Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression

Two novel small molecule gonadotropin-releasing hormone (GnRH) receptor antagonists (12 and 13) of the furamide-class were synthesized and evaluated in vitro for their receptor binding affinities for the rat GnRH receptor. Radiolabeling with no carrier added fluorine-18 of the appropriate precursors was investigated in a one-step reaction. Log P (Octanol/PBS pH 7.4) and serum stability of the compounds were investigated. The antagonists showed low nM affinity for the rat GnRH receptor. ¹⁸F-radiolabled compounds were obtained in high radiochemical purity (>95%) and specific activity (>75 GBq/μmol). These findings suggest this class of compounds holds promise as potential probes for PET targeting of GnRH-receptor expression.     

Cation export from Alaskan arctic watersheds

The concentrations and stream fluxes of Na, K, Ca and Mg were determined in 1978, 1980 and 1981 in the Toolik Lake watershed and in 1978 in the upper Kuparuk River watershed. The annual export of K was strongly influenced by high K concentrations at the initiation of spring melt. Potassium concentrations were positively correlated with concentrations of particulate and dissolved organic carbon, particulate and dissolved phosphorus, and particulate, dissolved organic and ammonium nitrogen, suggesting a common origin in the decomposition of tundra plants. Calcium and Mg stream concentrations were generally highest in July and August when the depth of the soil active layer reached a maximum of ∼ 0.5 m. Precipitation-derived Na and K accounted for up to half of the Na and K stream export while chemical weathering supplied > 85 % of exported Ca and Mg. Cation export rates in these arctic foothill watersheds are among the lowest recorded.     

Expression of pH-sensitive green fluorescent protein in Arabidopsis thaliana

This is the first report on using green fluorescent protein (GFP) as a pH reporter in plants. Proton fluxes and pH regulation play important roles in plant cellular activity and therefore, it would be extremely helpful to have a plant gene reporter system for rapid, non‐invasive visualization of intracellular pH changes. In order to develop such a system, we constructed three vectors for transient and stable transformation of plant cells with a pH‐sensitive derivative of green fluorescent protein. Using these vectors, transgenic Arabidopsis thaliana and tobacco plants were produced. Here the application of pH‐sensitive GFP technology in plants is described and, for the first time, the visualization of pH gradients between different developmental compartments in intact whole‐root tissues of A. thaliana is reported. The utility of pH‐sensitive GFP in revealing rapid, environmentally induced changes in cytoplasmic pH in roots is also demonstrated.     

MV-mimicking micelles loaded with PEG-serine-ACP nanoparticles to achieve biomimetic intra/extra fibrillar mineralization of collagen in vitro

Since their discovery, matrix vesicles (MVs) containing minerals have received considerable attention for their role in the mineralization of bone, dentin and calcified cartilage. Additionally, MVs' association with collagen fibrils, which serve as the scaffold for calcification in the organic matrix, has been repeatedly highlighted. The primary purpose of the present study was to establish a MVs–mimicking model (PEG-S-ACP/micelle) in vitro for studying the exact mechanism of MVs-mediated extra/intra fibrillar mineralization of collagen in vivo. In this study, high-concentration serine was used to stabilize the amorphous calcium phosphate (S-ACP), which was subsequently mixed with polyethylene glycol (PEG) to form PEG-S-ACP nanoparticles. The nanoparticles were loaded in the polysorbate 80 micelle through a micelle self-assembly process in an aqueous environment. This MVs–mimicking model is referred to as the PEG-S-ACP/micelle model. By adjusting the pH and surface tension of the PEG-S-ACP/micelle, two forms of minerals (crystalline mineral nodules and ACP nanoparticles) were released to achieve the extrafibrillar and intrafibrillar mineralization, respectively. This in vitro mineralization process reproduced the mineral nodules mediating in vivo extrafibrillar mineralization and provided key insights into a possible mechanism of biomineralization by which in vivo intrafibrillar mineralization could be induced by ACP nanoparticles released from MVs. Also, the PEG-S-ACP/micelle model provides a promising methodology to prepare mineralized collagen scaffolds for repairing bone defects in bone tissue engineering.     

Anatomical site of pheromone accumulation and temporal pattern of pheromone emission in the ambrosia beetle Megaplatypus mutatus

Megaplatypus mutatus (Chapuis) is a native South American ambrosia beetle that attacks live hardwood trees (e.g. Populus spp.), causing important economic losses to commercial plantations. Male beetles release the main components of the sex pheromone, namely (+)‐6‐methyl‐5‐hepten‐2‐ol [(+)‐sulcatol, or retusol] and 6‐methyl‐5‐hepten‐2‐one (sulcatone), when colonizing suitable hosts. The hindgut is shown to be the anatomical site of pheromone accumulation within males, the enantiomeric composition of sulcatol in this tissue is 99%‐(+) and sulcatol is first detectable in this tissue on days 1–2 after gallery initiation. Peak accumulation of sulcatol occurs on days 5–12 after gallery initiation. Trace quantities of sulcatone are also observed during the same period. Both pheromone components are present in male emissions from three host species (Populus×canadensis, Populus alba and Casuarina stricta) between days 2 and 12 after gallery initiation, although sulcatone is always present in low concentrations. The temporal patterns of sulcatol and sulcatone accumulation or storage in male M. mutatus correspond to the temporal patterns of emission.     

Rhythms of fragrance emission in flowers

A method for the sampling of volatiles emitted by individual flowers is described. Sampling over periods of 3 h allowed the examination of diurnal changes in quantity and quality of fragrance. In the species studied, Odontoglossum constrictum Lindl., Citrus medica L., Hoya carnosa R. Br., and Stephanotis floribunda Brongs., the fragrance was characterized by a few major components accompanied by a larger number of minor components. Flowers of all species produced volatiles in a rhythmical, diurnal fashion. Whereas in detached flowers of O. constrictum and C. medica rhythmicity could be observed for up to four cycles, flowers of H. carnosa showed this phenomenon only when attached to the plant. Maxima of emission were observed during the day in C. medica and O. constrictum whereas in H. carnosa it occurred during the night. In S. floribunda a conspicuous asynchronism of the emission of different volatiles was observed, resulting in the rhythmical change of fragrance quality.     

福建省土地利用碳排放空间关联性与碳平衡分区

全球变暖与二氧化碳浓度升高密不可分，在工业化及城镇化发展过程中，人类对土地的利用和改造是造成全球大气中含碳量迅速增加的重要原因，且土地在利用过程中碳减排的潜力较大。因此，从不同土地利用方式视角研究福建省碳排放量，采用基尼系数来衡量福建省各设区市碳收支的空间差异，探索区域内土地利用碳收支规模和空间分异；运用社会网络分析方法对福建省土地利用碳排放空间网络结构的整体特征和设区市在网络结构中的角色进行考察，有助于从基础层面对人类活动所造成的环境影响进行评估，及时调整土地利用方式从而促进低碳经济发展。结果表明：2006-2018年福建省土地利用净碳排放量逐年递增，呈现东高西低的空间分布特征，建设用地是主要碳源，而林地起到主要碳汇的作用；区域内碳补偿率逐年递减且存在明显的空间差异，经济较发达的区域碳补偿率低于经济欠发达的区域，生态承载系数东西差距不断加强，东部地区碳排放的比例明显超过了碳吸收的比例；福建省土地利用碳排放在空间上具有明显的关联性和溢出效应，碳排放空间关联网络越来越复杂、稳定，各设区市在网络中所处地位和作用存在明显的不均衡性，厦门市在整个碳排放网络中占据领导地位，其他城市的碳影响力在网络中的地位及作用随着经济联系逐渐加强正在逐步提高；对网络空间聚类发现，第一模块和第三模块对模块内外均有溢出效应且密度值较大，属于"双向溢出模块"，其余第二、四模块均属于"净收益模块"。在研究的基础上将福建省各设区市分为3类区域：低碳优化区、碳总量控制区和碳汇功能区，并提出协同减排的差异性对策建议。