Aspergillus niger-mediated biotransformation of methenolone enanthate, and immunomodulatory activity of its transformed products

作者：Hussain Zahid; Dastagir Nida; Hussain Shabbir; Jabeen Almas; Zafar Salman; Malik Rizwana; Bano Saira; Wajid Abdul; Choudhary M Iqbal^*

来源：Steroids, 2016, 112: 68-73.

DOI：10.1016/j.steroids.2016.04.007

• Biotransformation
• Aspergillus niger
• Cunninghamella blakesleeana
• Anabolic-androgenic steroids
• Methenolone enanthate
• Immunomodulatory
• Anti-inflammatory
• TNF-alpha inhibitors

Two fungal cultures Aspergillus niger and Cunninghamella blakesleeana were used for the biotransformation of methenolone enanthate (1). Biotransformation with A. niger led to the synthesis of three new (2-4), and three known (5-7) metabolites, while fermentation with C. blakesleeana yielded metabolite 6. Substrate 1 and the resulting metabolites were evaluated for their immunomodulatory activities. Substrate 1 was found to be inactive, while metabolites 2 and 3 showed a potent inhibition of ROS generation by whole blood (IC50= 8.60 and 7.05 mu g/mL), as well as from isolated polymorphonuclear leukocytes (PMNs) (IC50= 14.0 and 4.70 mu g/mL), respectively. Moreover, compound 3 (34.21%) moderately inhibited the production of TNF-alpha, whereas 2 (88.63%) showed a potent inhibition of TNF-alpha produced by the THP-1 cells. These activities indicated immunomodulatory potential of compounds 2 and 3. All products were found to be non-toxic to 3T3 mouse fibroblast cells.

• 出版日期2016-8