Abstract：
Hydrocortisone succinate (1) is a synthetic anti-inflammatory drug and key intermediate in the synthesis of other steroidal drugs. This work is based on the fungal biotransformation of 1, using Monascus purpureus and Cunninghamella echinulata strains. Comopound 1 was transformed into four metabolites, identified as hydrocortisone (2), 11β-hydroxyandrost-4-en-3,17-dione (3), Δ1-cortienic acid (4), and hydrocortisone-17-succinate (5), obtained through side chain cleavage, hydrolysis, dehydrogenation, and oxidation reactions. These compounds have previously been synthesized either chemically or enzymatically from different precursors. Though this is not the first report on the biotransformation of 1, but it obviously is a first, where the biotransformed products of compound 1 have been characterized structurally with the help of modern spectroscopic techniques. It is noteworthy that these products have already shown biological potential, however a more thorough investigation of the anti-inflammatory properties of these metabolites would be of high value. These results not only emphasize upon the immense potential of biotransformation in catalysis of reactions, otherwise not-achievable chemically, but also holds promise for the development of novel anti-inflammatory compounds.
摘要：
琥珀酸氢化可的松(1)是一种合成抗炎药,是合成其他甾体药物的关键中间体。这项工作是基于1的真菌生物转化，使用了红曲霉和棘刺Cunninghamella菌株。Comopound1转化为四种代谢产物，鉴定为氢化可的松(2)，11β-羟基雄激素-4-烯-3,17-二酮（3），Δ1-皮质酸（4），和氢化可的松-17-琥珀酸酯(5)，通过侧链裂解获得，水解，脱氢,和氧化反应。这些化合物先前已从不同的前体化学或酶促合成。虽然这不是关于1生物转化的第一份报告，但显然是第一次，其中化合物1的生物转化产物在现代光谱技术的帮助下进行了结构表征。值得注意的是，这些产品已经显示出生物潜力，然而，对这些代谢物的抗炎特性进行更彻底的研究将具有很高的价值。这些结果不仅强调了生物转化在催化反应中的巨大潜力，否则化学上无法实现，但也为新型抗炎化合物的开发带来了希望。
