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Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3?in vitro[1]. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease[2]. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury[1]. | [in vivo]
Colivelin(intracerebroventricular administration; 10 pmol/3 μl; 3 weeks) suppresses impairment in spatial working memory induced by repetitive intracerebroventricular injection of Aβ25-35 or Aβ1-42, in addition, it antagonizes neuronal loss in the CA1 region of hippocampus induced by hippocampal injection of Aβ1-42[1].
Colivelin (intraperitoneal administration; 1.4, 7, or 35 nM/0.21mL; on the Y-maze testday) suppresses memory impairment caused by 3-quinuclidinyl benzilateand restricts functional memory deficit[1].
Colivelin (intraperitoneal injection; 1 mg/kg; 14 days) results in improved motor and cognitive function with time by performance of mNSS, rotarod, and corner turning test.It also reduces lesion volume and improves neurological deficits after MCAO[1]. | Animal Model: | CD-1 mice[1] | | Dosage: | 10 pmol/3 μl | | Administration: | Intracerebroventricular administration | | Result: | Completely suppressed Aβ 25-35-mediated impairment in spatial working memory and increased the number of immunoreactive neurons. |
| Animal Model: | C57 mice[1] | | Dosage: | 1.4, 7, or 35 nM/0.21mL | | Administration: | Intraperitoneal administration | | Result: | Protected against cholinotoxin-induced amnesia in mice. |
| Animal Model: | Male C57BL/6 mice[3] | | Dosage: | 1 mg/kg | | Administration: | Intraperitoneal administration | | Result: | Protected against ischemic brain injury, and improves neurological outcomes. |
| [IC 50]
STAT3; Amyloid-β | [References]
[1] Chiba T, et al. Development of a femtomolar-acting humanin derivative named colivelin by attaching activity-dependent neurotrophic factor to its N terminus: characterization of colivelin-mediated neuroprotection against Alzheimer's disease-relevant insults in vitro and in vivo. J Neurosci. 2005 Nov 2;25(44):10252-61. DOI:10.1523/JNEUROSCI.3348-05.2005
[2] Zhao H, et al. Colivelin?Rescues?Ischemic?Neuron?and?Axons?Involving?JAK/STAT3?Signaling?Pathway.Neuroscience.?2019 Sep 15;416:198-206. DOI:10.1016/j.neuroscience.2019.07.020
[3] Pan Z, et al. Upregulation of HSP72 attenuates tendon adhesion by regulating fibroblast proliferation and collagen production via blockade of the STAT3 signaling pathway.Cell Signal. 2020 Mar 18:109606. DOI:10.1016/j.cellsig.2020.109606
[4] Fang YY, et al. MFG-E8 alleviates oxygen-glucose deprivation-induced neuronal cell apoptosis by STAT3 regulating the selective polarization of microglia. Int J Neurosci. 2020 Mar 12:1-10. DOI:10.1080/00207454.2020.1732971
[5] Chiu WC, et al. The Synthetic β-Nitrostyrene Derivative CYT-Rx20 Inhibits Esophageal Tumor Growth and Metastasis via PI3K/AKT and STAT3 Pathways. PLoS One. 2016 Nov 22;11(11):e0166453. DOI:10.1371/journal.pone.0166453 |
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