期刊
PROCESS BIOCHEMISTRY
卷 45, 期 10, 页码 1657-1663出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.procbio.2010.06.019
关键词
Silymarin; Silibinin; Silybin A; Lipase; Novozym 435; Diastereoselectivity
资金
- Czech Science Foundation [P207/10/0288, 303/08/0658]
- Ministry Education of the Czech Republic [CM0701, CM0602, LC06010]
The flavonolignan silybin (1), isolated from the seeds of milk thistle (Silybum marianum), occurs in nature as an equimolar mixture of two diastereoisomers, silybin A and silybin B, that exhibit different biological activities. The preparative production of optically pure silybin A and B in a diastereoisomeric purity greater than 95% was accomplished using immobilized Candida antarctica lipase B (Novozym 435) in a combination of two reactions: regioselective acetylation of a natural silybin mixture (1) and subsequent stereoselective alcoholysis of the resulting 23-O-acetylsilybin (2). Several grams of the optically pure substances can be produced within one week using this new, robust and scalable process, which is selective, mild and high-yielding. (C) 2010 Elsevier Ltd. All rights reserved.
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