Calomme M, Pieters L, Vlietinck A, Vanden Berghe D
Department of Pharmaceutical Sciences, University of Antwerp, Belgium.
Planta Med. 1996 Jun;62(3):222-6. doi: 10.1055/s-2006-957864.
The antimutagenicity of the Citrus flavonoids naringin, hesperidin, nobiletin, and tangeretin against the mutagens benzo[a]pyrene, 2-aminofluorene, quercetin, and nitroquinoline N-oxide was investigated in the Salmonella/microsome assay. Naringin and hesperidin showed a weak antimutagenic activity against benzo[a]pyrene. Tangeretin was antimutagenic against all indirectly-acting mutagens tested, but in general a large molar excess was necessary. Liquid preincubation increased the antimutagenicity of tangeretin against 2-aminofluorene. Nobiletin acted as an antimutagen against benzo[a]pyrene, but it enhanced the mutagenicity of 2-aminofluorene. However, in a liquid preincubation assay nobiletin also exhibited antimutagenicity against 2-aminofluorene. Both tangeretin and nobiletin inhibited the mutagenicity of quercetin. Quercetin itself acted as an antimutagen against 2-aminofluorene in a Salmonella strain (TA1538) where its mutagenicity was not expressed. Quercetin should not merely be regarded as a genotoxic risk factor in the human diet, since its mutagenicity may be inhibited by accompanying compounds including other flavonoids, and since quercetin itself also exhibits an antimutagenic action. Because of the antimutagenic properties the Citrus flavonoids tested, especially tangeretin and nobiletin, might play a role in the chemoprevention of cancer.
在沙门氏菌/微粒体试验中,研究了柑橘类黄酮柚皮苷、橙皮苷、川陈皮素和橘红素对诱变剂苯并[a]芘、2-氨基芴、槲皮素和N-氧化硝基喹啉的抗诱变活性。柚皮苷和橙皮苷对苯并[a]芘表现出较弱的抗诱变活性。橘红素对所有测试的间接作用诱变剂均具有抗诱变作用,但一般需要大量的摩尔过量。液体预孵育增加了橘红素对2-氨基芴的抗诱变活性。川陈皮素对苯并[a]芘起抗诱变作用,但增强了2-氨基芴的诱变活性。然而,在液体预孵育试验中,川陈皮素对2-氨基芴也表现出抗诱变活性。橘红素和川陈皮素均抑制了槲皮素的诱变活性。在一个未表达其诱变活性的沙门氏菌菌株(TA1538)中,槲皮素本身对2-氨基芴起抗诱变作用。槲皮素不应仅仅被视为人类饮食中的遗传毒性风险因素,因为其诱变活性可能会被包括其他黄酮类化合物在内的伴随化合物所抑制,并且槲皮素本身也表现出抗诱变作用。由于所测试的柑橘类黄酮,特别是橘红素和川陈皮素具有抗诱变特性,它们可能在癌症的化学预防中发挥作用。