Journal
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
Volume 68, Issue 48, Pages 14204-14211Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jafc.0c06363
Keywords
FabH; secondary metabolites; antibacterial activity; Xanthomonas oryzae pv. oryzae; endophytic fungi
Funding
- National Key Research and Development Program of China [2017YFD0200500]
- National Natural Science Foundation of China [31572043, 32072443]
- Jiangsu Agriculture Science and Technology Innovation Fund [CX(18)3055]
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beta-Ketoacyl-acyl carrier protein synthase III (KAS III, FabH) is essential for bacterial fatty acid biosynthesis. Recent studies indicate that FabH can be a potential target for bactericide development. In the present study, an immobilized FabH column was developed and used to screen FabH inhibitors from complex natural product extracts. Combined with HPLC, four secondary metabolites, alternariol (1), altenuisol (2), alterlactone (3), and dehydroaltenusin (4), were site-directed, isolated, and identified from the crude extract of Alternaria alternata ZHJG5. These compounds showed inhibitory activities on FabH of Xanthomonas oryzae pv. oryzae (Xoo) with IC50 values from 29.5 to 74.1 mu M and also displayed a varying degree of antibacterial activities against Xoo with minimal inhibitory concentration values from 4 to 64 mu g/mL. Molecular modeling was then used to picture how the compounds interact with XooFabH. Two inhibitors, compounds 1 and 3, exhibited significant bactericidal activity against rice bacterial leaf blight with a protective efficiency of 66.2 and 82.5% at the concentration of 200 mu g/mL, respectively, suggesting that they could be lead candidates to develop novel bactericides.
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