Selective delta-opioid receptor antagonism by ICI 174,864 in the central nervous system

The effects of the novel gamma-opioid receptor antagonist ICI 174,864 (N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH: Aib = alpha-aminoisobutyric acid) have been examined in the CNS in vivo using spontaneous reflex contractions of the rat urinary bladder as an index of activity. Bladder contractions were inhibited by equipotent intracerebroventricular (ICV) doses of the selective mu-agonist DAGO [D-Ala2, MePhe4,Gly-(ol)5]enkephalin and the delta-agonist DPDPE[D-Pen2, D-Pen5]enkephalin. ICI 174,864 (1-3 micrograms) administered by the same route produce a selective and reversible antagonism of DPDPE effects. At higher doses (6-15 micrograms, ICV) ICI 174,864 exhibited marked agonistic activity, producing inhibition of bladder contractions that were resistant to ICV naloxone (1-2 micrograms). Thus ICI 174,864 was considered a selective central delta-opioid receptor antagonist but its usefulness was limited by additional agonistic properties.     

Casein Kinase 1δ Stabilizes Mature Axons by Inhibiting Transcription Termination of Ankyrin

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In vivo CRISPR screens identify the E3 ligase Cop1 as a modulator of macrophage infiltration and cancer immunotherapy target

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马尾松和杉木树干韧皮部水溶性糖 δ13C值对气象因子的响应

通过测定亚热带马尾松和杉木树干韧皮部水溶性糖δ¹³C值的连日变化,及其对天气变化过程的响应,研究δ¹³C值对短期天气变化动态的响应特征。结果显示,春季马尾松和杉木树干韧皮部水溶性糖δ¹³C日均值分别介于-26.81‰到-26.49‰之间,以及-29.26‰到-27.47‰之间,平均值分别为(-26.58±0.12)‰和(-28.67±0.65)‰。进一步分析表明,马尾松树干韧皮部水溶性糖δ¹³C值与取样之前第4天的太阳辐射、水气压亏缺、相对湿度和空气温度显著相关(P≤0.05),杉木树干韧皮部水溶性糖δ¹³C值取样之前第3天的太阳辐射、水气压亏缺和相对湿度显著相关(P≤0.05),但与空气温度的相关性不显著(P≤0.05)。在所测定的环境因子中,太阳辐射是影响马尾松和杉木树干韧皮部水溶性糖δ¹³C值的首要因素。当天降水事件可能导致马尾松和杉木树干韧皮部水溶性糖δ¹³C值连日变化出现异常波动。马尾松和杉木韧皮部水溶性糖δ¹³C值可以敏感记录短期天气变化动态。     

基于稳定碳同位素技术的华北低丘山区核桃-小麦复合系统种间水分利用研究

农林复合系统的林木和作物会充分利用水肥光热等资源、而在资源亏缺时也可能产生竞争,在华北低丘山区等水资源紧缺地区,种间水分竞争尤为突出。在冬小麦返青期、拔节期、灌浆期和成熟期4个生育期,测算了该地区核桃-小麦间作系统和单作小麦不同组分的稳定碳同位素组成(Stable carbon isotope ratio,δ13C)和核桃树干液流,结合生物量和气象数据资料计算出水分利用效率(water use efficiency,WUE)和耗水量(Water use,WU)。结果表明,间作核桃树、间作小麦和单作小麦的WUE分别为10.771—21.233、9.946—19.149和9.878—18.431 mmol C/mol H2O。单作小麦WUE在拔节期显著小于间作小麦。间作系统总耗水量为1755.19 t/hm2,比单作系统的2538.13 t/hm2少30.85%。核桃-小麦间作系统中,核桃耗水量占系统总耗水量的36.34%,在小麦的生长前期所占比例最多、在小麦旺盛生长期所占比重较小,而小麦越往生长后期需水越多。核桃与间作小麦的需水期错开,在时间上避免水分竞争。距离核桃树越近浅层土土壤含水量越高、而深层土越低,表明核桃主要吸收深层水,而间作小麦主要吸收浅层水,从位置上避免水分竞争。单作小麦产量、总生物量和总耗水量分别比核桃间作小麦的高26.79%、27.12%、36.30%(P=0.001、P=0.033、P=0.050)。间作核桃和单作核桃的单株果实产量平均分别为0.88和0.94 kg(P=0.829)。然而,核桃-小麦间作系统的产量土地当量比(Land equivalent ratio,LER)和产值水分利用效率(WUE ofeconomics,WUEe)却分别达到1.67和25.92元.mm-.1hm-2,比单作系统明显提高、水资源获得高效利用,同时具备生产优势和经济优势。     

流溪河水库颗粒有机物及浮游动物碳、氮稳定同位素特征

为了解影响流溪河水库颗粒有机物(POM)碳和氮稳定同位素(δ¹³C和δ¹⁵N)变化的主要因素,及其与浮游动物δ¹³C和δ¹⁵N之间的关系,于2008年5月至12月份对POM及浮游动物的δ¹³C和δ¹⁵N进行了研究。颗粒有机物碳稳定同位素(δ¹³C_POM)和氮稳定同位素(δ¹⁵N_POM)的季节性变化幅度分别为5.1‰和2.2‰,5月和7月份δ¹³C_POM较高,而在10月和12月份降低,这主要与降雨将大量外源有机物带入水库而引起的外源及内源有机物在POM组成上发生变化有关。δ¹⁵N_POM总体呈上升趋势,可能是由降雨引起的外源负荷、初级生产力、生物固氮等因素共同作用的结果。浮游动物的δ¹³C及δ¹⁵N总的变化趋势与POM的相似,也具有明显的季节性变化,食物来源的季节变化可能是造成其变化的主要原因。在5月份,浮游动物的食物来源为POM中δ¹³C较高的部分,也就是外源有机物,而在10月及12月份,其食物则可能主要为浮游植物。     

Protein kinase Cdelta participates in insulin-induced activation of PKB via PDK1

PKCdelta has been shown to be activated by insulin and to interact with insulin receptor and IRS. PKB(Akt) plays an important role in glucose transport and glycogen synthesis. In this study, we investigated the possibility that PKCdelta may be involved in insulin-induced activation of PKB. Studies were conducted on primary cultures of rat skeletal muscle. PKB was activated by insulin stimulation within 5min and reached a peak by 15-30min. Insulin also increased the physical association between PKCdelta with PKB and with PDK1. The insulin-induced PKCdelta-PKB association was PI3K dependent. PKB-PKCdelta association was accounted for by the involvement of PDK1. Overexpression of dominant negative PKCdelta abrogated insulin-induced association of PKCdelta with both PKB and PDK1. Blockade of PKCdelta also decreased insulin-induced Thr308 PKB phosphorylation and PKB translocation. Moreover, PKCdelta inhibition reduced insulin-induced GSK3 phosphorylation. The results indicate that insulin-activated PKCdelta interacts with PDK1 to regulate PKB.     

Biochemical characterization of tau protein and its associated syndapin 1 and protein kinase Cɛ for their functional regulation in rat brain

Background

We recently reported that both sulfatide and cholesterol-3-sulfate (SCS) function as potent stimulators for the GSK-3β-mediated phosphorylation of tau protein (TP) in vitro [J. Biochem. 143 (2008) 359–367].

Methods

By means of successive gel filtration on a Superdex 200 pg column and three distinct ion-exchange column chromatographies, TP and its associated proteins were highly purified from the extract of rat brain.

Results

We found that (i) syndapin 1 and novel protein kinase C? (nPKC?) were identified as the TP-associated proteins; (ii) SCS highly stimulated the phosphorylation of TP and syndapin 1 by nPKC? as well as CK1; (iii) the full phosphorylation of TP and syndapin 1 by nPKC? in the presence of sulfatide resulted in their dissociation; (iv) TP primed by CK1 functioned as an effective phosphate acceptor for GSK-3β; (v) syndapin 1 highly stimulated the GSK-3β-mediated phosphorylation of TP; and (vi) TP isoforms were highly expressed in aged brain, whereas syndapin 1 was consistently detected in adult brain, but not in newborn brain.

General significance

These results provided here suggest that (i) TP-associated nPKC? suppresses the GSK-3β-mediated phosphorylation of TP through the phosphorylation of GSK-3β by the kinase in vitro; and (ii) SCS act as effective sole mediators to induce the GSK-3β-mediated high phosphorylation of both TP and its associated syndapin 1 involved in the biochemical processes of neuronal diseases, including Alzheimer's disease.