Elias Baydoun, Saira Bano, Hina Mahmood and M. Asif Iqbal
Department of Biology; American University of Beirut, Lebanon
Biotransformation is an important tool for food additive, pharmaceutical, agrochemical, and other industries. Biotransformations catalyzed by microorganisms have been used in industry for the production of pharmaceuticals. We used biotransformation to create new analogues of existing drugs with improved pharmacological activity and lower toxicity. This approach appears to be a solution to problems in the pharmaceutical industry including production and high cost.
Exemestane was biotransformed to produce various structural analogues that were evaluated for their cytotoxicity against cancerous cell lines. An analogue of exemestane showed significant activity against HeLa and PC3 cancer cell lines.
Similarly, biotransformation of melengestrol acetate resulted in the production of new analogues. They were found to be six-fold more potent in inhibiting T-cell proliferation compared to the standard drug, prednisolone. This discovery of potent anti-inflammatory compounds can lead to the development of new immunosuppressant compounds for clinical applications.
Furthermore, the biotransformation of nandrolone resulted in the synthesis of new analogues with significant activity against the protozoal tropical disease leishmaniasis. Some of these analogues could form the basis for the development of effective therapies against leishmaniasis.