the half time of descending(HT) and the mean transit time(MTT) of renal cortex were measured,and the graft biopsies were done simultaneously.Results The cortex of renal allograft with acute rejection showed nonenhancing defects after contrast agent injection. From 5 to 11 days after transplantation,the PI,AUC,HT,MTT of renal cortex were increasingly decreased,and the 50% wash-out slope was increasingly increased; furthermore,there were significant differences between those of the first day of post-operation(P

Identification of proteins and polypeptides from Fructus Lycii by HPCE / 中国药学杂志

BJECTIVE　To identify the fruits of Lycium barbarum L.(LB) and Lycium chinense Mill.(LC).METHODS　The proteins and polypeptides from the fruits of LB and LC were analysed by high-performance capillary electrophoresis.RESULTS　LB could be distinguished from LC by their electrophorograms.CONCLUSION　HPCE could be used for the pharmacognostic identification of Fructus Lycii.

Study on Mechanism of Action of Compound Huanggan Granules on the Kidney / 中国药房

OBJECTIVE:To research the mechanism of action of compound Huanggan gr anules(FHG) METHODS:To observe the effect of FHG on the renal blood flow and glomerular filtration rate,and its mechanism of diuresis by means of isotopic tracer,electromagnetic flowmeter and ureter catheterization RESULTS:FHG could significantly increase the renal blood flow and glomerular filtration rate,and enhance the diuresis CONCLUSION:Its diuresis is based on the increase of rena l blood flow and glomerular filtration rate,which results in the decrease of ne phrotoxic substances such as blood urea nitrogen and serum creatinine

Effect of Changtong Oral Liquid on TGF - ?1 Expression in Intestinal Wall of Rats with Postoperative Intestinal Adhesion / 中国药房

OBJECTIVE: To observe the preventive mechanism of Changtong oral liquid on postoperative intestinal adhesion .METHODS: The intestinal adhesion model was established by traumatizing cecal scrosa and ligating adjacent abdominal wall/The effect of Changlong oral liquid on the expression of TGF-?1 was examined by immunohistochemical method.RESULTS & CONCLUSION:Changtong oral liquid can decrease the expression of TGF - ?1 of rats with adhesion .Maybe it is one of the mechanism that Changtong oral liquid can prevent postoperative intestinal adhesion.

Determination of the Content of C 3 F 8 in Human Albumin Microspheres Filling-with C 3 F 8 / 中国药房

OBJECTIVE:To determine the content of C 3 F 8 in human albumin microspheres filling-with C 3 F 8 .METHODS:By Tekmar3000purge and trap concentrator coupled with a Hewlett-Packard5972GC/MSD.RESULTS:C 3 F 8 contents in samples were119.1～433.5?g/ml.CONCLUSION:The method is feasible and suitable for quality control.

Determination of Emodin in Changtong Oral Liquid by HPLC / 中国药房

OBJECTIVE:To determine the content of emodin in Changtong oral liquid.METHODS:HPLC was used.The stationary phase was Nova-Pak C 18 column and the mobile phase was methanol-0.1%phosphoric acid solution(85∶15).The UV detection wavelength was254nm.RESULTS:There was a good linear relationship within the concentration range of0.48～2.4?g/ml of emodin in Changtong oral liquid(r=0.9998).The average recovery was99.73%(n=5),RSD=1.42%. CONCLUSION:This method is simple,fast and accurate.