Antidiuretic Hormone Receptor Antagonists ; Heart Failure ; drug therapy ; Humans

An Aspergillus sp. strain F3 was isolated and identified from the rhizosphere soil of mangrove plant, Rhizophora stylosa Griff in Dongzhai harbor mangrove forest conservation in China. In this study, the effects of media salinity and pH on the mycelial biomass and the ability of producing antibacterial metabo- lites from this isolate were carefully analyzed. Results showed that this isolate can grow well on the SDA medium with higher salinity (3%~9%) and higher pH (8~10). Under the modified culturing conditions, this isolate can secret the antibacterial and antitumor metabolites. The extracts of acetic ether were about 448 mg/L of the fermentation broth. The antibacterial activities of the acetic ether extract were analyzed with bacteria and fungus. Results showed this extract can suppress the growth of Staphylococcus aureus、S. epi-dermidis、Sarcina lutea、Bacillus subtilis and Escherichia coli with MIC of 31.3 ?g/mL, 31.3 ?g/mL, 7.8 ?g/mL, 7.8 ?g/mL and 125.0 ?g/mL, respectively. It can also suppress the growth of Candida albicans with MIC of 125.0 ?g/mL. Further studies uncovered the cytotoxicity of this extract against the tumor cells, such as ECV304, Lovo and HepG2 with IC50 of 3.45 ?g/mL, 4.88 ?g/mL and 14.31 ?g/mL respectively.

Background and purpose:Chemotherapy plays an important role in the treatment of breast carcinoma by inhibiting the tumor growth and inducing the apoptosis.MAPK transduction pathway is closely related to proliferation and apoptosis of varieties of tumor cells,inhibition of MAPK pathway may increase the efficiency and decrease the toxicity of chemotherapy.Our study was to investigate the effect of MEK inhibitor PD98059 in response of breast cancer cell lines to Epirubicin.Methods:Human breast cancer cell lines MCF-7 and MCF-7/ADR were used as cell models.Epirubicin(EADM),PD98059(inhibitor of MAPK Kinase-MEK),or EADM+PD98059 was added into the culture medium,the expression of MEK2 and p-ERK were measured by Western blot,the growth of the two cell lines were measured by MTT.Results:ERK activity was elevated in MCF-7 after the treatment of EADM,the cells were more sensitive to EADM if combined with PD98059,while in MCF-7/ADR,ERK activity kept unchanged after EADM treatment,and PD98059 has no effect on the sensitivity of cells to EADM.Conclusion:MAPK signal transduction may be activated in some cells treated by EADM,adding inhibitor of MAPK signal transduction could improve the sensitivity of the cells to EADM.

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.
Humans ; Protein Tyrosine Phosphatase, Non-Receptor Type 1 ; antagonists & inhibitors ; Structure-Activity Relationship ; Sulfathiazoles ; chemistry ; pharmacology

Adenocarcinoma ; diagnosis ; pathology ; Carcinoma, Squamous Cell ; diagnosis ; pathology ; Cervical Intraepithelial Neoplasia ; diagnosis ; pathology ; Female ; Humans ; Precancerous Conditions ; diagnosis ; pathology ; Retrospective Studies ; Uterine Cervical Neoplasms ; diagnosis ; pathology ; Vaginal Smears ; methods

OBJECTIVETo study the effect of puerarin on angiotensin II type 1 receptor (AT1) and angiotensin-converting enzyme 2 (ACE2) in spontaneous hypertension rat (SHR).

METHODSSHRs, 12 weeks old, were randomly divided into four groups: the model control group (A), the Verapamil group (B), and the two puerarin groups (C and D) treated by low dose and high dose of puerarin respectively. After being treated for 3 weeks, total RNA from tissues of heart, aorta and kidney in rats were extracted and mRNA expression levels of AT1 and ACE2 were determined by RT-PCR.

RESULTSAs compared with Group A, the mRNA expressions of AT1 and ACE2 in heart tissue were lower in Group C, and those in kidney tissue were higher in Group D (all P < 0.05); ACE2 mRNA expression was higher in Group D than in Group C (P < 0.05); no significant differences of the two indexes in aorta were shown among various groups. Besides, mRNA expressions of AT1 and ACE2 in heart and kidney tissue were proved to be positively linearly correlated.

CONCLUSIONHigh dose puerarin could increase the mRNA expressions of AT1 and ACE2 in kidney, while low dose puerarin could decrease them in heart; there might be a feed back correlation between AT1 and ACE2.

Animals ; Disease Models, Animal ; Gene Expression ; drug effects ; Heart ; drug effects ; Humans ; Hypertension ; drug therapy ; genetics ; metabolism ; Isoflavones ; administration & dosage ; Kidney ; drug effects ; metabolism ; Male ; Myocardium ; metabolism ; Peptidyl-Dipeptidase A ; genetics ; metabolism ; RNA, Messenger ; genetics ; metabolism ; Random Allocation ; Rats ; Rats, Inbred Dahl ; Receptor, Angiotensin, Type 1 ; genetics ; metabolism

ObjectiveThe procedure of peroral endoscopic myotomy (POEM) was practiced in porcine esophagus-stomach model and the efficacy and safety of POEM for patients with achalasia were evaluated.MethodsThe ex-vivo esophagus-stomach was obtained and the pylorus was closed by hemostatic forceps.The entrance of the esophagus was fixed to foamed plastics.To perform POEM,a submucosal tunnel was created,after which the circular muscle layer was dissected and the mucosal entry was finally closed with clips.After successful animal experiment,we performed POEM on 4 patients with achalasia.Results POEM was completed in 5 porcine training models,in which 2 procedures were successful without any complication,2 were complicated with perforation in muscularis propria layer and 1 with rupture in mucosal layer.POEM was successfully performed in 4 patients with achalasia,with a mean operation time of 110min.The mean length of the submucosal tunnel was 10.5cm ( ranging 8-11 cm) and the mean length of myotomy of circular muscle layer was 7 cm (ranging 5-8 cm).The resting pressure of lower esophageal sphincter (LES) decreased from 52.4 mm Hg before POEM to 19.9 mm Hg.Massive bleeding occurred at the gastroesophageal junction in the first case and perforation occurred in mucosal layer during endoscopic hemostasis.All patients were followed up for 1-4 months,and the symptom of dysphasia was relieved significantly.ConclusionThe ex-vivo esophagus-stomach model can be used as training model for procedure of POEM,enabling endoscopists with enough experience for its use in patients.POEM is an effective therapy for achalasia,while the long-term efficacy and managements for complications are still to be elucidated.

OBJECTIVETo compare the effect of transumbilical single-site single-port with that of transumbilical single-site double-port laparoscopic varicocelectomy in the treatment of varicocele in adolescents.

METHODSWe randomly assigned 80 varicocele patients aged 10 - 16 years to two groups of equal number to receive transumbilical single-site single-port and single-site double-port laparoscopic varicocelectomy, respectively. We compared the operation time, postoperative hospital stay, incisional pain, complications and satisfaction with the abdominal cosmetic outcomes between the two groups.

RESULTSAll the operations were successfully performed. The double-port group showed a significantly higher score on the Visual Analogue Scale than the single-port group (4.8 +/- 1.4 vs 3.6 +/- 1.1, t = -4.986, P < 0.01), but there were no significant differences between the two groups in the operation time ([29.8 +/- 4.2] vs [31.2 +/- 4.6] min, t = 1.383, P = 0.171), postoperative hospital stay ([1.95 +/- 0.7] vs [1.82 +/- 0.8] d, t = -0.784, P = 0.436), complications (0 vs 0) and scores on the satisfaction with abdominal cosmetic outcomes (4.6 +/- 0.6 vs 4.8 +/- 0.5, t = 1.253, P = 0.214). No recurrence, umbilical hernia, hydrocele and orchiatrophy were found in the two groups of patients at 6 months after operation, and no visible scar was observed on the abdominal surface.

CONCLUSIONWith strict surgical indications, single-site single-port and single-site double-port laparoscopic varicocelectomies have similar clinical effects in the treatment of varicocele, which leave no scar on the abdominal surface. Single-site double-port laparoscopy needs no special instruments and therefore is worthier of wide clinical application.

Adolescent ; Child ; Humans ; Laparoscopy ; methods ; Length of Stay ; Male ; Operative Time ; Umbilicus ; surgery ; Varicocele ; surgery

OBJECTIVETo investigate the Bmi1 protein level in human colorectal cancer specimen and associated clinicopathological parameters, and to determine the influence of Bmi1 on the proliferation and apoptosis of colorectal cancer cells.

METHODSBmi1 protein level was assessed in 85 patients with colorectal cancer and adjacent normal tissue by immunohistochemistry. SW480 cells were transfected with Bmi siRNA plasmid. MTT assay and flow cytometry were used to measure the proliferation and apoptosis of SW480 cells. The expression of Bmi1 and Bcl-2 were measured by Western blot.

RESULTSThe positive rate of Bmi1 expression in colorectal cancer tissues was 56.5%(48/85), significantly higher than that in the adjacent noncancerous tissues[17.6%(15/85), P<0.05)]. It was found that the overexpression of Bmi1 was associated with degree of differentiation, status of lymph nodes metastasis, and TNM staging in colorectal cancer(P<0.05). After transfection of SW480 with Bmi1 siRNA, the cell proliferation was inhibited and the apoptosis was significant. The cell proliferation inhibitory rates were 13.1%, 16.5%, and 18.3% at 24 h, 48 h and 72 h after transfection. The apoptotic rates were 15.7%, 45.6%, 40.2%, respectively. Expression of Bmi1 was downregulated after 48 h, as was that of Bcl-2.

CONCLUSIONSBmi1 expression is associated with the clinicopathological characteristics of colorectal cancer. Blockade of Bmi1 can inhibit the proliferation and accelerate the apoptosis of colorectal cancer cells.

Aged ; Apoptosis ; Cell Line, Tumor ; Cell Proliferation ; Colorectal Neoplasms ; metabolism ; pathology ; Female ; Humans ; Male ; Middle Aged ; Neoplasm Staging ; Polycomb Repressive Complex 1 ; metabolism ; Proto-Oncogene Proteins c-bcl-2 ; metabolism