Cyclo(-Gly-Pro)是一种具有口服活性的环状二肽，并表现出抗伤害感受活性。
Cas No.:3705-27-9
Sample solution is provided at 25 µL, 10mM.
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Cyclo(-Gly-Pro) is a cyclic dipeptide with oral activity, and exhibits antinociceptive activity [1]. Cyclo(-Gly-Pro) inhibits the Escherichia coli tryptophan indole-lyase (TIL) with a Ki value of 17μM through a mixed-type mechanism, which can reduce indole production in bacterial cultures and human fecal samples [2]. Cyclo(-Gly-Pro) has been widely used to inhibit the growth of tumor cells, suppress chitinase and enhance the antibiotic production of microorganisms[3].
In vitro, Cyclo(-Gly-Pro) treatment for 1 hour significantly inhibited the production of TNF-α in RAW 264.7 macrophages induced by lipopolysaccharide (LPS), with an IC50 value of 4.5μg/ml[4].
In vivo, sixty minutes before subcutaneous injection of formalin, intraperitoneal injection of 10μmol/kg dose of Cyclo(-Gly-Pro) (dissolved in 0.9% NaCl) could alleviate the nociceptive behaviors and inflammatory responses in mice[5].
References:
[1] Liu S, Mohri S, Manabe Y, et al. Gly-Pro protects normal human dermal fibroblasts from UVA-induced damages via MAPK-NF-κB signaling pathway[J]. Journal of Photochemistry and Photobiology B: Biology, 2022, 237: 112601.
[2] Oikawa D, Nakayama T. Cyclo-glycylproline, a food-derived diketopiperazine, inhibits bacterial indole production: implications for diabetic nephropathy prevention[J]. Bioscience, Biotechnology, and Biochemistry, 2026, 90(1): 57-65.
[3] Hu L, Lin J, Qin F, et al. Exploring Sources, Biological Functions, and Potential Applications of the Ubiquitous Marine Cyclic Dipeptide: A Concise Review of Cyclic Glycine-Proline[J]. Marine Drugs, 2024, 22(6): 271.
[4] Khan R, Basha A, Goverdhanam R, et al. Attenuation of TNF-α secretion by L-proline-based cyclic dipeptides produced by culture broth of Pseudomonas aeruginosa[J]. Bioorganic & Medicinal Chemistry Letters, 2015, 25(24): 5756-5761.
[5] Ferro J N S, de Aquino F L T, de Brito R G, et al. Cyclo‐Gly‐Pro, a cyclic dipeptide, attenuates nociceptive behaviour and inflammatory response in mice[J]. Clinical and Experimental Pharmacology and Physiology, 2015, 42(12): 1287-1295.
Cyclo(-Gly-Pro)是一种具有口服活性的环状二肽，并表现出抗伤害感受活性[1]。Cyclo(-Gly-Pro)通过混合型机制抑制大肠杆菌色氨酸吲哚裂解酶，Ki值为17μM，可减少细菌培养物和人类粪便样本中吲哚的产生。Cyclo(-Gly-Pro)已被广泛用于抑制肿瘤细胞生长、抑制几丁质酶并增强微生物的抗生素产生[3]。
在体外，Cyclo(-Gly-Pro)处理脂多糖诱导的RAW 264.7巨噬细胞1小时，显著抑制了TNF-α的产生，IC50值为4.5μg/ml [4]。
在体内，在皮下注射福尔马林前60分钟，腹腔注射10μmol/kg剂量的Cyclo(-Gly-Pro)（溶于 0.9% NaCl），可减轻小鼠的伤害性行为和炎症反应[5]。
| Cell experiment [1]: | |
Cell lines | RAW 264.7 cells |
Preparation Method | RAW 264.7 cells were cultured in DMEM medium supplemented with 10% FBS in a humidified atmosphere of 5% CO2 at 37°C and passaged every 1-2 days to maintain logarithmic growth. 10000 cells were seeded per well in a 96-well plate overnight. Cells were pre-incubated with different concentrations of Cyclo(-Gly-Pro) (0.1, 1, 10, and 100μg/ml) for 1h, and then stimulated with 1mg/mL LPS for another 6h. The cytokine concentrations were calculated. |
Reaction Conditions | 0.1, 1, 10, and 100μg/ml; 1h |
Applications | Cyclo(-Gly-Pro) treatment reduced the TNF-α production in RAW 264.7 cells in a dose-dependent manner after treatment with LPS. |
| Animal experiment [2]: | |
Animal models | Male Swiss mice |
Preparation Method | Male Swiss mice (weighing 18-22g) were housed in a temperature/humidity-controlled room on a 12h/12h light/dark cycle with free access to food and water. Mice were injected with formalin (2.5%, 20μl) in the subplantar area of the right hind paw. The time of paw licking (in seconds) was determined over 0-5min (early phase, neurogenic) and 15-30min (late phase, inflammatory) after formalin injection. Mice (n=6) were pretreated with Cyclo(-Gly-Pro) (10μmol/kg; i.p.) 60min before intraplantar injection of the stimulus or the reference compound, morphine (17.5μmol/kg, i.p.), 1h before administration of formalin. Control mice were treated with sterile saline. Analysis of the effect of Cyclo(-Gly-Pro) treatment on the harmful sensation induced by formalin. |
Dosage form | 10μmol/kg for once; i.p. |
Applications | Cyclo(-Gly-Pro) treatment significantly reduced nociceptive behaviors and inflammatory responses in mice. |
References: | |
| Cas No. | 3705-27-9 | SDF | |
| 别名 | 六氢吡咯并[1,2-A]吡嗪-1,4-二酮 | ||
| 分子式 | C7H10N2O2 | 分子量 | 154.17 |
| 溶解度 | Soluble 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 | 6.4863 mL | 32.4317 mL | 64.8635 mL |
| 5 mM | 1.2973 mL | 6.4863 mL | 12.9727 mL |
| 10 mM | 648.6 μL | 3.2432 mL | 6.4863 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 | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00% Appearance: A solid
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