Background

Artemisinin (1) and its derivatives are now being widely used as antimalarial drugs, and they also exhibited good antitumor activities. So there has been much interest in the structural modification of artemisinin and its derivatives because of their effective bioactivities. The microbial transformation is a promising route to obtain artemisinin derivatives. The present study focuses on the microbial transformation of artemisinin by Aspergillus terreus.

Results

During 6 days at 28 °C and 180 rpm, Aspergillus terreus transformed artemisinin to two products. They were identified as 1-deoxyartemisinin (2) and 4α-hydroxy-1-deoxyartemisinin (3) on the basis of their spectroscopic data.

Conclusions

The microbial transformation of artemisinin by Aspergillus terreus was investigated, and two products (1-deoxyartemisinin and 4α-hydroxy-1-deoxyartemisinin) were obtained. This study is the first to report on the microbial transformation of artemisinin by Aspergillus terreus.

中文翻译：

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曲霉菌对青蒿素的微生物转化。

背景

青蒿素（1）及其衍生物现在被广泛用作抗疟药，它们还表现出良好的抗肿瘤活性。因此，由于青蒿素及其衍生物的有效生物活性，对其结构修饰引起了极大的兴趣。微生物转化是获得青蒿素衍生物的有前途的途径。本研究的重点是曲霉菌对青蒿素的微生物转化。

结果

在28°C和180 rpm下的6天中，曲霉曲霉将青蒿素转化为两种产物。根据它们的光谱数据，它们被鉴定为1-脱氧青蒿素（2）和4α-羟基-1-脱氧青蒿素（3）。

结论

研究了曲霉菌对青蒿素的微生物转化，获得了两种产物（1-脱氧青蒿素和4α-羟基-1-脱氧青蒿素）。这项研究是第一个报道土曲霉对青蒿素进行微生物转化的报道。