Department of Chemistry and Biochemistry, The University of North Carolina at Greensboro, Greensboro, NC 27402, USA.
J Antibiot (Tokyo). 2010 Sep;63(9):539-44. doi: 10.1038/ja.2010.77. Epub 2010 Jul 21.
Macrocyclic trichothecenes (MTs), which have potent cytotoxicity, have been isolated from many different fungal species. These compounds were evaluated clinically by the US National Cancer Institute in the 1970s and 1980s. However, they have yet to be advanced into viable drugs because of severe side effects. Our team is investigating a diverse library of filamentous fungi for new anticancer leads. To avoid reisolating MTs through bioactivity-directed fractionation studies, a protocol for their facile dereplication was developed. The method uses readily available photodiode array detectors to identify one of two types of characteristic UV spectra for these compounds. In addition, diagnostic signals can be observed in the (1)H-NMR spectra, particularly for the epoxide and conjugated diene moieties, even at the level of a crude extract. Using these techniques in a complementary manner, MTs can be dereplicated rapidly.
大环三萜烯（MTs）具有很强的细胞毒性，已从许多不同的真菌物种中分离出来。这些化合物在 20 世纪 70 年代和 80 年代由美国国家癌症研究所进行了临床评估。然而，由于严重的副作用，它们尚未成为可行的药物。我们的团队正在研究各种丝状真菌，以寻找新的抗癌先导化合物。为了避免通过基于生物活性的分离研究重新分离 MTs，我们开发了一种简便的去重复方法。该方法使用现成的光电二极管阵列检测器来识别这两种特征紫外光谱之一。此外，即使在粗提物水平上，也可以在（1）H-NMR 谱中观察到特征信号，特别是对于环氧化物和共轭二烯部分。通过互补使用这些技术，可以快速去重复 MTs。
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