Enantiomeric Cyclic Peptides with Different Caco‐2 Permeability Suggest Carrier‐Mediated Transport

Recently, oral absorption of cyclic hexapeptides was improved by N‐methylation of their backbone amides. However, the number and position of N‐methylations or of solvent exposed NHs did not correlate to intestinal permeability, measured in a Caco‐2 model. In this study, we investigate enantiomeric pairs of three polar and two lipophilic peptides to demonstrate the participation of carrier‐mediated transporters. As expected, all the enantiomeric peptides exhibited identical lipophilicity (logD_7.4) and passive transcellular permeability determined by the parallel artificial membrane permeability assay (PAMPA). However, the enantiomeric polar peptides exhibited different Caco‐2 permeability (P_app) in both directions a–b and b–a. The same trend was observed for one of the lipophilic peptide, whereas the second lipophilic enantiomer pair showed identical Caco‐2 permeability (within the errors). These findings provide the first evidence for the involvement of carrier‐mediated transport for peptides, especially for those of polar nature.     

A characterization of adding machine maps

Let f :X→X be a continuous map of a compact metric space to itself. We prove that f is topologically conjugate to an adding machine map if and only if X is an infinite minimal set for f and each point of X is regularly recurrent. Moreover, if X is an infinite minimal set for f and one point of X is regularly recurrent, then f is semiconjugate to an adding machine map.     

THE CLASSIFICATION AND PERIOD OF STATES FOR MARKOV CHAIN IN RANDOM ENVIRONMENT

This paper is a continuation of [8]. In Section 1, three kinds of communication are introdnced for two states and the relations among them are investigated. In Section 2, two kinds of period of a state are introdnced and it is obtained that the period is a “class property” ,i.e. two states x and y belong to same class implies the period of x is equal to the period of y.     

一类递归集的Hausdorff维数及Bouligand维数

本文给出递归集的Ｈａｕｓｄｏｒｆｆ维数的下界估计，并由此确定了一类递归集的维数，所获结果包含并推广了Ｂｅｄｆｏｒｄ，Ｄｅｋｋｉｎｇ及文志英、钟红柳等人的有关结果。     

On distributionally regenerative processes

The paper is concerned with characterization results for distributional regeneration. It is shown that distributional regeneration is equivalent to renewal representation of the associated (shift) Markov operator. A sufficient condition for the distributional regeneration of the transfer operator in terms of variation is also formulated. Finally, a minorization condition is formulated and proved to be sufficient for recurrent co-Feller operators.     

Subchronic oral toxicity (six months) of carboxyethylgermanium sesquioxide [(HOOCCH2CH2Ge)2O3]n in rats

After briefly renewing toxicological data on germanium compounds, the authors report on the subchronic oral toxicity of carboxyethylgermanium sesquioxide in rats. During six months, male and female animals received 1 g kg^?1. day^?1. No particular toxic symptoms, and no behaviour problems except a small decrease of body weight in male rats, at the end of the six-month experimentation period, were observed. A significant decrease of erythropoiesis and some significant changes in leucocyte ratios were demonstrated. The main marked effect was a moderate renal dysfunction characterized by a tubular disease with the presence of cylinders, swelling of tubulus cells and flocculus deposits. Germanium urinary excretion was constant and linked to the received dose. Six months later, no preferential accumulation in organs was evident.     

Different acute effects of oral and intratracheal administration of disodium arsenate and gallium arsenide on heme synthesis in rats

The acute influences of arsenic compounds on the metabolism of porphyrins and heme in various organs of rats after oral or intratracheal administration of disodium arsenate (Na₂HAsO₄) and gallium arsenide (GaAs) were examined and compared. For the oral administration experiments, 21 or 84 mg of Na₂HAsO₄, or 2 or 4 g of GaAs, per cm³ saline per kg body weight of each animal was administered to Jcl: Wistar male rats and the organs were removed after exsanguination from the vein of the right axilla under anesthesia with ether, 16 h after administration. In the case of intratracheal administration, rats given 8.2 or 16.4 mg of Na₂HAsO₄, or 0.2 or 0.4 g GaAs per cm³ saline per kg body weight were examined under the same experimental conditions as for the administration route. Increase in the body weight of rats was suppressed after intratracheal administration of the two arsenic compounds. In these rats the hematocrit value increased significantly. These changes were not shown by the orally administered rats. Elevation in δ-aminolevulinate synthase (ALA-S, EC 2.3.1.37) activity in erythroblasts by Na₂HAsO₄ was much higher after intratracheal administration than after oral administration. Suppression in the activities of δ-aminolevulinate dehydratase (ALA-D, EC 4.2.1.24) and porphobilinogen deaminase (PBG-D, EC 4.3.1.8) in peripheral erythrocytes by Na₂HAsO₄ and GaAs were stronger by intratracheal administration than by the oral route. Influences of GaAs on the activity of PBG-D in rat liver were shown to be more effective by oral administration than by the intratracheal route. Oral administration of Na₂HAsO₄ and GaAs had a stronger suppression effect on the activities of ALA-D and PBG-D in rat kidney. It seems from these results that the different extents of the influence of arsenic compounds might depend on the routes of intake.     

慢性胃炎、溃疡病患者血清、胃液和胃组织微量元素的测定及其临床意义

对慢性胃炎、溃疡病患者血清、胃液、胃组织中多种微量元素采用高频等离子体发射光谱法测定．结果：胃溃疡血清、胃组织钼低，Ｐ均＜０．０５；胃组织钙低，Ｐ＜０．０１．十二指肠溃疡血清、胃组织钼低，Ｐ均＜０．０５；胃组织钙高于对照组，Ｐ＜０．０１．并对健康人血清、胃液、胃组织微量元素进行测定，为科研提供了血清、胃液、胃组织微量元素的正常值。     

口腔癌相关唾液肿瘤生物标志物的分析检测研究进展

口腔癌系头颈部癌，癌组织均位于口腔内，其非侵入性早期诊断是减少该病死亡的有效手段.唾液系口腔癌变相关物质首先释放进入的体液，取材方便，安全无创，是口腔癌普查筛选、早期诊断的首选指标.本文对唾液肿瘤生物标志物的种类、目前国内外常用的检测方法进行概述，重点阐述新型电化学生物传感方法在口腔癌相关唾液肿瘤生物标志物检测方面的相关应用及其最新研究进展.并对口腔癌相关唾液肿瘤生物标志物电化学传感技术的未来发展方向提出展望，拟为其深入研究与应用提供参考.