A Calluna vulgaris extract 5-lipoxygenase inhibitor shows potent antiproliferative effects on human leukemia HL-60 cells.

Eicosanoids Pub Date : 1992-01-01
A Najid, A Simon, C Delage, A J Chulia, M Rigaud
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Abstract

A water-Calluna vulgaris extract (water-CVE) was found to be a relatively specific arachidonate 5-lipoxygenase inhibitor and showed potent anti-proliferative effects on human leukemic HL60 cells. Water-CVE completely inhibited potato 5-lipoxygenase activity at 250 micrograms/ml, partially inhibited soybean 15-lipoxygenase at pH 7.4 and had no effect either on this 15-lipoxygenase at its optimal activity pH (pH 9) or on Lupinus albus 5-, 8-, 15-lipoxygenase. In culture, the proliferation and DNA synthesis of HL60 cells were decreased by water-CVE in a dose-dependent manner with an IC50 of 200 micrograms/ml at day 4. This effect of water-CVE is related to the starting density of HL60 cells. These results suggest that arachidonate 5-lipoxygenase metabolites and/or leukotrienes could play an essential role in cellular functions of leukemic cells and may explain the success of the use of Calluna vulgaris as tea and baths in folk medicine.

愈伤草提取物5-脂氧合酶抑制剂对人白血病HL-60细胞有明显的抗增殖作用。
水芥提取物(water-Calluna vulgaris extract, water-CVE)是一种特异性较强的花生四烯酸5-脂氧合酶抑制剂,对人白血病HL60细胞具有较强的抗增殖作用。水- cve在250微克/ml时完全抑制马铃薯5-脂肪加氧酶活性,在pH 7.4时部分抑制大豆15-脂肪加氧酶活性,在最佳活性pH (pH 9)时对15-脂肪加氧酶无影响,对白豆5-,8-,15-脂肪加氧酶无影响。在培养过程中,水- cve对HL60细胞的增殖和DNA合成呈剂量依赖性,第4天的IC50为200微克/毫升。水- cve的这种作用与HL60细胞的起始密度有关。这些结果表明花生四烯酸5-脂氧合酶代谢物和/或白三烯可能在白血病细胞的细胞功能中起重要作用,并可能解释了民间医学中将芥花用作茶和浴的成功。
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