Research progress on Astragali Radix and prediction of its quality markers (Q-markers) / 中国中药杂志

Astragali Radix, a medicinal herb for invigorating Qi, has anti-aging, anti-tumor, immunoregulatory, blood sugar-and lipid-lowering, anti-fibrosis, anti-radiation and other pharmacological effects. This article reviewed the studies about the chemical components and pharmacological effects of Astragali Radix. According to the theory of quality markers(Q-markers) of Chinese medicinal materials, we predicted the Q-markers of Astragali Radix from traditional efficacy, chemical component validity, measurability, plant phylogeny, and pharmacokinetis. The results showed that total polysaccharides, flavonoids(e.g., calycosin-7-O-β-D-glucoside, formononetin, calycosin, quercetin, and ononin), and saponins(e.g., astragalosides Ⅱ, Ⅲ, and Ⅳ) can be taken as the main Q-markers. This review lays a foundation for regulating the quality research and standard establishment of Astragali Radix, and benefits the control and quality supervision of the production process of Astragali Radix and its related products.

Network pharmacological study of Schizonepetae Herba and Saposhnikoviae Radix in treatment of ulcerative colitis / 中国中药杂志

The aim of this paper was to screen the active targets of Schizonepetae Herba and Saposhnikoviae Radix in the treatment of ulcerative colitis by means of network pharmacology,and to investigate their mechanism of action. The effective components of Schizonepetae Herba and Saposhnikoviae Radix were screened out by traditional Chinese medicine systematic pharmacological( TCMSP)database,with oral bioavilability( OB) ≥30% and drug-like( DL) ≥18% selected as the thresholds. Target PPI network was built between the main components and their corresponding targets. One hundred and eighty-two human genes corresponding to the medicine target sites were obtained from Uniprot database; 3 874 genes corresponding to ulcerative colitis were obtained from Genecard database.A total of 115 intersection genes were screened from disease genes and medicine genes,and the PPI interaction analysis was conducted by using String tool. Disease-target PPI network was drawn by using Cytoscape software,and component-target-disease network was constructed. One hundred and eight nodes and 1 882 connections were found,and then Cytoscape software was used to merge the networks and filter the core network for gene GO function analysis and KEGG pathway enrichment analysis. The mechanism of Schizonepetae Herba and Saposhnikoviae Radix was then verified by animal experiment. Gene GO functional analysis suggested that biological process,molecular functions and cell components were involved,and it was found that ulcerative colitis might be related to transcription factor activity,and cytokine receptor binding,etc. Gene KEGG pathway enrichment analysis showed that the mechanism of ulcerative colitis might be associated with TNF and Toll-like receptors( TLRs) signaling pathway-mediated cytoinflammatory factors interleukin-1( IL-1) and interleukin-6( IL6). The possible mechanism of the effective components of Schizonepetae Herba and Saposhnikoviae Radix in treating ulcerative colitis might be related to intervening the cytokine receptor binding of TNF and TLRs signaling pathways,reducing the transcription of nuclear factor-kappaB( NF-κB),and inhibiting the secretion of intestinal inflammatory factors IL-1 and IL-6.

Design, synthesis and evaluation of cytisinic derivatives for hypoglycemic activity / 药学学报

Taking cytosine, an unique natural product alkaloid as the lead, we designed thirty cytisinic derivatives with different types of 12N-substituents, which were synthesized and evaluated for their activity in the regulation of glucose metabolism in vitro. The compounds 3d, 3g and 6h exhibited the potential hypoglycemic activity and compound 3d had a good pharmacokinetics profile. In terms of mechanism of glucose consumption, the compounds 3d and 6h increased cellular glucose consumption. which might be associated with up-regulation of glucose transporter Glut4 expression and activation of AMPK. The results revealed important roles of these new skeleton compounds as potential new drug candidates for control of blood glucose.

Discussion of the Correlation between Voriconazole's Trough Concentration and Mental Abnormity Rate / 中国药学杂志

OBJECTIVE: To explore the correlation between voriconazole's trough concentration and mental abnormity. METHODS: Retrospectively analyze voriconazole's trough concentration and the occurrence of mental abnormity in 151 patients from May 2016 to May 2017 in Xiangya Hospital. RESULTS: In 151 patients, Insomnia rate is 21.85%, binary logistic regression analysis showd that the insomnia rate is positively related to voriconazole's trough concentration(P = 0.02). Illusion rate is 15.23%, binary logistic regression analysis showd that the illusion rate is positively related to voriconazole' s trough concentration (P = 0.002). CONCLUSION: There is a significant correlation between voriconazole's mental abnormity and trough concentration.

Suppression of Epithelial Mesenchymal Transition and Metastasis in Nasopharyngeal Carcinoma via SOD1 Inhibition / 中山大学学报(医学科学版)

Objective]To explore the aberrant expression of SOD1 gene in nasopharyngeal carcinoma tissues and adjacent tissues,as well as in NPC cell lines,then to observe the effect of SOD1 on NPC cells metastatic ability and investigate the intrinsic?mechanism.[Methods]Immunohistochemical technique was used to examine SOD1 expression in carcinoma tissues and adjacent tissues(n=10). Small interfering RNAs and inhibitor LCS-1 were used to knockdown of SOD1 expression and inhibit SOD1 activity, respectively. Then,wound healing test and migration assay were applied to detect cell metastatic ability in vitro. Real-time PCR and Western Blot were used to analyze the expression of EMT-related genes(E-cadherin,Vimentin,Twist).[Results]SOD1 was found to be significantly up-regulated in nasopharyngeal carcinoma tissues(n = 7 ,70%),compared to control. SOD1 was also highly expressed in highly metastatic potential NPC cell lines(CNE2,5-8F,S18)compared with low metastatic ability cell lines(6-10B). Knockdown SOD1 expression or inhibit SOD1 activity suppress cell motility in CNE2 and 5-8F cells. Finally,we demonstrate that SOD1 inhibition plays a role in induction of epithelial marker E-cadherin and has an opposite effect on mesenchymal marker vimen tin and transcriptional factor twist.[Conclusion]These results suggest that SOD1 contributes to EMT and might be important for tumor metastasis in NPC.

Research progress of fecal microbiota transplantation / 中华胃肠外科杂志

Intestinal microbial ecosystem is the most complex and the largest micro-ecosystem of the mammals. The use of antibiotics can lead to a lot of major changes of the flora, making the intestinal flora damaged and impacted, even developing Clostridium difficile infection. Fecal microbiota transplantation (FMT) as a special organ transplant therapy, which can rebuild the intestinal flora, has raised the clinical concerns. It has been used in the refractory Clostridium difficile, inflammatory bowel disease, irritable bowel syndrome, chronic fatigue syndrome, and some non-intestinal diseases related to the metabolic disorders. But this method of treatment has not become a normal treatment, and many clinicians and patients can not accept it. This paper reviews relevant literature in terms of origin, indications, mechanism, production process, current situation and future research, and provide a reference for the clinical application of the treatment of fecal microbiota transplantation.

Determination of yogliptin and its metabolite in Wistar rat plasma by liquid chromatography-tandem mass spectrometry / 药学学报

A rapid, sensitive and simple liquid chromatography-tandem mass spectrometric (LC-MS/MS) method was developed for the simultaneous determination of yogliptin and its metabolite in Wistar rat plasma. Linagliptin and dexamethasone were chosen as the internal standards of yogliptin and its metabolite, (R)-8-(3-hydroxypiperidine- -yl)-7-(but-2-yn-1-yl)-1-((5-fluorobenzo[d]thiazol-2-yl)methyl)-3-methyl- H-purine-2, 6 (3H, 7H)-dione, respectively. After a simple protein precipitation using acetonitrile as the precipitating solvent, both analytes and ISs were separated on a Grace Altima HP C18 column (2.1 mm x 50 mm, 5 microm) with gradient elution using methanol (containing 0.1% formic acid, 4 mmol x L(-1) ammonium acetate)-0.1% formic acid (containing 4 mmol x L(-1) ammonium acetate) as the mobile phase. A chromatographic total run time of 4.4 min was achieved. Mass spectrometric detection was conducted with electrospray ionization under positive-ion and multiple-reaction monitoring modes. Linear calibration curves for yogliptin and its metabolite were over the concentration range of 0.5 to 500 ng x mL(-1) with a lower limit of quantification of 0.5 ng x mL(-1). The intra- and inter- assay precisions were all below 14%, the accuracies were all in standard ranges. The method was used to determine the concentration of yogliptin and M1 in Wistar rat plasma after a single oral administration of yogliptin (27 mg x kg(-1)). The method was proved to be selective, sensitive and suitable for pharmacokinetic study of yogliptin and M1 in Wistar rat plasma.

Study on the levels of DA and metabolite in striatum in rats with Parkinson's disease treated by BDNF gene modified bone mesenchymal stem cells / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To investigate the effects of dopamine (DA) and metabolite in striatum of Parkinson's disease (PD) rats treated by bone mesenchymal stem cells (MSCs) modified by plasmid pIRESneo-EGFP-BDNF.</p><p><b>METHOD</b>pIRESneo-EGFP-BDNF was transfected to MSCs with electroporation. The rat models of PD were set up by 6-OHDA and then divided into four groups randomly, which were Sham group, PD group, BDNF group. The rotating behavior of rat models induced by apomorphine (APO) intraperitoneally which transplanting bone MSCs or MSCs modified by plasmid pIRESneo-EGFP-BDNF through cerebral lateral ventricle after 2, 4 and 8 weeks. The levels of DA, homovanillic acid (HVA), dihydroxy-phenylacetic acid (DOPAC) were measured by high performance liquid chromatography (HPLC) in striatum of each group.</p><p><b>RESULTS</b>The rotation numbers (r/min) of MSCs group or BDNF group in the 2nd, 4th and 8th week after transplanting were significantly decreased compared with that of PD group (P < 0.05). Those of BDNF group were specially significant compared with those of MSCs group (P < 0.05). The levels of DA, HVA, DOPAC and the ratios of DA/HVA, DA/DOPAC in stratum after PD rats intervened by transplanting cells through cerebral lateral ventricle after eight weeks were increased significantly in BDNF group or MSCs group while compared with PD group, especially in BDNF group.</p><p><b>CONCLUSION</b>The behavior of rat with PD was improved significantly by increasing the levels of DA and decreasing metabolic rate of DA in striatum while transplanting BDNF modified bone MSCs through cerebral lateral ventricle.</p>

The Localization and Expression of Tyrosine Phosphorylated Proteins During In Vitro Capacitation of Guinea Pig Sperm / 中国生物工程杂志

The aim of this study was to detect the localization and level of tyrosine phosphorylated proteins during in vitro capacitation of guinea pig sperm. Sperm from mature guinea pigs were incubated in modified TALP under 5% CO_2 in air at 37 ℃. The capacitation effect was assessed by chlortetracycline (CTC) staining. Western blotting and indirect immunofluorescence were used to analyze the level and localization of tyrosine phosphorylation. The results showed that guinea pig sperm underwent a time-dependent increase in protein tyrosine phosphorylation during the in vitro capacitation and the percentage of protein tyrosine phosphorylated sperm increased from 36% to 92% from the beginning of incubation to 7h incubation. Also, there was a shift in the site of phosphotyrosine-specific fluorescence from the head of sperm to both the head and the flagellum of sperm. Moreover, there were three proteins phosphorylated in this experiment. After 0 to 0.5h incubation, the protein of 40kDa was detected by anti-phosphotyrosine monoclonal antibody, and the intensity of this protein increased in the following incubation. Then, after 1h incubation, another protein of 80kDa was found and the level of this protein reached the highest point at 3h. Also, in 3h incubation, a protein of 45kDa was detected and the intensity of this protein increased in the following incubation.

Early ST resolution after successful primary PCI is related to a favorable outcome in ST elevated AMI patients / 中华心血管病杂志

<p><b>OBJECTIVE</b>To analyze the relationship between the early ST resolution magnitude and TIMI flow, MACE and the cardiac function in ST elevated AMI (STEMI) patients after successful primary PCI.</p><p><b>METHODS</b>A total of 120 consecutive patients with STEMI underwent primary PCI within 12 hours after the onset of chest pain were enrolled in this study, the ST segment resolution was calculated and the patients were divided into group A (n = 81, Sigma STE resolved > or = 50%) and group B (n = 39, Sigma STE resolved < 50%). TIMI flow after PCI, clinical events up to 30 days post PCI and cardiac function 30 days post PCI were assessed.</p><p><b>RESULTS</b>LVEF was higher in group A than that of group B (58.6% +/- 7.1% vs. 50.5% +/- 7.1%, P < 0.05). There are fewer patients with Killip III and IV in group A than in group B (1.2% vs. 12.8%, P < 0.05). The incidence of in-hospital MACE was also significantly less in group A than in group B (0 vs. 7.7%, P < 0.001). As expected, there were more patients with TIMI 3 flow (95.1% vs. 79.5%, P < 0.05) and fewer TIMI 2 (4.9% vs. 20.5%, P < 0.05) flow post PCI in group A than in group B and all 3 patients with MACE were group B patients with TIMI 2 flow.</p><p><b>CONCLUSION</b>Early ST resolution post PCI represents improved myocardial perfusion and function and is related to a favorable clinical outcome in STEMI patients.</p>