Abstract
Objective: The present study was aimed at developing a rapid, cost effective and accurate method for quantification of exemestane using thin layer chromatography (TLC) separation followed by image analysis and to test it for monitoring the accumulation of exemestane during microbial bioconversion.Methods: After microbial bioconversion and TLC separation of products formed, exemestane was quantified using ImageQuant TL v2003 image analysis software and the results were compared with high performance liquid chromatography (HPLC) analysis.Results: The percentage error between TLC and HPLC analyses was ranged from (-) 5.18 to (+) 5.51. Bacterial strains Arthrobacter simplex IAM 1660, Nocardia sp. MTCC 1534, Pseudomonas putida MTCC 1194 and Rhodococcus rhodochorus MTCC 291 respectively yielded 79.7 (72 h), 63.9 (72 h), 69.8 (96 h) and 83.2 (96 h) mole percent bioconversion of 6-methylene androstenedione to exemestane. Conclusion: Rhodococcus rhodochorus MTCC 291 was found to be the most suitable organism for the bioconversion and may be used to develop an eco-friendly route to replace chemical synthesis that eliminates the use of toxic chemicals and side products.
Highlights
Exemestane, a third generation steroidal aromatase inhibitor, is a widely used drug for the treatment of breast cancer in postmenopausal patients [1,2,3]
The plate was activated at 100 °C for 10 min, cooled and spotted with chloroform solutions containing 2, 3 and 4 μg of authentic 6-methylene androstenedione (6-MeAD) synthesized in the laboratory as described earlier [12] and exemestane procured from Cipla Ltd., Mumbai, India
The spot area on the plate and concentrations of 6-MeAD and exemestane determined by image analysis software yielded a linear response for three point calibration
Summary
Exemestane, a third generation steroidal aromatase inhibitor, is a widely used drug for the treatment of breast cancer in postmenopausal patients [1,2,3]. The synthesis of exemestane is based on chemical conversion of a variety of steroid substrates [4,5,6,7,8,9]. Alternative route of microbial C-1(2)-dehydrogenation of 6-methylene androstenedione (6-MeAD) to yield exemestane has been developed and patented [10, 11]. The later is an eco-friendly route that eliminates the use of toxic chemicals and side products formed during chemical synthesis. Patil et al [12, 13] have reported C-1(2)-dehydrogenation of 6-MeAD to exemestane by of several bacterial strains
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