PAF 拮抗剂 PMS-1077 具有诱导 HL-60 细胞分化的新活性。

PMS-1077, a PAF antagonist, induced differentiation of HL-60 cells with its novel activity.

机构信息

Institute of Cancer Biology and Drug Screening, School of Life Sciences, Lanzhou University, Lanzhou 730000, Peoples Republic of China.

出版信息

Cell Biol Int. 2010 Dec;34(12):1227-30. doi: 10.1042/CBI20100168.

DOI:10.1042/CBI20100168

PMID:20812915

Abstract

The cell differentiation-inducing effect of 2-N,N-diethylaminocarbonyloxymethyl-1-diphenylmethyl-4-(3,4,5-trimethoxybenzoyl) piperazine, hydrochloride (PMS-1077) was determined in human leukaemic HL-60 cells with profiling of cell proliferation, analysis of cell cycling, characterization of expression of various CD molecules and determination of phagocytotic activity of differentiated HL-60 cells. After treatment with PMS-1077, HL-60 cells exhibited a decreased cell viability during which cell cycle was arrested in G₀-/G₁-phase. Flow cytometric analysis showed CD11b and CD14 were up-regulated, whereas CD15 was unaffected. Together with the finding that PMS-1077-treated HL-60 cells exhibited activities of differentiation by examining their ability of phagocytosing latex beads, an antiproliferative effect and a differentiation-inducing role were determined for PMS-1077 in HL-60 cells.

摘要

2-N,N-二乙基氨甲酰氧甲基-1-二苯甲基-4-(3,4,5-三甲氧基苯甲酰基)哌嗪盐酸盐（PMS-1077）在人白血病 HL-60 细胞中的细胞分化诱导作用通过细胞增殖分析、细胞周期分析、各种 CD 分子的表达特征和分化的 HL-60 细胞的吞噬活性来确定。用 PMS-1077 处理 HL-60 细胞后，细胞活力下降，细胞周期停滞在 G₀-/G₁ 期。流式细胞术分析显示 CD11b 和 CD14 上调，而 CD15 不受影响。与 PMS-1077 处理的 HL-60 细胞通过吞噬乳胶珠的能力显示出分化活性的发现一起，确定了 PMS-1077 在 HL-60 细胞中的增殖抑制作用和诱导分化作用。