抗菌肽改良设计及抗炎作用的研究进展

抗菌肽因其具有广谱抗菌活性、不容易引起抵抗性,被认为是先天免疫系统对抗微生物感染的多功能工具。然而,天然抗菌肽存在抗菌活性低、稳定性低、溶血性高等问题,使其较难应用于临床,所以研究人员对抗菌肽进行改良设计以期获得更高抗菌活性、更低溶血活性的新型抗菌肽。另外,天然抗菌肽作为一类免疫效应因子而被发现,其表现出的抑菌、免疫调节、内毒素中和等作用,使得研究人员对抗菌肽在抗炎作用的研究表现出极大的兴趣。就抗菌肽的药物设计方法及抗炎作用机制进行综述。     

Aromatic l-Amino Acid Decarboxylase Activity of the Rat Retina Is Modulated In Vivo by Environmental Light Maria Hadjiconstantinou

Aromatic L-amino acid decarboxylase (AAAD) activity of rat retina is low in animals placed in the dark. When the room lights are turned on, activity rises for almost 3 h and reaches values that are about twice the values found in the dark. A study of the kinetics of the enzyme revealed that the apparent Km values for L-3,4-dihydroxyphenylalanine and pyridoxal-5'-phosphate were unchanged in light- and dark-exposed animals, whereas the Vmax increased in the light. Treating the animals with cycloheximide before exposure to light prevented the increase of enzyme activity. Immunotitration with antibodies to AAAD suggested that more enzyme molecules are present in the light than in the dark. When the room lights are turned off AAAD activity drops rapidly at first and then more slowly, suggesting that at least two processes are responsible for the fall of enzyme activity. Exposure to short periods of dark followed by light results in a rapid increase of AAAD activity. Mixing homogenates from light- and dark-exposed rats results in activity values that are less than expected, suggesting the presence of an endogenous inhibitor(s). These studies demonstrate that AAAD activity is modulated in vivo.     

Identification of a deoxyribonuclease activity in the nuclei of the cervical carcinoma HeLa

A deoxyribonuclease activity has been identified in the nuclei of the human cervical carcinoma HeLa. This activity has the novel property of existing as a single strand specific endo- and exodeoxyribonuclease activity. These activities are ionic strength sensitive, with retardation of activity occurring at 50 mM NaCl and above, with the Mn++ ion preferred over the Mg++ ion as activating cation. This activity extensively damages DNA via its single strand nicking and gaping activity. The method used to solubilize this activity as well as the enzyme's characteristics are discussed.     

Outline of a matrix calculus for neural nets

The activity of a neural net is represented in terms of a matrix vector equation with a normalizing operator in which the matrix represents only the complete structure of the net, and the normalized vector-matrix product represents the activity of all the non-afferent neurons. The activity vectors are functions of a quantized time variable whose elements are zero (no activity) or one (activity). Certain properties of the structure matrix are discussed and the computational procedure which results from the matrix vector equation is illustrated by a specific example.     

Imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV-1

Synthesis of several novel imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV are described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity and pharmacokinetics are highlighted. Several compounds with low nanomolar anti-HIV activity and oral bioavailability are described.     

Enzymatic and chemical inactivation of partially purified prothoracicotropic (brain) hormone of the silkworm,Bombyx mori

The effects of various enzymatic and chemical treatments on the biological activity of the partially purified PTTH are described. PTTH was inactivated by pepsin, trypsin and α-chymotrypsin. Leucine aminopeptidase and carboxypeptidase A did not affect the biological activity of PTTH, suggesting that N- and C-terminus are blocked. Treatments with chemical reagents suggest that the tryptophan residue and disulfide bond are essential for the activity, whereas the sulfhydryl group is not. Tyrosinase exerted no effects. Glycosidases, neuraminidase, and periodate oxidation did not affect the activity, suggesting that carbohydrates are not essential for the biological activity of PTTH.     

龟类野外活动节律的研究进展

龟类野外活动具有时间尺度上的差异性和周期性,温度、湿度、光照、天气、年龄和性别差异等各种因子对龟的野外活动有着不同程度的影响.从日活动、季节活动两个不同时间尺度对龟类野外活动节律的研究成果做了系统总结,将休眠作为一种特殊的季节活动进行了小结,并对影响龟类野外活动节律的相关因子进行了分析和探讨.     

江滩与兴林垦种区钉螺体内几种酶活性的比较

在自动化分析仪上分析了兴林垦种林区内钉螺和草和滩钉螺的总蛋白（ＴＰｒ）含量和谷丙转氨酶（ＧＰＴ）、谷草转氨酶（ＧＯＴ）以及碱性磷酸脂酶（ＡＬＰ）的活力和比活力,及其受林地地下水位高度的影响,结果表明,林地钉螺的ＧＯＴ、ＧＰＴ酶活力和比活力均比滩于钉螺显著提高,ＡＬＰ活力较稳定,但比活力增加,林地内随地下水位降低,钉螺体内总蛋白含量下降,ＧＯＴ、ＧＰＴ比活力均显著升高。     

Enzyme histochemistry of malignant T cell lymphoma due to chronic magnesium deficiency in rats

The lymphocytes of the rat thymus can be grossly differentiated by their cell membrane-bound proteinases. Subcapsular thymocytes lack aminopeptidase A (APA) and AMP and gamma-glutamyltranspeptidase (GGT). Cortical thymocytes show a high activity of APA but no APM and no GGT. Medullar thymocytes possess a high GGT and APM activity but are free of APA. Under Mg deficiency, the APA-negative subcapsular thymocytes are reduced. In lymphoma and beginning lymphoma, APA, APM and GGT are absent. In lymphoma, the alkaline phosphatase activity is increased. Differences are found for dipeptidylpeptidase IV (DPP IV). In some lymphoma, its activity is reduced, in others the DPP IV activity is increased.     

Activity-dependent clustering of functional synaptic inputs on developing hippocampal dendrites

During brain development, before sensory systems become functional, neuronal networks spontaneously generate repetitive bursts of neuronal activity, which are typically synchronized across many neurons. Such activity patterns have been described on the level of networks and cells, but the fine-structure of inputs received by an individual neuron during spontaneous network activity has not been studied. Here, we used calcium imaging to record activity at many synapses of hippocampal pyramidal neurons simultaneously to establish the activity patterns in the majority of synapses of an entire cell. Analysis of the spatiotemporal patterns of synaptic activity revealed a fine-scale connectivity rule: neighboring synapses (<16?μm intersynapse distance) are more likely to be coactive than synapses that are farther away from each other. Blocking spiking activity or NMDA receptor activation revealed that the clustering of synaptic inputs required neuronal activity, demonstrating a role of developmentally expressed spontaneous activity for connecting neurons with subcellular precision.     

Reconstruction of behavior-relevant individual brain activity: an individualized fMRI study

Different patterns of brain activity are observed in various subjects across a wide functional domain.However,these individual differences,which are often neglected through the group average,are not yet completely understood.Based on the fundamental assumption that human behavior is rooted in the underlying brain function,we speculated that the individual differences in brain activity are reflected in the individual differences in behavior.Adopting 98 behavioral measures and assessing the brain activity induced at seven task functional magnetic resonance imaging states,we demonstrated that the individual differences in brain activity can be used to predict behavioral measures of individual subjects with high accuracy using the partial least square regression model.In addition,we revealed that behavior-relevant individual differences in brain activity transferred between different task states and can be used to reconstruct individual brain activity.Reconstructed individual brain activity retained certain individual differences which were lost in the group average and could serve as an individual functional localizer.Therefore,our results suggest that the individual differences in brain activity contain behavior-relevant information and should be included in group averaging.Moreover,reconstructed individual brain activity shows a potential use in precise and personalized medicine.     

Differences in cellulose digestive systems among castes in two termite lineages

Abstract.  Termites (Isoptera) are eusocial insects and express polyphenism. Soldiers have specialized morphology for colony defense, but their feeding activity is dependent on other colony members. To determine differences in cellulose degradation between soldier and worker termites, enzymatic activity and cellulase gene expression, as well digestive tract histology, are examined in two phylogenetically distant species. In Hodotermopsis sjostesti (family Termopsidae) , endo-β-1,4-glucanase activity is identified in the salivary glands, whereas β-glucosidase activity is identified in salivary glands and hindgut. The relative expression levels of endo-β-1,4-glucanase genes in soldiers are significantly lower than in workers. Thin sections of salivary gland of workers and soldiers are different in H. sjostedti . In Nasutitermes takasagoensis (family Termitidae), the endo-β-1,4-glucanase activity is restricted to the midgut in four tested castes (i.e. three types of workers and soldier). Examination of activity per termite reveals the highest activity in minor workers and the lowest activity in major workers and soldiers. The β-glucosidase activity is also concentrated on the midgut in all four castes. The relative expression level of the endo-β-1,4-glucanase gene does not correspond with its activity in the midgut. In thin sections prepared from N. takasagoensis , the folds and pulvillus in the gizzards, and cuticle structure of soldiers are less developed compared with the other three worker castes. The differences in digestive system among termite castes in terms of caste development in each species are discussed.     

Ornithine decarboxylase activity in relation to DNA synthesis in mouse interfollicular epidermis and hair follicles.

The relationship between ornithine decarboxylase (L-ornithine carboxylyase, EC 4.1.1.17) activity and DNA synthetic activity was studied in mouse epidermis. Interfollicular epidermis and hair follicles were investigated separately. It was found that, in hair follicles, the variations of DNA replicative activity, which are reflected in the cyclic growth of hair, are paralleled by corresponding changes in ornithine decarboxylase activity. In both interfollicular epidermis and hair follicles, stimulation of DNA synthetic activity by plucking of hair induced a rapid and marked increase in ornithine decarboxylase activity. The relationship of steady-state and induced ornithine decarboxylase activity to DNA synthetic activity was compared in hair follicles and interfollicular epidermis. A correlation between the activity of this enzyme and DNA replication was found thereby in each of these tissues.     

Ultrastructural distribution of peroxidase in thrombocytes of mammals and submammals

The localization and distribution of peroxidase (PPO) activity were studied ultracytochemically in thrombocytes from lampreys, carps, frogs, snakes, tortoises, rabbits, sheep, dogs, and monkeys. PPO activity was not detectable in the thrombocytes of lampreys, carps, frogs, and snakes. However, this enzyme activity was demonstrated in the nuclear envelope and endoplasmic reticulum of tortoise thrombocytes. Dog and monkey thrombocytes (blood platelets) exhibited PPO activity in the dense tubular system, but this enzyme activity was not detectable in rabbit and sheep thrombocytes. Our observations are interpreted to suggest that thrombocytes from animals lower than amphibia are peroxidase negative. Furthermore, it can be said that thrombocytes from animals higher than reptiles are generally positive, although there are exceptions. PPO activity was localized in the endoplasmic-reticulum system, but not in the cytoplasmic granules of thrombocytes common to submammals and mammals. In this study, we also compared the distribution of peroxidase activity in thrombocytes, neutrophils, and eosinophils and conclude that these are significant differences in the distribution of PPO and myeloperoxidase.     

河西走廊芦苇的光合碳同化途径对生境条件的适应

 本文以甘肃省河西走廊生长的四个不同生境芦苇为对象,比较研究了它们的叶解剖结构、光合关键酶活力、乙醇酸氧化酶活力和稳定碳同位素组成(δ13C)。结果发现,沼泽芦苇叶中虽具有不典型的花环结构,但维管束鞘细胞中不含叶绿体,RUBPcase活力／PEPcase活力比值为24.4,乙醇酸氧化酶活力为1218Unit mgpro-1·min-1δ13C值为-34‰,这些测值位于C3植物(小麦)的范围内。生长于沙丘上的芦苇叶片具有明显的花环结构,维管束鞘细胞内含异型叶绿体,RUBPcase活力／PEPcase活力比值为0.985, 乙醇酸氧化酶活力为504 Unitmgpro-1·min-1,δ13C值为-20.9‰,这些测值与典型C4植物(玉米)十分相似。盐化草甸芦苇和盐化草一沙丘过渡地带芦苇叶中均具有明显的花环结构,维管束鞘细胞中含大型叶绿体,RUBPcase活力／PEPcase活力比值分别为2.45和1.53,但乙醇酸氧化酶活力分别为1470和2058Unitmgpro-1·min-1,δ13C值分别为35.6和30.6‰,综合盐化草甸芦苇和过渡地带芦苇的上述指标,似介于沼泽芦苇和沙丘芦苇之间。由这些结果可以认为,分布于甘肃省河西走廊的芦苇,在种内发生有由环境因子引起的光合碳代谢途径的适应性改变。     

Bordetella pertussis adenylate cyclase toxin. Structural and functional independence of the catalytic and hemolytic activities.

The Bordetella pertussis calmodulin-dependent adenylate cyclase (CyaA) is a 1706-residue-long toxin, endowed with hemolytic activity. We have constructed B. pertussis mutant strains producing modified CyaAs devoid of adenylate cyclase activity. Our results show that such modified CyaAs display hemolytic activity identical to the wild-type toxin, thus demonstrating that the hemolytic activity is independent of the adenylate cyclase activity. Furthermore, B. pertussis and Escherichia coli strains producing CyaA lacking the catalytic domain (residues 1-373) were constructed. The truncated protein exhibits hemolytic activity comparable to the wild-type toxin, thus establishing that the carboxyl-terminal 1332 residues alone are endowed with hemolytic activity. Together, these findings show that adenylate cyclase and hemolytic activities are located in two distinct regions of the molecule (respectively, approximately amino acids 1-400 and 401-1706) and that the two regions of CyaA are functionally independent.     

高原鼠兔似昼夜活动节律的研究

本文对高原鼠兔活动节律的季节变化,不同光强对高原鼠兔似昼夜活动节律的影响,以及温度效应,饥俄效应等问题进行了研究。同时对昼夜节律研究中长期存在的理论问题,内源性和外源性观点提出探讨。     

Alcohol dehydrogenase thermostability variants in Drosophila melanogaster: Comparison of activity ratios and enzyme levels

Representatives of five allozymic classes of Drosophila alcohol dehydrogenase have been compared with respect to their activity levels on two alcohol substrates, quantities of ADH protein, and stability in crude extracts. Within each allozymic class, strains from widely diverse geographic locations differ in their enzyme activity levels but are identical for a measure known as "activity ratio," which is obtained by dividing the average activity reading on isopropanol by that obtained with ethanol. They are also similar in the rate at which ADH activity declines in crude extracts held at 25 degrees C. For several of the fast-resistant and fast-moderate strains, differences in ADH activity are associated with differences in the amount of enzyme present. The catalytic efficiencies of the fast-resistant forms are considerably lower than those of the fast-moderate allozymes. The origin and persistence of the rare but ubiquitous fast-resistant allozyme is discussed.     

Enzymes of the Glyoxylate Cycle in Chlorella vulgaris

The detection and assay of the enzymes of the glyoxylate cyclein Chlorella are described. The activity of the enzymes in cellsgrown on acetate is about adequate to account for the rate ofgrowth with acetate as sole carbon source. Isocitratase activity increases markedly when cells are incubatedwith acetate in darkness; malate synthetase activity also increasesbut the activity of the other enzymes is unaffected. Isocitrataseactivity does not increase when glucose is added as well asacetate or the cells are illuminated and supplied with carbondioxide. When cells are given acetate as sole carbon sourcethere is a lag of 24 hrs. before cell division begins; duringthis period, isocitratase activity increases greatly.