Mastoparan
(Synonyms: 黄峰毒素) 目录号 : GC12692
Mastoparan是一种来源于黄蜂毒液的肽类毒素，可刺激磷酸肌醇分解，EC50值为9μM。
Cas No.:72093-21-1
Sample solution is provided at 25 µL, 10mM.
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Mastoparan, a peptide toxin from wasp venom, induces stimulation of phosphoinositide breakdown with an EC50 value of 9μM[1]. Mastoparan accelerates guanosine-5'-3-O-thiotriphosphate binding and consequent GTP-binding regulatory protein (G protein) activation in part by enhancing the dissociation of bound GDP[2]. Mastoparan has been widely used in anti-inflammatory studies and as a model compound to develop related derivatives[3].
In vitro, Mastoparan exhibited an anticancer towards Hep-G2 cells with IC50=189.59±0.6µg/ml after 24h treatment[4]. Treatment with 25μM Mastoparan for 8h significantly induced cell death in Jurkat T leukemia cells and normal peripheral blood cells[5]. Mastoparan treatment at 20μM within 1min significantly induced a rapid increase in cytosolic-free Ca2+ concentration elevation in Tobacco BY-2 cells[6].
In vivo, Mastoparan treatment via a peritumor route at 5 mg/kg/day for 5 consecutive days inhibited the tumor growth in the murine melanoma model[7]. The combination therapy of gemcitabine (60mg/kg/day) and Mastoparan (6mg/kg/day) for 14 days via intraperitoneal injection significantly inhibited tumor progression in a mouse model of breast cancer[5].
References:
[1] Gusovsky F, Soergel D G, Daly J W. Effects of mastoparan and related peptides on phosphoinositide breakdown in HL-60 cells and cell-free preparations[J]. European Journal of Pharmacology: Molecular Pharmacology, 1991, 206(4): 309-314.
[2] Higashijima T, Uzu S, Nakajima T, et al. Mastoparan, a peptide toxin from wasp venom, mimics receptors by activating GTP-binding regulatory proteins (G proteins)[J]. Journal of Biological Chemistry, 1988, 263(14): 6491-6494.
[3] Chen X, Zhang L, Wu Y, et al. Evaluation of the bioactivity of a mastoparan peptide from wasp venom and of its analogues designed through targeted engineering[J]. International journal of biological sciences, 2018, 14(6): 599.
[4] Elsharkawy A M, Galhom R A, Amin B H, et al. In Vitro Evaluation of Some Therapeutic Applications of Wasp Venom and Mastoparan[J]. Egyptian Academic Journal of Biological Sciences. A, Entomology, 2024, 17(1): 121-130.
[5] Hilchie A L, Sharon A J, Haney E F, et al. Mastoparan is a membranolytic anti-cancer peptide that works synergistically with gemcitabine in a mouse model of mammary carcinoma[J]. Biochimica Et Biophysica Acta (BBA)-Biomembranes, 2016, 1858(12): 3195-3204.
[6] Takahashi K, Isobe M, Muto S. Mastoparan induces an increase in cytosolic calcium ion concentration and subsequent activation of protein kinases in tobacco suspension culture cells[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 1998, 1401(3): 339-346.
[7] de Azevedo R A, Figueiredo C R, Ferreira A K, et al. Mastoparan induces apoptosis in B16F10-Nex2 melanoma cells via the intrinsic mitochondrial pathway and displays antitumor activity in vivo[J]. Peptides, 2015, 68: 113-119.
Mastoparan是一种来源于黄蜂毒液的肽类毒素，可刺激磷酸肌醇分解，EC50值为9μM[1]。Mastoparan通过促进结合态GDP的解离，加速鸟苷-5'-3-O-硫代三磷酸结合并激活GTP结合调节蛋白（G蛋白）[2]。Mastoparan被广泛应用于抗炎研究，并作为开发相关衍生物的模型化合物[3]。
在体外，Mastoparan处理24小时对Hep-G2细胞表现出抑制作用（IC50=189.59±0.6µg/ml）[4]。25μM浓度的Mastoparan处理8小时可显著诱导Jurkat T白血病细胞和正常外周血细胞死亡[5]。20μM浓度的Mastoparan在1分钟内即可引起烟草BY-2细胞胞浆游离Ca2+浓度快速升高[6]。
在体内，连续5天经瘤周途径给药施用5mg/kg/day剂量的Mastoparan，可抑制小鼠黑色素瘤模型的肿瘤生长[7]。吉西他滨（60mg/kg/day）与Mastoparan（6mg/kg/day）联合腹腔注射治疗14天，能显著抑制乳腺癌小鼠模型的肿瘤进展[5]。
| Cell experiment [1]: | |
Cell lines | Immortalized human dermal microvessel endothelial cells |
Preparation Method | The growth of immortalized human dermal microvessel endothelial cells (HMECs) occurred in MCDB-131 medium which contained 10% inactivated FBS and 2mM glutamine as well as 100U/ml penicillin and 100μg/ml streptomycin. HMECs were seeded in 24-well culture plates (approximate cell density, 3×105 cells/well) containing medium supplemented with 5% heat-inactivated FBS. After cells reached confluence, cells were stimulated for 6h with lipopolysaccharide (LPS) at 10ng/ml, with or without a 30min preincubation of cells with Mastoparan (0, 5, 10, 15, 20, and 25μM). Supernatants were harvested and assayed for IL-6 activity by ELISA. |
Reaction Conditions | 0, 5, 10, 15, 20, and 25μM; 30min |
Applications | Mastoparan exerted a dose-dependent inhibition on the expression and secretion of IL-6 induced by LPS. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | At 6 to 8 weeks of age of male C57BL/6 mice, 5×104 viable B16F10-Nex2 cells were subcutaneously (s.c.) inoculated on the right side of male C57BL/6 mice. When the tumor reached a volume of 100mm3, the mice received 5 weekly intratumoral doses of Mastoparan (5mg/kg/day). The untreated tumor control group received 100μL PBS. After administration of the therapeutic dose, the tumor size was measured daily using a caliper. The tumor volume (V) was calculated using the formula V=0.52×d2×D, where d and D are the short and long diameters of the tumor, respectively. When the tumor size reached a maximum of 3000mm3, the animals were sacrificed for subsequent experimental analysis. |
Dosage form | 5mg/kg/day for 5 weeks a day; i.t. |
Applications | Mastoparan treatment inhibited the growth of subcutaneous melanoma in mice and increased the survival rate. |
References: | |
| Cas No. | 72093-21-1 | SDF | |
| 别名 | 黄峰毒素 | ||
| 化学名 | (S,Z)-2-((Z)-((2S,3S)-2-amino-1-hydroxy-3-methylpentylidene)amino)-N'1-((4S,5Z,7S,8Z,10S,11Z,13S,14Z,16S,17Z,19S,20Z,22S,23Z,25S,26Z,28S,29Z,31S,32Z,34S,35Z,37S)-10,13,34-tris(4-aminobutyl)-7-((S)-sec-butyl)-6,9,12,15,18,21,24,27,30,33,36-undecahydroxy-4- | ||
| Canonical SMILES | CC[C@]([C@@](N)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC(C)C)([H])[C@@](CC)([H])C)([H])CCCCN)([ | ||
| 分子式 | C70H131N19O15 | 分子量 | 1479 |
| 溶解度 | Soluble to 2.60 mg/ml in sterile water | 储存条件 | Desiccate 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 | 0.6761 mL | 3.3807 mL | 6.7613 mL |
| 5 mM | 0.1352 mL | 0.6761 mL | 1.3523 mL |
| 10 mM | 0.0676 mL | 0.3381 mL | 0.6761 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 | ||||||||||
| 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%
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