Isolation, characterization and antifungal docking studies of wortmannin isolated from Penicillium radicum

Show full item record



Permalink

http://hdl.handle.net/10138/162438

Citation

Singh , V , Praveen , V , Tripathi , D , Haque , S , Somvanshi , P , Katti , S B & Tripathi , C K M 2015 , ' Isolation, characterization and antifungal docking studies of wortmannin isolated from Penicillium radicum ' , Scientific Reports , vol. 5 , 11948 . https://doi.org/10.1038/srep11948

Title: Isolation, characterization and antifungal docking studies of wortmannin isolated from Penicillium radicum
Author: Singh, Vineeta; Praveen, Vandana; Tripathi, Divya; Haque, Shafiul; Somvanshi, Pallavi; Katti, S. B.; Tripathi, C. K. M.
Contributor: University of Helsinki, Faculty of Pharmacy
Date: 2015-07-10
Language: eng
Number of pages: 13
Belongs to series: Scientific Reports
ISSN: 2045-2322
URI: http://hdl.handle.net/10138/162438
Abstract: During the search for a potent antifungal drug, a cell-permeable metabolite was isolated from a soil isolate taxonomically identified as Penicillium radicum. The strain was found to be a potent antifungal agent. Production conditions of the active compound were optimized and the active compound was isolated, purified, characterized and identified as a phosphoinositide 3-kinase (PI3K) inhibitor, commonly known as wortmannin (Wtmn). This is very first time we are reporting the production of Wtmn from P. radicum. In addition to its previously discovered anticancer properties, the broad spectrum antifungal property of Wtmn was re-confirmed using various fungal strains. Virtual screening was performed through molecular docking studies against potential antifungal targets, and it was found that Wtmn was predicted to impede the actions of these targets more efficiently than known antifungal compounds such as voriconazole and nikkomycin i.e. 1) mevalonate-5-diphosphate decarboxylase (1FI4), responsible for sterol/isoprenoid biosynthesis; 2) exocyst complex component SEC3 (3A58) where Rho-and phosphoinositide-dependent localization is present and 3) Kre2p/Mnt1p a Golgi alpha1,2-mannosyltransferase (1S4N) involved in the biosynthesis of yeast cell wall glycoproteins). We conclude that Wtmn produced from P. radicum is a promising lead compound which could be potentially used as an efficient antifungal drug in the near future after appropriate structural modifications to reduce toxicity and improve stability.
Subject: AEROMONAS-HYDROPHILA
NEGATIVE REGULATION
INHIBITOR
3-KINASE
BIOSYNTHESIS
PURIFICATION
EFFICIENT
WHEAT
317 Pharmacy
Rights:


Files in this item

Total number of downloads: Loading...

Files Size Format View
srep11948.pdf 1008.Kb PDF View/Open

This item appears in the following Collection(s)

Show full item record