Aged ; Biopsy ; Bone Marrow Examination ; Female ; Humans ; Lymph Nodes ; pathology ; Lymphoma, B-Cell ; diagnosis ; pathology ; Male ; Middle Aged ; Retrospective Studies ; Young Adult

Objective: To prepare ligustrazine pamoate (Lig-PAM) sustained-release nanosuspension (Lig-PAM-NSps) and determine its in vitro release characteristics. Methods: Lig-PAM was prepared by hydrophobic salt formation method and its physicochemical properties were characterized. Then, Lig-PAM-NSps was prepared by miniaturized medium grinding method. The prescription and preparation process of Lig-PAM-NSps were optimized by the single factor and orthogonal experiment with average particle size, polydispersity index (PDI) and stability coefficient (SI) as indicators. Lig-PAM-NSps was characterized, and its stability and in vitro release was also investigated. Results: The compound ratio of Lig-PAM prepared by Lig and PAM in the amount of 1:1 was (97.48 ± 0.04)%. Compared with Lig, the solubilities of Lig-PAM in water and simulated body fluids were decreased by 95.50% and 77.39%, respectively. Fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRD) showed that the Lig and PAM formed Lig-PAM. The optimum prescription size of Lig-PAM-NSps was (585 ± 5) nm, PDI was (0.328 ± 0.015) and SI was (0.928 ± 0.012). The scanning electron microscopy (SEM) showed that Lig-PAM-NSps was spherical with uniform size distribution, and the particle size was about 600 nm and its physical stability was good within 60 d. The results of in vitro release showed that Lig-PAM-NSps had obvious sustained-release effect compared with Lig solution within 48 h, and showed the first-order release characteristics [ln(1-Q) = 0.153 67 t + 80.458 14, r = 0.998 26]. Conclusion: The preparation progress of Lig-PAM-NSps is stable and can release Lig slowly in vitro.

Melittin exhibits high antibacterial potency against drug-resistant bacteria. However, the clinical utility of melittin is limited by its serious hemolytic activity. Thus, the need for developing novel melittin analogues with high antimicrobial activity and low hemolytic activity has grown. We designed, synthesized, and evaluated 20 novel melittin analogues with varying hydrophobic, polar or positively charged amino acids. The results showed that 8 compounds had antimicrobial activity (MIC: 1-4 μg·mL^-1) against gram-positive pathogens equal to or better than that of melittin, and 16 compounds had low hemolytic activity (HC₅₀ ≥ 11.9 μg·mL^-1). Compounds 13 (MIC: 2-4 μg·mL^-1) and 15 (MIC: 1-2 μg·mL^-1) showed equal or better antimicrobial activity against both susceptible and resistant strains of Staphylococcus aureus and Enterococcus faecium compared to melittin (MIC: 4 μg·mL^-1). Compound 13 (HC₅₀: 24.0 ± 4.3 μg·mL^-1) displayed noticeably decreased hemolytic activity compared to melittin (HC₅₀: 5.3 ± 0.4 μg·mL^-1). This work established a base for further study on the structure-activity relationships and structure-toxicity relationships of melittin.

Inosine 5′-monophosphate dehydrogenase (IMPDH) is a key enzyme catalyzing the rate-limiting step of de novo nucleotide synthesis in vivo. In recent years, it has become a therapeutic target for anti-virus, anti-bacterial, anti-cancer, anti-parasitic and other diseases. IMPDH inhibitors have been shown to inhibit viral prolife-ration in host cells by depleting guanosine 5′-monophosphate (GMP), the raw material required for viral replication in host cells, with broad-spectrum antiviral properties. In order to find novel anti-coronavirus drugs, this study screened 22 potential IMPDH inhibitors from 70 000 natural small molecule libraries based on IMPDH protein structure using molecular docking and ROC calculation for virtual screening. With ribavirin as the positive control drug, Huh7 cell and H460 cell models were used to verify the anti-coronavirus HCoV-229E and HCoV-OC43 activities of 22 selected target compounds. Among them, compounds 11, 12, 15 and 16 showed inhibitory activity against coronavirus HCoV-229E. The compounds 4, 12, 13 and 15 showed inhibitory activities against coronavirus HCoV-OC43. 12 and 15 showed significant inhibitory activity against both two coronaviruses, and their efficacy was similar to ribavirin at the same dose, which can be further studied as a lead compound for IMPDH inhibitors.

Octapeptin has strong antibacterial activity against Gram-negative bacteria such as Escherichia coli, Klebsiella pneumoniae and Acinetobacter baumannii, while it also has activity against some Gram-positive bacteria. This study used natural octapeptin A3 and B3 as lead compounds for structural modification. Twenty-one peptide derivatives (including A3 and B3) containing eight amino acid residues were prepared by solid-phase synthesis, and evaluated for antibacterial activity and renal cytotoxicity. Among them, three compounds 6, 7 and 17 exhibited broad-spectrum antibacterial activity and significantly enhanced the activity for Gram-positive bacteria while maintaining the activity of Gram-negative bacteria. Several compounds improved the activity for Pseudomonas aeruginosa. Compound 7 was active against all test strains and had relatively low renal cytotoxicity. The results provide a basis for the further development of novel polypeptide antibiotics.

Fluorescent carbon dots(CDs)were synthesized via a solvothermal method with citric acid and urea as raw materials,and ethylene glycol as reaction solvent.The micromorphology,crystal structure,elemental composition,surface functional group,and optical property of as-synthesized CDs were characterized.The excitation-dependent fluorescence property of CDs was investigated,and the effects of synthesis conditions including reaction temperature,reaction time and raw materials on excitation and emission wavelengths of the CDs were also discussed.Then,a series of CDs-based fluorescent composites were prepared by combining CDs with starch,nano-silica,montmorillonite,kaoline,kieselguhr and magnesium oxide,respectively.Finally,the CDs-starch composites were used for latent fingerprint development on smooth substrates,and the qualitative as well as quantitative evaluation of the contrast,sensitivity and selectivity in fingerprint development were also made.Enhanced development of latent fingerprints was thus achieved by the aid of the excitation-dependent fluorescence property of CDs-starch composite combined with the optical filtering technique,which could decrease the background noise interference to a great extent.Experimental results showed that,the contrast between fingerprint(developing signal)and substrate(background noise)was obvious,exhibiting a strong contrast;the minutiae of papillary ridges were clear,indicating a high sensitivity;the adsorption between CDs-starch composites and fingerprint residues was specific,showing a good selectivity.

OBJECTIVETo investigate the best combination of monoclonal antibodies for the diagnosis of hepatobiliary intraepithelial neoplasia and/or cancer.

METHODSCK7, CK20, Villin, CEA, P53 and Ki-67 antigens were detected in the tissues of high-level hepatobiliary intraepithelial neoplasia and cancer by immunohistochemistry and the results were analyzed statistically.

RESULTSVillin was 100% positive in hepatobiliary intraepithelial neoplasia and/or cancer, while 100% negative in the adjacent normal bile duct epithelium. The expression rate of CEA was significantly lower in high-level hepatobiliary intraepithelial neoplasia tissues than in the cancer tissues (P<0.05). Ki-67 indexes were significantly lower in most of the high-level hepatobiliary intraepithelial neoplasia than in the cancer tissue (P<0.01). P53 indexes were also lower in high-level hepatobiliary intraepithelial neoplasia (P<0.01).

CONCLUSIONDetection of multiple antigens (CEA, Villin, Ki-67 and P53) provides specific clues to the diagnosis of high-grade hepatobiliary intraepithelial neoplasia and/or cancer.

Adult ; Aged ; Antibodies, Monoclonal ; Antigens, Neoplasm ; analysis ; Bile Duct Neoplasms ; diagnosis ; pathology ; Bile Ducts, Intrahepatic ; pathology ; Carcinoma in Situ ; diagnosis ; pathology ; Epithelium ; pathology ; Female ; Humans ; Immunohistochemistry ; Male ; Middle Aged

BACKGROUNDThe effect of selective and non-selective cyclooxygenase (COX) inhibitors on tendon healing was variable. The purpose of the study was to evaluate the influence of non-selective COX inhibitor, ibuprofen and flurbiprofen axetil and selective COX-2 inhibitor, celecoxib on the tendon healing process in a rabbit model.

METHODSNinety-six New Zealand rabbits were used as rotator cuff repair models. After surgery, they were divided randomly into four groups: ibuprofen (10 mg·kg-1·d-1), celecoxib (8 mg·kg-1·d-1), flurbiprofen axetil (2 mg·kg-1·d-1), and control group (blank group). All drugs were provided for 7 days. Rabbits in each group were sacrificed at 3, 6, and 12 weeks after tendon repair. Tendon biomechanical load failure tests were performed. The percentage of type I collagen on the bone tendon insertion was calculated by Picric acid Sirius red staining and image analysis. All data were compared among the four groups at the same time point. All data in each group were also compared across the different time points. Qualitative histological evaluation of the bone tendon insertion was also performed among groups.

RESULTSThe load to failure increased significantly with time in each group. There were significantly lower failure loads in the celecoxib group than in the control group at 3 weeks (0.533 vs. 0.700, P = 0.002), 6 weeks (0.607 vs. 0.763, P = 0.01), and 12 weeks (0.660 vs. 0.803, P = 0.002), and significantly lower percentage of type I collagen at 3 weeks (11.5% vs. 27.6%, P = 0.001), 6 weeks (40.5% vs. 66.3%, P = 0.005), and 12 weeks (59.5% vs. 86.3%, P = 0.001). Flurbiprofen axetil showed significant differences at 3 weeks (failure load: 0.600 vs. 0.700, P = 0.024; percentage of type I collagen: 15.6% vs. 27.6%, P = 0.001), but no significant differences at 6 and 12 weeks comparing with control group, whereas the ibuprofen groups did not show any significant difference at each time point.

CONCLUSIONSNonsteroidal anti-inflammatory drugs can delay tendon healing in the early stage after rotator cuff repair. Compared with nonselective COX inhibitors, selective COX-2 inhibitors significantly impact tendon healing.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Biomechanical Phenomena ; Celecoxib ; pharmacology ; Cyclooxygenase 2 Inhibitors ; pharmacology ; Flurbiprofen ; pharmacology ; Ibuprofen ; pharmacology ; Male ; Rabbits ; Rotator Cuff ; drug effects ; pathology ; Tendon Injuries ; drug therapy ; Wound Healing ; drug effects

OBJECTIVETo understand the epidemiological characteristics of essential hypertension in the northern and western areas of China.

METHODSA community-based sampling survey.

RESULTSRates of awareness, treatment and control were 78.6%, 59.7% and 5.9%, respectively. About half of the diagnosed and treated patients took antihypertensive medicine irregularly before the survey was carried out.

CONCLUSIONIt is necessary to carry out education, prevention and control on hypertension and to establish a series of standards for the management and treatment on cases of hypertension.

Adult ; Age Factors ; Aged ; Blood Pressure ; China ; epidemiology ; Drug Administration Schedule ; Female ; Health Surveys ; Humans ; Hypertension ; epidemiology ; prevention & control ; therapy ; Male ; Middle Aged ; Risk Factors ; Social Class

OBJECTIVETo evaluate the value of spiral computed tomography in the preoperative assessment of the degree of tumor infiltration in mesorectum and circumferential resection margin status of rectal cancer compared with large tissue slice technique.

METHODSFifty-seven patients with rectal cancer diagnosed by fiber colonoscopy and pathology from March 2007 to December 2007 underwent preoperative 64-layers spiral CT examination. The degree of tumor infiltration in mesorectum and circumferential resection margin status were evaluated. Large tissue slice technique was applied in the pathologic study after the total mesorectal excision of the rectum to determine the degree of tumor infiltration in mesorectum and the circumferential resection margin status. The spiral CT findings were compared with pathologic results. The accuracy, sensitivity, specificity, positive predictive value (PPV) and negative predictive value (NPV) of the CT results were assessed respectively.

RESULTSThe overall spiral CT accuracy was 93.0% (53/57) for the degree of tumor infiltration in mesorectum, and it was 94.7%, 94.7% and 96.5% for degree I, II, III infiltration, respectively. Fifty-three cases (93.0%) were accurately predicated with the circumferential resection margin status. The sensitivity, specificity, PPV and NPV of spiral CT measurement was 80.0%, 97.6%, 92.3% and 93.2%, respectively, and was consistent well with the histopathological diagnosis.

CONCLUSIONSSpiral CT provides accurate preoperative assessment for the degree of tumor infiltration in mesorectum and circumferential resection margin status of rectal cancer.

Adult ; Aged ; Aged, 80 and over ; Female ; Humans ; Male ; Mesentery ; diagnostic imaging ; pathology ; Middle Aged ; Neoplasm Invasiveness ; diagnostic imaging ; Neoplasm Staging ; Predictive Value of Tests ; Rectal Neoplasms ; diagnostic imaging ; pathology ; Rectum ; diagnostic imaging ; pathology ; Sensitivity and Specificity ; Tomography, Spiral Computed