生物活性 | |||
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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 | |||||
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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 | |||
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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 |
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