Objective:Selection ofthe optimal formulation for IL-2 targeting liposome and determination ofcontent for 5-FUR.Methods:orthogonal test method was used to selection the optimal formulation,UV spectrophotometry was used to determine the 5-FUR prodrug content,and the detection wavelength was at 267 nm.Results:The optimal formulation showed Drug/EPC 1∶10,EPC/Ch 3∶1.The absorbency and concentration of 5-FUR prodrug had good linearity in the range of 2.0～20.0?g/mL.The regression equation was y=16.357x+0.007,r= 0.999 7(n=3),The 5-FUR prodrug content was 18.84～18.91?g/ml.The average recovery rate was 97.09%,and RSD=2.05%(n=3).Conclusion:Formulation was designed reasonablely.The method is simple,stable and reliable,which can be used to determine the 5-FUR prodrug in IL-2 targeting liposome.

OBJECTIVE: To study the effect of Xingding Injection on the expression of heat shock protein 72 (HSP 72) in vascular endothelial cells after ultraviolet radiation. METHODS: Porcine aortic endothelial cells were cultured for 72 hours in culture mediums with different concentrations (0.1, 0.5, 1.0, 5.0, 10 mg/ml) of Xingding Injection. Ultraviolet radiation was administered to the cultured cells for 30 minutes. Western-blot assay was used to measure the expression of HSP 72 in the vascular endothelial cells. RESULTS: There was no expression of HSP 72 in the cultured vascular endothelial cells without ultraviolet radiation, but there was some expression of HSP 72 after ultraviolet radiation. Xingding Injection of different concentrations could significantly improve the expression of HSP 72. The expression of HSP 72 in the vascular endothelial cells cultured in culture medium with 1.0 mg/ml Xingding Injection was the highest, and there was no more increase of expression when the concentration was higher, instead the expression decreased. CONCLUSION: Xingding Injection can protect the vascular endothelial cells from injury during stress. It may be one of its mechanisms in preventing and treating cardio-cerebrovascular disorders.

Objective To explore the serum expression of DKK1 protein, a Wnt signaling pathway inhibitor in patients with non-small cell lung cancer (NSCLC) and its relationship with osseous metastasis. Methods Serum DKK1 protein levels were assayed by enzyme-linked immunosorbent assay (ELISA) in NSCLC patients, including 33 NSCLC patients with osseous metastasis and 41 NSCLC patients without respectively, and 32 healthy volunteers were served as the control group. Furthermore, the differential expression of the serum DKK1 protein level between the patients and the volunteers was compared by using the variance analysis and the independent sample t test. The correlation between DKK1 expression and bone metastasis was detected by Pearson correlation analysis. Results Serum DKK1 protein level of NSCLC patients was (79.6±8.3) ng/ml, which was significantly higher than that in healthy volunteers [(21.5±6.4) ng/ml, t=13.17, P=0.001]. The serum DKK1 level in osseous metastasis group was (110.3±11.4) ng/ml, which was significantly higher than that in non-skeletal metastasis group [(60.7±10.5) ng/ml, t=14.128, P=0.003]. The positive association was observed between the DKK1 level in the peripheral blood and osseous metastasis in NSCLC patients (r=0.855, P<0.001). Conclusion The serum expression level of DKK1 protein in NSCLC patients is closely related to the osseous metastasis, which may be a predicting biomarker for the osseous metastasis.

OBJECTIVE:To determine the content of IL-2 in IL-2 targeting liposomes of 5-FURP. METHODS: The sample solution was stained by Coomassie brillant blue G-250 solution. Using blank liposome as blank,the absorbability of the IL-2 was determined by ultraviolet spectrophotometry at a wavelength of 595 nm;meanwhile its content was determined. RESULTS: The linear range of IL-2 was 1～100 ?g?ml-1(r=0.999 7) and the average recovery rate was 99.26% (RSD=0.59%,n=5). CONCLUSION: The method was proved to be simple,rapid,sensitive and reproducible,and it is applicable for the determination of IL-2 in liposome of 5-FURP.

ATM: To explore the effect and mechanism on blood pressure and heart protection of renal hypertension in rats treated with ?_1 receptor antisense oligodeoxynucleotides (?_1-AS-ODN) by delivery with cationic liposomes DOTAP/DOPE. METHODS: 24 SD rats were divided randomly into 4 groups of 6 each group: two groups of 2K1C rats were treated via tail vein injection with ?_1-AS-ODN or inverted oligonucleotides against rat ?_1-AR mRNA (?_1-IN-ODN) of 0.5 mg?kg~(-1) once. 6 untreated 2K1C rats and shamed rats served as positive and normal controls. Blood pressure (BP), cardiac haemodynamics, and left ventricular index (LVW/BW) were measured. The histological changes of myocardium were observed by optical microscope and the expressions of Bcl-2 and Bax in myocardium were examined by immunohistochemical method. RESULTS: The single dose management of ?_1-AS-ODN decreased blood pressure to 120 mmHg for 27 days and improved the LV function obviously (P

Objective To describe the current situation of pre-hospital delay and health belief in patients with colorectal cancer and explore the relationship between them. Methods With convenient sampling methods,totally 385 patients with colorectal cancer were recruited from January to June 2016. Patients with colorectal cancer were investigated using a general data survey questionnaire, visit situation questionnaire and the Champion Health Belief Model Scale. Results The median pre-hospital delay time was 3.00 months.The rate of pre-hospital delay was 43.1%(166/385). The score of the overall health belief was (119.52 ± 12.62) points. The two dimensions of"perceived susceptibility and perceived severity" scored lower, and the two dimensions of "health motivation and perceived therapeutic benefits" scored higher. The health belief was negatively correlated with the pre- hospital delay among colorectal cancer patients (r=- 0.737, P<0.01). Conclusions Pre-hospital delay occurred among patients with colorectal cancer is severe. Patients with a higher level of health belief have shorter pre-hospital delay.It′s important to improve the level of health belief of"perceived susceptibility and perceived severity"and reduce the time of pre-hospital delay to improve outcomes in patients with colorectal cancer.

Kv2.1 channel currents in pancreatic beta-cells are thought to contribute to action potential repolarization and thereby modulate insulin secretion. Because of its central role in this important physiological process, Kv2.1 channel is a promising target for the treatment of type 2 diabetes. Jingzhaotoxin-XI (JZTX-XI) is a novel peptide neurotoxin isolated from the venom of the spider Chilobrachys jingzhao. Two-microelectrode voltage clamp experiments had showed that the toxin inhibited Kv2.1 potassium currents expressed in Xenopus Laevis oocytes. In order to investigate the structure-function relationship of JZTX-XI, the natural toxin and a mutant of JZTX-XI in which Arg3 was replaced by Ala, were synthesized by solid-phase chemistry method with Fmoc-protected amino acids on the PS3 automated peptide synthesizer. Reverse-phase high performance liquid chromatography (RP-HPLC) and matrix assisted laser desorption/ ionization time-of-flight mass spectrometry (MALDI-TOF/TOF MS) were used to monitor the oxidative refolding process of synthetic linear peptides to find the optimal renaturation conditions of these toxins. The experiments also proved that the relative molecular masses of refolded peptides were in accordance with their theoretical molecular masses. RP-HPLC chromatogram of co-injected native and refolded JZTX-XI was a single peak. Under the whole-cell patch-clamp mode, JZTX-XI could completely inhibit hKv2.1 and hNav1.5 channels currents expressed in HEK293T cells with IC50 values of 95.8 nmol/L and 437.1 nmol/L respectively. The mutant R3A-JZTX-XI could also inhibit hKv2.1 and hNav1.5 channel currents expressed in HEK293T cells with IC50 values of 1.22 micromol/L and 1.96 micromol/L respectively. However, the prohibitive levels of R3A-JZTX-XI on hKv2.1 and hNav1.5 channels were reduced by about 12.7 times and 4.5 times respectively, indicating that Arg3 was a key amino acid residue relative to the hKv2.1 channel activity of JZTX-XI, but it is also an amino acid residue correlated with the binding activity of JZTX-XI to hNav1.5 channel. Our findings should be helpful to develop JZTX-XI into a molecular probe and drug candidate targeting to Kv2.1 potassium channel in the pancreas.
Animals ; HEK293 Cells ; Humans ; Insulin-Secreting Cells ; metabolism ; Mutant Proteins ; genetics ; pharmacology ; NAV1.5 Voltage-Gated Sodium Channel ; metabolism ; Neurotoxins ; chemical synthesis ; genetics ; pharmacology ; Protein Refolding ; Shab Potassium Channels ; antagonists & inhibitors ; metabolism ; Sodium Channel Blockers ; pharmacology ; Spider Venoms ; genetics ; pharmacology ; Transfection

Objective: To evaluate the effect of biofeedback training on bowl function among rectal cancer patients with chemoradiotherapy and temporary enterostomy. Methods: Using randomized controlled trial design, 109 rectal cancer patients were randomly divided into three groups, the first blank control group, the second group pelvic floor muscle exercise group, the third group biofeedback group. High resolution anorectal manometry was used for 6 longitudinal traces in 16 months. Data of bowel function were collected by Memorial Sloan Kettering Cancer Center (MSKCC) Bowel Function Instrument. Results: The main effect of the change of five indicators, anal resting pressure, rectal resting pressure, maximum squeeze pressure, maximum squeeze time and high pressure zone, was time. The other four indicators, rectal volume at first senory, rectal volume at sense of convenience, maximal tolerable rectal volume and rectal compliance, among patients of biofeedback group were (32.71±5.00) ml, (74.26±8.30) ml, (188.40±12.68) ml, (5.69±1.18) ml/kPa and (68.09±6.38). The rectal volume at first senory, rectal volume at sense of convenience, maximal tolerable rectal volume and rectal compliance, among patients of biofeedback group were significant higher than blank control group and pelvic floor muscle exercise group (F=3.589-26.826, P<0.05). Conclusion The biofeedback could significantly improve the sensory indicators of patients with middle and low rectal cancer. High-resolution anorectal manometry could effectively evaluate the effect of biofeedback training in patients with middle and low rectal cancer.

Plastics are widely used in daily life. Due to poor management and disposal, about 80% of plastic wastes were buried in landfills and eventually became land and ocean waste, causing serious environmental pollution. Recycling plastics is a desirable approach, but not applicable for most of the plastic waste. Microbial degradation offers an environmentally friendly way to degrade the plastic wastes, and this review summarizes the potential microbes, enzymes, and the underpinning mechanisms for degrading six most commonly used plastics including polyethylene terephthalate, polyethylene, polyvinyl chloride, polypropylene, polystyrene and polyurethane. The challenges and future perspectives on microbial degradation of plastics were proposed.
Biodegradation, Environmental ; Plastics ; Polyurethanes ; Recycling