Using brartemicin as the leading compound, fifteen novel trehalose derivatives were designed and synthesized, and the structures were determined by 11H NMR, MS and element analysis. Inhibitory effects of the target compounds on the proliferation of A549, HepG2 and HUVEC cells were detectec by MTT assay. The abilities of adhesion, invasion and migration of A549 and HepG2 cells inhibited by the synthesized compounds were evaluated through Matrigel experiment and Transwell assay. The results showed that, the target compounds had no significant cytotoxicity (compared with the control, P>0.05) to A549, HepG2 and HUVEC cells at the dose range of 1-32 µmol.L-1. At the above dose range, the inhibitory effects of A549 cells adhesion, invasion and migration and HepG2 cells adhesion and invasion by compounds 79 and 82 are better than brartemicin.
Antineoplastic Agents ; chemical synthesis ; pharmacology ; Cell Adhesion ; Cell Line, Tumor ; drug effects ; Drug Design ; Hep G2 Cells ; drug effects ; Human Umbilical Vein Endothelial Cells ; drug effects ; Humans ; Trehalose ; analogs & derivatives ; chemistry

Using brartemicin as the leading compound, fifteen novel trehalose derivatives were designed and synthesized, and the structures were determined by 11H NMR, MS and element analysis. Inhibitory effects of the target compounds on the proliferation of A549, HepG2 and HUVEC cells were detectec by MTT assay. The abilities of adhesion, invasion and migration of A549 and HepG2 cells inhibited by the synthesized compounds were evaluated through Matrigel experiment and Transwell assay. The results showed that, the target compounds had no significant cytotoxicity (compared with the control, P>0.05) to A549, HepG2 and HUVEC cells at the dose range of 1-32 µmol.L-1. At the above dose range, the inhibitory effects of A549 cells adhesion, invasion and migration and HepG2 cells adhesion and invasion by compounds 79 and 82 are better than brartemicin.

Objective The hippocampus has been used in Chinese medicine for a long time.Although it has the anti-decrepitude,anti-fatigue and anti-tumor effect,the molecular mechanism is not yet known.PI4-K,the first protein kinase in the PI pathway,should be the target molecular for drug screening.Methods We prepared antigen protein IOV-PI4-K through inside-out ghost,then the antibody-antigen reaction between IOV-PI4-K and its antibody A6D was tested by ELISA.Results Two different function groups,which could increase or decrease the binding affinity of PI4-K to its antibody,were screened out from the extracts of hippocampus.This fact indicated that there might be two different components to up-regulate or down-regulate the activity of PI4-K respectively.Conclusion Derivatives of the components could be developed into anti-tumor or anti-decrepitude drugs.Meanwhile,a new way for performing drug screen through ELISA was established.

Objective To compare the reliability of acute physiology and chronic health evaluation Ⅱ (APACHE Ⅱ) and APACHE Ⅲ to estimate mortality of critical patients in abdominal surgery. Methods Two hundred and sixty-one critical patients in abdominal surgery were included in this study. The clinical data of the first day in ICU were collected and evaluated with both APACHE Ⅱand APACHE Ⅲ prognostic systems and statistical analysis were performed. Probability of survival (Ps) was compared with actual mortality. Results The scores of APACHE Ⅱ and APACHE Ⅲ of death group were significantly higher than those of survival group respectively (P

OBJECTIVE:To investigate the preventive use of antibacterials in patients undergoing cesarean section in our hospital.METHODS:A total of 360 medical records of patients undergoing cesarean section were randomly sampled in 2006(30 cases per month)for an analysis of the correlation between choice of antibacterials,combination rate and course of treatment etc and curative effects.RESULTS:Of the 360 cases,86.8% used second and third generation cephalosporins,6.3% fourth generation cephalosporin(cefepime),3.8% cephradine.CONCLUSION:No positive correlation was noted between choice of antibacterials and course of treatment and the curative effects in the prevention of postoperative infection.

Urethral stricture is one of the common complications after hypospadias repair,and it is related with the blood supply of materials used in urethra formation.The more severe and proximal hypospadias is,the higher possibility of stricture is.The patients with urethral stricture have the symptoms of stranguria and urinary retention,and they usually need re-surgery.The repair with well vascularized flap can decrease the occurrence of urethral stricture after hypospadias repair.

Burns, Inhalation ; complications ; Humans ; Male ; Middle Aged ; Nitric Acid ; adverse effects ; Pulmonary Edema ; chemically induced ; therapy

Objective To analyze the clinical risk factors of the occurrence of severe proliferative vitreoretinopathy (PVR) after scleral reattachment surgery. Methods A total of 4 031 eyes of 4 031 consecutive patients with reghmatogenous retinal detachment (RRD) and PVR (grade C1 or less), on whom the scleral buckling was performed, were retrospectively studied. Twenty-two clinical characteristics of the patients (including the ocular tension, condition of lens and vitreous, characteristics of retinal detachment, whether or not with choroidal detachment, et al) were recorded. In 4 031 patients, 2 660 were followed up for more than 3 months, and 72 (in PVR group) of the 2 660 patients underwent the second surgery (vitreoretinal surgery) because of the occurrence of postoperative severe PVR; in the other 2 588patients, 72 (72 eyes) with retinal reattachment for more than 3 months were selected randomly as the control. The data were analyzed in SPSS (10.0) software. Results Logistic regression analysis revealed that the significant risk factors for PVR were incomplete posterior vitreous detachment (P2 DD,P

AIM: To explore the possible anti apoptotic mechanism of ginsenoside Rg1 on MPP + induced cellular apoptosis. METHODS: The apoptosis of SHSY5Y induced by MPP + was observed by AO EB staining. Flow cytometry was used to quantitate mitochondrial transmembrane potential (△?m) and reactive oxygen species (ROS) . Western Blot was used to detect the expression of bcl 2 and bax proteins in SHSY5Y cells. RESULTS: MPP + induced apoptosis in SHSY5Y cells was obviously inhibited by pretreatment with 10 ?mol?L -1 Rg1. Although there was no difference of mitochondrial transmembrane potential between Rg1 pretreated groups and MPP + groups, the level of ROS in Rg1 pretreated groups decreased, the expression of bcl 2 protein increased and expression of bax protein decreased. CONCLUSION: Rg1 protects against MPP + induced apoptosis in SHSY5Y cells and the effect may be attributed to its remove of ROS and its regulation of expression of bcl 2 and bax proteins.