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Title: Discovery of a nonsteroidal brassinolide-like compound, NSBR1
Authors: Sugiura, Airi
Horoiwa, Shinri
Aoki, Takanori
Takimoto, Seisuke
Yamagami, Ayumi
Nakano, Takeshi  kyouindb  KAKEN_id  orcid (unconfirmed)
Nakagawa, Yoshiaki  kyouindb  KAKEN_id
Miyagawa, Hisashi  kyouindb  KAKEN_id  orcid (unconfirmed)
Author's alias: 杉浦, 愛理
幌岩, 真理
青木, 孝憲
瀧本, 征佑
山上, あゆみ
中野, 雄司
中川, 好秋
宮川, 恒
Keywords: brassinolide
rice lamina inclination assay
Arabidopsis thaliana
molecular dynamics
docking simulation
Issue Date: 20-Aug-2017
Publisher: Pesticide Science Society of Japan
Journal title: Journal of Pesticide Science
Volume: 42
Issue: 3
Start page: 105
End page: 111
Abstract: Fourteen compounds screened from 5 million compounds in silico were submitted to bioassay to find brassinolide (BL) agonists/antagonists against Arabidopsis thaliana. Of these, two N-benzoyl-N′-phenylpiperazine (NBNPP)-type compounds showed antagonistic activity; however, none showed agonistic activity against A. thaliana. The substituents at the benzoyl moiety of NBNPP were changed to OH groups to derive N-(3, 4-dihydroxybenzoyl)-N′-(4-butanoyl-2-fluorophenyl)pyrazine, which was named NSBR1. NSBR1 was rationally designed based on docking simulations and molecular dynamics. NSBR1 significantly suppressed the gene expression of CPD and BR6-ox2, which are known as marker genes for the action of BL. This novel NSBR1 was also effective in the rice lamina inclination assay (RLIA), and the activity in terms of the 50% effective dose (ED₅₀) was determined as 0.79 nmol/plant from the dose–response curve for RLIA.
Rights: ©Pesticide Science Society of Japan 発行元の許可を得て掲載しています。
DOI(Published Version): 10.1584/jpestics.D17-035
PubMed ID: 3036386
Appears in Collections:Journal Articles

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