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Enzymatic synthesis and antibacterial activity of andrographolide derivatives

Paper ID Volume ID Publish Year Pages File Format Full-Text
35261 45083 2011 5 PDF Available
Title
Enzymatic synthesis and antibacterial activity of andrographolide derivatives
Abstract

A series of andrographolide derivatives have been synthesized through enzymatic acylation reactions. Immobilized Candida antarctica lipase B (Novozym 435) was found to be a useful biocatalyst for the 35-gram scale syntheses of these acylated derivatives, and the biocatalyst displayed excellent regioselectivity and high operational stability during the transformation. The 14-substituted andrographolide derivative was the sole detectable product from each acylation reaction. The acylated andrographolides showed antibacterial activity against representative Gram-positive and Gram-negative bacteria [with minimal inhibitory concentrations (MICs) as low as 4 μg/mL], whereas andrographolide exhibited no such activity. Chain length of acyl moiety on the lactone-ring at the C-14 position plays an important role in determining the potency of the antibacterial activity. These results indicate an enzymatic modification was not only facile and green, but an effective method for the preparation of an andrographolide monoester.

Keywords
Andrographolide; Enzymatic acylation; Regioselectivity; Derivatives; Antibacterial activity
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Publisher
Database: Elsevier - ScienceDirect
Journal: Process Biochemistry - Volume 46, Issue 8, August 2011, Pages 1649–1653
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
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Don't Miss Today's Special Offer
Price was $35.95
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