Bradykinin
(Synonyms: 缓激肽) 目录号 : GC35548
Bradykinin是一种强效血管舒张肽，通过刺激特异性内皮B2受体发挥血管舒张作用，诱导前列环素、一氧化氮和内皮衍生超极化因子的释放。
Cas No.:58-82-2
Sample solution is provided at 25 µL, 10mM.
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Bradykinin is a potent vasodilator peptide that exerts the vasodilatory action through stimulation of specific endothelial B2 receptors, thereby causing the release of prostacyclin, NO, and Endothelium-derived hyperpolarization factor[1]. Bradykinin is associated with the pathological physiological processes accompanying tissue damage and inflammation, and has been used as a regulator in studies on pain and hyperalgesia[2].
In vitro, Bradykinin treatment at 1µM for 16 hours significantly enhanced cell invasion and migration of SW480 cells, and stimulated the activation of ERK1/2 and the production of IL-6 in SW480 cells[3]. Treatment with 1 µM Bradykinin for 24 hours significantly increased the expression of tissue factor and plasminogen activator inhibitor-1 (PAI-1) at both mRNA and protein levels in rat aortic endothelial cells (RAEC)[4]. The treatment with Bradykinin (0.001µM) for 24 hours significantly reduced the senescence of cultured bovine aortic endothelial cells induced by 25μM H2O2, which was manifested by the complete inhibition of the increase in the number of senescent cells and a remarkable decrease in the level of the senescence-associated cell cycle protein p21[5].
In vivo, Bradykinin treatment via intraperitoneal injection at dose of 10mg/kg/day for 5 days significantly reduced the expression of fibrin, inhibiting deep vein thrombosis in mice with inferior cava vein ligation[6]. Intravenous injection of Bradykinin (40µg/kg) in mice can inhibit bronchial contraction caused by acetylcholine (0.5mg/kg; intravenous injection) within 15min[7].
References:
[1] Hornig B, Kohler C, Drexler H. Role of bradykinin in mediating vascular effects of angiotensin-converting enzyme inhibitors in humans[J]. Circulation, 1997, 95(5): 1115-1118.
[2] Dray A, Perkins M. Bradykinin and inflammatory pain[J]. Trends in neurosciences, 1993, 16(3): 99-104.
[3] Wang G, Ye Y, Zhang X, et al. Bradykinin stimulates IL-6 production and cell invasion in colorectal cancer cells[J]. Oncology reports, 2014, 32(4): 1709-1714.
[4] Kimura S, Tsuji H, Nishimura H, et al. Bradykinin enhances in vitro procoagulant and antifibrinolytic properties of rat vascular endothelial cells[J]. Thrombosis research, 2002, 106(1): 41-50.
[5] Oeseburg H, Iusuf D, van der Harst P, et al. Bradykinin protects against oxidative stress–induced endothelial cell senescence[J]. Hypertension, 2009, 53(2): 417-422.
[6] Dong R, Chen W, Feng W, et al. Exogenous bradykinin inhibits tissue factor induction and deep vein thrombosis via activating the eNOS/phosphoinositide 3-kinase/Akt signaling pathway[J]. Cellular Physiology and Biochemistry, 2015, 37(4): 1592-1606.
[7] Folkerts G, van Heuven-Nolsen D, Nijkamp F P. Bradykinin causes inhibition of methacholine-induced bronchoconstriction in vivo in mice[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2001, 364(1): 53-58.
Bradykinin是一种强效血管舒张肽，通过刺激特异性内皮B2受体发挥血管舒张作用，诱导前列环素、一氧化氮和内皮衍生超极化因子的释放[1]。Bradykinin参与组织损伤和炎症相关的病理生理过程，常作为疼痛和痛觉过敏研究的调节剂[2]。
在体外，1µM的Bradykinin处理16小时可显著增强SW480细胞的侵袭和迁移能力，并激活ERK1/2通路及促进IL-6生成[3]。1µM的Bradykinin处理24小时能显著提高大鼠主动脉内皮细胞（RAEC）组织因子和纤溶酶原激活物抑制因子-1（PAI-1）的mRNA及蛋白表达水平[4]。0.001µM的Bradykinin处理24小时可显著抑制25μM H2O2诱导的牛主动脉内皮细胞衰老，完全阻止衰老细胞数量增加并显著降低衰老相关细胞周期蛋白p21水平[5]。
在体内，腹腔注射Bradykinin（10mg/kg/day，持续5天）可显著抑制小鼠下腔静脉结扎模型中的纤维蛋白表达，减少深静脉血栓形成[6]。静脉注射Bradykinin（40µg/kg）能在15分钟内抑制乙酰胆碱（0.5mg/kg;静脉注射）引起的小鼠支气管收缩[7]。
| Cell experiment [1]: | |
Cell lines | SW480 cells |
Preparation Method | The SW480 cells were cultured in a DMEM medium containing 10% fetal bovine serum (FBS) at 37°C in a CO2 incubator. A 24-well transwell plate was used, which contained a 8-micron pore polyethylene terephthalate (PET) membrane. The upper layer of the plate was coated with a thin matrix gel. The cells (0.2ml of DMEM per well with 1.0×105 cells) were pretreated with different doses of Bradykinin (0.1, 0.5, and 1µM) and then added to the upper wells. The chemical attractant (20% FBS) was placed in the lower wells. After incubation in the CO2 incubator for 16 hours, the cells passing through the membrane were fixed and stained with eosin. The invasion of cells was observed under a microscope (100× magnification), and the number of invading cells was counted from five random fields. |
Reaction Conditions | 0.1, 0.5, and 1µM; 16h |
Applications | Bradykinin enhanced the invasion of SW480 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | The C57BL/6J mice were randomly divided into 3 groups: the sham operation group, the model group, and the Bradykinin group. Before the operation, the bradykinin group mice were intraperitoneally injected with Bradykinin (10mg/kg/day) for three consecutive days. On the fourth day, after being anesthetized by intraperitoneal injection of 60mg/kg pentobarbital, the midline incision was made to ligate the inferior vena cava (IVC), and the renal vein was dissected at the level of the renal vein. Then, the ligations were performed below the renal vein. After the ligations, the mice continued to receive Bradykinin injection for two more days, and 0.1mg/kg of buprenorphine was administered for analgesia for three days. The other groups of mice were given the same volume of normal saline as a control. The mice in the sham operation group underwent the same surgical procedures except for the ligation of the inferior vena cava. 48 hours later, the mice were euthanized by intraperitoneal injection of 100mg/kg pentobarbital, and the thrombosed inferior vena cava was collected after blood collection, weighed, and measured in length. The samples were frozen or stored for histological analysis. |
Dosage form | 10mg/kg/day for 5 days; i.p. |
Applications | Bradykinin treatment significantly led to a decrease in the expression of fibrin, significantly inhibiting thrombosis in the inferior vena cava of mice. |
References: | |
| Cas No. | 58-82-2 | SDF | |
| 别名 | 缓激肽 | ||
| 分子式 | C50H73N15O11 | 分子量 | 1060.21 |
| 溶解度 | Water: ≥ 100 mg/mL (94.32 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9432 mL | 4.716 mL | 9.4321 mL |
| 5 mM | 0.1886 mL | 0.9432 mL | 1.8864 mL |
| 10 mM | 0.0943 mL | 0.4716 mL | 0.9432 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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