Toxicology and Ethnoveterinary Medicine, ARC-Onderstepoort Veterinary Institute, Onderstepoort, South Africa.
Department of Paraclinical Sciences, University of Pretoria, Onderstepoort, South Africa.
J Pharm Pharmacol. 2018 Jul;70(7):976-984. doi: 10.1111/jphp.12918. Epub 2018 Apr 6.
Monanthotaxis caffra (Sond.) Verdc. (Annonaceae) has been reported to possess antitumoural properties. Preliminary screening showed that the crude methanolic leaf extract had strong antimutagenic effects against aflatoxin B -induced mutagenicity. The aim of this study was to isolate and evaluate the antimutagenic properties of the active constituents from M. caffra.
Different chromatographic, spectroscopic and spectrometric techniques were used for the isolation and identification of the antimutagenic constituents. The antimutagenic effect of the extract and compounds was evaluated using Ames, Vitotox and Comet assays.
Bioassay-guided fractionation of the methanolic leaf extract yielded two antimutagenic compounds identified as (+)-crotepoxide and 5,6-diacetoxy1-benzoyloxymethyl-1,3-cyclohexadiene. Crotepoxide had strong antimutagenicity in the Vitotox assay with an IC value of 131 μg/ml. 5,6-Diacetoxy-1-benzoyloxymethyl-1,3-cyclohexadiene showed strong antimutagenic activity in the Ames assay with an IC value of 348.9 μg/plate and no antimutagenic activity in the Vitotox test. Furthermore, the compound was able to inhibit, block or prevent biotransformation of aflatoxin B by repressing the proteins involved in transcription.
Crotepoxide and 5,6-diacetoxy-1-benzoyloxymethyl-1,3-cyclohexadiene have the potential to mitigate the risks arising from consumption of aflatoxin B -contaminated food and feed.
蒙塔诺托萨卡弗尔(Sond.)Verdc.(番荔枝科)已被报道具有抗肿瘤特性。初步筛选表明,粗甲醇叶提取物具有很强的抗黄曲霉毒素 B 致突变作用。本研究的目的是从蒙塔诺托萨卡弗尔中分离和评估其活性成分的抗突变特性。
采用不同的色谱、光谱和光谱技术分离和鉴定具有抗突变特性的成分。采用 Ames、Vitotox 和 Comet 测定法评价提取物和化合物的抗突变作用。
甲醇叶提取物的生物测定指导分离得到两种具有抗突变作用的化合物,鉴定为(+)-克罗托氧化物和 5,6-二乙酰氧基-1-苯甲酰氧基-1,3-环己二烯。克罗托氧化物在 Vitotox 测定中具有很强的抗突变活性,IC 值为 131μg/ml。5,6-二乙酰氧基-1-苯甲酰氧基-1,3-环己二烯在 Ames 测定中具有很强的抗突变活性,IC 值为 348.9μg/板,在 Vitotox 试验中无抗突变活性。此外,该化合物能够通过抑制参与转录的蛋白质来抑制、阻断或防止黄曲霉毒素 B 的生物转化。
克罗托氧化物和 5,6-二乙酰氧基-1-苯甲酰氧基-1,3-环己二烯有可能减轻食用黄曲霉毒素 B 污染的食物和饲料带来的风险。