Applications and constructions of benzazepine scaffolds in drug molecular design / 药学学报

Benzazepine is a kind of fused ring structure, which is composed of nitrogen-containing seven-membered ring and benzene ring. The introduction of benzazepine scaffolds into compounds can not only adjust the physicochemical properties, maintain or enhance the biological activities of the compounds, but also improve the pharmacokinetic properties, increase the brain permeability, and reduce the toxicity of hERG of the compounds, which is one of the privileged scaffolds for rational design and structural optimization of drug molecules. Benzazepine scaffolds can be constructed by different synthetic methods such as Dickmann condensation reaction, Mitsunobu reaction, Pictet-Spengler reaction, CMD reaction, multicomponent reactions (MCRs), metal catalysis reactions and asymmetric catalysis etc., which play an important role in enriching the structure diversity of drug molecules.

Anatomical study of the atypical azygos venous system and its clinical significance / 局解手术学杂志

Objective To investigate the morphology and classification of the atypical azygos venous system,and to provide reference for diagnosis and treatment of mediastinal and thoracic vascular diseases.Methods Thirty cadavers were perfused with 10%formalin solution, and immersed in the solution for one month before dissection.The vertebral levels of termination and diameters of the azygos,hemiazygos and accessory hemiazygos veins were examined.Results There were 24 cases of classical azygos venous system,which contained the azygos, hemiazygos and accessory hemiazygos veins.And there were 6 cases of atypical azygos venous system,which were further divided into 4 sub-groups.Namely,type a(2 cases)which showed an inverted"Y"shape;type b(2 cases)which was single column with hemiazygos and ac-cessory hemiazygos veins absent;type c(1 case)which showed an accessory hemiazygos vein draining into the left brachiocephalic vein;and type d(1 case)with azygos vein and double superior vena cava variation.Diameters of termination of the azygos,hemiazygos and accessory hemiazygos veins were(10.39 ±1.98)mm,(8.51 ±2.28)mm,and(6.29 ±1.56)mm,respectively.The vertebral levels of termination of the azygos,hemiazygos and accessory hemiazygos veins were T 4(83.3%),T7to T10,T4to T8respectively.Conclusion All morphometrical diameters and their termination levels can be used during preoperative CT evaluations before planning invasive mediastinal procedures.The re-sults of this study could be helpful in mediastinal surgery,mediastinoscopy and the surgery of the deformations of the vertebral column in the thoracic cavity.

Comparison of the flaps made by femtosecond laser and automated keratomes for sub-bowman keratomileusis / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Thin-flap laser in situ keratomileusis (LASIK) is the new trend of refractive error correction surgery, the formation of corneal flap is crucial for a success of LASIK surgery. This study aimed to assess and compare the variations of LASIK flap created by the IntraLase femtosecond laser, Moria One Use-Plus SBK and Moria M2 Single-Use 90 µm-head microkeratome using Anterior segment optical coherence tomography (Visante OCT).</p><p><b>METHODS</b>One hundred and sixty-one eyes of 81 consecutive patients were enrolled in this prospective study and randomly divided into three groups depending on the flap creation method: flap creation with the the IntraLase femtosecond laser (IntraLase group, 59 eyes), flap creation with the Moria One Use-Plus SBK (SBK group, 44 eyes), and flap creation with the Moria M2 Single-Use 90 µm-head microkeratome (M2SU90 group, 58 eyes). The nominal flap thickness was 110 µm for all patients and for the three devices. One month after surgery, Visante OCT was used to measure the flap thickness at 20 locations on each cornea and the results were assessed for uniformity, regularity, and accuracy.</p><p><b>RESULTS</b>At 1 month after surgery, the mean central flap thickness was (111 ± 3) µm in the IntraLase group, (114 ± 8) µm in the SBK group, and (118 ± 13) µm in the M2SU90 group respectively. The flaps in the IntraLase group and the SBK group were more regular, showing an almost planar configuration, than the meniscus-shaped flaps in the M2SU90 group. The maximum deviation from the intended flap thickness (110 µm) was 6 µm in the IntraLase group, 10 µm in the SBK group, and 20 µm in the M2SU90 group respectively. A difference greater than 20 µm was observed in 0.42% of measurements in the IntraLase group; 2.95% of the measurements in the SBK group and 21.12% of measurements in the M2SU90 group.</p><p><b>CONCLUSIONS</b>The flaps created by the IntraLase femtosecond laser and Moria One Use-Plus SBK are more uniform; more regular, and more accurate than those created by the Moria M2 Single-Use 90 µm-head microkeratome. The first two methods can make precise flaps for Sub-Bowman Keratomileusis.</p>

Identification of Chinese traditional medicine Angelicae Pubescentis Radix from different places by fourier transform infrared spectrometry / 中国中药杂志

Common and variation peak rates were calculated as dual-index for drug samples based on the infrared spectrogram of Angelicae Pubescentis Radix samples from different places. The results indicated that the common peak rates of 4 samples from Sichuan province, 2 samples from Gansu province, and 2 samples from Hubei province were higher than 73% , 79. 5% and 76. 3%, respectively. Also, the variation peak rates of 2 samples from Gansu province were lower than 12. 9%. Therefore, there is similar germplasm resources and similar chemical composition in the samples originated from the same place. However, for the samples originated from different places, their germplasm resources and chemical composition maybe have been changed. Fourier transform infrared spectrometry could be used to evaluate the rule of the fingerprint and overview of Angelicae Pubescentis Radix originated from different places by its changes of germplasm resources and chemical composition.

Comparison of flaps created with the Moria M2 microkeratome with regular blade Versus Med-Logics 0 blade / 中华实验眼科杂志

BackgroundFlap creation is one of the most important steps during laser in situ keratomileusis (LASIK). As the microkeratome blade technology is developing, the accuracy, uniformity and reproducibility of corneal flaps created by the microkeratome blade are of high clinical concern. ObjectiveThe aim of this trial was to compare the features of corneal flaps created using the Moria M2 microkeratome 110 μm-knife with regular blade versus the Med-Logics O blade. MethodsA pilot and prospective study was designed. Two hundred and four eyes of one hundred and two patients were enrolled in this clinical trial. The patients were divided into the Moria M2 microkeratome 110 μm-knife with Med-Logics 0 blade group ( 110-0 group) ( 102 eyes) and Moria M2 microkeratome with 110 μm-knife with regular blade group (110 group) (102 eyes),with the matched demography. Fourier-domain optical coherence tomography ( RTVue OCT) was used to measure flap thickness using 28 settings on the 204 corneas at one week postoperatively. The features of the LASIK flaps were analyzed on the basis of the outcomes. Written informed consent was obtained from each patient prior to LASIK. Results There was no statistically significant difference in uncorrected visual acuity and the mean spherical equivalent between the 110-0 group and 110 group ( Z =-0. 375,P =0. 708 ; u =0. 056, P =0. 956 ) one week after LASIK. The mean flap thickness of the 110-0 group was considerably thinner than that of the 110 group ( 133.28+15.41μ m versus 142.81 ±10. 07μm) ( u =-5. 227,P＜0. 001 ). The corneal flaps in both the 110-0 group and in 110 group showed a meniscus shape. The nasal flap thickness of the right eyes was not evidently different from that of temporal ( P＞0. 05 ) , but in the left eyes, nasal flap thickness was obviously thicker than the temporal flap thickness (P＜0. 05) in both groups. The mean deviation between the achieved and attempted flap thickness ( 130 μm) were (17.46±2.28) μm in the 110-0 group and ( 16. 82±6. 12) μm in the 110 group, showing a significant difference between them ( u ==0. 517, P=0. 608 ).ConclusionsThe shape of flaps created using the Moria M2 110-0 is more uniform and closer to the expected thickness of 130 μm than the ones created using the Moria M2 110 microkeratome.

Effects of HepII domain peptides V of fibronectin on corneal permeability, endothelial cells, intraocular pressure and morphology of trabecular meshwork in rats / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Trabecular meshwork (TM) cell volume may be an important determinant of aqueous humor outflow in the eye. This study aimed to evaluate the role of HepII domain peptides V on corneal permeability, corneal endothelial cells, intraocular pressure (IOP) and morphology of trabecular meshwork in rats.</p><p><b>METHODS</b>The IOP of rat eyes was measured before and 3, 5, 7 and 8 hours after topical delivery of HepII domain peptides V through intracameral injections. The peptide's concentration in aqueous humor was assessed by high performance liquid chromatography (HPLC). The shape and density of endothelial cells were observed by laser confocal microscopy 8 hours, 3 and 14 days after intracameral injections of HepII domain peptides V. The morphological changes in TM of rat eyes were assessed by transmission electron microscopy (TEM).</p><p><b>RESULTS</b>Intracameral injection of HepII domain peptides V significantly (P < 0.001) decreased IOP by (5.71 ± 2.10) mmHg in rats at 5 hours after injection. There were no obvious changes of the shape and the density of corneal endothelial cells. In addition, morphological changes in the TM of rats were observed including the expansion of intercellular spaces in the juxtacanalicular meshwork, removal of extracellular material, cellular relaxation, and cytoskeleton reorganization.</p><p><b>CONCLUSIONS</b>HepII domain peptides V could not penetrate cornea and was safe to corneal endothelial cells. HepII domain peptides V could significantly decrease IOP in rat probably by disorganizing actin cytoskeleton and cell-junction in the TM.</p>

Amic solution hydrolysis for improving content of astragaloside IV in extract of Radix Astragali / 中国中药杂志

<p><b>OBJECTIVE</b>To optimize amic solution hydrolysis technique for improving the content of astragaloside IV in extract of Radix Astragali.</p><p><b>METHOD</b>Orthogonal design was adopted to investigate the main factors that influenced hydrolysis. Choosing the content of astragaloside IV as inspecting index which determined by HPLC, total saponins was purified with the macro-reticular resine, and contents of saponins before and after hydrolysis were determined by colorimetry at 544 nm.</p><p><b>RESULT</b>The ratio of amic solution to herb medicine was most notable in the four inspected factors. The optimal technique of hydrolysis was that the ratio was 1:5, concentration of amic solution was 2%, and the time of regurgitant extraction at 90 degrees C was two hours. The content of astragaloside IV was notably higher than before by hydrolysis. Difference wasnt significant between the content of saponins before and after hydrolysis by colorimetry.</p><p><b>CONCLUSION</b>Content of astragaloside IV was obviously higher than that before hydrolysis,but the content of total saponins was not changed before and after hydrolysis. The results showed that the other saponins can be transformed into astragaloside IV by hydrolysis. This method was valuable, which provided basis on its industrialization.</p>