合成查尔酮(E)-3-(4-氯苯基)-1-苯基-2-丙烯-1- 1 (4-CL)和(E)-3-(3,4-二甲氧基苯基)-1-苯基-2-丙烯-1- 1 (DMF)的遗传毒性、细胞毒性和保护作用的体外和体内评价

E. B. Nunes, Priscila Zei Melo, Jefté Barbosa, Jefferson Hollanda Véras, C. R. Silva
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引用次数: 0

摘要

查尔酮(E)-3-(4-氯苯基)-1-苯基-2-丙烯-1- 1- 1 (4-CL)和(E)-3-(3,4-二甲氧基苯基)-1-苯基-2-丙烯-1- 1- 1 (DMF)是一种用途广泛且易于合成的低成本化合物,具有广泛的生物活性。本研究采用Ames试验和小鼠微核试验对4-CL和DMF的细胞毒性、基因毒性和调节活性进行了评价。Ames试验结果表明,两种查尔酮对鼠伤寒沙门菌TA98和TA100均无致突变性,与叠氮化钠(SA)对TA100均有显著的抗诱变作用(p< 0.05)。在微核实验中,两者在24 h和48 h时微核多染红细胞(MNPCE)的频率显著增加,显示出遗传毒性作用。在与丝裂霉素C (MMC)共处理时,在查尔酮24h和DMF低浓度48h中,MNPCE的频率均显著降低(p< 0.05),表明其具有抗毒活性。4-CL在24和48 h显著降低了小鼠的多染/正染红细胞(PCE/ NCE)比率(p< 0.05),提示细胞毒性。然而,当4-CL和DMF与MMC共同给药时,24小时内PCE/NCE比值显著增加,显示出抗细胞毒性。此外,在暴露48小时的微核试验中,两种查尔酮(4-CL与SA共给药,Ames试验和DMF与MMC共处理)均观察到双相剂量反应行为。在本研究中,4-CL和DMF表现出基因毒性、细胞毒性、抗原毒性、抗细胞毒性和无致突变性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vitro and in vivo evaluation of genotoxicity, cytotoxicity, and protective effects of synthetic chalcones (E)-3-(4-chlorophenyl)-1-phenyl-2-propen-1-one (4-CL) and (E)-3-(3,4-dimethoxyphenyl)-1- phenyl-2-propen-1-one (DMF)
The chalcones (E)-3-(4-chlorophenyl)-1-phenyl-2-propen-1-one (4-CL) and (E)-3-(3,4-dimethoxyphenyl)-1-phenyl-2 -propen-1-one (DMF) are versatile and easily synthesized into low-cost compounds that have a wide spectrum of biological activities. In this study, the cytotoxic, genotoxic and modulatory activities of 4-CL and DMF were evaluated using the Ames test and the mouse micronucleus assay. The results of the Ames test revealed that both chalcones did not show mutagenic activity in Salmonella typhimurium strains TA98 and TA100, and demonstrated significant antimutagenicity (p< 0.05) when co-administered with sodium azide (SA) in strain TA100. In the micronucleus assay, both showed a significant increase in the frequency of micronucleated polychromatic erythrocytes (MNPCE) at 24 h and 48 h, revealing a genotoxic effect. In the co-treatment with mitomycin C (MMC) there was a significant decrease (p< 0.05) in the frequency of MNPCE both in chalcones at 24h and in the less concentrated dose of DMF at 48h, demonstrating its antigenotoxic activity. 4-CL showed a significant decrease in the polychromatic/ normochromatic erythrocyte (PCE/ NCE) ratio at 24 and 48 h (p< 0.05), indicating cytotoxicity. However, 4-CL and DMF when co-administered with MMC showed a significant increase in the PCE/NCE ratio within 24 hours, demonstrating anticytotoxicity. Furthermore, a biphasic dose-response behavior was observed in both chalcones, 4-CL in the co-administration with SA, in the Ames Test and DMF in the co-treatment with MMC, at 48 hours of exposure, in the micronucleus assay. In this study, 4-CL and DMF showed genotoxic, cytotoxic, antigenotoxic, anticytotoxic and no mutagenic properties.
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