To assess and grade facial nerve dysfunction according to the extent of facial paralysis in the clinical course of acupuncture treatment for Bell's palsy, and to observe the interrelationship between the grade, the efficacy and the period of treatment, as well as the effect on prognosis.

In recent years, artificial intelligence (AI) technology has advanced rapidly and has been widely applied in various fields such as medicine and pharmacy, accelerating the drug development process. Focusing on the application of AI in the discovery and optimization of lead compounds, this review provides a detailed introduction to AI-assisted virtual screening and molecular generation methods for discovering lead compounds, while particularly highlighting the cases of AI-drived drugs into clinical trials. Additionally, we briefly outline the application of AI basic algorithm models in quantitative structure-activity relationship (QSAR) and drug repurposing, offering insights for AI-based drug discovery.

[Objective]To explore an individualized treatment measure enjoying more practical,effective and safe characteristics through evaluating the efficacy and safety of combined medications of low-dose urokinase,low-molecular weight heparin nadroparin calcium and ozagrel sodium in treating patients with acute cerebral infarction.[Methods]One-hunderd patients with acute cerebral infarction patients were recruited in this trail,and grouped according to different treatment times:Group A (n=40,from January 2005 to February 2008,being selected into the group in accordance with standards of China Guideline for Cerebrovascular Disease Prevention and Treatment) and Group B (n=60,from March 2008 to June 2011,being selected into the group in accordance with indications for onset time within 24 h and allowing age more than 75 years).Standard thrombolytic therapy (high dose urokinase) was performed on Group A and combined medications of low-dose urokinase,low-molecular weight heparin nadroparin calcium and ozagrel sodium (triple antithrombotic therapy) were performed on group B.National Institute of Health Neurological Deficit Scale (NIHSS) and Evaluation Standard of Clinical Efficacy were used to evaluate the recovery of neurological function before treatment and 24 h,7 and 14 d after treatment.[Results] NIHSS scores after therapy rapidly decreased in both groups as compared with those before treatment (P＜0.05).The NIHSS scores of Group B at 24 h,and 7 and 14 d after treatment were significantly decreased as compared with those of Group A (P＜0.05).The efficacy rate of Group B was significantly higher than that of Group A (P＜0.05).Intraparenchymal hemorrhage rate was 10.0％ (4/40) in Group A and 3.3％ (2/60) in Group B.[Conclusion] Triple antithrombotic therapy is more effective and relatively safer than standard thrombolytic therapy in treatment of patients with acute cerebral infarction.

OBJECTIVETo evaluate the effect of irbesartan on the proliferation, apoptosis, and VEGF mRNA expression of human umbilical vein cell line EA.hy926 in vitro.

METHODSThe human umbilical vein cell line EA.hyY926 were treated with various concentrations of irbesartan for 24 h. The cell proliferation after the treatment was detected by CCK8 assay, flow cytometry and FITC Annexin V/PI kit were used to detect changes in the cell apoptosis. RT-PCR was used to evaluate the expression of VEGF mRNA.

RESULTSThere were no changes in cell shape with various concentration of irbesartan. CCK-8 assay showed a greater rate of the cell proliferation in irbesartan group than that in control group with a dose-independent manner after 24 h treatment. After incubation with irbesartan, cell proliferation rate was significant (P < 0.05). FCM analysis showed no significantly changes in the cell apoptosis. Irbesartan increased the proliferation of EA.hy926 cells. At concentration of 1 x 10(-4), 1 x 10(-5), 1 x 10(-6) mol/L, VEGF mRNA expression enhanced either (P < 0.05).

CONCLUSIONIrbesartan could promote the proliferation and up-regulated VEGFmRNA expression in EA.hy926 cell line. This result suggested that in addition to antihypertensive effect, angiotensin receptor antagonist might be a novel therapeutic approach to chronic ischemic heart disease as heart failure.

Apoptosis ; drug effects ; Biphenyl Compounds ; pharmacology ; Cell Line ; Cell Proliferation ; drug effects ; Humans ; RNA, Messenger ; genetics ; Tetrazoles ; pharmacology ; Umbilical Veins ; cytology ; metabolism ; Vascular Endothelial Growth Factor A ; metabolism

In order to develop potent antidiabetic agents that have inhibitory effect to a-glucosidase, twelve β-acetamido ketone derivatives such as N-{[(substituted-4-oxo-thiochroman-3-yl)phenyl]-methyl}acetamide are designed and synthesized through one-pot Dakin-West reaction. Their chemical structures are confirmed by 1H NMR, 13C NMR, IR and HR-MS. In vitro α-glucosidase inhibition assays of compounds 4a-41 were carried out using glucose oxidase method. The result indicated that most of them possess inhibitory activity in vitro. Compound 4k showed the most potent inhibitory activity with 87.3% inhibition of α-glucosidase at the concentration of 5.39 mmol x L(-1). The structure-activity relationship of these β-acetamido ketone derivatives was discussed preliminarily. Moreover, the molecular docking method was used to study the interaction mode of compound 4k and α-glucosidase. Our results will be helpful for designing of α-glucosidase inhibitors in the future.
Acetamides ; Glycoside Hydrolase Inhibitors ; chemical synthesis ; pharmacology ; Hypoglycemic Agents ; chemical synthesis ; pharmacology ; Molecular Docking Simulation ; Structure-Activity Relationship ; alpha-Glucosidases ; metabolism

OBJECTIVETo understand the regularity of Rh blood typing of valunteary blood donors in Chinese Nanyang city, and to estabbish a Rh DC/c/E/e antigen negative donor base so as to provide the help for clinical emergent blood transfusion to patients and ensure the safety of blood transfusion.

METHODSThe Rh D blood group of blood samples from 81462 voluntary blood donors in Chinese Nanyang city in 2014 was identified by serologic method; after first screening and confirmation, the RhE/e/C/c typing of Rh D negative samples was performed; the detailed infornation of donors was registered seriously by using unified creteria; the data base and base in kind of RhE/e/C/c types of valuntary donors were established by means of compater-mamayement system.

RESULTS300 cases (0.37%) were RhD negative blood donors, and the Rh antigen was Ccdee and ccdee in 83%.

CONCLUSIONThe proportion of RhD negative donors accounts for 4% of Chinese Nanyang peoples, the RhE/e/C/c types of RhD negative donors are ccdee (50.67%)>Ccdee (33.00%)>ccdEe(5.67%)>CCdee (5.33%)>CcdEe(5.33%). The establisment of RhE/e/C/c subbase can show importent significance for clinical blood transfusion.

BACKGROUNDTreatment for malignant glioma generally consists of cytoreductive surgery followed by radiotherapy and chemotherapy. In this study, we intended to investigate the effects of 2-propylpentanoic acid (VPA), a histone deacetylase inhibitor, on chemosensitivity and radiosensitivity in human glioma cell lines.

METHODSHuman glioma cell lines, T98-G, and SF295, were treated with temozolomide (TMZ) or irradiation (IR), with or without VPA (1.0 mmol/L). Then, cytotoxicity and clonogenic survival assay was performed. Cell cycle stage, apoptosis, and autophagy were also detected using flow cytometry and dansyl monocadaverin (MDC) incorporation assay. One-way analysis of variance (ANOVA) and t-test were used to analyze the differences among variant groups.

RESULTSMild cytotoxicity of VPA was revealed in both cell lines, T98-G and SF295, with the 50% inhibiting concentration (IC50) value of (3.85 ± 0.58) mmol/L and (2.15 ± 0.38) mmol/L, respectively; while the IC50 value of TMZ was (0.20 ± 0.09) mmol/L for T98-G and (0.08 ± 0.02) mmol/L for SF295. Moreover, if combined with VPA (1.0 mmol/L) for 96 hours, the sensitivity of glioma cells to TMZ was significant increased (P < 0.05). The surviving fractions at 2 Gy (SF2) of T98-G and SF295 cells exposed to IR alone were 0.52 and 0.58. However, when VPA was combined with IR, the SF2 of T98-G and SF295 dropped to 0.39 (P = 0.047) and 0.49 (P = 0.049), respectively. Treatment with VPA plus TMZ or IR also resulted in a significant decrease in the proportion of cells in the G2 phase and increased apoptotic rates as well as autophagy in T98-G and SF295 cell lines (P < 0.01).

CONCLUSIONVPA may enhance the activities of TMZ and IR on glioma cells possibly through cell cycle block and promote autophagy, and thus could be a potential sensitizer of glioma treatment.

Apoptosis ; drug effects ; radiation effects ; Blotting, Western ; Cell Line, Tumor ; Cell Survival ; drug effects ; radiation effects ; Dacarbazine ; analogs & derivatives ; pharmacology ; Flow Cytometry ; Glioma ; metabolism ; Histone Deacetylase Inhibitors ; pharmacology ; Humans ; Valproic Acid ; pharmacology

OBJECTIVETo analyze the degrees on the epidemic foci of Angiostronglus cantonensis and to explore the measurement methods.

METHODSSnails (Pila gigas) were collected from the spots of Wenzhou, Cangnan, Yongjia, Yueqing in Zhejiang province and Minhou, Changle, Ningde in Fujian province. The snails were examined microscopically in order to calculate their infection rates and the average worm number in the positive snails, then taking the product of multiplication of both values as infestation index.

RESULTSThe infection rates of the epidemic foci were 10.59% (9/85), 60.74% (181/298), 34.96% (79/226), 32.90% (76/231), 57.50% (184/320), 40.00% (82/205), 17.65% (12/68) and the rates of infectivity were 6.57, 183.54, 121.73, 93.45, 276.36, 76.08, 12.65, respectively.

CONCLUSIONThe epidemic foci were divided into five ranks (super, high, mid-range, low and non-epidemic foci) according to the value of infestation index which ranked from > 75, 30-75, 5-29, < 5 to 0.

Angiostrongylus ; pathogenicity ; Animals ; China ; Disease Outbreaks ; Snails ; parasitology ; Strongylida Infections ; epidemiology

OBJECTIVETo characterize the effect of omeprazole on the spectrum of gene expression in the cultured human umbilical vein endothelial cell (HUVEC) line (EA.hy926), and explore the underlying molecular mechanism.

METHODSAffymetrix U133 plus2.0 oligonucleotide microarray was used to detect the alteration in the gene expression profiles induced by 1×10(-5) mol/L omeprazole in HUVECs. Real-time PCR was employed to verify the results of selected differentially expressed genes, and Western blotting was performed to test the expression levels of the related proteins.

RESULTSA total of 282 genes were found to show at least 1.5-fold changes in EA.hy926 cells after treatment with omeprazole for 48 h, including 236 up-regulated and 46 down-regulated ones. These genes were involved in the regulation of transcription, inflammatory response, immune response, cell adherence, anti-apoptosis, and signal transduction.

CONCLUSIONOmeprazole modulates the function of endothelial cells by regulating the gene expression profiles of multiple pathways.

Cell Line ; Computational Biology ; Human Umbilical Vein Endothelial Cells ; drug effects ; Humans ; Oligonucleotide Array Sequence Analysis ; Omeprazole ; pharmacology ; Transcriptome ; drug effects

This study was purposed to characterize the effect of carboxylic acid metabolite (SR26334) of clopidogrel bisulfate deprived of antiplatelet efficacy on the spectrum of gene expression in the cultured human umbilical vein endothelial cell (HUVEC) line (EA.hy926), and to explore the potential molecule mechanism of SR26334 impact on HUVEC. By using a Affymetrix HU133 plus 2.0 oligonucleotide microarray, the alteration of gene expression spectrum induced by SR26334 in HUVEC was detected, the real-time PCR was used to confirm the results of selected differentially expressing genes. The results indicated that total 235 including 176 up-regulated and 59 down-regulated genes were obtained with change more than 1.5-fold after SR26334 (10 µmol/L) acted on HUVEC for 48 h. SR26334 affected the expression levels of genes involved regulation of transcription, transcription, positive regulation of transcription from RNA polymerase II promoter, cell cycle, cell division, protein amino acid dephosphorylation in HUVEC. It is concluded that carboxylic acid metabolite SR26334 of clopidogrel bisulfate modulates function of endothelial cells through different pathway at gene level.
Cell Line ; Human Umbilical Vein Endothelial Cells ; cytology ; drug effects ; Humans ; Ticlopidine ; analogs & derivatives ; pharmacology ; Transcriptome ; drug effects