Aoi Kimishima, Yukihiro Asami, Naozumi Kondo, Sota Negami, Sota Honma, Yukiko Ujie
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Threonyl-tRNA Synthetase Is the Target of Borrelidin Insecticidal Activity against Silkworms.
We explore borrelidin and semisynthetic derivatives as promising pesticide candidates targeting threonyl-tRNA synthetase (ThrRS). Enzymatic inhibition assays and pull-down assays supported ThrRS as the target of borrelidins for insecticidal activity. Interestingly, derivative 6 showed weak in vitro inhibition but comparable in vivo insecticidal activity to borrelidin. Comparative efficacy tests via intravenous (i.v.) and intraperitoneal (i.p.) administration in silkworm larvae indicated improved pharmacokinetics for compound 6. These findings highlight ThrRS as a valuable insecticidal target and demonstrate the effectiveness of our original silkworm-based screening platform in identifying lead compounds with favorable pharmacokinetics that are often overlooked by conventional in vitro screening approaches.
期刊介绍：
The Journal of Natural Products invites and publishes papers that make substantial and scholarly contributions to the area of natural products research. Contributions may relate to the chemistry and/or biochemistry of naturally occurring compounds or the biology of living systems from which they are obtained.
Specifically, there may be articles that describe secondary metabolites of microorganisms, including antibiotics and mycotoxins; physiologically active compounds from terrestrial and marine plants and animals; biochemical studies, including biosynthesis and microbiological transformations; fermentation and plant tissue culture; the isolation, structure elucidation, and chemical synthesis of novel compounds from nature; and the pharmacology of compounds of natural origin.
When new compounds are reported, manuscripts describing their biological activity are much preferred.
Specifically, there may be articles that describe secondary metabolites of microorganisms, including antibiotics and mycotoxins; physiologically active compounds from terrestrial and marine plants and animals; biochemical studies, including biosynthesis and microbiological transformations; fermentation and plant tissue culture; the isolation, structure elucidation, and chemical synthesis of novel compounds from nature; and the pharmacology of compounds of natural origin.
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