Department of Experimental and Clinical Neuropathology, M. Mossakowski Medical Research Centre, Polish Academy of Sciences, 5 Pawinskiego Str., 02-106 Warsaw, Poland.
Peptides. 2010 Aug;31(8):1606-12. doi: 10.1016/j.peptides.2010.05.002. Epub 2010 May 24.
Biphalin is a new type of opioid peptide analog with high analgesic potency that is over 1000-fold greater than morphine. Because of its less addictive nature, biphalin has been suggested as a prospective new analgesic drug. Its high analgesic activity may be related to synergic interaction with all three types of opioid receptors (mu, delta, and kappa). Earlier data implicating involvement of opioid receptors, particularly MOR (mu opioid receptor) and KOR (kappa opioid receptor), in cell cycle regulation prompted us to investigate the effect of biphalin and morphine on human glioma T98G cell proliferation in vitro. We have documented an inhibitory effect of biphalin on tumor cell growth related to a decreased proliferation rate, decline of cell ability to form colonies, and modulation of the Ki-67 proliferation index. Morphine displayed the opposite effect and triggered stimulation of T98G cell proliferation. Our experiments have shown that biphalin might constitute an alternative solution for morphine application in anti-pain and anti-cancer therapy.
脑啡肽是一种新型阿片肽类似物，具有高效的镇痛作用，是吗啡的 1000 多倍。由于其成瘾性较低，脑啡肽被认为是一种有前途的新型镇痛药。它的高镇痛活性可能与其与三种类型的阿片受体（μ、δ 和 κ）的协同相互作用有关。早期的数据表明，阿片受体（特别是 MOR（μ阿片受体）和 KOR（κ阿片受体））参与细胞周期调控，这促使我们研究脑啡肽和吗啡对体外人神经胶质瘤 T98G 细胞增殖的影响。我们已经记录到脑啡肽对肿瘤细胞生长的抑制作用与增殖率降低、细胞形成集落能力下降以及 Ki-67 增殖指数的调节有关。吗啡则表现出相反的效果，引发 T98G 细胞的增殖刺激。我们的实验表明，脑啡肽可能为吗啡在抗痛和抗癌治疗中的应用提供了另一种选择。
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