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KMID : 0620720160220030216
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Natural Product Sciences
2016 Volume.22 No. 3 p.216 ~ p.219
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New Production of Antibacterial Polycyclic Quinazoline Alkaloid, Thielaviazoline, from Anthranilic Acid by the Marine-Mudflat-Derived Fungus Thielavia sp.
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Alain Simplice Leutou
Son Byeng-Wha
Yun Keum-Ja
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Abstract
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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 and¹³ C) data with those of reported compound (2). Compound 2 displayed in vitro antimicrobial activity against methicillinresistant 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).
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KEYWORD
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Thielaviazoline, Polycyclic quinazoline alkaloid, Thielavia sp., Microbial transformation
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