Microbial process for preparation of glucuronides of raloxifene

Autor:	J W Paschal, Barbara Shreve Briggs, P J Baker, B G Getman, Muth William Lawrence, Robert J. Strobel, Milton J. Zmijewski, Matthew D. Belvo, C A J Kemp, Thomas J. Perun, T D Black
Rok vydání:	1999
Předmět:	biology Chemistry Bioconversion Glucuronidation Bioengineering biology.organism_classification Applied Microbiology and Biotechnology Streptomyces Biotransformation medicine Organic chemistry Raloxifene Fermentation Chemical route Reference standards Biotechnology medicine.drug
Zdroj:	Journal of Industrial Microbiology and Biotechnology. 23:194-197
ISSN:	1476-5535 1367-5435
DOI:	10.1038/sj.jim.2900716
Popis:	Raloxifene, also known as Evista®, has recently been approved for the prevention of osteoporosis. Three glucuronidated compounds: raloxifene-6-glucuronide, raloxifene-27-glucuronide, and raloxifene-6,27-diglucuronide are known metabolites of raloxifene in man. Reference standards of the three glucuronides were needed for clinical trials. Although chemical routes exist to make the two mono-glucuronides, these routes were unable to provide material to meet the needs of clinical trial standards. No chemical route existed to synthesize the di-glucuronide. A bioconversion process using the microorganism Streptomyces sp NRRL 21489 was identified and scaled up. The biotranformation products were prepared in a tank fermentation, purified, and characterized by UV, LC/MS and NMR spectroscopy.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::fafee61f988080817d8322d47811a0d9 https://doi.org/10.1038/sj.jim.2900716 Zobrazit plný text záznamu Plný text ve formátu PDF