The steroidal enzyme cytochrome P45017alpha catalyzes the conversion of progesterone and pregnenolone into androgens, androstenedione and dehydroepiandrosterone, respectively, the direct precursors of estrogens and testosterone. Dihydrotestosterone is the principal active androgen in the prostate, testosterone is also an active stimulant of the growth of prostatic cancer tissue. Inhibition of this enzyme as a mechanism for inhibiting androgen biosynthesis could be a worthwhile therapeutic strategy for the treatment of PCA. In this paper, four categories of steroidal inhibitors of cytochrome P45017alpha will be reviewed, a diverse range of steroidal inhibitors had been synthesized and shown to be potent inhibitors of P45017alpha.

The in vitro antitumor activity of bakuchiol was exploited, compared with tamoxifen. The result of biological activities showed that bakuchiol could inhibit human breast cancer and the IC50 values were 2.89 x 10(-5) mol L(-1) and 8.29 x 10(-3) mol L(-1) against the cells line T-47D and MDA-MB-231 respectively. On the other hand, the key intermediate to synthesize bakuchiol was obtained by the method of Ireland-Claisen rearrangement. Comparing with traditional Claisen rearrangement, the reaction conditions are milder and the reaction reagents are safer.

Objective To construct a recombinant plasmid for expressing the HPV18 E2 gene and develop some materials for HPV18 related disease.Methods The E2 gene of HPV18 was amplified by PCR from PBR322-HPV18 and cloned into PIRES2-EGFP.The sequence of cloned HPV18E2 was confirmed by restriction analysis and DNA sequencing,then transfected into HeLa cells.E2 gene was detected by RT-PCR.Results HPV18 E2 gene fragment was amplified by PCR and ligated to PIRES2-EGFP,then transfected into HeLa cells successfully.The expression of green fluorescence cells was observed by fluorescence microscopy.Specific band could be seen in transfected cells by RT-PCR.Conclusion Recombinant plasmid PIRES2-EGFP is effectively expressed after being transfected into HeLa cells in vitro.

Objective To compare the clinical effects of high flow nasal cannula (HFNC) and non-rebreathing oxygen face mask (NRB) in post-extubation patients.Methods 88 critically ill patients with machinery ventilations were divided into HFNC group and NRB group randomly.Blood gas analysis and hemodynamic parameters were assessed 1 hour prior to extubation and 6 hours after extubation.The primary clinical outcomes measured were ventilation-free days,re-intubation patient numbers,length of stay in ICU (Intensive Care Unite),total duration of hospitalization and mortality.The scant of breath degree and comfortableness of patient were recorded according to the Visual analogue scale.The measurement data were described by mean ± standard deviation ((x) ± s) and analyzed with t test,enumeration data were described by number of cases and composition ratio and analyzed with X2test,P ＜ 0.05 was considered to have statistical difference.Results There was no significant difference in clinical features between the two groups,The oxygenation index of HFNC group is significantly higher than that of NRB group after extubation [(251.4 ±43.9) vs.(201.7 ±60.7),P =0.037)].There were more ventilator-free days in the HFNC group than NRB group [(4.2 ± 2.1) vs.(3.4 ± 2.8),P =0.037)] and fewer patients required reintubation (P =0.028).The rate of ventilator associated pneumonia is also lower than NRB group (P =0.024).The patients' scant of breath feeling were obviously allevated comparing with the NRB group [(2.9 ± 1.1) vs.(3.7 ± 1.8),P =0.042)].The oxygenation index of NRB group significantly decreased after extubation [(242.9 ±68.4vs.201.7 ±60.7 P =0.048)].The two groups demonstrated similar hemodynamic patterns before and after extubation.And there were no statistically significant clinical differences in PaCO2,length of ICU stay,total duration of hospitalization or mortality.Conclusions Compared with NRB,HFNC is a more safe and effective clinical tool in the prevention and treatment of critical adult patients with extubation failure.

Objective To evaluate the effect of different blood purification modes on patients with hyperlipidemic pancreatitis (HLP).Methods 28 patients with HLP in our department were enrolled into this study from January 2010 to June 2013.The patients were randomly divided into the HP/CVVH group (15 patients) and CVVH group (13 patients).The clinical symptoms and signs of the two groups were observed.The plasma levels of TNF-α,IL-6,IL-8,blood triglyceride and APACHE Ⅱ score before and after treatment were compared between the two groups.The duration of mechanical ventilation,ICU stay and mortality rate were compared between the two groups.Results The clinical symptoms improved in the two groups after treatment.The plasma levels of TNF-α,IL-6,IL-8,blood triglyceride and APACHE Ⅱ score were all reduced.However,the plasma levels of TNF-o,IL-6,IL-8,blood triglyceride and APACHE Ⅱ score in the HP/CVVH group were lower than the CVVH group at the same time points,showing significant differences (P ＜ 0.05).The duration of mechanical ventilation,ICU stay and mortality rate decreased in the HP/CVVH group (P ＜ 0.05).Conclusions HP/CVVH was more efficacious in the treatment of HLP.

Objective:To screen the antagonist of C5a anaphylatoxin,and further to study the dinetic characteristics of interaction between C5a and its anti-sense peptides.Methods:The anti-sense peptides were screened that can interact with C5a selectively by means of dinetic analysis,via biosensor technique.Results:There is one piece of anti-sense peptide(R4) being screened from these four synthesized peptides.The dissociation equilibrium constant(K D) between R4 and the immobilized hC5a is 6.62?10 -6 mol/L and the K D between R4 and L2 is 7.02?10 -7 . Conclusion:Based on the results obtained,it was concluded that the optic biosensor is a ideal and powerful tool to facilitate the kinetic analysis of interaction between sense peptide and its anti-sense peptide and to screen antagonist of biologic activity molecule.

OBJECTIVE:To optimize the extraction technics of liver-strengthening cholagogue oral preparation.METHODS:The effects of the four factors-the quantity of the added water,the decoction time,the decoction times and the alcohol precipitation concentration on the extraction results were determined with content of total flavonoids taken as index.RESULTS:The best extracting condition was the following,the amount of the added water was 10 times that of the medicinal materials,the decoction duration was 60min,the alcohol precipitation concentration was 50%and the decoction was carried out twice.CONCLUSION:The preparation under this technics is of high clarity and stable contents.

Objective To explore the mechanism that Staphylococcus aureus(S.aureus) α-toxin(Hla) regulate miR-142 expression and inhibit macrophage phagocytosis.Methods BALB/C mice and RAW264.7 cells were infected with wild type S.aureus(WT S.aureus),Hla deletion S.aureus(△HlaS.aureus) or phosphate buffered saline(PBS),and the expression level of miR-142 of skin tissues and cells were detected.miR-142 mimics and inhibitor were then applied in the RAW264.7 culture to examine the effect on phagocytosis.Direct targeting of miR-142 on protein kinase Cα(PKCα) was assessed by luciferase assay and western blotting.Results miR-142 expression in △HlaS.aureus group were significantly down-regulated than WT S.aureus group(P<0.05).MiR-142 mimics inhibited RAW264.7 phagocytosis ability and inhibitor enhanced RAW264.7 phagocytosis ability.PKCα was directly targeted by miR-142.MiR-142 mimics significantly decreased the mRNA expression levels of PKCα in RAW264.7 cells(P<0.05).Conclusion Hla could promote miR-142 expression in macrophages.MiR-142 could inhibit macrophage phagocytosis through down-regulated PKCα.

Objective To study on the measurement of glycyl-proline dipeptidyl aminopeptidase (GPDA) in urine and its clinical application. Methods GPDA in urine was measured by continuously monitoring method using substrate. The assay conditions and interference factors were investigated. GPDA activities in urine specimens from 334 healthy persons, 55 diabetes mellitus patients and 36 hypertension patients were measured. The differences between the kidney injured and non-kidney injured groups were analyzed. Results The linearity of the method was up to 350 U/L. The intra CV and inter CV were 1.27% and 1.33% respectively. The GPDA activity in urine specimen was stable for 7 days at 4℃. There was no interference of bilirubin, glucose, vitamins, dimethylbiguanide and gliben-clamide. No significant interference was found by hemoglobin less than 500 mg/L. GPDA level in urine specimens of 334 healthy persons were (12.9?4.2) U/g?Cr. The GPDA levels of diabetes mellitus and hypertension groups combined with kidney injured were obviously higher than that of the control group and the non-kidney injured group ( P

Objective To compare the therapeutic effects of continuous veno-venous hemofiltration (CVVH) versus repeated intermittent veno-venous hemofiltration (RIVVH) on patients with severe acute pancreatitis (SAP).Methods Fifty-six patients with SAP were randomly divided into the CVVH group (n =28) and the RIVVH group (n =28).The clinical symptoms and signs,the APACHE Ⅱ and MODS scores,the result of biochemistry including amylase and lipase,and the plasma levels of TNF-α,IL-6,IL8 before and after treatment,the duration of mechanical ventilation,boosting drug application time,the length of stay in ICU,the surgical intervention rate and the mortality were compared between the two groups.Results The clinical symptoms improved in the two groups after treatment (P ＜ 0.05).The APACHE Ⅱ and MODS scores were all reduced in the two groups after treatment (P ＜ 0.05).When compared with the RIVVH group,the result of biochemistry including amylase and lipase,and the plasma levels of TNF-α,IL6,IL-8 were significantly decreased (P ＜ 0.05).The duration of mechanical ventilation,the length of stay in ICU and the mortality were also significantly decreased in the CVVH group (P ＜ 0.05).Conclusions CVVH was more efficacious than RIVVH in the treatment of SAP.