Advanced Materials Research Vols. 881-883

Abstract: (R)-tert-butyl (1-hydroxybut-3-yn-2-yl) carbamate, an key intermediate of the natural product jaspine B which was isolated from various sponges and endowed with cytotoxic activity against several human carcinoma cell lines, was synthesized from L-Serine in overall yield 41% through seven steps, including esterification, Boc protection, acetonization, reduction,Corey-Fuchs reaction and deprotection.

Abstract: Five alkaloids, (Z)-N-(4-hydroxystyryl) formamide (1), (E)-N-(4-hydroxystyryl) formamide (2), 2-(4-hydroxybenzyl) quinazolin-4(3H)-one (3), penipanoid A (4), asperazine (5), were isolated from cultures of Penicillium oxalicum, a fungus residing in Acrida cinerea. Their chemical structures were determined on the basis of spectroscopic data and chemical evidence. Compounds 1-5 were evaluated for their cytotoxic activity against the HepG2 and CaSki cell lines.

Abstract: Four 3-aminoindolizines were synthesized from the substituted 2-bromopyridines and propargyl amines with the aim of obtaining potential anti-inflammatory compounds, which were characterized by NMR, IR, ESI-MS and elemental analysis. Their biological activities were evaluated by the bacterial lipopolysaccharide (LPS) stimulation of mouse cells in the RAW264.7 inflammation model. The target compounds 4a-4d revealed moderate anti-inflammatory effects with the inhibitions of 45%~61% at 50 μM. The bioactive 3-aminoindolizines might be used for further optimization as potential anti-inflammatory drugs.

Abstract: Abstract:The blood substitutes refer to the substitutes of red blood cell with the ability to carry oxygen. This paper adopts open-loop coordination polymerization and gets amphiphilic triblock copolymer of mPEG-PAGE-PDLLA with the hydrophilic end-mPEG segment, and hydrophobic end-PLA segment. And it can be automatically assembled into vesicles in the water. The hemoglobin nanoparticles can be obtained by combining with Vesicle-coated hemoglobin, which are independently blended with oxygen and biodegradable. Meanwhile the paper makes an analysis of various physical and chemical properties to hemoglobin nanoparticles.

Abstract: The chemical composition of urinary crystallites of less than 1000 nm from 10 calcium phosphate (CaP) stone-formers were investigated and compared with that from healthy subjects using X-ray power diffraction, Fourier transform infrared spectroscopy and nanoparticle size analyzer. Although there were some calcium oxalate monohydrate (COM) crystals in CaP stones, the main components of crystallites in urine of CaP stone formers were uric acid (UA), CaP and COM, while that in healthy urine was mainly UA and a small amount of COM. That is, the CaP content in urinary crystallites of CaP stone-formers was significantly higher than that of controls. The particle size range of crystallites in lithogenic urine was 3~1000 nm and most of these crystallites were aggregated, but it was 30~500 nm in healthy subjects.

Abstract: The 1,7-dioxadispiro [5.1.5.-pentadecane spirocyclic architecture is the main structural feature in the aculeatins which attracted scientists interesting for the remarkably high cytotoxicity, anti-bacterial and anti-protozoal activities. A prophase study on concise synthesis of the core 1,7-dioxadispiro [5.1.5.-pentadecane spirocyclic architecture of aculeatins was accomplished by using Mukaiyama aldol reaction.

Abstract: Venlafaxine (Figure 1) is the new generation antidepressant drug. A synthetic route to the asymmetric synthesis of (R)-venlafaxine through Evans Aldol protocol was designed. The key intermediate, (R)-2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl) ethyl4-methylbenzenesulfonate was prepared from cyclohexanone.

Abstract: Heme oxygenase (HO) is the rate-limiting intracellular enzyme of heme catabolism. Overexpressed HO-1 can inhibit the apoptosis of tumor cells and promote tumor growth and metastasis, and (HO-1) has been considereded to play a major role in the pathogenesis of many tumors. Medulloblastomas (MB) are the most common malignant brain tumors in children and constitute 20% of all pediatric brain tumors. However, there is no report about clinicopathological significance of HO-1 and HO-2 expression in medulloblastoma (MB). In the present study, to explore the expression and potential function of HO in MBs, immunohistochemistry was used to examine the HO-1 and HO-2 expression in 41 MBs. The result showed that immunoreactivity of HO-1 was detected in 32 of 41 MBs and HO-2 was detected in 30 of 41 MBs, and their expression level had no significant correlations with the clinical features of the patients and subtypes of MB. In addition, the prognoses were better in those high HO-1 expression and low HO-2 expression cases. Taken together, the expression of HO-1 and HO-2 protein is significantly correlated with tumor growth in MB. The co-ordinated expression of HO-1 and HO-2 may affect the survival of MB patients. These results suggest that HO-1 may be a potential therapeutic target for MB.

Abstract: To meet the bone defect on the personalized needs of implantation, this study presents the manufacture of personalized thyroid cartilage hydroxyapatite (HA) scaffold by the rapid prototyping(RP) technique combined with CT image reconstruction and employs the foaming of suspensions prior to the in situ polymerization of organic monomers contained in the compositions. The organic additives are eliminated at temperatures above 300°C, and sintering is carried out for consolidation of the ceramic matrix. Spherical interconnected cells with sizes ranging from 100μm to 250μm characterize the porous structure, depending on the specimen density. The biological properties of porous personalized scaffolds loaded with bone morphogenetic protein 2 (rhBMP-2) were evaluated, by which a simulated surgical method of thyroid cartilage defects in rabbits and repairing with artificial scaffolds, and compared with rhBMP-2 loaded dense personalized or porous non-personalized scaffolds. The results of the histological analysis and the electronic laryngoscope inspection of airway indicate that rhBMP-2/HA/ porous personalized scaffolds is a promising composite having osteogenic efficient enough for repairing thyroid cartilage defects.

Abstract: In the present work,we developed a simple,fast,sensitive and inexpensive method to determine 6-mercaptopurine (6-MP) in pharmaceutical sample using Fe (III)-potassium ferricyanide system by spectrophotometry.The results show that in acid medium, Fe (Ш) can be reduced to Fe (II) by hydrosulfuryl (-SH) in 6-Mercaptopurin molecule, and then Fe (II) reacts with potassium ferricyanide to form a soluble Prussian blue (KFe^III[Fe^II(CN)₆]),the content of 6-MP was determinated indirectly through determinating the absorbance of the soluble Prussian blue.The various effect factors on the determination of 6-MP by spectrophotometry using potassium Fe (III)-ferricyanide system were investigated in detail.The maximum absorption wavelength of chromogenic system was 755 nm, good linear relationship was obtained between the absorbance and the concentration of 6-MP in the range of 0.4120~2.884 μ g·/mL,the equation of the linear regression was A=0.0411+0.1462C (μ g·/mL),with a linear correlation coefficient was 0.9991.This proposed method had been successfully applied to determinate of 6-MP in real pharmaceutical,and the results agreed well with those obtained by pharmacopoeial method.