3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) 是一种结构改良的多巴胺类似物细胞毒物，抑制黑色素瘤细胞中 DNA 聚合酶 (DNA polymerase) 活性。3,4-Dihydroxybenzylamine hydrobromide 在不同程度的酪氨酸酶活性的黑色素瘤细胞系中显示不同的生长抑制活性。
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells[2]. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity[2].
3,4-Dihydroxybenzylamine hydrobromide (1 μM-10 mM; 48 hours) inhibits the growth of all melanoma cell lines with an IC50 of 100 μM, while the SK-MELB cell line exhibits an IC50 of 122 μM. The IC50 values are 30, 84,90, and 68 μM for Human SK-MEL-30, SK-MEL-2, SK-MEL-3,RPMI-7951 cells, respectively. It exhibits IC50values of 10, 25, 67, and 184 μM for S91A,S91B, L1210, and SCC-25 cells, respectively[2].3,4-Dihydroxybenzylamine hydrobromide (1 μM-10 mM; 48 hours) cytotoxicity in SK-MEL-2 and SK-MEL-28 cell lines can be enhanced by application of buthionine sulfoximine (BSO). BSO treatment sensitizes marginally pigmented cells to the effects of 3,4-DHBA, and the presence of decreses IC50 values of 3,4-DHBA by 127% in the SK-MEL-28 cell line and by 148% in the SK-MEL-2 cell line[2].
3,4-Dihydroxybenzylamine hydrobromide (intraperitoneal injection; 1000 mg/kg; 7 days) has the least toxic effect in non-tumor-bearing B6D2F1 mice,and mice is tolerated at this dose[3].3,4-Dihydroxybenzylamine hydrobromide (intraperitoneal injection; 200-800 mg/kg; 21 days) has different effects at different doses, the median life-span are 17, 24.5, 26, 29 and 25 days for 0 mg/kg, 200 mg/kg, 400 mg/kg, 600 mg/kg, and 800 mg/kg, respectively[3].
[1]. FitzGerald GB, et al. 3,4-Dihydroxybenzylamine: an improved dopamine analog cytotoxic for melanoma cells in part through oxidation products inhibitory to dna polymerase.J Invest Dermatol. 1983 Feb;80(2):119-23.
[2]. Prezioso JA1,et al.Effects of tyrosinase activity on the cytotoxicity of 3,4-dihydroxybenzylamine and buthionine sulfoximine in human melanoma cells.Pigment Cell Res. 1990 Mar-Apr;3(2):49-54.
[3]. Mlchael M. Wick,et al. 3,4-Dihydroxybenzylamine: Antitumor Activity Against A Dopamine Analog B16 Melanoma.
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