Preparation and 99mTc labeling of hydrazino nicotinamide modified RC-160 conjugate

1 INTRODUCTIONRadiopharmaceuticals based on small peptide have been currently received considerable illterests for the development of target specific imaging and therapeutic agents.lllln-DTPA-D-Phel-octreotide (Octreoscan), a synthetic peptide analogue of the somatostatin (SST), has fou-nd a widely clinical application for adaging a range of tumorsto date. RC-160 (Vapreotide) is another synthetic analogue of the native SST, which hasaffinity for a different set of SST sub-receptors …     

Adsorption of amino acids by fullerenes and fullerene nanowhiskers

We have investigated the adsorption of some amino acids and an oligopeptide by fullerene (C₆₀) and fullerene nanowhiskers (FNWs). C₆₀ and FNWs hardly adsorbed amino acids. Most of the amino acids used have a hydrophobic side chain. Ala and Val, with an alkyl chain, were not adsorbed by the C₆₀ or FNWs. Trp, Phe and Pro, with a cyclic structure, were not adsorbed by them either. The aromatic group of C₆₀ did not interact with the side chain. The carboxyl or amino group, with the frame structure of an amino acid, has a positive or negative charge in solution. It is likely that the C₆₀ and FNWs would not prefer the charged carboxyl or amino group. Tri-Ala was adsorbed slightly by the C₆₀ and FNWs. The carboxyl or amino group is not close to the center of the methyl group of Tri-Ala. One of the methyl groups in Tri-Ala would interact with the aromatic structure of the C₆₀ and FNWs. We compared our results with the theoretical interaction of 20 bio-amino acids with C₆₀. The theoretical simulations showed the bonding distance between C₆₀ and an amino acid and the dissociation energy. The dissociation energy was shown to increase in the order, Val < Phe < Pro < Asp < Ala < Trp < Tyr < Arg < Leu. However, the simulation was not consistent with our experimental results. The adsorption of albumin (a protein) by C₆₀ showed the effect on the side chains of Try and Trp. The structure of albumin was changed a little by C₆₀. In our study Try and Tyr were hardly adsorbed by C₆₀ and FNWs. These amino acids did not show a different adsorption behavior compared with other amino acids. The adsorptive behavior of mono-amino acids might be different from that of polypeptides.     

C谱紫外线对体外培养小鼠胚细胞的影响

本实验对紫外线致体外培养的小鼠胚细胞的效应进行了研究。胚细胞取自１１天胎龄绵小鼠前，后肢芽及中脑，并用小脑成纤维母细胞株３Ｔ３进行参照。实验结果表明，在０－３０Ｊ／ｍ＾２的紫外线照射下观察到胚细胞生长和分化抑制作用及胸腺嘧啶聚合物和光产物的形成。紫外线对胚细胞分化的抑制作用比对增殖和抑制作用强，其对ＤＮＡ的损伤作用在胚细胞与参照细胞间相似，这两类细胞对ＤＮＡ损伤的修复动力学相似。     

Effects of porosity on leaching of Ca from hardened ordinary Portland cement paste

Aiming at evaluating the effects of porosity in hardened cement paste on dissolution phenomena, we prepared hardened ordinary Portland cement (OPC), with variation in pore volume, and then leached them in deionized water. It was found that the bulk density and pore volume were affected by the dissolution of portlandite. The larger the pore volume of the sample, the more rapidly portlandite is dissolved. An electron probe microanalysis (EPMA) performed on the cross-section of the solid phase showed the ‘portlandite (CH) dissolution front’. As the leaching period became longer, the CH dissolution front shifted towards the inner part. In addition, the movement of the CH dissolution front was described by the diffusion model, with consideration of the dissolution of portlandite. It was concluded that the transport of leached constituents is diffusion controlled, and the major leached constituents of hardened OPC are portlandite and C-S-H gel. Large pore, which was generated associated with the leaching of portlandite, was considered significantly to affect the diffusion of leached constituents.     

Effect of reaction temperature on Fe–Al analcime formation

The effects of reaction period, temperature, and iron species on the zeolite framework type were studied in this work. Gismondine (GIS) is usually synthesized by hydrothermal method at 80°C from sodium metasilicate and aluminum nitrate as starting materials preferentially independent of the presence/absence of iron source. However, the present work revealed that pure analcime (ANA) could be formed at temperatures more than 120°C. A large polyhedral ANA crystal with a diameter of 180 μm was obtained even at a comparatively low temperature such as 150°C at a short reaction period of 1 week. The presence of iron source promoted the formation of pure ANA. Infrared spectroscopy, X-ray diffraction, and ICP-OES analysis suggested that the iron component added as a reactant was incorporated into the ANA framework through the isomorphous substitution for Al.     

The Role of Blood-Derived Factors in Protection and Regeneration of Aged Tissues

Tissue regeneration substantially relies on the functionality of tissue-resident endogenous adult stem cell populations. However, during aging, a progressive decline in organ function and regenerative capacities impedes endogenous repair processes. Especially the adult human heart is considered as an organ with generally low regenerative capacities. Interestingly, beneficial effects of systemic factors carried by young blood have been described in diverse organs including the heart, brain and skeletal muscle of the murine system. Thus, the interest in young blood or blood components as potential therapeutic agents to target age-associated malignancies led to a wide range of preclinical and clinical research. However, the translation of promising results from the murine to the human system remains difficult. Likewise, the establishment of adequate cellular models could help to study the effects of human blood plasma on the regeneration of human tissues and particularly the heart. Facing this challenge, this review describes the current knowledge of blood plasma-mediated protection and regeneration of aging tissues. The current status of preclinical and clinical research examining blood borne factors that act in stem cell-based tissue maintenance and regeneration is summarized. Further, examples of cellular model systems for a more detailed examination of selected regulatory pathways are presented.     

Neutrophil Elastase Deficiency Ameliorates Myocardial Injury Post Myocardial Infarction in Mice

Neutrophils are recruited into the heart at an early stage following a myocardial infarction (MI). These secrete several proteases, one of them being neutrophil elastase (NE), which promotes inflammatory responses in several disease models. It has been shown that there is an increase in NE activity in patients with MI; however, the role of NE in MI remains unclear. Therefore, the present study aimed to investigate the role of NE in the pathogenesis of MI in mice. NE expression peaked on day 1 in the infarcted hearts. In addition, NE deficiency improved survival and cardiac function post-MI, limiting fibrosis in the noninfarcted myocardium. Sivelestat, an NE inhibitor, also improved survival and cardiac function post-MI. Flow cytometric analysis showed that the numbers of heart-infiltrating neutrophils and inflammatory macrophages (CD11b⁺F4/80⁺CD206^low cells) were significantly lower in NE-deficient mice than in wild-type (WT) mice. At the border zone between intact and necrotic areas, the number of terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL)-positive apoptotic cells was lower in NE-deficient mice than in WT mice. Western blot analyses revealed that the expression levels of insulin receptor substrate 1 and phosphorylation of Akt were significantly upregulated in NE-knockout mouse hearts, indicating that NE deficiency might improve cardiac survival by upregulating insulin/Akt signaling post-MI. Thus, NE may enhance myocardial injury by inducing an excessive inflammatory response and suppressing Akt signaling in cardiomyocytes. Inhibition of NE might serve as a novel therapeutic target in the treatment of MI.     

Effects of the degree of crosslinking and test rate on the tensile properties of a crosslinked polyacrylic pressure-sensitive adhesive and vulcanized rubber

The effects of the tensile test rate on the properties of a pressure-sensitive adhesive (PSA) and of vulcanized rubber were ascertained and compared, using a poly(n-butyl acrylate-acrylic acid) random copolymer with varying degrees of crosslinking as the PSA. The 100% modulus of the PSA was found to increase along with the crosslinking degree and with faster tensile test rates. In contrast, the 100% modulus of the vulcanized rubber did not exhibit any test rate dependence. To assess this effect, the molecular weights between chemical and physical crosslinking points were determined via equilibrium swelling, dynamic mechanical analysis, and tensile tests. The proportion of physical crosslinking points was found to be far larger in the crosslinked PSA. Because these entanglement points can readily disentangle in response to slow deformation, variations in the test rate only affected the PSA. © 2018 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2019 , 136, 47272.