Bilirubin
(Synonyms: 胆红素) 目录号 : GN10555
Bilirubin是血红素分解代谢产生的黄色终产物，可抑制ADAMTS13对F485-rVWF73-H、D633-rVWF73-H和GST-rVWF71-11K的切割活性，IC50值分别为13μM、70μM和17μM。
Cas No.:635-65-4
Sample solution is provided at 25 µL, 10mM.
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Bilirubin, a yellow breakdown product of heme catabolism, inhibits the cleavage of F485-rVWF73-H, D633-rVWF73-H, and GST-rVWF71-11K by ADAMTS13, with the IC50 values of 13μM, 70μM, and 17μM, respectively[1]. Bilirubin is the ultimate breakdown product of haemoglobin and serves as a diagnostic marker of liver and blood disorders[2].
In vitro, Bilirubin treatment at 0.4μM for 24h significantly restored cell viability in both hypoxic (5% O2) and hyperoxic (80% O2) conditions and attenuated oxidative stress-induced responses in rat type II alveolar cells[3]. Treatment of rat hepatic stellate cells with 20mg/L bilirubin for 24 hours significantly inhibited cell viability, decreased the protein expression level of α-smooth muscle actin, and promoted cell apoptosis[4]. Bilirubin treatment at 600μM for 20 min significantly attenuated the bactericidal activity of E. coli in isolated human neutrophils[5].
In vivo, Bilirubin treatment via twice daily intraperitoneal injections at 25mg/kg for 10 days can effectively inhibit tumor growth and prolong the survival time of the mice 14 days after the establishment of the transplanted tumor model[6]. Sprague Dawley rats were intravenously injected with 60mg/kg Bilirubin within 5min, the hippocampal CA3 region of rats showed prolongation of peak latencies and a decrease of slopes of the evoked potentials[7]. Bilirubin treatment (100 mg/kg twice daily; i.p.) for two weeks effectively suppressed experimental autoimmune encephalomyelitis in SJL/J mice[8].
References:
[1] Lu R N, Yang S, Wu H M, et al. Unconjugated bilirubin inhibits proteolytic cleavage of von Willebrand factor by ADAMTS13 protease[J]. Journal of Thrombosis and Haemostasis, 2015, 13(6): 1064-1072.
[2] Fevery J. Bilirubin in clinical practice: a review[J]. Liver International, 2008, 28(5): 592-605.
[3] Endesfelder S, Schmitz T, Bührer C. Bilirubin Exerts Protective Effects on Alveolar Type II Pneumocytes in an In Vitro Model of Oxidative Stress[J]. International Journal of Molecular Sciences, 2024, 25(10): 5323.
[4] Tang Y, Zhang Q, Zhu Y, et al. Low concentrations of bilirubin inhibit activation of hepatic stellate cells in vitro[J]. Molecular Medicine Reports, 2017, 15(4): 1647-1653.
[5] Arai T, Yoshikai Y, Kamiya J, et al. Bilirubin impairs bactericidal activity of neutrophils through an antioxidant mechanism in vitro[J]. Journal of Surgical Research, 2001, 96(1): 107-113.
[6] Ollinger R, Kogler P, Troppmair J, et al. Bilirubin inhibits tumor cell growth via activation of ERK[J]. Cell Cycle, 2007, 6(24): 3078-3085.
[7] Zhang L, Liu W, Tanswell A K, et al. The effects of bilirubin on evoked potentials and long-term potentiation in rat hippocampus in vivo[J]. Pediatric research, 2003, 53(6): 939-944.
[8] Liu Y, Li P, Lu J, et al. Bilirubin possesses powerful immunomodulatory activity and suppresses experimental autoimmune encephalomyelitis[J]. The Journal of Immunology, 2008, 181(3): 1887-1897.
Bilirubin是血红素分解代谢产生的黄色终产物，可抑制ADAMTS13对F485-rVWF73-H、D633-rVWF73-H和GST-rVWF71-11K的切割活性，IC50值分别为13μM、70μM和17μM[1]。作为血红蛋白的最终分解产物，Bilirubin是肝脏和血液疾病的诊断标志物[2]。
在体外，0.4μM的Bilirubin处理24小时能显著恢复大鼠II型肺泡细胞在低氧（5% O2）和高氧（80% O2）条件下的细胞活力，并减轻氧化应激反应[3]。20mg/L的Bilirubin处理大鼠肝星状细胞24小时可显著抑制细胞活力、降低α-平滑肌肌动蛋白表达并促进细胞凋亡[4]。600μM的Bilirubin处理20分钟会显著减弱分离的人中性粒细胞对大肠杆菌的杀菌活性[5]。
在体内，移植瘤模型小鼠经腹腔注射Bilirubin（25mg/kg，每日两次，持续10天）可有效抑制肿瘤生长并延长生存期[6]。Sprague Dawley大鼠静脉注射60mg/kg剂量的Bilirubin（5分钟内完成）后，海马CA3区诱发电位的峰值潜伏期延长且斜率下降[7]。SJL/J小鼠经腹腔注射Bilirubin（100mg/kg，每日两次，持续两周）可有效抑制实验性自身免疫性脑脊髓炎的发展[8]。
| Cell experiment [1]: | |
Cell lines | Rat type II alveolar cells |
Preparation Method | Rat type II alveolar cells (AEC II) were seeded at a density of 2.5×104 cells /cm2 in complete Ham's F12 medium and cultured for 24 h before processing. Bilirubin was dissolved in 0.1M NaOH and filtered aseptically. The concentration of the Bilirubin stock solution was then adjusted to 1mM with sterile water. Aliquots of the stock solution can be stored in dark tubes at −20 °C until further use. On the day of the experiment, a fresh working solution of bilirubin was prepared with bovine serum albumin (BSA), dissolved in phosphate buffer solution (PBS, pH 7.4) at a concentration of 3% (w/v) and aseptically filtered. Further dilutions in complete cell medium were used to adjust the final Bilirubin concentration (0.1, 0.2, 0.3, and 0.4μM). To avoid photoisomerization of Bilirubin, all studies were performed in low light. One day after inoculation (DIV 1), AEC II cells were placed in a suitable cell incubator equipped with oxygen sensors and exposed to different oxygen concentrations (5%, 21%, and 80%). Exposure times were set at 4 h and 24 h, and cells were left untreated or treated with Bilirubin in the medium for 24h. Then, the medium was removed, the cells were washed once with PBS, and fresh medium containing MTT solution at a final concentration of 0.5mg/mL was added. After 4 hours, to dissolve formazan, a mixture of detergent and organic solvent (dimethyl sulfoxide; sodium dodecyl sulfate; glacial acetic acid) was added and shaken for 15 minutes. The absorbance of AEC II cells was measured at 570nm using a microplate reader. |
Reaction Conditions | 0.1, 0.2, 0.3, and 0.4μM; 24h |
Applications | Bilirubin treatment at 0.4μM significantly restored cell viability in both hypoxic (5% O2) and hyperoxic (80% O2) conditions and reduced cell death. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | BALB/c nude mice were maintained under specific pathogen-free conditions, food and water were supplied ad libitum. 2.5×106 HRT‑18 colon cancer cells were injected subcutaneously into the lower flank of the BALB/c nude mice. At 14 days, treatment was started by injection of 25mg/kg Bilirubin or PBS twice daily intraperitoneally for 10 days, and tumor diameters were measured daily using a caliper. Results are expressed as mean ± SD or mean ± SEM when indicated. |
Dosage form | 25mg/kg twice daily for 10 days; i.p. |
Applications | Bilirubin treatment potently inhibited tumor growth in mice and prolonged survival. |
References: | |
| Cas No. | 635-65-4 | SDF | |
| 别名 | 胆红素 | ||
| 化学名 | 3-[2-[[3-(2-carboxyethyl)-5-[(Z)-(3-ethenyl-4-methyl-5-oxopyrrol-2-ylidene)methyl]-4-methyl-1H-pyrrol-2-yl]methyl]-5-[(Z)-(4-ethenyl-3-methyl-5-oxopyrrol-2-ylidene)methyl]-4-methyl-1H-pyrrol-3-yl]propanoic acid | ||
| Canonical SMILES | CC1=C(NC(=C1CCC(=O)O)CC2=C(C(=C(N2)C=C3C(=C(C(=O)N3)C)C=C)C)CCC(=O)O)C=C4C(=C(C(=O)N4)C=C)C | ||
| 分子式 | C33H36N4O | 分子量 | 584.66 |
| 溶解度 | ≥ 8.85mg/mL in DMSO | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7104 mL | 8.552 mL | 17.104 mL |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4208 mL |
| 10 mM | 0.171 mL | 0.8552 mL | 1.7104 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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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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1. 首先保证母液是澄清的；
2.
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- Purity: >99.00%
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