Action mechanism of the novel rice blast fungicide tolprocarb distinct from that of conventional melanin biosynthesis inhibitors
Open accessAbstract
The target site of tolprocarb, a novel systemic fungicide used for controlling rice blast, was investigated. Tolprocarb decolorized the mycelia of Magnaporthe grisea; the decolorization was reversed by adding scytalone or 1,3,6,8-tetrahydroxynaphthalene (1,3,6,8-THN). This result suggested that the target site of tolprocarb was polyketide synthase (PKS), which regulated polyketide synthesis and pentaketide cyclization in melanin biosynthesis. Further, we produced a transgenic Aspergillus oryzae, which possessed the PKS gene of M. grisea, and performed in vitro assays of PKS using membrane fractions from the transgenic A. oryzae. Compared with some conventional melanin biosynthesis inhibitors (cMBIs), tolprocarb only inhibited PKS activity in vitro. These results indicated that tolprocarb’s target protein in M. grisea was PKS, which differentiates this fungicide from other cMBIs.
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Melanin inhibitors can bind to the active site of PKS, altering its conformation and inhibiting catalytic activity, thereby blocking polyketide chain synthesis.
“Melanin inhibitors can bind to the active site of PKS, altering its conformation and inhibiting catalytic activity, thereby blocking polyketide chain synthesis.”
From Fungal Melanin in Plant Pathogens: Complex Biosynthesis Pathways and Diverse Biological Functions (2025) · cites this paper as [90]
The Discussion reports that tolprocarb inhibits the PKS of M. grisea, which catalyzes an early step in melanin synthesis. It does not establish that tolprocarb binds a PKS active site or changes the enzyme’s conformation. It also reports that the conventional melanin inhibitors tested did not affect PKS activity, so the claim is too broad as stated. (LLM, conf=0.87)
Experimental — accuracy not yet measuredPKS is essential for polyketide chain synthesis in the DHN pathway.
“PKS is essential for polyketide chain synthesis in the DHN pathway.”
From Fungal Melanin in Plant Pathogens: Complex Biosynthesis Pathways and Diverse Biological Functions (2025) · cites this paper as [90]
This prevents the formation of melanin precursors, ultimately halting DHN melanin production.
“This prevents the formation of melanin precursors, ultimately halting DHN melanin production [90,91].”
From Fungal Melanin in Plant Pathogens: Complex Biosynthesis Pathways and Diverse Biological Functions (2025) · cites this paper as [90]
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Cited by
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Fungal Melanin in Plant Pathogens: Complex Biosynthesis Pathways and Diverse Biological Functions
Jia, H., Liu, N., Zhang, L., Li, P., Meng, Y., Yuan, W., Li, H., Tantai, D., Qu, Q., Cao, Z., et al. (2025) · Plants · doi:10.3390/plants14142121 · Cited by 18 · see citing works
- Authors
- Hamada, T., Asanagi, M., Satozawa, T., Araki, N., Banba, S., Higashimura, N., Akase, T., & Hirase, K.
- Affiliations
- Mitsui Chemicals Crop & Life Solutions, Inc (Japan) (JP)
- Japan Science and Technology Agency (JP)
- Mitsui Chemicals (Japan) (JP)
- Venue
- Journal of Pesticide Science
- Publisher
- Pesticide Science Society of Japan
- Published
- 2014
- Volume
- 39
- Issue
- 3
- Pages
- 152-158
- ISSN
- 0385-1559 (ISSN-L)
- 1348-589X
- 1349-0923
- OpenAlex
- W2332886407
- Cited by
- 35
- References
- 0
- Citations by year
- 2026: 1 · 2025: 2 · 2024: 1 · 2023: 2 · 2022: 3 · 2021: 4 · 2019: 7 · 2018: 7 · 2017: 3 · 2016: 4 · 2015: 1
- FWCI
- 2.50
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Journal of Pesticide Science (publishedVersion)
- Topics
- Life Sciences › Agricultural and Biological Sciences › Ecology, Evolution, Behavior and Systematics › Fungal Plant Pathogen Control
- Health Sciences › Medicine › Pharmacology › Microbial Natural Products and Biosynthesis
- Health Sciences › Medicine › Infectious Diseases › Antifungal resistance and susceptibility
- Keywords
- rice blast, Magnaporthe grisea, polyketide synthase, melanin biosynthesis inhibitors, scytalone, Aspergillus oryzae, transgene expression
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