Research Centre for Toxic Compounds in the Environment (RECETOX), Faculty of Science, Masaryk University, Kamenice 126/3, 625 00 Brno, Czech Republic.
Aquat Toxicol. 2011 Oct;105(3-4):497-507. doi: 10.1016/j.aquatox.2011.08.002. Epub 2011 Aug 9.
The biological activity of cyanobacteria and their chemical components have been widely studied due to their blooms in eutrophic waters worldwide. The primary goal of this study was to determine if individual cyanobacterial species and mixtures of cyanobacteria collected from the environment contain compounds with the potential for interaction with signaling pathways of the aryl hydrocarbon receptor (AhR), androgen receptor (AR), estrogen receptor (ER), glucocorticoid receptor (GR) and retinoid acid receptor (RAR). Cytotoxicity and specific toxic potencies of products of freshwater cyanobacteria were determined by use of in vitro reporter gene trans-activation assays. The testing included samples prepared from five selected single cyanobacterial species cultivated in laboratory and five complex cyanobacterial biomasses collected from blooms in surface waters in the Czech Republic. The results demonstrate estrogenic potencies of extracts of cyanobacterial biomasses. Among the laboratory single species, the extract of Planktothrix agardhii (intracellular metabolites) had a potency of estrogenic equivalents (EEQ) of 3.8 ng 17β-estradiol/g dw. The estimates of EEQs of samples prepared from complex cyanobacterial biomasses collected from freshwaters in the Czech Republic ranged from 19 to 2200 ng 17β-estradiol/g dw. Several samples prepared from the environmental cyanobacterial biomasses potentiated the androgenic potency of dihydrotestosterone. There was no dioxin-like, glucocorticoid or anti/retinoic activity observed for any of the extracts studied. Extracts of natural complex cyanobacterial biomasses exhibited greater and more frequent presence of compounds with specific modes of action, mainly estrogenic, and also greater cytotoxicity than extracts of single cyanobacterial species. The demonstrated estrogenic potency of the compounds present in complex cyanobacterial biomasses is of environmental relevance, and could potentially contribute to endocrine disruptive effects in aquatic ecosystems in case of great bloom densities.
由于蓝藻在世界范围内富营养化水域中的大量繁殖，其生物活性及其化学成分已得到广泛研究。本研究的主要目的是确定从环境中采集的单个蓝藻物种和蓝藻混合物是否含有具有与芳香烃受体 (AhR)、雄激素受体 (AR)、雌激素受体 (ER)、糖皮质激素受体 (GR) 和视黄酸受体 (RAR) 信号通路相互作用潜力的化合物。通过使用体外报告基因转激活测定法，确定淡水蓝藻产物的细胞毒性和特定毒性效价。测试包括从实验室培养的五种选定的单一蓝藻物种和从捷克共和国地表水水华采集的五种复杂蓝藻生物量中制备的样品。结果表明，蓝藻生物量提取物具有雌激素活性。在实验室的单一物种中，颤藻属（细胞内代谢物）的提取物具有 3.8ng 17β-雌二醇/g dw 的雌激素当量 (EEQ)。从捷克共和国淡水采集的复杂蓝藻生物量制备的样品的 EEQ 估计值范围从 19 到 2200ng 17β-雌二醇/g dw。从环境蓝藻生物量中制备的几种样品增强了二氢睾酮的雄激素效力。在所研究的任何提取物中，均未观察到类似二恶英、糖皮质激素或抗/视黄酸活性。天然复杂蓝藻生物量的提取物表现出更大和更频繁存在具有特定作用模式的化合物，主要是雌激素，并且比单一蓝藻物种的提取物具有更大的细胞毒性。复杂蓝藻生物量中存在的化合物所表现出的雌激素活性与环境有关，如果水华密度很大，可能会对水生生态系统中的内分泌干扰产生影响。
