The
control of harmful cyanobacterial blooms has been becoming
a global challenge. The development of eco-friendly algicides with
strong specificity is urgently needed. The photosynthetic apparatus
is a promising target site for algicides to minimize the possible
harmful effects on animals and humans. In this study, biologically
derived 2-hydroxychalcone efficiently inhibited the growth of bloom-forming M. aeruginosa by selectively interfering with photosynthesis.
2-Hydroxychalcone targeting Photosystem II (PSII) inhibited electron
transfer between the primary and secondary electron acceptors (QA and QB) and the binding of plastoquinone (PQ)
molecules to the QB binding pocket at the acceptor side
of PSII, as revealed by polyphasic chlorophyll (Chl) a fluorescence
induction and QA
– reoxidation kinetics.
Molecular docking for 2-hydroxychalcone to D1 protein and the proteomic
responses of M. aeruginosa suggested that 2-hydroxychalcone
formed a stable monodentate ligand with the nonheme iron in D1 protein,
provoking significant modulation of PSII proteins. The unique binding
mode of 2-hydroxychalcone with PSII differentiated it from classical
PSII inhibitors. Furthermore, 2-hydroxychalcone down-regulated the
expression of microcystin (MC) synthesis-related genes to restrain
MC synthesis and release. These results indicated the potential application
of 2-hydroxychalcone as an algicide or a template scaffold for designing
novel derivatives with superior algicidal activity.
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