运动对心血管系统内皮素的影响

采用文献资料研究法,分析了内皮素的产生及作用机制,探讨了运动对内皮素的影响,提出不同运动使内皮素发生不同改变,在运动过程中内皮素参与机体水、电解质平衡的调节及心脏的重塑.为心脏内分泌功能的研究提供新的思路和参考.     

Cloning of a cDNA encoding a non-isopeptide-selective subtype of the endothelin receptor

Endothelin-1 was initially identified as a 21-residue potent vasoconstrictor peptide produced by vascular endothelial cells, but was subsequently found to have many effects on both vascular and non-vascular tissues. The discovery of three isopeptides of the endothelin family, ET-1, ET-2 and ET-3, each possessing a diverse set of pharmacological activities of different potency, suggested the existence of several different endothelin receptor subtypes. Endothelins may elicit biological responses by various signal-transduction mechanisms, including the G protein-coupled activation of phospholipase C and the activation of voltage-dependent Ca2+ channels. Thus, different subtypes of the endothelin receptor may use different signal-transduction mechanisms. Here we report the cloning of a complementary DNA encoding one subtype belonging to the superfamily of G protein-coupled receptors. COS-7 cells transfected with the cDNA express specific and high-affinity binding sites for endothelins, responding to binding by the production of inositol phosphates and a transient increase in the concentration of intracellular free Ca2+. The three endothelin isopeptides are roughly equipotent in displacing 125I-labelled ET-1 binding and causing Ca2+ mobilization. A messenger RNA corresponding to the cDNA is detected in many rat tissues including the brain, kidney and lung but not in vascular smooth muscle cells. These results indicate that this cDNA encodes a 'nonselective' subtype of the receptor which is different from the vascular smooth muscle receptor.     

运动训练与内皮素

内皮素对人体具有广泛的生物学效应.简要介绍了内皮素的生物学功能,并从不同方式运动对内皮素分泌的影响、运动影响心血管系统内皮素分泌的机制及内皮素对运动时心血管系统的作用等几个方面进行综述.     

内皮素与妇产科疾病

为探讨内皮素含量的高低与某些妇产科疾病的关系，从内皮素的产生、分布及其与妇产科疾病的关系等方面进行了简要综述。     

运动对内皮素分泌影响的分析与研究

运动作为一种特殊刺激会引起机体内皮细胞分泌水平发生改变．该文总结人们研究的不同运动形式、不同运动强度及运动训练对内皮素分泌的影响，旨在促进运动对内皮素分泌的影响的研究，并为在运动训练中，探索合理的运动强度和运动时间，提高运动成绩，防止运动性疾病产生提供科学的依据。     

Endothelins are vascular-derived axonal guidance cues for developing sympathetic neurons

During development, sympathetic neurons extend axons along a myriad of distinct trajectories, often consisting of arteries, to innervate one of a large variety of distinct final target tissues. Whether or not subsets of neurons within complex sympathetic ganglia are predetermined to innervate select end-organs is unknown. Here we demonstrate in mouse embryos that the endothelin family member Edn3 (ref. 1), acting through the endothelin receptor EdnrA (refs 2, 3), directs extension of axons of a subset of sympathetic neurons from the superior cervical ganglion to a preferred intermediate target, the external carotid artery, which serves as the gateway to select targets, including the salivary glands. These findings establish a previously unknown mechanism of axonal pathfinding involving vascular-derived endothelins, and have broad implications for endothelins as general mediators of axonal growth and guidance in the developing nervous system. Moreover, they suggest a model in which newborn sympathetic neurons distinguish and choose between distinct vascular trajectories to innervate their appropriate end organs.     

内皮素对心脏功能的影响

内皮素(Endothelin,ET)是由血管内皮细胞产生的具有强烈缩血管作用的血管活性肽.大量实验表明,内皮素对心脏具有广泛的影响,使冠状血管收缩,对心脏产生正性肌力作用,通过内皮素受体参与神经体液因素对心肌细胞的调节作用.     

EGF receptor transactivation by G-protein-coupled receptors requires metalloproteinase cleavage of proHB-EGF

Cross-communication between different signalling systems allows the integration of the great diversity of stimuli that a cell receives under varying physiological situations. The transactivation of epidermal growth factor receptor (EGFR)-dependent signalling pathways upon stimulation of G-protein-coupled receptors (GPCRs), which are critical for the mitogenic activity of ligands such as lysophosphatidic acid, endothelin, thrombin, bombesin and carbachol, provides evidence for such an interconnected communication network. Here we show that EGFR transactivation upon GPCR stimulation involves proHB-EGF and a metalloproteinase activity that is rapidly induced upon GPCR-ligand interaction. We show that inhibition of proHB-EGF processing blocks GPCR-induced EGFR transactivation and downstream signals. The pathophysiological significance of this mechanism is demonstrated by inhibition of constitutive EGFR activity upon treatment of PC3 prostate carcinoma cells with the metalloproteinase inhibitor batimastat. Together, our results establish a new mechanistic concept for cross-communication among different signalling systems.     

ET_A受体拮抗剂杨梅酸A的半合成研究

合成了潜在的特定ETA受体拮抗剂杨梅酸A。合成方法是通过廉价易得的齐墩果酸为原料,通过3-OH Dess-Martin（DMP）氧化、臭氧化、液氨还原等11步反应,得到杨梅酸A,中间体及目标产物的结构通过^1H NMR、^13C NMR进行了表征。     

慢性肝病患者血浆内皮素含量与肝损害的关系研究

探讨血浆内皮素（ET）在慢性肝病患者中的变化规律以及与肝损害的关系。用放射免疫法测定110例慢性肝病患者及30例正常人血浆ET含量。结果表明，各种类型的慢性肝病患者血浆ET水平均显著高于正常组，且与临床类型有关。ET水平与谷丙转氨酶（ALT）及血清胆红素（SB）呈正相关，与白／球比例（A／G）和凝原酶原时间（PT）呈负相关，与甲胎球蛋白（AFP）无显著相关性。提示ET与肝病的慢性化程度及肝损害程度有关，可作为病情及预后判断的一项指标。