New Production of Antibacterial Polycyclic Quinazoline Alkaloid, Thielaviazoline, from Anthranilic Acid by the Marine-Mudflat-Derived Fungus Thielavia sp..
10.20307/nps.2016.22.3.216
- Author:
Alain Simplice LEUTOU
1
;
Keumja YUN
;
Byeng Wha SON
Author Information
1. Department of Chemistry, Pukyong National University, Busan 608-737, Korea. sonbw@pknu.ac.kr
- Publication Type:Original Article
- Keywords:
Thielaviazoline;
Polycyclic quinazoline alkaloid;
Thielavia sp.;
Microbial transformation
- MeSH:
Ascorbic Acid;
Fungi*;
In Vitro Techniques;
Methicillin Resistance;
Microbial Sensitivity Tests;
Staphylococcus aureus;
Statistics as Topic
- From:Natural Product Sciences
2016;22(3):216-219
- CountryRepublic of Korea
- Language:English
-
Abstract:
The microbial transformation of anthranilic acid (1) by the marine-mudflat-derived fungus Thielavia sp. produced an antibacterial polycyclic quinazoline alkaloid, thielaviazoline (2). The stereostructure of the metabolite was assigned based on detailed spectroscopic data analyses including comparison of the NMR (¹H and ¹³C) data with those of reported compound (2). Compound 2 displayed in vitro antimicrobial activity against methicillin-resistant and multidrug-resistant Staphylococcus aureus (MRSA and MDRSA), with minimum inhibitory concentrations (MICs) of 6.25 and 12.5 µg/mL, respectively. Compound 2 also showed potent radical-scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) with an IC₅₀ of 11 µM, which was more active than the positive control, L-ascorbic acid (IC₅₀, 20.0 µM).
