OBJECTIVE:To prepare Clopidogrel bisulfate tablets,and to optimize its formulation and technology. METHODS:The single factor test and compatibility test were used to optimize the fillers,disintegrating agents,adhesive,lubricants and prepa-ration technology;using sticking situation and disintegration time as indexes,the orthogonal test was used to optimize the amount of disintegrating agents [low substituted hydroxypropyl cellulose(L-HPC)],lubricants(hydrogenated vegetable oil and PEG6000), and the optimal technology was validated. The dissolution of prepared tablet and imported tablet(Plavix)in water,pH 2.0 hydro-chlorate buffer,pH 4.5 phosphate buffer(PBS)and pH 6.8 PBS were investigated,and influential factor test was conducted. RE-SULTS:Clopidogrel bisulfate tablets were prepared with dry granulating. The optimal formulation (1 000 tablets) was as follows as clopidogrel bisulfate 97.8 g,mannitol 84 g,amylum pregelatinisatum 36 g,L-HPC 8 g,hydrogenated vegetable oil 8 g, PEG6000 6 g;no tablet compressing sticking situation was found in prepared tablets and it owned medium disintegration time;ac-cumulative dissolution curves of prepared tablets in 4 kinds of medium were similar to those of Plavix;there were no significant dif-ference in results of influential factor test between prepared tablet and Plavix. CONCLUSIONS:Clopidogrel bisulfate tablets are prepared successfully,and the formulation is reasonable,practical,stable and controllable in quality.

Objective To investigate the effect of comprehensive intervention therapy of losing weight on leptin and blood lipid,blood glucose,insulin in adolescent girl students with simple obesity.Methods Simple obesity adolescent girl students were accepted the losing weight therapy composed of the aerobic exercise,reasonable diet,behavior modification and medical supervision for 10 months.Then the changes of blood leptin and correlated hormone were examined before test,during test and after test,respectively.Results The leptin and correlated hormone levels were significantly higher in obesity subjects than that in normal subjects,and the levels of serum leptin was positively correlated with BMI and insulin.The blood leptin and blood lipid,blood glucose,insulin were decreased obviously after experimental losing weight.Conclusion Comprehensive intervention therapy of losing weight can significantly lose weight,leptin and insulin,so it plays an important role in modifying the metabolism disorder

0.05).However,neither CpG-ODN nor hTNF-? failed in improving the expression rates of CD1a.Conclusions CpG-ODN,like hTNF-?,has remarkable im- munostimulatory effect on the differentiation and maturation of monocyte-derived DC from patients with chronic hepatitis B.

The tail suspension test (TST), forced swimming test (FST) and chronic unpredictable mild stress (CUMS) model were used to evaluate the anti-depressant effect of supercritical CO2 extract from Compound Chaigui Fang (FFCGF). A nuclear magnetic resonance (NMR)-based metabonomics combined with multivariate statistical analysis was performed to explore the mechanism of FFCGF. Rats were conducted by CUMS procedure for 28 days and drugs were administrated at the same time. The body weight, sucrose preference, crossings and rearings in open-field tests were evaluated and the urine was collected simultaneously. The metabonomic profiles of rats' urine were analyzed by NMR and potential biomarkers were searched by multivariate statistical analysis. The results showed that administration of FFCGF significantly decreasing the immobility time in FST and TST and improving rats' body weight, sucrose preference, crossings and rearings in CUMS, which were indication that the anti-depressant effect of FFCGF was abvious. Significant differences in the metabolic profile of the CUMS treated group and the control group were observed, which were consistent with the results of behavioral tests. Decreased levels of acetic acid, succinic acid, 2-oxidation glutaric acid and citric acid and increased glycine and pyruvic acid in urine were significantly affected by the CUMS procedure and the 6 biomarkers were reversed evidently after administration of FFCGF. These changes were suggestion that the anti-depressant mechanism of FFCGF was associated with energy metabolism, lipid metabolism and amino acid metabolism.
Animals ; Antidepressive Agents ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Behavior, Animal ; drug effects ; Body Weight ; Carbon Dioxide ; chemistry ; Depression ; drug therapy ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; therapeutic use ; Male ; Mice

Background Wearing contaclenincreasethe risk of infection of the cornea.Some studieshowed the gas-permeability of materialused foconstructing corneal contaclenione of the contributing factorrelated to corneal health.Objective Thistudy wato observe the in vitro adherence ability of differenbacterito rigid gas-permeable contaclense(RGP-CL) made with varioumaterials.MethodContaclensemade with hexafocon,enflufocon opolymethyl methacrylate (PMMA) were placed into Staphylococcuaureus,Staphylococcuepidermidis,oPseudomonaaeruginosbacterial suspension(0.5 MCF) fo24 hours.The strength of bacterial adherence watested and studied by the methyl thiazolyl tetrazolium (MTT) colorimetrimethod based on absorbance (value),and the vortex method waused to calculate the colony forming units.The bactericlump formation waexamined with scanning electron microscope (SEM).ResultMTcolorimetrimethod showed thathe adherence ability of Staphylococcuaureuto hexafocon (value) wasignificantly lowethan thato enflufocon and PMMA,respectively (q=7.379,8.207,P＜0.01),buno significandifference wafound in the adherence ability of Staphylococcuaureubetween enflufocon and PMM(q =0.828,P＞0.05).The adherence ability of Staphylococcuepidermidito XO and enflufocon walowethan thato PMM(q =14.000,12.800,P＜0.01),buno significandifference wafound between the adherence of Staphylococcuepidermidito hexafocon and enflufocon material (q =1.200,P＞0.05).There wano significandifference in the adherence ability of Pseudomonaaeruginosto all three material(F=2.155,P=0.138).The vortex method presented the colony forming unitof Staphylococcuaureuto hexafocon,enflufocon and PMMwith (37.9± 1.5)×106,(49.9±2.2)×106 and (67.4± 1.6)×106,respectively,with significandifference among them (F =206.240,P＜0.01),showing the lowesvalue in hexafocon,the highesvalue in PMMand middle value in enflufocon (q=11.650,28.640,16.990,P＜0.01),Moreover,colony forming uniof Staphylococcuepidermidito hexafocon,enflufocon and PMMwa(7.9 ± 1.3) × 106,(10.5 ± 1.5) × 106,(11.2 ±1.2) × 106,respectively.And thaof hexafocon walowethan one of the PMMmaterial (q =5.060,P＜0.05).No significandifference wafound between hexafocon and enflufocon nobetween hexafocon and PMM(q =3.290,1.770,P＞0.05).In addition,the resultthacorresponded to the vortex method were seen in the MTcolorimetriassay (F =0.232,P =0.799).SEM examination showed dispersed population of Staphylococcuaureuand Staphylococcuepidermidion the surfaceof hexafocon and enflufocon;while much more Staphylococcuaureuand Staphylococcuepidermidiadhered on the surface of PMMA,forming net-like appearance.Conversely,high numbeof Pseudomonaaeruginoswaseen on the surface of all three materials,withounoticeable differencein the bacterial shape and quantity on each of the material.ConclusionThe adherence ability of bacterito PMMistrongethan thaof hexafocon and enflufocon,and gas-permeable material of RGP-CL doenoimpacthe adherence ability of bacteria.

Heme oxygenase-1 (HO-1) is a cellular stress protein, and its expression plays an important regulatory role in a lot of physiological and pathological processes. Although the expression of HO-1 in most tissues of body is low, a number of clinical and pharmacological experiments have proved that many compounds can induce HO-1 expression. The increase of HO-1 expression is the result of regulating different signaling pathways and transcription factors, and this induction of HO-1 is suggested to be partially therapeutic efficacy of these compounds. This article summarizes some kinds of compounds in this field of research at home and abroad over the last 10 years, and provides a brief analysis of the mechanism.
Animals ; Antineoplastic Agents ; pharmacology ; Antioxidants ; pharmacology ; Coumarins ; pharmacology ; Drugs, Chinese Herbal ; pharmacology ; Enzyme Induction ; drug effects ; Gene Expression Regulation, Enzymologic ; Heme Oxygenase-1 ; genetics ; metabolism ; Humans ; Lovastatin ; pharmacology ; Nitric Oxide ; pharmacology ; Peptide Hormones ; pharmacology ; Probucol ; pharmacology ; Signal Transduction ; Transcription Factors ; metabolism

In recent years, root rot diseases of Chinese herbal medicine have been posing grave threat to the development of the traditional Chinese medicine industry. This article presents a review on the occurring situation of the root rot disease, including the occurrence of the disease, the diversity of the pathogens, the regional difference in dominant pathogens,and the complexity of symptoms and a survey of the progress in bio-control of the disease using antagonistic microorganisms. The paper also discusses the existing problems and future prospects in the research.
Animals ; Antibiosis ; Bacteria ; growth & development ; Fungi ; physiology ; Nematoda ; growth & development ; Pest Control, Biological ; methods ; Plant Diseases ; microbiology ; parasitology ; prevention & control ; Plant Roots ; microbiology ; parasitology ; Plants, Medicinal ; microbiology ; parasitology

ObjectiveTo observe protective effects of agmatine (AGM) on inflammatory response and spleen immune function in mice with trauma.Methods Forty-eight adult male C57BL/6 mice were randomly divided into three groups (n= 16 each), including control group, model group (bilateral femoral fracture and removal of 35% of the total blood volume), and AGM group (trauma/hemorrhage & AGM 200 mg/kg). Eight mice in each group were sacrificed at 3 hours and 24 hours, respectively, after modeling, and blood samples and tissue homogenate of spleen and liver were collected. The contents of tumor necrosis factor-α (TNF-α), interleukins (IL-6, IL-1β) in serum and liver tissue were determined with enzyme linked immunosorbent assay (ELISA). Serum aspartate transaminase (AST), alanine aminotransferase (ALT) and lactic dehydrogenase (LDH) were determined with automatic biochemistry analyzer. Spleen proliferation response stimulated with concanavalin A (ConA) was evaluated with methyl thiazolyl tetrazolium colourimetry (MTT).γ-interferon (IFN-γ) and IL-2 releases were determined with ELISA.Results Compared with control group, 3 hours after trauma/hemorrhage, the levels of serum TNF-α, IL-6, and IL-1β in model group were significantly elevated [TNF-α (ng/L): 145.38±31.50 vs. 23.06±11.14, IL-6 (ng/L): 496.94±50.76 vs. 47.13±17.47, IL-1β (ng/L): 321.31±43.02 vs. 29.25±16.24,allP< 0.01]. It was found that AGM treatment could alleviate the increase in serum pro-inflammatory mediators induced by trauma/hemorrhage, such as TNF-α (ng/L:111.56±25.47 vs. 145.38±31.50), IL-6 (ng/L: 412.56±44.33 vs. 496.94±50.76), IL-1β (ng/L: 273.38±45.25 vs. 321.31±43.02,P< 0.05 orP< 0.01). Twenty-four hours after trauma/hemorrhage, serum pro-inflammatory mediators were recovered to the levels in control group. There was no significant difference in TNF-α and IL-6 levels at 3 hours after trauma/hemorrhage among groups. Compared with control group, the expressions of liver TNF-α and IL-6 in model group were increased at 24 hours following trauma [TNF-α (ng/mg): 32.93±4.90 vs. 26.58±2.33, IL-6 (ng/mg): 11.20±1.66 vs. 8.38±0.89,bothP< 0.01]. However, AGM inhibited the level of TNF-α (ng/mg:28.92±3.16 vs. 32.93±4.90) and IL-6 (ng/mg: 9.03±1.28 vs. 11.20±1.66) in the liver as induced by trauma/hemorrhage (P< 0.05 andP< 0.01). At 24 hours after modeling, model group and AGM group had distinctly higher serum AST, ALT, LDH levels than those of control group [AST (U/L): 405.9±31.2, 245.7±22.1 vs. 128.2±15.9; ALT (U/L): 92.1±6.3, 51.6±5.0 vs. 30.1±3.2; LDH (U/L): 606.7±36.3, 478.7±25.3 vs. 384.0±16.6, allP< 0.01]. Nevertheless,the increase in serum AST, ALT and LDH was alleviated in AGM group (allP< 0.01). Meantime, trauma/hemorrhage produced a noticeable depression of proliferation of splenic cells and IFN-γ and IL-2 release stimulated with ConA compared with control group [proliferation rate: (40.97±4.13)% vs. (89.99±7.76)%, IFN-γ(ng/L): 91.6±12.3 vs. 353.2±21.5,IL-2 (ng/L): 53.4±6.4 vs. 91.0±12.2,allP< 0.01]. In contrast, AGM notably restored the capacity of proliferation response of splenic cells [proliferation rate: (74.86±5.75)% vs. (40.97±4.13)%, P< 0.01],enhanced the release of IFN-γ and IL-2 stimulated with ConA [IFN-γ (ng/L): 327.8±23.6 vs. 91.6±12.3, IL-2 (ng/L): 74.8±10.4 vs. 53.4±6.4, bothP< 0.01].Conclusion AGM can dramatically alleviate spleen immunosuppression, excessive inflammation and organ damage induced by trauma/hemorrhage.

Objective To improve the diagnosis and treatment quality of juxtaglomerular cell tumor of the kidney. Methods Three patients(2 females, 1 male) were diagnosed with juxtaglomerular cell tumor of kidney and underwent nephron-sparing surgery. Case 1 was female, 15 years old. She presented with hypertention of 245/135 mm Hg. The serum kalium was 2.5--3.0 mmol/L. Thelaboratory examination suggested that in decubitus and standing position, the plasma renin activity (PRA) was 2.2 and 3.5 μg · L-1 · h-1 , angiotensin Ⅱ (ATⅡ) was 181.2 and 481.4 ng/L; aldosterone(ALD) was 332.4 and 747.9 pmol/L, respectively. Dynamic enhanced CT scanning demonstrated a tumor with the diameter of 1.3 cm in right kidney. Case 2 was male, 39 years old. He presented with hypertention of 180/120 mm Hg. The serum kalium was 2. 7--3.0 mmol/L. In decubitus and standing position, PRAwas8.1 and 9.2 μg·L-1 · h-1, ATⅡ was 198.3 and 279.1 ng/L, ALD was 285.3 and 761.7 pmol/L, respectively. Dynamic enhanced CT scanning showed a tumor with the diameter of 1.2 cm in right kidney. Case 3 was female, 26 years old. She presented with hypertention of 210/120 mm Hg. The serum kalium was 4. 1 mmol/L. In decubitus and standing position, PRA was 0.1 and 0.3 μg · L-1·h-1 , ATⅡ 56.2 and 71.5 ng/L, ALD 321.3 and 421.1 pmol/L, respec tively. On dynamic enhanced CT scanning, a tumor with a diameter of 3.0era was located in left kidney. Results Partial nephrectomy was successfully performed in 3 patients, including 1 (case 2) retroperitoneal laparoscopic surgery. Pathologic examination revealed encapsulated tumors in all cases. Light microscopically, the tumor consisted of clusters of polygonal cells, and the cell had centrally located nuclei and slightly eosinophilic cytoplasm. Thick walled vessels were usually present. The tumors showed positive immunostaining for actin and CD34. Three patients were followed up for 23,4, 26 months respectively and all remained normotensive without any treatment. No recurrence or metastasis occurred. Conclusions Hypertention, increased PRA, secondary aldosteronism, hypokalemia are characteristics for juxtaglomerular cell tumor of the kidney. Dynamic enhanced CT scanning has high sensitivity. Partial nephrectomy or enucleation of tumor are both effective surgical treatment. Retroperitoneal laparoscopic surgery is safe and effective as well.

The present study aims to predict the action targets of antidepressant active ingredients of Xiaoyaosan to understand the "multi-components, multi-targets and multi-pathways" mechanism. Using network pharmacology, the reported antidepressant active ingredients in Xiaoyaosan (saikosaponin A, saikosaponin C, saikosaponin D, ferulic acid, Z-ligustilide, atractylenolide I, atractylenolide II, atractylenolide III, paeoniflorin, albiflorin, liquiritin, glycyrrhizic acid and pachymic acid), were used to predict the targets of main active ingredients of Xiaoyaosan according to reversed pharmacophore matching method. The prediction was made via screening of the antidepressive drug targets approved by FDA in the DrugBank database and annotating the information of targets with the aid of MAS 3.0 biological molecular function software. The Cytoscape software was used to construct the Xiaoyaosan ingredients-targets-pathways network. The network analysis indicates that the active ingredients in Xiaoyaosan involve 25 targets in the energy metabolism-immune-signal transmutation relevant biological processes. The antidepressant effect of Xiaoyaosan reflects the features of traditional Chinese medicine in multi-components, multi-targets and multi-pathways. This research provides a scientific basis for elucidation of the antidepressant pharmacological mechanism of Xiaoyaosan.
Antidepressive Agents ; pharmacology ; Benzoates ; Bridged-Ring Compounds ; Coumaric Acids ; Drug Evaluation, Preclinical ; Drugs, Chinese Herbal ; pharmacology ; Flavanones ; Glucosides ; Glycyrrhizic Acid ; Lactones ; Medicine, Chinese Traditional ; Monoterpenes ; Sesquiterpenes ; Software