人内皮素3性质、用途与生产工艺
内皮素是1988年由日本学者Yanagisawa从猪主动脉内皮细胞培养液中发现的一种强有力的血管收缩肽，它由21个氨基酸组成，是体内作用最强、持续时间最久的一种收缩血管的活性多肽。它不仅是存在于内皮细胞中的收缩血管、升高血压的循环激素，而且是广泛分布于神经组织、血管平滑肌及巨噬细胞中的一种潜在的神经递质和细胞生长因子。除血管内皮细胞外，其他多种细胞如神经元、表皮细胞、心肌细胞、肾上腺等细胞均能分泌内皮素，并以自分泌/旁分泌的方式参与促进细胞增殖及体内多系统的生理功能调节。目前发现生物体内有内皮素-1，2，3(ET-1，ET-2，ET-3)及血管活性肠收缩肽(vasoactiveintestinalconstrictor，VIC)4种异构肽，称为“内皮素家族”。ET-1主要在内皮细胞中表达，ET-2以肾脏表达较多，内皮素3主要在神经系统中表达，而VIC则是在小鼠体内发现的一种对肠道平滑肌有收缩作用的活性多肽。
人内皮素3与细胞表面上的内皮素受体B相互作用。在整个胚胎发育期间，EDN3参与神经嵴细胞，其从发育中的脊髓迁移到胚胎中的特定区域，在那里它们产生许多不同类型的细胞。人内皮素3和EDN3R对于大肠（肠神经）和黑素细胞（产生黑色素）中神经的形成是必需的。EDN3基因的突变与Waardenburg综合征相关，IV型的特征在于皮肤，毛发和眼睛着色的变化。人内皮素3基因的突变与导致严重便秘或肠梗阻的先天性巨结肠症相关。
Endothelin-3, human, mouse, rabbit, rat 是由21个氨基酸组成的血管活性肽，可与G蛋白连接的跨膜受体，ET-RA 和ET-RB 结合。
The endothelins (ETs) are a family of 21-amino-acid vasoconstrictor peptides comprising three distinct isoforms: ET-1, ET2 and Endothelin-3. Endothelin-3 is detected in plasma, heart, brain and vascular smooth muscle cells (VSMCs). The surface enzymes of VSMCs break down big Endothelin-3 to the corresponding mature peptide, Endothelin-3. Endothelin-3 down-regulate endothelin ETA receptor expression in coronary artery VSMCs without affecting receptor density or functional ETA receptor responses. By contrast, high concentrations of Endothelin-3 (100 nM) increase the expression of ETB receptors but abolish the vasoconstrictor response of the receptors, possibly due to the desensitizing effect of Endothelin-3. Endothelin-3 stimulates ENCC adhesion to various ECM components. Endothelin-3 induces rapid changes in ENCC shape and protrusion dynamics favouring sustained growth and stabilization of lamellipodia, a process coincident with the increase in the number of focal adhesions and activated β1-integrins.
Endothelin-3 at low concentrations may attenuate inflammatory responses via ETB2 activation and NO production. Endothelin-3, which acts mainly on ETB, at low concentrations specifically inhibited platelet-activating factor (PAF)-induced paw oedema, whereas neither ET-1 nor Endothelin-2, both of which act on ETA and ETB, showed inhibitory activity. The inhibition by ET-1 and Endothelin-3 (each 0.5 pmol/paw) in the presence of BQ-123 (66.4 ± 6.7 % and 65.4 ± 22.6 %, respectively), is comparable to that by Endothelin-3 (0.5 pmol/paw) alone (65.4 ± 10.9 %), whereas neither ET-1 nor Endothelin-3 in the presence of BQ-788 showed inhibitory activity.
人内皮素3
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