Department of Biology, University of Rome "Tor Vergata", Via della Ricerca Scientifica, 00133 Rome, Italy.
Life Sci. 2011 Nov 21;89(21-22):812-20. doi: 10.1016/j.lfs.2011.09.008. Epub 2011 Sep 24.
Aloe-emodin (AE), a plant derived anthraquinone, has been shown to have anticancer activity in various human cancer cell lines. We have recently reported that AE possesses a differentiative potential on melanoma cells. The purpose of this study was to investigate the possible modulation of defined markers of monocytic differentiation of AE on human U937 cell line.
U937 cells differentiation has been confirmed unequivocally by Griess and nitroblue tetrazolium reduction assays, protoporphyrin IX accumulation, expression of CD14 and CD11b surface antigens, phagocytic activity, migration and attachment ability. The effect on polyamine metabolism, apoptosis and cytokine production was also investigated.
We showed that AE-treated U937 cells exhibit a noticeably rise in transglutaminase activity. This enhanced enzyme activity correlates with AE-induced growth arrest and differentiation to functionally mature monocytes.
Taken together, the results reported here show that AE can promote the macrophage differentiation of U937 cells, suggesting that this anthraquinone could be a potential candidate as a differentiation-inducing selective agent for therapeutic treatment of leukemia.
大黄素（AE）是一种植物来源的蒽醌类化合物，已在各种人类癌细胞系中显示出抗癌活性。我们最近报道 AE 对黑色素瘤细胞具有分化潜能。本研究的目的是研究 AE 对人 U937 细胞系单核细胞分化的特定标志物的可能调节作用。
通过格里修斯（Griess）和硝基四唑蓝还原测定、原卟啉 IX 积累、CD14 和 CD11b 表面抗原表达、吞噬活性、迁移和附着能力，明确证实 U937 细胞的分化。还研究了对多胺代谢、细胞凋亡和细胞因子产生的影响。
我们表明，AE 处理的 U937 细胞表现出转谷氨酰胺酶活性明显升高。这种增强的酶活性与 AE 诱导的生长停滞和向功能成熟单核细胞的分化相关。
综上所述，这里报道的结果表明 AE 可以促进 U937 细胞的巨噬细胞分化，表明这种蒽醌类化合物可能是治疗白血病的诱导分化选择性药物的潜在候选物。
