Alpha-glucosidase and tyrosinase inhibitors from fungal hydroxylation of tibolone and hydroxytibolones

作者：Choudhary M Iqbal; Shah S Adnan Ali^*; Atta ur Rahman; Khan Shamsun Nahar; Khan Mahmud Tareq Hassan

来源：Steroids, 2010, 75(12): 956-966.

DOI：10.1016/j.steroids.2010.05.017

• Microbial transformation
• Tibolone
• alpha-Glucosidase inhibitors
• Tyrosinase inhibitors
• Enzyme inhibition assay
• Hydroxytibolone

Sixteen new and one known metabolites 4-20 were obtained by incubation of tibolone (1) and hydroxytibolones (2 and 3) with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. Metabolites of tibolone (1) exhibited significant inhibitory activities against alpha-glucosidase and tyrosinase enzymes. Hydroxylations at C-6, C-10, C-11, C-15 positions and alpha,beta-unsaturation at C-1/C-2, C-4/C-5 showed potent inhibitory activities against these enzymes.

• 出版日期2010-12