Angiotensin (1-7)
(Synonyms: Asp-Arg-Val-Tyr-Ile-His-Pro ) 目录号 : GP10077
Angiotensin (1-7)是一种存在于心脏和肾脏的七肽，在血浆和心房组织中抑制血管紧张素转换酶(ACE)的IC50值分别为3.0和4.0μM。
Cas No.:51833-78-4
Sample solution is provided at 25 µL, 10mM.
Angiotensin (1-7), a heptapeptide found in the heart and kidney, inhibits angiotensin-converting enzyme (ACE) in plasma and atrial tissue with an IC50 of 3.0 and 4.0μM, respectively[1]. Angiotensin (1-7) has been identified as regulating blood pressure, cardiac function and smooth muscle and myocardial cell growth as well as renal function regulation[2]. Angiotensin (1-7) has been extensively studied for modulation of vascular function in various cellular and animal models[3].
In vitro, Angiotensin (1-7) treatment (1nM; 48h) effectively reduced the proliferation of DU-145 prostate cancer cells and induced a significant reduction in the expression of MKI67[4]. Treatment of mouse podocytes with Angiotensin (1-7) at 10μM for 24 hours reversed high glucose-induced reduction of podocyte viability, increase of podocyte apoptosis, reduction of nephrin, podocin, WT-1 and MasR protein expression, and up-regulation of AT1R expression[5]. Angiotensin (1-7) treatment (1.7μM; 18 hours) effectively reduced tube formation in human umbilical vein endothelial cells[6].
In vivo, Angiotensin (1-7) treatment via daily intraperitoneal injection at 2mg/kg ameliorated sepsis-induced cardiomyopathy in mice by reducing inflammatory response and mitochondrial damage through NF-κB and MAPK pathways[7]. A single dose of 45μg/kg Angiotensin (1-7) administration via gavage promoted the resolution of lipopolysaccharide-induced pleurisy in mice by reducing neutrophil numbers and M1 inflammatory macrophage frequency after 24h treatment[8].
References:
[1] Roks A J M, Van Geel P P, Pinto Y M, et al. Angiotensin-(1–7) is a modulator of the human renin-angiotensin system[J]. Hypertension, 1999, 34(2): 296-301.
[2] Padda R S, Shi Y, Lo C S, et al. Angiotensin-(1-7): a novel peptide to treat hypertension and nephropathy in diabetes?[J]. Journal of diabetes & metabolism, 2015, 6(10): 10.4172/2155-6156.1000615.
[3] Durand M J, Zinkevich N S, Riedel M, et al. Vascular actions of angiotensin 1–7 in the human microcirculation: novel role for telomerase[J]. Arteriosclerosis, Thrombosis, and Vascular Biology, 2016, 36(6): 1254-1262.
[4] Domińska K, Okła P, Kowalska K, et al. Angiotensin 1–7 modulates molecular and cellular processes central to the pathogenesis of prostate cancer[J]. Scientific Reports, 2018, 8(1): 15772.
[5] Lu J, Chen G, Shen G, et al. Ang-(1-7) attenuates podocyte injury induced by high glucose in vitro[J]. Archives of Endocrinology and Metabolism, 2023, 67: e000643.
[6] Anton L, Merrill D C, Neves L A A, et al. Angiotensin-(1–7) inhibits in vitro endothelial cell tube formation in human umbilical vein endothelial cells through the AT1–7 receptor[J]. Endocrine, 2007, 32(2): 212-218.
[7] Chen X S, Cui J R, Meng X L, et al. Angiotensin-(1–7) ameliorates sepsis-induced cardiomyopathy by alleviating inflammatory response and mitochondrial damage through the NF-κB and MAPK pathways[J]. Journal of Translational Medicine, 2023, 21(1): 2.
[8] de Carvalho Santuchi M, Dutra M F, Vago J P, et al. Angiotensin‐(1‐7) and alamandine promote anti‐inflammatory response in macrophages in vitro and in vivo[J]. Mediators of Inflammation, 2019, 2019(1): 2401081.
Angiotensin (1-7)是一种存在于心脏和肾脏的七肽，在血浆和心房组织中抑制血管紧张素转换酶(ACE)的IC50值分别为3.0和4.0μM[1]。Angiotensin (1-7)已被证实具有调节血压、心脏功能、平滑肌和心肌细胞生长以及肾功能的作用[2]。在多种细胞和动物模型中，Angiotensin (1-7)对血管功能的调节功能已被广泛研究[3]。
在体外，1nM浓度的Angiotensin (1-7)处理48小时能有效抑制DU-145前列腺癌细胞的增殖，并显著降低MKI67的表达[4]。用10μM浓度的Angiotensin (1-7)处理小鼠足细胞24小时，可逆转高糖环境导致的足细胞活力下降、细胞凋亡增加、nephrin/podocin/WT-1/MasR的蛋白表达降低，以及AT1R表达上调等现象[5]。1.7μM浓度的Angiotensin (1-7)处理18小时能有效抑制人脐静脉内皮细胞的管腔形成[6]。
在体内，每日腹腔注射2mg/kg剂量的Angiotensin (1-7)可通过NF-κB和MAPK通路减少炎症反应和线粒体损伤来改善脓毒症诱导的小鼠心肌病[7]。单次45μg/kg剂量的Angiotensin (1-7)经灌胃给药24小时后，能促进脂多糖诱导的小鼠胸膜炎的消退，表现为中性粒细胞数量和M1型炎症巨噬细胞频率的降低[8]。
| Cell experiment [1]: | |
Cell lines | DU-145 cell |
Preparation Method | The DU-145 cells underwent two or more passages following recovery from liquid nitrogen storage and cultured in DMEM medium under humidity-controlled conditions at 37 °C with 5% CO2. The standard supplements were also used, including 10% heat-inactivated Fetal Bovine Serum (FBS), 1mM Sodium Pyruvate, 10mM HEPES buffer, and antibiotics (penicillin 50U/ml; streptomycin 50mg/ml; neomycin 100mg/ml). Angiotensin (1-7) was added to the cell culture medium at concentration 1nM. Four hours before the end of incubation period (48 hours) a MTT working solution at final concentration of 0.5mg/ml was added to each well. Formazan crystals formed by viable cells were dissolved in 10% sodium deodecyl sulfate (SDS) solution in 0.01M HCl. The absorbance was measured at 570nm using a microplate reader. Cell viability (% of control) was calculated in relation to untreated cells. The changes in cell proliferation after Angiotensin (1-7) treatment (1nM; 48 hours) were determined using a BrdU Cell Proliferation Assay. |
Reaction Conditions | 1nM; 48h |
Applications | Angiotensin (1-7) significantly inhibited the viability and proliferation of DU-145 cells. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Male Wistar rats (10 weeks old, 200-250g) were given free access to standard rat chow and water during the experiment. Following a 5-day period of acclimatization, 120 rats were randomly divided into two groups: control group (n=15), receiving an intraperitoneal injection of normal saline, and diabetic group (n=105), receiving intraperitoneal injection of 65mg/kg streptozotocin (STZ) dissolved in sodium citrate buffer (pH 4.5). All diabetic rats received an intraperitoneal injection of insulin (2-3U) every 3 days to maintain blood glucose levels between 16.7 and 25mM to avoid death induced by excessively high blood glucose level. Twelve weeks after STZ injection, the diabetic rats were randomly divided into 7 treatment groups (n=15 per group): no-treatment group and Angiotensin (1-7) group that received subcutaneous injection of 800ng/kg/min of Angiotensin (1-7) by an embedded mini-osmotic pump. After treatment for 4 weeks, all rats were killed. Plasma and kidney samples from rats were collected for cytokine and histological analysis. |
Dosage form | 800ng/kg/min for 4 weeks; s.c. |
Applications | Angiotensin (1-7) treatment ameliorated streptozotocin-induced renal injury, attenuated glomerulosclerosis, and reduced the expression of TGF-β1, VEGF and NOX4. |
References: | |
| Cas No. | 51833-78-4 | SDF | |
| 别名 | Asp-Arg-Val-Tyr-Ile-His-Pro | ||
| 化学名 | Angiotensin (1-7) | ||
| Canonical SMILES | CCC(C)C(C(=O)NC(CC1=CN=CN1)C(=O)N2CCCC2C(=O)O)NC(=O)C(CC3=CC=C(C=C3)O)NC(=O)C(C(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC(=O)O)N | ||
| 分子式 | C41H62N12O11 | 分子量 | 899 |
| 溶解度 | ≥ 89.9mg/mL in DMSO | 储存条件 | Desiccate at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1123 mL | 5.5617 mL | 11.1235 mL |
| 5 mM | 0.2225 mL | 1.1123 mL | 2.2247 mL |
| 10 mM | 0.1112 mL | 0.5562 mL | 1.1123 mL |
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动物数量 | 只 |
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