Horikawa K, Mohri T, Tanaka Y, Tokiwa H
Department of Health Sciences, Fukuoka Institute of Health and Environmental Sciences, Japan.
Mutagenesis. 1994 Nov;9(6):523-6. doi: 10.1093/mutage/9.6.523.
The activity of six Chinese medicinal herbs against the environmental mutagens and carcinogens benzo[a]pyrene (B[a]P), 1,6-dinitropyrene (1,6-diNP) and 3,9-dinitrofluoranthene (3,9-diNF) was determined. Samples of Prunella spica, Rheum palmatum, Polygonum multiflorum, Agrimonia pilosa, Ephedra sinica and Teitoutou were tested in an in vitro system. Antimutagenic activity against B[a]P was marked in the presence of extracts (boiled for 2 h in a water bath) whereas that against 1,6-diNP and 3,9-diNF varied from 20 to 86%. The differences in inhibition might be due to inactivation of metabolic enzymes. An extract of P. multiflorum was divided into ether, ethyl acetate and water soluble fractions, which were tested for antimutagenic activity against B[a]P. The antimutagenic action of the ethyl acetate soluble fraction was substantial and dose-dependent. Tannins and related compounds were the major components of the extract, of which epigallocatechin, epigallocatechin gallate, epicatechin gallate and tannic acid strongly inhibited the mutagenicity of B[a]P (2.5 micrograms/plate) in Salmonella typhimurium TA98 with S9 mix. To confirm the results of the in vitro test system, F344/DuCrj male rats were given a subcutaneous injection of B[a]P. Thereafter, they received water extracts of the six Chinese medicinal herbs for 50 weeks and were examined for tumors. The P. multiflorum extract significantly reduced the tumor incidence.
测定了六种中草药对环境诱变剂和致癌物苯并[a]芘(B[a]P)、1,6-二硝基芘(1,6-diNP)和3,9-二硝基荧蒽(3,9-diNF)的活性。对夏枯草、大黄、何首乌、仙鹤草、麻黄和铁透透的样品进行了体外系统测试。在提取物(在水浴中煮沸2小时)存在的情况下,对B[a]P的抗诱变活性显著,而对1,6-diNP和3,9-diNF的抗诱变活性在20%至86%之间变化。抑制作用的差异可能是由于代谢酶的失活。何首乌提取物被分为乙醚、乙酸乙酯和水溶性部分,测试了它们对B[a]P的抗诱变活性。乙酸乙酯可溶部分的抗诱变作用显著且呈剂量依赖性。单宁及相关化合物是提取物的主要成分,其中表没食子儿茶素、表没食子儿茶素没食子酸酯、表儿茶素没食子酸酯和单宁酸强烈抑制了鼠伤寒沙门氏菌TA98中B[a]P(2.5微克/平板)在S9混合液存在下的诱变性。为了证实体外测试系统的结果,给F-344/DuCrj雄性大鼠皮下注射B[a]P。此后,它们接受六种中草药的水提取物50周,并检查肿瘤情况。何首乌提取物显著降低了肿瘤发生率。