Use of extracts cluster analysis (EXCLAN) to rapidly screen for enzyme 1 inhibitors in microbial fermented extracts

Author(s): Vasantha K. Y., Murugesh C. S., Sattur A. P.

Abstract

The success of a new molecule discovery programme lies in the effectiveness of the primary screen for desired activities. A rapid screen, Extracts Cluster Analysis (ExCLAN) was used for the screening of lipoxygenase inhibitors from microbial extracts. About 50 crude extracts were randomly grouped as 5 clusters and screened for inhibition. Cluster C3, which showed 93% inhibition, was further deconvoluted, to pinpoint isolate P25 as the extract with the inhibitor. Further isolation and purification identified the inhibitor as sclerotiorin with an IC50 value of 4.6µM against soybean lipoxygenase. This method helped in significantly reducing the time and number of assays with subsequent savings in costs of conducting the assays.

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