- Aspergillus Niger-mediated biotransformation of methenolone enanthate, and immunomodulatory activity of its transformed products
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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 μg/mL), as well as from isolated polymorphonuclear leukocytes (PMNs) (IC50 = 14.0 and 4.70 μg/mL), respectively. Moreover, compound 3 (34.21%) moderately inhibited the production of TNF-α, whereas 2 (88.63%) showed a potent inhibition of TNF-α 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.
- Hussain, Zahid,Dastagir, Nida,Hussain, Shabbir,Jabeen, Almas,Zafar, Salman,Malik, Rizwana,Bano, Saira,Wajid, Abdul,Choudhary, M. Iqbal
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