Pololike kinase 1(Plk1)contain an Nterminal Ser/Thr kinase catalytic domain and a Cterminal region that contains two poloboxes.As a key regulator of multiple steps during cell cycle across eukaryotic species,many proteins interact with Plk1.Plk1 is highly expressed in malignant cells and serves as a negative prognostic marker in specific human cancer types.Plk1 is a potential target for cancer therapy.Some novel smallmolecule inhibitors of pololike kinase 1 provide novel opportunities for cancerdrug discovery,such as BI 2536,ON01910.

Acorus ; chemistry ; classification ; Alkaloids ; isolation & purification ; pharmacology ; Animals ; Anticonvulsants ; isolation & purification ; pharmacology ; Antineoplastic Agents, Phytogenic ; isolation & purification ; pharmacology ; Flavonoids ; isolation & purification ; pharmacology ; Gastrointestinal Agents ; isolation & purification ; pharmacology ; Humans ; Plants, Medicinal ; chemistry ; Sesquiterpenes ; isolation & purification ; pharmacology

OBJECTIVETo study the chemical constituents of Abelmoschus manihot.

METHODChromatographic methods were used to isolate compounds from A. manihot, and spectroscopic methods were used to identify the structures.

RESULTThirteen compounds, myricetin (1), cannabiscitrin (2), myricetin-3-O-beta-D-glucopyranoside (3), glycerolmonopalmitate (4), 2, 4-dihydroxy benzoic acid (5), guanosine (6), adenosine (7), maleic acid (8), heptatriacontanoic acid (9), 1-triacontanol (10) , tetracosane (11), beta-sitosterol (12), beta-sitosterol-3-O-beta-D-glucoside (13) were obtained.

CONCLUSION2-11 were obtained from the genus for the first time.

Abelmoschus ; chemistry ; Alkanes ; chemistry ; isolation & purification ; Fatty Alcohols ; chemistry ; isolation & purification ; Flavanones ; chemistry ; isolation & purification ; Flowers ; chemistry ; Glucosides ; chemistry ; isolation & purification ; Maleates ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry

Objective To investigate the clinical features of Guillain-Barre syndrome (GBS) and clarify the long-term prognosis of acute inflammatory demyelinating polyneuropathy (AIDP) and acute motor axonal neuropathy (AMAN). Methods We conducted an analysis of the clinical data of 50 patients with GBS treated in our hospital between 2003 and 2007. According to the eleetrophysiological criteria, the eases were classified into AIDP (n=24) and AMAN eases (n=22), with 4 eases of unknown classification. The patients unable to walk upon discharge were followed up for more than 6 months, and the clinical features and prognosis of the two groups were compared. Results The age, gender, cranial nerve involvement, Hughes grade at the initial neurological examination and at the time of symptom peak did not differ significantly between the patients with AIDP and AMAN (P>0.05), and most of the AMAN patients had a good recovery. The number of patients capable of walking at one month after the onset was comparable between the two groups (P>0.05). In AMAN group, the percentages of patients with slow recovery and those having rapid recovery were significantly higher than those in AIDP group (P<0.05). Conclusion The clinical recovery of AMAN patients can be either rapid or prolonged, and rigorous immunotherapy should be administered to achieve early recovery and ensure more favorable outcomes of the patients.

To observe the therapeutic effects of lamivudine treatment in patients with early- to mid-stage hepatitis B virus-related acute-on-chronic liver failure (HBV-ACLF). Clinical data of 73 hospitalized patients with HBV-ACLF were retrospectively analyzed. Prothrombin time (PT, active coagulation), HBV DNA, and model for end-stage liver disease (MELD) score data from treatment weeks 4, 8, 24, and 48 were collected and analyzed using the statistical t-test. During the treatment duration, the complete virologic response rates were 57.5% (42/73) at 4 weeks, 71.0% (44/62) at 8 weeks, 83.1% (49/59) at 24 weeks, and 86.5% (45/52) at 48 weeks. The partial virologic response rates were 30.1% (22/73) at 4 weeks, 25.8% (16/62) at 8 weeks, 17.0% (10/59) at 24 weeks, and 13.5% (7/52) at 48 weeks. At week 48, the survival rate was 71.2% (52/73) and the probability of survival was higher in the complete virological response rate (VRR) group than in the partial VRR group [45/73 (61.6%) vs. 7/73 (30.1%), respectively; P = 0.000]. In addition, there were significant improvements in the serum normalization rate of HBV DNA, alanine aminotransferase, aspartate aminotransferase, albumin, total bilirubin, PT and MELD score in surviving patients compared to baseline (P less than 0.05) and in the complete VRR group compared to the partial VRR group (P less than 0.05). Antiviral therapy using lamivudine may be an effective therapeutic option for patients with HBV-ACLF.
Adolescent ; Adult ; Aged ; Antiviral Agents ; therapeutic use ; Female ; Hepatitis B, Chronic ; complications ; drug therapy ; Humans ; Lamivudine ; therapeutic use ; Liver Failure, Acute ; drug therapy ; etiology ; Male ; Middle Aged ; Retrospective Studies ; Survival Rate ; Treatment Outcome ; Young Adult

OBJECTIVETo study the apoptosis inducing effects of bufalin on various human osteosarcoma cells and the concerning molecular mechanisms.

METHODMTT assay was used to detect the growth inhibition rates of osteosarcoma cells U-20S, U-20S/MTX300, SaOS-2, IOR/OS9 treated with bufalin in different concentrations and times. The apoptosis of cells was observed flow cytometry 48 h following bufalin treatment. The proteomic techniques were used to separate and compare the treated and control groups 48 h after bufalin-incubation. Then, the proteomic results were validated by western blot.

RESULTBufalin inhibited the growth of human osteosarcoma cells U20S, U20S/MTX300 (methotrexate resistant cells), SAOS2, IOR/OS9 in a dose- and time-dependent manner. The 72 h IC50 were (37.43 +/- 4.1), (32.24 +/- 5.3) nmol x L(-1) in U20S,U20S/MTX300 cells,respectivly. Flow cytometry showed that the apoptosis cells were increased following bufalin treatment. The protein expression profile showed 24 differentiated expression proteins. Among these proteins, the level of an anti-apoptotic protein, heat shock protein 27 (Hsp27) decreased significantly and the result was then validated by western blot. Ectopic expression of Hsp27 could reduce the bufalin-induced apoptosis remarkably in U20S and U20S/MTX300 cells.

CONCLUSIONBufalin could inhibit the cell growth and induce apoptosis on human osteosarcoma cells. The effect of bufalin may be related to the joint intervention with multiple protein targets. Among them, downregulation of Hsp27 plays a critical role in the bufalin-induced apoptosis in human osteosarcoma cells.

Antineoplastic Agents ; pharmacology ; Apoptosis ; drug effects ; Bufanolides ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Gene Expression Regulation, Neoplastic ; drug effects ; Humans ; Osteosarcoma ; pathology ; Proteomics

OBJECTIVETo elucidate the relationship between collagen degradation and cervical ripening by detecting dynamic expressions of matrix metalloproteinases 2 (MMP-2) and 8 (MMP-8) in rat cervix.

METHODSPF rats were divided into 5 groups (n=6), namely non-pregnancy estrus interval group, gestational days 10, 16, and 19 groups, and immediately postpartum group. The wet weight of the cervix was measured and HE staining was used to display the general structure of the cervix. VG staining was applied to visualize the collagen fibers and muscular fibers. Immunohistochemistry was performed to observe the expressions of MMP-2 and MMP-8 in the cervix.

RESULTSHE staining showed that the rat uterine cervix consisted mainly of fibroblasts and fibrous connective tissues. A small quantity of neutrophils could be seen in the cervix stroma of the rats immediately after immediately parturition, but not at the other time points. The wet weight of the antepartum cervix had increased, and a more obvious increase was seen in the wet weight of the cervix immediately after parturition. The collagen fibers of the cervix consisted of collagen fibers and smooth muscle fibers, and their proportions showed no significant variation at the time points around the parturition. Immediately after parturition, the collagen fibers and muscular fibers in the cervix became loosened as compared with that before parturition. MMP-2 expression was found in the cervical stroma but not in the squamous epithelium in nonpregnancy, term pregnancy, and immediately after parturition; the smooth muscle cells, vascular wall, and stromal fibroblasts showed positive expression of MMP-2. Enhanced intensity of MMP-2 staining was seen in term pregnancy and postpartum group in comparison with that in the other groups. MMP-8 expression was observed in the cervix of rats immediately after parturition, with scattered neutrophils positive for MMP-8 spotted in the stroma of the ripened cervix. MMP-8 expression was not detected in the other groups.

CONCLUSIONRipened cervical fibrous tissue becomes loose and broken, and cervical ripening is accompanied by infiltration of neutrophils from exogenous vessels. These changes are particularly evident after parturition. MMP-2 and MMP-8 cooperate to degrade the cervical fibers, leading to cervical softening and expansion.

Animals ; Cervical Ripening ; metabolism ; Cervix Uteri ; enzymology ; Female ; Matrix Metalloproteinase 2 ; metabolism ; Matrix Metalloproteinase 8 ; metabolism ; Pregnancy ; Rats ; Rats, Sprague-Dawley

Adult ; Female ; Fractures, Bone ; complications ; Hernia, Diaphragmatic, Traumatic ; diagnosis ; etiology ; Humans ; Pelvic Bones ; injuries

OBJECTIVETo investigate the drug resistance of flavobacterium and its ability to produce BLA (beta-lactamases) and ESBLs (Extended-spectrum beta-lactamases).

METHODSThe production of BLA and ESBLs from 6 clinical isolated flavobacterium strains was determined by nitrocefin disc test and double-disc synergy method, respectively. The antibiotic susceptibilities of the strains were determined by Kirby-Bauer disc diffusion test and the agar dilution method and the MIC was assessed.

RESULTSAll the six flavobacteria were BLA-producing strains and more than 80% of them were ESBLs-producing, and they were highly resistant to beta-lactamase antibiotics (MIC 32 - 256 mg/L), but susceptible to fluoroquinolones and cephalosporin with beta-lactamase inhibitors (MIC 0.125 - 8 mg/L).

CONCLUSIONMost of the flavobacteria in nosocomial infections were beta-lactamase-producing and were highly resistant to beta-lactamase antibiotics. Fluoroquinolones and beta-lactamase antibiotics with lactamase inhibitors should be the first choice for the management of infection caused by flavobacterium.

Anti-Bacterial Agents ; pharmacology ; Drug Resistance, Bacterial ; drug effects ; Flavobacterium ; drug effects ; enzymology ; Humans ; Membrane Proteins ; analysis ; metabolism ; Microbial Sensitivity Tests ; Ribosomal Proteins ; analysis ; metabolism

Objective To analyze the general characteristics of voluntary blood donors, and to provide the basis for establishing effective recruitment mechanism. Methods The information of all whole blood donors (including mobile blood collection cars on the streets , blood donation houses and team blood donors) from 2006 to 2015 was obtained from the Zhejiang blood management information system. The sex, age, occupation, weight, and the amount of blood donation at a time of blood donors were descriptively analyzed. Results There were 5299700 frequencies of donating blood in Zhejiang Province from 2006 to 2015. The annual frequency was on the rise, with an average annual growth rate of 2.99％. There were 3098500 frequencies of male and 2201300 of female with the ratio of 1.4 :1. The frequency of female has declined since 2010. The majority of voluntary blood donors ranged from 18 to 45 years old, and the percentage was 91.44％ . The ratios of staff, students and workers were 14.61％, 12.27％, 10.09％, respectively. The annual frequency of staff was on the rise, with an average annual growth rate of 7.71％. The frequency of workers was on the decline, and the frequency of students fluctuated over the years. The ratio of blood donation 400 mL at a time was 41.23％. For 400 mL blood donation at a time, the ratio of male donors (48.86％) was significantly higher than the female donors (30.50％, P<0.001) . In addition, the ratio of blood donation 400 mL at a time was proportional to age and body weight (P<0.001) . Conclusion In Zhejiang Province, the frequency of blood donation has increased year by year. Staff, students and workers with 18 to 45 years old are the main force of blood donation. The frequency of female blood donation has a tendency of dropping, and the ratio of blood donation 400 mL at a time is relatively low. It's necessary to strengthen the propaganda of blood donation.