Westendorf J, Poginsky B, Marquardt H, Groth G, Marquardt H
Department of Toxicology, University of Hamburg Medical School, Federal Republic of Germany.
Cell Biol Toxicol. 1988 Jun;4(2):225-39. doi: 10.1007/BF00119248.
The genotoxic activity of lucidin (1,3-dihydroxy-2-hydroxymethyl-9,10-anthraquinone), a natural component of Rubia tinctorum L., was tested in a battery of short-term tests. The compound was mutagenic in five Salmonella typhimurium strains without metabolic activation, but the mutagenicity was increased after addition of rat liver S9 mix. In V79 cells, lucidin was mutagenic at the hypoxanthine-guanine phosphoribosyl transferase gene locus and active at inducing DNA single-strand breaks and DNA-protein cross-links as assayed by the alkaline elution method. Lucidin also induced DNA repair synthesis in primary rat hepatocytes and transformed C3H/M2-mouse fibroblasts in culture. We also investigated lucidinethylether, which is formed from lucidin by extraction of madder roots with boiling ethanol. This compound was also mutagenic in Salmonella, but only after addition of rat liver S9 mix. Lucidinethylether was weakly mutagenic to V79 cells which were cocultivated with rat hepatocytes. The compound did not induce DNA repair synthesis in hepatocytes from untreated rats, but positive results were obtained when hepatocytes from rats pretreated with phenobarbital were used. We conclude that lucidin and its derivatives are genotoxic.
茜草素(1,3 - 二羟基 - 2 - 羟甲基 - 9,10 - 蒽醌)是茜草的一种天然成分,其遗传毒性活性在一系列短期试验中进行了测试。该化合物在五种鼠伤寒沙门氏菌菌株中无代谢活化时具有致突变性,但添加大鼠肝脏S9混合液后致突变性增强。在V79细胞中,茜草素在次黄嘌呤 - 鸟嘌呤磷酸核糖基转移酶基因位点具有致突变性,并且通过碱性洗脱法测定,在诱导DNA单链断裂和DNA - 蛋白质交联方面具有活性。茜草素还能诱导原代大鼠肝细胞中的DNA修复合成,并在培养中转化C3H/M2 - 小鼠成纤维细胞。我们还研究了茜草素乙醚,它是通过用沸腾乙醇提取茜草根由茜草素形成的。该化合物在沙门氏菌中也具有致突变性,但仅在添加大鼠肝脏S9混合液后。茜草素乙醚对与大鼠肝细胞共培养的V79细胞致突变性较弱。该化合物未诱导未处理大鼠肝细胞中的DNA修复合成,但使用经苯巴比妥预处理的大鼠肝细胞时获得了阳性结果。我们得出结论,茜草素及其衍生物具有遗传毒性。