An unprecedented pair of Z/E isomeric pyridinium compound from the aqueous extract of Aspongopus chinensis Dallas / 药学学报

A novel pair of Z/E isomeric compounds with unprecedented carbon skeleton were isolated from an aqueous extract of Aspongopus chinensis Dallas by macroporous resin, silica gel, and semi-preparative high performance liquid chromatography (HPLC). Their structures were identified by nuclear magnetic resonance (NMR), Infrared spectroscopy (IR), Mass spectroscopy (MS) and other spectroscopic methods as (Z)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine A, and (E)-3-(but-1″-en-1″-yl)-1-(2ʹ-hydroxyethyl)-4-propylpyridin-1-ium, namely aspongopyridine B, respectively. Besides, the anti-inflammatory, anti-tumor, acetylcholinesterase inhibition and butyrylcholinesterase inhibition activities of the compounds 1 and 2 were evaluated. The results showed that compounds 1 and 2 have no anti-inflammatory, anti-tumor, and butyrylcholinesterase inhibition activities instead of weak acetylcholinesterase inhibition activity.

Nurses' Colleague Solidarity and Job Performance: Mediating Effect of Positive Emotion and Turnover Intention

Background@#Job performance is known as an essential reflection of nursing quality. Colleague solidarity, positive emotion, and turnover intention play effective roles in a clinical working environment, but their impacts on job performance are unclear. Investigating the association between nurses’ colleague solidarity and job performance may be valuable, both directly and through the mediating roles of positive emotion and turnover intention. @*Methods@#In this cross-sectional study, a total of 324 Chinese nurses were recruited by convenience sampling method from July 2016 to January 2017. Descriptive analysis, Spearman’s correlation analysis, and the structural equation model were applied for analysis by SPSS 26.0 and AMOS 24.0. @*Results@#A total of 49.69% of participants were under 30 years old, and 90.12% of participants were female. Colleague solidarity and positive emotion were positively connected with job performance. The results indicated the mediating effects of positive emotion and turnover intention in this relationship, respectively, as well as the chain mediating effect of positive emotion and turnover intention. @*Conclusions@#In conclusion, dynamic and multiple supportive strategies are needed for nurse managers to ameliorate nursing job performance by improving colleague solidarity and positive emotion and decreasing turnover intention based on the job demand-resource model.

Magnolol attenuates right ventricular hypertrophy and fibrosis in hypoxia-induced pulmonary arterial hypertensive rats through inhibition of the JAK2/STAT3 signaling pathway / 中国药理学与毒理学杂志

OBJECTIVE Right ventricular (RV) remodeling is one of the essential pathological features in pulmonary arterial hypertension (PAH). RV hypertrophy or fibrosis are the leading causes of RV remodeling. Magnolol is a com?pound isolated from Magnolia officinalis. It possesses multiple pharmacological activities, such as anti-oxidation and anti-inflammation. This study aims to evaluate the effects and underlying mechanisms of magnolol on RV remodeling in hypoxia-induced PAH. METHODS ① Male SD rats (220 g) were randomly divided into 5 groups (n=10): the normoxia group, the hypoxia group, the hypoxia plus Magnolol (10 and 20 mg·kg-1·d-1) group, and the vehicle group. Rats in the normoxia group were kept in a normoxia environment for 4 weeks, while rats in the hypoxia group were kept in a hypoxic chamber (10％ O2). The rats in the hypoxia plus magnolol groups were administered with magnolol at 10 or 20 mg·kg-1 (ip) once a day for 4 weeks. At the end of 4 weeks, the heart function was assessed by Doppler echocardiography, and then the rats were anesthetized with sodium pentobarbital (30 mg·kg-1, ip). The RVSP was measured by the right heart catheterization method. The heart tissues were collected and dissected to calculate the index of RV remodeling (RV/LV+IVS, RV/tibial length, or RV/body weight). Part of the RV samples was fixed with 4％paraformaldehyde for morphological analysis, while other samples were frozen at-80℃for molecular studies (measurements of ANP, BNP,α-SMA, and col?lagen Ⅰ/Ⅲ mRNA expression as well as p-JAK2/JAK2 and p-STAT3/STAT3 protein levels). ② To evaluate the effect of magnolol on hypoxia-induced myocardial hypertrophy and fibrosis, H9c2 or cardiac fibroblasts were divided into 7 groups: the control group, cells were cultured under normal conditions; the hypoxia group, cells were cultured under hypoxic condition (3％ O2);the hypoxia plus magnolol 10 mg·kg-1 group, magnolol10μmol·L-1 was added to the culture medium before the hypoxia treatment;the hypoxia plus magnolol 30 mg·kg-1 group, magnolol 20μmol·L-1 was added to the culture medium before the hypoxia treatment;the hypoxia plus TG-101348 group, TG-101348 (a specific inhibitor of JAK2) 1μmol·L-1 was added to the culture medium before the hypoxia treatment;the hypoxia plus JSI-124 group, JSI-124 (a specific inhibitor of JAK2) 1μmol·L-1 was added to the culture medium before the hypoxia treatment;and the hypoxia plus vehicle group, an equal volume of vehicle (DMSO) was added to the culture medium before the hypoxia treatment. At the end of the experiments, the cells were collected for morphological and molecular analysis. RESULTS In vivo, male Sprang-Daley rats were exposed to 10％ O2 for 4 weeks to establish an RV remodeling model, which showed hypertrophic and fibrotic features (increases of RV remodeling index, cellular size, hypertrophic and fibrotic marker expression), accompanied by an elevation in phosphorylation levels of JAK2 and STAT3;these changes were attenuated by treating rats with magnolol. In vitro, the cultured H9c2 cells or cardiac fibroblasts were exposed to 3％ O2 for 48 h to induce hypertrophy or fibrosis, which showed hypertrophic (increases in cellular size as well as the expression of ANP and BNP) or fibrotic features (increases in the expression of collagenⅠ, collagenⅢandα-SMA). Administration of mag?nolol and TG-101348 or JSI-124 (JAK2 selective inhibitors) could prevent the process of myocardial hypertrophy and fibrosis, accompanied by the decrease in the phosphorylation level of JAK2 and STAT3. CONCLUSION Magnolol can attenuate RV hypertrophy and fibrosis in hypoxia-induced PAH rats through a mechanism involving inhibition of the JAK2/STAT3 signaling pathway.

Study on anti-osteoporosis effect of Eucommiae Cortex based on GC-MS metabonomics / 中国中药杂志

Based on GC-MS metabolomics and biochemical index analysis, the mechanism of bone mass loss in osteoporosis and the evaluation of anti-osteoporosis in Eucommiae Cortex were studied. The OVX rats model was established by bilateral ovariectomized. The routine indexes such as BMC, BMD, BGP and TRAP5 b were determined. The GC-MS technique was used to analyze the metabolism profile of serum samples between the control group, model group and medicine group, and multiple statistical analysis methods including principal component analysis(PCA), partial least squares-linear discriminant analysis(PLS-LDA) and subwindow rearrangement analysis(SPA) were used to screen and identify biomarkers. Five metabolites were selected as potential biomarkers, glycine, lysine, tryptophan, docosahexaenoic acid and glucose. Except for the significant increase of tryptophan in serum of OVX rats, the other four metabolites were significantly decreased. Moreover, the five biomarkers of the medicine group had a trend of returning to rats in control group. The significantly altered metabolite levels indicated that Eucommiae Cortex may relieve the symptoms of osteoporosis by regulating amino acid metabolism and oxidative stress.

Pharmacological mechanism of traditional sedative effect of alkaloids in Nelumbinis Plumula based on network pharmacology / 中国中药杂志

Nelumbinis Plumula has the traditional sedative effect,but its mechanism is unclear. In this study,the relationship between traditional sedative effect and hypnotic effect of Nelumbinis Plumula was taken as the starting point to study the hypnotic mechanism of the major medicinal components in Nelumbinis Plumula by the network pharmacology method. Targets of active Nelumbinis Plumula alkaloids were screened by Swiss Target Prediction server,TCMSP and BATMAN-TCM. Targets of hypnotic drugs approved by FDA were screened from Drug Bank,OMIM,TTD databases. The common targets were screened by GO and KEGG pathways. Cytoscape 3. 7. 1 software was used to construct the network of " active component-target-pathway-disease". The results of network analysis showed that 21 active compounds were associated with 44 targets and 28 pathways. Among them,21 compounds,35 targets and 15 pathways were predicted to be related to sedative hypnosis. Nelumbinis Plumula showed the hypnotic effect by acting on neuroactive ligand-receptor interaction pathway,regulation of actin cytoskeleton pathway,calcium signaling pathway,cholinergic synapse pathway.This study preliminarily revealed the potential active compounds and possible mechanisms of traditional sedative effect of Nelumbinis Plumula,which provided a theoretical basis for further experimental studies on medicinal materials and its mechanisms.

Virtual screening of antithrombotic alkaloids from Houttuynia cordata / 中国中药杂志

Antithrombus is one of the effective methods to prevent and treat cardiovascular diseases. Based on the theory of traditional Chinese medicine,the author's previous research and relevant literature,it was found that the alkaloids in Houttuynia cordata has potential antithrombotic effect. However,the pharmacological substance basis and antithrombotic mechanism of H. cordata have not been clarified. In this study,molecular docking was used for virtual screening of antithrombotic alkaloids from H. cordata. Seventy alkaloids selected from H. cordata were screened in the docking ligand data-base with teen thrombosis targets with known crystal structures as the receptors. In addition,the small-molecule approved or to be approved drugs of targets from Drug Bank database were set as a positive reference with minimum score(S value) of each target's approved or to be approved drugs as threshold. The Dock module in Molecular Operating Environment(Version 2016) software was applied to screen the potential active compounds which their scores(S value) were lower than the minimum score of reference. At last the mechanism of antithrombotic effect was preliminarily revealed by compared the main active sites of the test alkaloids with original ligands and references. This study provided some useful information to development of antithrombus drugs.

Construction of the mindfulness intervention program for patients with chronic obstructive pulmonary disease at home based the solution focused approach / 中国实用护理杂志

Objective Based on the Kabat-Zinn's mindfulness decompression therapy and Teasdale's mindfulness cognitive therapy,and using the solution-focused approach as the frame structure,we establish comprehensive,standard mindfulness interventions scheme of domiciliary patients with chronic obstructive pulmonary disease,which can provide the basis for the development of the community and residential care.Methods Twenty-six experts were selected as the target of the study and two rounds of correspondence were used to establish the final mindfulness intervention plan of the domiciliary patients with chronic obstructive pulmonary disease.Meanwhile,the reliability and representativeness of the consultation are tested by using the coordination degree,positive coefficient and authoritative coefficient of expert opinions.Results The positive coefficient of the two round correspondence experts were 88.46%(23/26)and 100.00%(23/23),and the expert authority coefficient was 0.90 and 0.91.The variation coefficient of the indicators after two rounds of expert consultation was 0.04-0.14,the coordination coefficient of experts was 0.32(P＜0.01)and 0.59(P＜0.01)respectively.The final construct of domiciliary patients of chronic obstructive pulmonary disease with the intervention programme consists of 5 steps,25 entries,which was suitable for the positive reading intervention scheme.Conclusions The results show that experts enquiry for representative and high credibility,and the mindfulness intervention plan of domiciliary patients with chronic obstructive pulmonary disease is scientific and practical.

Cannabinoid receptor system regulates ion channels and synaptic transmission in retinal cells / 生理学报

Endocannabinoid receptor system is extensively expressed in the vertebrate retina. There are two types of cannabinoid receptors, CB1 and CB2. Activation of these two receptors by endocannabinoids N-arachidonoylethanolamide (anandamine, AEA) and 2-arachidonyl glycerol (2-AG) regulates multiple neuronal and glial ion channels, thus getting involved in retinal visual information processing. In this review, incorporating our results, we discuss the modulation of cannabinoid CB1 and CB2 receptors on retinal neuronal and glial ion channels and retinal synaptic transmission.

Questionnaire on Awareness and Consumption Situation of Health Care Products in Hospitalized Patients / 中国药师

Objective:To investigate the consumption situation and cognition of health care products in hospitalized patients, ana-lyze the problems in purchasing and use of health care products to provide evidence for the correct selection and rational use of health care products. Methods:The investigation and analysis was conducted with an anonymous questionnaire on awareness and consumption situation of health care products in hospitalized patients. Results:The survey received 129 valid questionnaires, and more than 1/3 re-spondents did not know the differences between health care products and medicines, and 27. 91％ of them treated diseases with health care products, 57. 36％ of them purchased health care products per month, and 96. 12％ of them thought the efficacy of health care products were inconsistent with the advertising efficacy. Conclusion:Patients cannot distinguish health care products from medicines, and lack of trust in the health care products market. Corresponding measures should be performed to help patients purchase and use of health care products and safeguard their legitimate rights and interests.

Injectable hyaluronic acid carrying autologous chondrocytes repairs cartilage defects / 中国组织工程研究

BACKGROUND: In the cartilage tissue engineering materials, hyaluronic acid as the representative of polysaccharide materials has good material-cell interface that is beneficial to the growth of chondrocytes, which has become a hot research topic in recent years. OBJECTIVE: To explore the feasibility of injectable hyaluronic acid material loaded with chondrocytes to repair cartilage defects in rats. METHODS: Ninety Sprague-Dawley rats were selected to prepare a cartilage defect model, and they were randomly divided into three groups at the 2nd day after modeling. The experimental group was injected hyaluronic acid hydrogel loaded with chondrocytes into the articular cavity, the control group was injected with hyaluronic acid hydrogel into the articular cavity, and the blank control group received no intervention. At 1, 3 and 6 weeks after injection, the repaired cartilage tissues were taken out for hematoxylin eosin staining, Masson staining, and scanning electron microscope observation, and the expression of heme oxygenase and level of collagen were detected.RESULTS AND CONCLUSION: (1) Hematoxylin eosin staining: at 6 weeks after injection, granulation tissues filled the repair area in the blank control group. The control group was full of yellowish white tissues in the repair area, with distinct boundary with the normal cartilage, the surface was not smooth and the lymphocytes were reduced compared with those at 3 weeks. Repair tissue of the experimental group was semi-transparent and showed a fuzzy boundary with the normal cartilage, and moreover, lymphocyte was significantly reduced compared with those at 3 weeks. (2) Masson staining: at 6 weeks after injection, collagen fiber synthesis in the repair area in the experimental group was the best, successively followed by the control group and the blank control group. (3) Scanning electron microscope observation: at 6 weeks after injection, collagen fiber arrangement in the repair area was irregular and partially broken in the blank control group, and the arrangement became more orderly in the control group but still partially broken. The collagen fibers in the experimental group were arranged orderly, and the boundary with normal cartilage was unclear. (4) Expression of heme oxygenase and level of collagen: at 6 weeks after injection, the expression of heme oxygenase in the experimental group was higher than that in the control group and blank control group (P < 0.05). The levels of collagen in the experimental group at 1, 3 and 6 weeks after injection were higher than those in the control group and the blank control group (P < 0.05). To conclude, hyaluronic acid injectable material loaded with chondrocytes can promote the repair of cartilage defects in rats.

Injectable hyaluronic acid carrying autologous chondrocytes repairs cartilage defects / 中国组织工程研究

BACKGROUND: In the cartilage tissue engineering materials, hyaluronic acid as the representative of polysaccharide materials has good material-cell interface that is beneficial to the growth of chondrocytes, which has become a hot research topic in recent years. OBJECTIVE: To explore the feasibility of injectable hyaluronic acid material loaded with chondrocytes to repair cartilage defects in rats. METHODS: Ninety Sprague-Dawley rats were selected to prepare a cartilage defect model, and they were randomly divided into three groups at the 2nd day after modeling. The experimental group was injected hyaluronic acid hydrogel loaded with chondrocytes into the articular cavity, the control group was injected with hyaluronic acid hydrogel into the articular cavity, and the blank control group received no intervention. At 1, 3 and 6 weeks after injection, the repaired cartilage tissues were taken out for hematoxylin eosin staining, Masson staining, and scanning electron microscope observation, and the expression of heme oxygenase and level of collagen were detected.RESULTS AND CONCLUSION: (1) Hematoxylin eosin staining: at 6 weeks after injection, granulation tissues filled the repair area in the blank control group. The control group was full of yellowish white tissues in the repair area, with distinct boundary with the normal cartilage, the surface was not smooth and the lymphocytes were reduced compared with those at 3 weeks. Repair tissue of the experimental group was semi-transparent and showed a fuzzy boundary with the normal cartilage, and moreover, lymphocyte was significantly reduced compared with those at 3 weeks. (2) Masson staining: at 6 weeks after injection, collagen fiber synthesis in the repair area in the experimental group was the best, successively followed by the control group and the blank control group. (3) Scanning electron microscope observation: at 6 weeks after injection, collagen fiber arrangement in the repair area was irregular and partially broken in the blank control group, and the arrangement became more orderly in the control group but still partially broken. The collagen fibers in the experimental group were arranged orderly, and the boundary with normal cartilage was unclear. (4) Expression of heme oxygenase and level of collagen: at 6 weeks after injection, the expression of heme oxygenase in the experimental group was higher than that in the control group and blank control group (P < 0.05). The levels of collagen in the experimental group at 1, 3 and 6 weeks after injection were higher than those in the control group and the blank control group (P < 0.05). To conclude, hyaluronic acid injectable material loaded with chondrocytes can promote the repair of cartilage defects in rats.

Meta-analysis for efficacy and safety of rosuvastatin and simvastatin in the treatment of hyperlipidemia / 天津医药

Objective To investigate the effectiveness and safety of rosuvastatin and simvastatin in the treatment of hyperlipidemia. Methods The database including CNKI, VIP, Wanfang data base and CBM were retrieved to search the clinical randomized controlled trials (RCT) of rosuvastatin and simvastatin in the treatment of hyperlipidemia, and the data were analyzed with Review Manager 5.2. Results Eighteen RCTs were included with a total sample size of 1819 cases with hyperlipidemia, in which there were 917 patients in rosuvastatin group and 902 in simvastatin group. The Meta-analysis results showed that there were significantly lower serum levels of total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), triglyceride (TG) and significantly higher level of high-density lipoprotein cholesterol (HDL-C) in rosuvastatin group compared with those of simvastatin group [(MD=-0.15, 95%CI:-0.22--0.09, P<0.01), (MD=-0.18, 95%CI:-0.25--0.11, P<0.01), (MD=-0.23, 95%CI:-0.28--0.19, P<0.01) and (MD=-0.11, 95%CI:-0.06--0.15, P<0.01)]. There was no significant difference in the incidence of gastrointestinal adverse reaction between the two groups. Conclusion The current clinical evidences show that rosuvastatin has a better effect on the treatment of hyperlipidemia, and has no adverse reactions.

Pharmacokinetics Comparison of Baicalin between Traditional Slice Decoction and Dispensing Granule De-coction of Huanglianjiedu Decoction / 中国药师

Objective:To compare the pharmacokinetics consistence of baicalin between traditional slice decoction and dispensing granule decoction of Huanglianjiedu decoction. Methods:After the gastric administration of the two decoctions at low, middle and high dose in rats, an HPLC method was used to detect the content of baicalin in the plasma, and then DASS 2. 1. 1 software was used to cal-culate the pharmacokinetic parameters. Results:After the administration of the two decoctions at low, middle and high dose, the phar-macokinetic parameters were as follows:Cmax of 0. 25 and 0. 27μg·ml-1 ,0. 30 and 0. 31 μg·ml-1 ,0. 40 and 0. 45 μg·ml-1;AUC of 2. 48 and 2. 59μg·ml-1 ·h,3. 59 and 3. 71μg·ml-1 ·h,5. 71 and 6. 16μg·ml-1 ·h;Tmax of 3. 0 and 3. 0 h,3. 0 and 3. 0 h, 4.0 and 4.0 h;Vd of (2 822.4 ±118.2) and (2 998.9 ±255.6) L·kg-1,(3 102.6 ±176.3) and (3 405.3 ±213.8) L·kg-1, (4 231.2 ±155.4) and (4 486.0 ±187.0) L·kg-1;CL of (2 923.3 ±215.6) and (2 767.5 ±184.6)L·h-1·kg-1,(4 921.7 ± 225.4) and (4 040.8 ±246.7)L·h-1·kg-1,(5 255.9 ±189.7) and (4 868.7 ±260.4)L·h-1·kg-1;and t1/2 of (3.88 ± 0.41) and (3.71 ±0.37)h,(4.19 ±0.36) and (3.73 ±0.51)h, (5.54 ±0.38) and (5.80 ±0.54)h. Conclusion: The pharma-cokinetic parameters of baicalin have no significant difference between traditional slice decoction and dispensing granule decoction of Huanglianjiedu decoction.

GC-MS determination of metabolites in rat kidneys / 中南大学学报(医学版)

Objective:To establish a method to determine the metabolites in rat kidney tissues by gas chromatography-mass spectrometry (GC-MS) combined with chemometric techniques. Methods:Metabolites were separated and identiifed on HP-5MS column (30 m × 0.25 μm × 0.25 mm). The initial column temperature was 100℃lasting 3 min, and then programmed at 8℃/min to 300℃, maintaining at this temperature for 6 min. hTe internal standard was heptadecanoic acid. hTe grinded kidney tissue was exacted by methanol. hTe supernatant was dried by nitrogen. Atfer the oximation and derivation, the supernatant was analyzed by GC-MS. hTe overlapped peaks were resolved into pure chromatogram and mass spectra with chemometric techniques. Qualitative analysis was performed by comparing the obtained pure mass spectra with those in NIST mass spectra database and certiifcated by the standards and the references. hTe internal method was used for semi-quantitation. Results:A total of 53 compounds were identiifed. hTe main constitutions in the kidney tissue were amino acids, saccharides, fatty acids and urea. Conclusion:hTe combination of methods is rapid and accurate for the analysis of metabolites in the kidney tissue, which provides more information for further study of metabonomics in kidney tissues.

Studies on chemical constituents in stems of Zanthoxylum dissitum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from the stems of Zanthoxylum dissitum.</p><p><b>METHOD</b>Column chromatography on macroporous resin and silica gel, and spectral analysis were used to isolate and elucidate the constituents.</p><p><b>RESULT</b>Seven compounds were isolated and identified as 5,8-dimethoxyethane-3,4-epoxy-furanocoumarin (1), isoimpinellin (2), beta-sitosterol (3), lupeol (4), neohesperidin (5), beta-daucosterol (6), ursolic acid (7).</p><p><b>CONCLUSION</b>All above the compounds were isolated from the plant for the first time and the compound 1 is a new compound.</p>

Separation and purification of total flavones from Herba Epimedii by macroporous adsorption resin with the help of ultrasonic extraction / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the optimal separation of the total flavones from Herba Epimedii by macroporous adsorption resin.</p><p><b>METHOD</b>Nine types of macroporous adsorption were evaluated for separating efficiency by measuring the adsorption ratio, eluting ratio of total flavones.</p><p><b>RESULT</b>The D-101 macroporous adsorption resin had the best separating efficiency. After enrichment and purification with it, the product purity of total flavones was up to 63.8%.</p><p><b>CONCLUSION</b>This method is simple, feasible and fit for industry production.</p>

Pharmacokinetics of 6beta-naltrexol after single and multiple intramuscular injections in Beagle dogs / 药学学报

The pharmacokinetics of 6beta-naltrexol (6beta-NOL) following single intramuscular administration and multiple intramuscular injection once per day for seven days was studied in 4 Beagle dogs. Plasma concentration of 6beta-NOL in dogs was analyzed by a combination of high performance liquid chromatography (HPLC) and electrochemical detection with naloxone (NLX) as internal standard. After single intramuscular injection of 0.2 mg x kg(-1) 6beta-NOL, the plasma concentration-time curve of the drug was found to fit to a two compartment model with first-order absorption. The main parameters of single dosing were as follows: t1/2alpha was (0.26 +/- 0.23) h, t1/2beta was (4.77 +/- 1.65) h, C(max) was (81.65 +/- 5.61) ng x mL(-1), t(peak) was (0.27 +/- 0.07) h, CL(s) was (1.20 +/- 0.06) L x kg(-1) x h(-1), V/F(c) was (1.94 +/- 0.15) L x kg(-1), and AUC(0-t) was (166.82 +/- 7.68) ng x h x mL(-1), separately. After multiple intramuscular injection of 0.2 mg x kg(-1) 6beta-NOL once per day for seven days, the plasma concentration-time curve of the drug fitted to a two compartment model with first-order absorption too. The main parameters of the last dosing were as follows: t1/2alpha was (0.19 +/- 0.18) h, t1/2beta was (5.79 +/- 1.50) h, C(max) was (79.82 +/- 10.5) ng x mL(-1), t(peak) was (0.18 +/- 0.08) h, CL(s) was (1.12 +/- 0.07) L x kg(-1) x h(-1), V/F(c) was (2.10 +/- 0.27) L x kg(-1), and AUC(0-t) was (173.23 +/- 9.49) ng x h x mL(-1), separately. The difference of the parameters between the first and the last dosing was not significant, showing that the plasma kinetics of 6beta-naltrexol was not changed after multiple administrations. In the course of multiple administration, the peak and valley concentration of plasma 6beta-naltrexol were (79.03 +/- 10.3) and (1.50 +/- 0.93) ng x mL(-1), respectively. No clear adverse events were noted during this study. These results showed that plasma 6beta-naltrexol fits to a two compartment model with first-order absorption in dog after intramuscular administration and their pharmacokinetic parameters were reported. There was no remarkable change on plasma pharmacokinetics of 6beta-naltrexol after multiple intramuscular administrations.

Structure-activity relationships analysis of thienorphine and its derivatives / 药学学报

Thienorphine is a chemically-new opioid developed in Beijing Institute of Pharmacology and Toxicology. To elucidate the chemical basis for the unique pharmacological effects of thienorphine, 15 derivatives were synthesized according to combinatorial chemistry and the structure-activity relationships of these compounds were studied. It is demonstrated that thienorphine is a potent long-acting partial agonist. N-Cyclopropylmethyl is responsible for the antagonist effect of thienorphine. More importantly, thiophene at the end of side chain is most likely the pharmacophore accounts for the long-lasting effect of thienorphine. Change of the connection of thiophene and the side chain does not result in changes in the antinociceptive activity.

Separation and purification of alkaloids from radix of Zanthoxylum nitidum by macroporous adsorption resin / 中国中药杂志

<p><b>OBJECTIVE</b>To obtain the optimal conditions for separating the alkaloids from the extract of Radix of Zanthoxylum nitidum by selecting appropriate macroporous adsorption resins.</p><p><b>METHOD</b>Eight types of macroporous adsorption were evaluated in separating efficiency with measuring the adsorption ratio and eluting ratio of Alkaloids as indexes.</p><p><b>RESULT</b>The XDA-5 macroporous adsorption resin had the best separating efficiency. After enrichment and purification with it, the product purity and yield of alkaloids were up to 33.25% and 90.15%, respectively.</p><p><b>CONCLUSION</b>This method is simple, feasible and fit for industry production.</p>

Neferine protects endothelial cells against damages induced by LPC and relationship with asymmetric dimethylarginine / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the protective effect of neferine against damages of endothelial cells induced by lysophos-phatidylcholine (LPC) and the relationship with asymmetric dimethylarginine (ADMA).</p><p><b>METHOD</b>The human umbilical vein endothelial cells (HUVEC-12) were treated with LPC (10 mg x L(-1)) for 24 h to establish the model of endothelial cells damages; HUVECs were prior exposed to neferine (0.1, 1.0 or 10.0 micromol x L(-1) ) for 1 h, and then exposed to LPC in the presence of the neferine for 24 h. At the end of the experiment, the cultured medium was collected for measuring the concentration of nitric oxide (NO), aleic dialdehyde (MDA) as well as ADMA and the cells were collected for measuring the level of intracellular reactive oxygen species (ROS).</p><p><b>RESULT</b>Compared with control group, exposure of endothelial cells to LPC (10 mg x L(-1)) for 24 h significantly increased the concentration of MDA and ADMA in the medium and the level of intracellular ROS and coinstantaneously significantly decreased the concentration of NO in the medium. Neferine (0.1, 1.0 or 10.0 micromol x L(-1)) significantly inhibited the elevated concentration of MDA, ADMA as well as the level of intracellular ROS and coinstantaneously significantly attenuated the decreased level of NO induced by LPC.</p><p><b>CONCLUSION</b>Neferine can protect the endothelial cells against damages induced by LPC and the protective effect is related to the decrease of the concentration of ADMA.</p>