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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Microbial transformation of anti-cancer steroid exemestane and cytotoxicity of its metabolites against cancer cell lines
Chemistry Central Journal, Volume 7, No. 1, Article 57, Year 2013
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Description
Background: Microbial transformation of steroids has been extensively used for the synthesis of steroidal drugs, that often yield novel analogues, not easy to obtain by chemical synthesis. We report here fungal transformation of a synthetic steroidal drug, exemestane, used for the treatment of breast cancer and function through inhibition of aromatase enzyme.Results: Microbial transformation of anti-cancer steroid, exemestane (1), was investigated by using two filamentous fungi. Incubation of 1 with fungi Macrophomina phaseolina, and Fusarium lini afforded three new, 11α-hydroxy-6-methylene-androsta-1, 4-diene-3,17-dione (2), 16β, 17β-dihydroxy-6-methylene-androsta-1, 4-diene-3-one (3), and 17β-hydroxy-6-methylene-androsta-1, 4-diene-3, 16-dione (4), and one known metabolites, 17β-hydroxy-6-methylene-androsta-1, 4-diene-3-one (5). Their structures were deduced spectroscopically. Compared to 1 (steroidal aromatase inactivator), the transformed metabolites were also evaluated for cytotoxic activity by using a cell viability assay against cancer cell lines (HeLa and PC3). Metabolite 2 was found to be moderately active against both the cell lines.Conclusions: Biotransformation of exemestane (1) provides an efficient method for the synthesis of new analogues of 1. The metabolites were obtained as a result of reduction of double bond and hydroxylation. The transformed product 2 exhibited a moderate activity against cancer cell lines (HeLa and PC3). These transformed products can be studied for their potential as drug candidates. © 2013 Baydoun et al.; licensee Chemistry Central Ltd.
Authors & Co-Authors
Baydoun, Elias Abdel Hasan
Lebanon, Beirut
American University of Beirut
Bibi, Marium
Pakistan, Karachi
University of Karachi
Iqbal, Muhammad Asif
Pakistan, Karachi
University of Karachi
Atia-tul-Wahab,
Pakistan, Karachi
University of Karachi
Farran, Dina
Lebanon, Beirut
American University of Beirut
Smith, Colin
Lebanon, Beirut
American University of Beirut
Sattar, Samina Abdul
Pakistan, Karachi
University of Karachi
Rahman, Atta Ur
Pakistan, Karachi
University of Karachi
Choudhary, Mohammed Iqbal
Pakistan, Karachi
University of Karachi
Saudi Arabia, Jeddah
King Abdulaziz University
Statistics
Citations: 20
Authors: 9
Affiliations: 3
Identifiers
Doi:
10.1186/1752-153X-7-57
e-ISSN:
1752153X
Research Areas
Cancer