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Insect glutathione S-transferases (GSTs) play important roles in detoxifying toxic compounds and eliminating oxidative stress caused by these compounds. In this study, detoxification activity of the epsilon GST SlGSTE1 in Spodoptera litura was analyzed for several insecticides and heavy metals. SlGSTE1 was significantly up-regulated by chlorpyrifos and xanthotoxin in the midgut of S. litura. The recombinant SlGSTE1 had Vmax (reaction rate of the enzyme saturated with the substrate) and Km (michaelis constant and equals to the substrate concentration at half of the maximum reaction rate of the enzyme) values of 27.95 ± 0.88 μmol/min/mg and 0.87 ± 0.028 mmol/L for glutathione, respectively, and Vmax and Km values of 22.96 ± 0.78 μmol/min/mg and 0.83 ± 0.106 mmol/L for 1-chloro-2,4-dinitrobenzene, respectively. In vitro enzyme indirect activity assay showed that the recombinant SlGSTE1 possessed high binding activities to the insecticides chlorpyrifos, deltamethrin, malathion, phoxim and dichloro-diphenyl-trichloroethane (DDT). SlGSTE1 showed higher binding activity to toxic heavy metals cadmium, chromium and lead than copper and zinc that are required for insect normal growth. Western blot analysis showed that SlGSTE1 was induced in the gut of larvae fed with chlorpyrifos or cadmium. SlGSTE1 also showed high peroxidase activity. All the results together indicate that SlGSTE1 may play an important role in the gut of S. litura to protect the insect from the toxic effects of these compounds and heavy metals. [ABSTRACT FROM AUTHOR]

A novel method for synthesizing carfentanil is researched in this work. N-Boc-protected piperidinone was used as the starting material. The carfentanil was achieved via synthetic rout involving five steps: Bargellini reaction, N-acylation, methylation, deprotection and N-alkylation. The overall yield of target compound was 31. 6%. The structures of intermediates and final product were determined by infrared spectroscopy, nuclear magnetic resonance spectroscopy and mass spectrograph. [ABSTRACT FROM AUTHOR]

This paper studies two-step synthetic process of TEX (4,10-dinitro-2,6, 8,12-tetraoxa-4, 10-diazatetracyclo-[5. 5. 0. 05,9 03,11]-dodecane) and the effects of key factors on the yield of DFTHP (intermediate) and TEX. The results show that the yield of DFTHP could reach to 68. 3% when the adjusted pH value of reaction solution reaches to 9 by saturated NaOH solution. When the volume ratio of fuming HNO3 to concentrated H2SO4 is 3 : 2, and the ratio of nitrating agent (mL) to DFTHP(g) is 3 : 1, the yield of TEX raises to 59. 7% . The optimized overall yield of TEX obtained from two-step synthetic process could be 40. 8%. [ABSTRACT FROM AUTHOR]

Objective: To study the effect of the bladder wall neourethra (BWN) technique on early urinary continence after laparoscopic radical prostatectomy (LRP)., Methods: We prospectively selected 40 cases of LRP performed in our hospital from August 2020 to August 2021 and randomly divided them into a BWN group (n = 20) and a control group (n = 20). We recorded the urinary continence rate of the two groups of patients at 7, 30, 90 and 180 days, and measured the maximum urethral pressure (MUP), functional urethral length (FUL) and functional urethral area (UFA) and observed the shape of the neourethra closure by MRI at 1 month after catheter removal., Results: The urinary continence rates were significantly higher in the BWN than in the control group at 7 days (90.0% vs 25.0%, P < 0.001), 30 days (95.0% vs 35.0%, P < 0.001), 90 days (100% vs 60.0%, P < 0.05) and 180 days (100% vs 90.0%, P > 0.05) after catheter removal. No statistically significant difference was observed in MUP between the two groups (P > 0.05). FUL and FUA were remarkably higher in the BWN than in the control group (P < 0.01). MRI showed tight closure of the neourethra in the BWN group in the urine storage period., Conclusion: The BWN technique can significantly prolong FUL and improve early urinary continence after LRP.

Objective: To compare the clinical efficacy of distal radius T-plate combined with suture anchor and distal clavicle anatomical locking plate combined with suture anchor in the treatment of Neer Ⅱb distal clavicle fracture., Methods: From June 2014 to June 2018, 42 patients with Neer Ⅱb distal clavicle fractures were retrospectively analyzed. According to different surgical methods, they were divided into the observation group (T-shaped plate combined with suture anchor) and the control group (anatomical locking plate combined with suture anchor). There were 22 patients in the observation group and 20 patients in the control group. In the observation group, there were 13 males and 9 females, aged from 22 to 70 (45.78± 14.44) years old, 12 cases on the left side and 10 cases on the right side, 8 cases of traffic accident injury and 14 cases of fall. In the control group, there were 12 males and 8 females, aged from 24 to 66 (44.17±15.58) years, 13 cases on the left side and 7 cases on the right side, 6 cases of traffic accident injuryand 14 cases of fall. The operation time, intraoperative blood loss and fracture healing time were compared between the two groups, and Constant Murley score was used to evaluate shoulder joint function., Results: The patients in both groups were followed up for 18 to 24 (20.96±2.02) months. The incisions of both groups were healed at stageⅠ. The fracture ends of both groups were bony healed at the last follow up. There was no significant difference in operation time, intraoperative blood loss and fracture healing time between two groups ( P >0.05);there was no significant difference in shoulder joint function between two groups at 3 months after operation ( P >0.05)., Conclusion: The two methods can obtain satisfactory results in the treatment of Neer Ⅱb distal clavicle fractures, especially suitable for patients with comminuted distal clavicle fractures or osteoporosis; the clinical effect of the treatment of NeerⅡb distal clavicle fractures with T type distal radius plate combined with suture anchor is satisfactory, which provides another feasible treatment scheme for clinic.

Bladder cancer is one of the most common cancers diagnosed in the world and leads to significant mortality and morbidity among affected patients. The retinoblastoma (Rb) protein is a main tumor suppressor, controlling cellular responses to potentially oncogenic stimulation. E2F3 was invariably disrupted in different human cancers for its central role in the control of cellular proliferation. Here, we investigated how Rb is integrated to control bladder cancer progression through E2F3 and p53 regulation. The results exhibit that Rb expression is lower in patients with bladder tumor, while E2F3 level is high. Rb knockdown enhanced bladder tumor cell proliferation and migration, aggravated with p53 silence. Interestingly, Rb silence results in E2F3, Myc and mTOR signaling pathway activation, contributing to bladder cancer cell proliferation and apoptosis suppression mainly through caspase-3 inhibition in vitro and in vivo. Immunohistochemical analysis revealed that Rb is highly expressed in normal bladder cells, but was repressed in tumor tissues of the bladder completely, suggesting a possible role of Rb as a tumor suppressor.

Objective: To observe the clinical effects of clavicular hook plate combined with suture anchor in treating type Tossy III chronic acromioclavicular dislocation., Methods: From January 2008 to December 2012,18 patients with type Tossy III chronic acromioclavicular dislocation were treated with clavicular hook plate and suture anchor. There were 12 males and 6 females, aged from 20 to 56 years old with an average of 31.5 years. Ten cases were left dislocation and 8 cases were right dislocation. Operation time was 3 weeks to 4 months after injury with a mean of 1.8 months. Functional exercise was adopted 2 weeks after operation. And Karlsson standard was used to evaluate curative effect., Results: All patients were followed up for 6 to 24 months with an average of 16 months. According to Karlsson standard, 17 cases were excellent and 1 was poor., Conclusion: Clavicular hook plate combined with suture anchor can repair conoid ligament and trapezoid ligament in treating type Tossy III chronic acromioclavicular dislocation, and had advantages of simple operation, less trauma, stable fixation, it can obtain satisfactory effects.

Objective: To evaluate the long-term effect and clinical value of endoscopic mucosal resection (EMR) with transparent cap for dysplasia and early-stage cancer of the esophagus and gastric cardia., Methods: From September 1996 to June 2007, 154 lesions in the esophagus or gastric cardia of 147 patients were treated using EMR with transparent cap. Among the lesions, there were 69 early-stage squamous-cell carcinomas in 64 patients and 47 squamous cell precancerous lesions of the esophagus in 45 patients, with an average lesion size of (14.8 +/- 6.1) mm (range, 3-40 mm), furthermore, there were 23 early-stage adenocarcinomas in 23 patients and 15 precancerous lesions in the gastric cardia in 15 patients, with an average lesion size of (8.2 +/- 4.3) mm (rang, 5-25 mm). All lesions were finally confirmed histopathologically., Results: Of the 154 lesions, 139 (90.3%) were resected completely through EMR procedure. A close relationship between the complete resection rate and the lesion size was observed. The bigger the lesion size, the lower the complete resection rate. Endoscopic follow-up was carried out in 7 patients for more than 10 years, in 43 for 5 - 10 years, in 31 for 3 - 5 years and in 66 for less than 3 years. Of 11 dead patients during following-up, 10 died of other diseases, only 1 of recurrence. The 5-year survival rate was 96.2% for early-stage esophageal cancer, and 100% for early cancer of the gastric cardia. Perioperative complications included oozing bleeding in 5 patients (3.4%) and stricture in 1 (0.7%), no perforation occurred in this series., Conclusion: Endoscopic mucosal resection is suitable to treat precancerous lesions or early-stage esophageal cancers without invasion into submucosa. Compared with conventional resection through open thoracotomy, similar long-term survival and curative effect can be achieved by this EMR treatment, preserving a good quality of life.

A 9 kDa non-specific lipid-transfer protein (nsLTP) from mung bean (Phaseolus mungo) seeds, displaying antifungal activity, antibacterial activity and lipid-transfer activity, was crystallized at 297 K using ammonium sulfate as a precipitant by means of the hanging-drop vapour-diffusion method. Native X-ray diffraction data were collected to a resolution of 2.4 A. The crystals are rhombohedral, belonging to space group P2(1)2(1)2(1), with unit-cell parameters a = 38.671, b = 51.785, c = 55.925 A. Assuming the presence of one molecule in the crystallographic asymmetric unit results in a Matthews coefficient (V(M)) of approximately 3.0 A(3) Da(-1), corresponding to a solvent content of about 58%.

Aim: To study the mechanism of interaction between a series of potent racemic selective estrogen receptor modulators (SERM) and estrogen receptors (ER)., Methods: Active conformations of these conformationally restricted raloxifene analogues in binding pocket were determined by molecular mechanics. The interactive energies between ligand and receptor were calculated by docking program., Results: Both R and S configurations of these SERM were accommodated by the binding pocket of ER. The hydroxy group of compounds forms hydrogen bonds with amino acid residues of ER and the phenolic group mimics the A ring of estradiol. The most potential compounds were those with two hydroxy groups and accommodated by binding pocket in S configuration with phenolic group at C(16) imitating A ring of estradiol., Conclusion: Chiral center conferred little effect on the binding affinity of these conformationally restricted raloxifene analogues. The hydroxy group(s) play(s) a critical role to the orientation of compounds in active pocket of ER and the binding between ligand and receptor.