Activity of Liposome‐entrapped Immunomodulator Oligopeptides on Human Epithelial Thymic Cells

V. Cardile, M. Renis, B. Gentile, A. Panico
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Abstract

We have studied the in-vitro effects of liposomal formulations loaded with three oligopeptides (Tp3, Tp4, Tp5), synthetic analogues corresponding to the active site of thymopoietin, on human thymic epithelial cells. The activity of the peptides entrapped in multilamellar vesicles and in stable plurilamellar liposomal vesicles, with or without cholesterol and containing stearylamine or dipalmitoylphosphatidyl serine, as positive or negative charge-inducer, was tested. The tetrazolium salt assay was performed as a marker of cell growth. To study the response of thymic epithelial cell cultures to liposome addition-dependent stress, we investigated the changes in the level of heat shock proteins (HSPs70). The results indicated that in-vitro among the peptides tested only Tp4 increased thymic epithelial cell growth. These stimulating effects were improved further when the peptide was entrapped in neutral 1,2-dipalmitoyl-L-α-phosphatidylcholine/cholesterol liposomes. Tp4 was also effective in modulating HSP70 protective effects.
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脂质体包裹免疫调节剂寡肽对人胸腺上皮细胞的活性
我们研究了装载三种寡肽(Tp3, Tp4, Tp5)的脂质体制剂对人胸腺上皮细胞的体外作用,它们是胸腺生成素活性位点对应的合成类似物。测试了多肽在多层囊泡和稳定的多层脂质体囊泡中,含或不含胆固醇,含硬脂胺或双棕榈酰磷脂酰丝氨酸作为正负电荷诱导剂的活性。四氮唑盐试验作为细胞生长的标记物。为了研究胸腺上皮细胞培养物对脂质体添加依赖性应激的反应,我们研究了热休克蛋白(HSPs70)水平的变化。结果表明,在体外测试的肽中,只有Tp4能促进胸腺上皮细胞的生长。当肽被中性的1,2-二棕榈酰- l- α-磷脂酰胆碱/胆固醇脂质体包裹时,这些刺激作用进一步增强。Tp4也能有效调节HSP70的保护作用。
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