- 期刊
Effect of Lomustine on N-Acetyltransferase Activity in RAT Glioma in Vitro Cultured Cells
Lomustine對大白鼠神經膠質瘤之體外培養細胞中乙醯轉移酶活性的影響
摘要
目的：芳香胺化合物經N基乙醯轉移?( N-acetyltransferase )之N 基乙醯化可誘發癌，lomustine是常用於治療腦瘤的一種抗癌物藥，本研究是in vitro 探討lomustine 對大白鼠神經膠質細胞瘤之體外培養細胞中乙醯轉移臨活性的影響。 材料與方法：取大白鼠神經膠質細胞瘤之體外培養細胞( n = 12)用乙醯化輔?A 作乙醯基而再利用高壓液相層析儀分析乙醯轉移?的活性及lomustine對大白鼠神經膠質細胞瘤之體外培養細胞中乙醯轉移由活性的影響，以2-aminofluorene (2-AF)和 p-minobenzoic acid (PABA)作受質。 結果：結果顯示大白鼠神經膠質細胞瘤之體外培養細胞對AF及PABA 受質皆有乙醯轉移?活性存在，其對AF及PABA 的活性平均值各為1.08±0.18及0.96±0.16 nmol/min/mg protein。在0.8μM，8μM and 80μM 的lomustine 濃度中，大白鼠神經膠質細胞瘤之體外培養細胞中AF-NAT活性降低約17.6%，31.5% and 45.4%，PABA-NAT活性降值約10.4%，27.1 % and 45，8%。 結論：Lomustine可降低大白鼠神經膠質細胞瘤之體外培養細胞中乙醯轉移?的活性。
並列摘要
Purpose: Arylamine N-acetylation capacity by the N-acetyltransferase (NAT) may be an important causative factor in the initiation of cancer. Lomustine is a commercially avail-able nitrosourea derivative and chloroethyl nitrosourea compound which applied in antineopstic therapy especially in central nervous system. The aaffect of lomustine on the activity of NAT in rat glioma in vitro cultured cells were investigated. Materials and Methods: Rat glioma in vitro cultured cell cytosol (n=12) were used to investigate for the effect of lomustine on the activity of NAT toward 2-amniofluorene (AF) and p-aminiobenzoic acid (PABA) using an acetyl coenzyme A (AcCoA) recycling assay and high pressure liquid chromatography (HPLC). Results: Activity of N-acetyltransferase in rat glioma in vitro cultured cell cytosol is found to be inhibited by lomustine. Its presence in the assay medium shows an inhibition in aminofluorene-N-acetyltransferase (AF-NAT) activity about of 17.6%, 31.5% and 45.4% in rat glioma in vitro cultured cells at 0.8 μM, 8 μM and 80 μM of lomustine concentrations respectively; while as p-aminobenzoic acid-N-acetyltransferase (PABA-NAT) activity decreased about 10.4%, 27.1% and 45.8% in rat glioma cells with 0.8μM,8μM and 80(M of lomustine concentrations respectively. Conclusion: The results of this study show that the NAT activity of rat glioma cultured cells are decreased by lomustine.
延伸閱讀
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