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Melittin

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Chemical Structure| 20449-79-0 同义名 : Melittin游离
CAS号 : 20449-79-0
货号 : A407328
分子式 : C131H229N39O31
纯度 : 99%
分子量 : 2846.463
MDL号 : MFCD00076868
存储条件:

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 50 mg/mL(17.57 mM)

动物实验配方:
生物活性
描述 Melittin is a PLA2 activator, stimulates the activity of the low molecular weight PLA2, while it does not increase activity of the high molecular weight PLA2[1]. Melittin is a cytotoxic peptide from bee venom. Melittin exhibits toxicity against both A2780CR and A2780 cells, with IC50 values of 4.5 and 6.8 μg/mL, respectively. Melittin has natural anti-bacterial, anti-viral, and anti-inflammatory properties. Melittin, an amphipathic haemolytic peptide, exerts its potential anticancer effects include inhibition of cell proliferation, induction of apoptosis, and direct necrosis. The changes induced by melittin in the cisplatin-sensitive cells led mostly to reduced levels of amino acids in the proline/glutamine/arginine pathway, as well as to decreased levels of carnitines, polyamines, adenosine triphosphate (ATP) and nicotinamide adenine dinucleotide (NAD+)[2]. Melittin is the major pain-producing substance of bee venom, by which peripheral persistent pain and hyperalgesia (or allodynia), primary nociceptive neuronal sensitization, and CNS synaptic plasticity (or metaplasticity) can be readily induced and the molecular and cellular mechanisms underlying naturally-occurring venomous biotoxins can be experimentally unraveled[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02535416 Healthy Phase 1 Completed - Australia, Queensland ... 展开 >> QPharm, Pty Limited, Royal Brisbane Hospital Herston, Queensland, Australia, 4029 收起 <<
NCT02363946 Alpha-1 Antitrypsin Deficiency Phase 1 Terminated(Company decision to... 展开 >> terminate the trial) 收起 << - Australia, Victoria ... 展开 >> Nucleus Network Ltd Melbourne, Victoria, Australia, 3004 Germany Universitatsklinikum des Saarlandes Homburg, Germany Netherlands Leiden University Medical Center Leiden, Netherlands, 2333ZA United Kingdom Queen Elizabeth Hospital Edgbaston, Birmingham, United Kingdom, B15 2WB 收起 <<
NCT02363946 - Terminated(Company decision to... 展开 >> terminate the trial) 收起 << - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.35mL

0.07mL

0.04mL

1.76mL

0.35mL

0.18mL

3.51mL

0.70mL

0.35mL

参考文献

[1]Steiner MR, Bomalaski JS, Clark MA. Responses of purified phospholipases A2 to phospholipase A2 activating protein (PLAP) and melittin. Biochim Biophys Acta. 1993 Feb 10;1166(1):124-30

[2]Alonezi S, Tusiimire J, Wallace J, Dufton MJ, Parkinson JA, Young LC, Clements CJ, Park JK, Jeon JW, Ferro VA, Watson DG. Metabolomic Profiling of the Effects of Melittin on Cisplatin Resistant and Cisplatin Sensitive Ovarian Cancer Cells Using Mass Spectrometry and Biolog Microarray Technology. Metabolites. 2016 Oct 13;6(4):35

[3]Chen J, Guan SM, Sun W, Fu H. Melittin, the Major Pain-Producing Substance of Bee Venom. Neurosci Bull. 2016 Jun;32(3):265-72. doi: 10.1007/s12264-016-0024-y. Epub 2016 Mar 17