Picada J N, da Silva K V, Erdtmann B, Henriques A T, Henriques J A
Departamento de Produção de Matéria Prima da Faculdade de Farmácia, UFRGS, Porto Alegre, RS, Brazil.
Mutat Res. 1997 Oct 6;379(2):135-49. doi: 10.1016/s0027-5107(97)00116-4.
beta-Carboline alkaloids, found in medicinal plants, tobacco smoke and well-cooked foods, have shown a variety of actions in biological systems related to their interaction with DNA. Therefore, these alkaloids can be considered potentially mutagenic. In this work, the genotoxic, mutagenic, and cytotoxic activities of three aromatic beta-carboline alkaloids (harman, harmine, and harmol) and two dihydro-beta-carboline alkaloids (harmaline and harmalol) were evaluated by means of the Salmonella/microsome assay (Salmonella typhimurium TA98, TA97, TA100, and TA102) and SOS chromotest (Escherichia coli PQ37) with and without metabolic activation. Moreover, harman and harmine were analyzed by the micronucleus assay in vivo. It was shown that genotoxicity was inhibited by the addition of S9 mix for aromatic beta-carbolines harman and harmol in TA97. However, harmine showed signs of mutagenicity only in the presence of S9 mix in TA98 and TA97 frameshift strains. In the SOS chromotest, only harman induced SOS functions in the absence of S9 mix. Dihydro-beta-carbolines were not genotoxic in any of the microorganisms used. The negative responses obtained in the micronucleus assay indicated that harman and harmine were not able to induce chromosomal mutations.
β-咔啉生物碱存在于药用植物、烟草烟雾和烹饪熟透的食物中，已显示出在生物系统中与其与DNA相互作用相关的多种作用。因此，这些生物碱可被认为具有潜在的致突变性。在这项工作中，通过沙门氏菌/微粒体试验（鼠伤寒沙门氏菌TA98、TA97、TA100和TA102）和SOS色变试验（大肠杆菌PQ37），在有和没有代谢活化的情况下，评估了三种芳香族β-咔啉生物碱（哈尔满、去氢骆驼蓬碱和去甲骆驼蓬碱）和两种二氢-β-咔啉生物碱（骆驼蓬碱和去氢骆驼蓬醇）的遗传毒性、致突变性和细胞毒性。此外，通过体内微核试验分析了哈尔满和去氢骆驼蓬碱。结果表明，在TA97中，添加S9混合物可抑制芳香族β-咔啉哈尔满和去甲骆驼蓬碱的遗传毒性。然而，去氢骆驼蓬碱仅在TA98和TA97移码菌株中存在S9混合物时才显示出致突变迹象。在SOS色变试验中，只有哈尔满在没有S9混合物的情况下诱导了SOS功能。二氢-β-咔啉在所用的任何微生物中均无遗传毒性。微核试验中获得的阴性反应表明，哈尔满和去氢骆驼蓬碱不能诱导染色体突变。
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