Department of Biotechnology, Chemistry and Environmental Engineering, Aalborg University, Sohngaardsholmsvej 49, DK-9000 Aalborg, Denmark.
Toxicol Lett. 2012 Nov 15;214(3):259-62. doi: 10.1016/j.toxlet.2012.09.004. Epub 2012 Sep 13.
The fusarielins are a group of metabolites found in several Aspergillus and Fusarium species that have been reported to have with weak antifungal, antibiotic and cytotoxic effects. This study identifies fusarielin A, F, G and H isolated from Fusarium as mycoestrogens. Mycoestrogens are compounds from fungi that bind to the estrogen receptors and induce an estrogenic response in targeted cells. All four tested fusarielins stimulate MCF-7 cell proliferation with fusarielin H as the most potent, able to stimulate cell proliferation 4-fold in a resazurin metabolism assay at 25μM. MDA-MB-231 cells without the estrogen receptor-α and MCF-10a cells without estrogen receptors were not stimulated by fusarielins. Furthermore, the stimulation was prevented in MCF-7 cells when fusarielins were incubated in the presence of the estrogen receptor antagonist fulvestrant. These observations suggest that fusarielins bind to the estrogen receptor and act as weak mycoestrogens.
镰刀菌素是一组在几种曲霉属和镰刀菌属物种中发现的代谢产物，据报道具有较弱的抗真菌、抗生素和细胞毒性作用。本研究从镰刀菌中分离出的镰刀菌素 A、F、G 和 H 鉴定为真菌雌激素。真菌雌激素是真菌中的化合物，与雌激素受体结合，并在靶细胞中诱导雌激素反应。四种测试的镰刀菌素都能刺激 MCF-7 细胞增殖，其中镰刀菌素 H 的作用最强，在 25μM 的 Resazurin 代谢测定中，能将细胞增殖刺激 4 倍。缺乏雌激素受体-α的 MDA-MB-231 细胞和缺乏雌激素受体的 MCF-10a 细胞不受镰刀菌素的刺激。此外，当用雌激素受体拮抗剂氟维司群孵育 MCF-7 细胞时，镰刀菌素的刺激作用被阻止。这些观察结果表明，镰刀菌素与雌激素受体结合并作为弱真菌雌激素发挥作用。
