Identification of a Novel Retinoid X Receptor Agonist from <i>Boenninghausenia albiflora</i> var. <i>japonica</i>

Retinoid X receptors (RXRs) are nuclear receptors involved in various crucial biological processes, such as gene regulation, metabolism, and cell differentiation. They predominantly function as heterodimers with other nuclear receptors and modulate gene expression in response to ligand binding. Additionally, they act as therapeutic targets for different conditions, such as cancer and metabolic disorders. Although synthetic RXR agonists, such as bexarotene, are used in clinical settings, they exert adverse side effects. In this study, to explore insights into potential natural RXR agonists as alternatives to existing drugs, we isolated 14 coumarins, including 1 new compound from Boenninghausenia albiflora var. japonica (Rutaceae). Among them, daphnoretin methyl ether (14), a known biscoumarin, was found to exhibit subtype-nonspecific RXR agonist activity.

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Publication Details

Journal
Chemical and Pharmaceutical Bulletin
Published
2025-03-06
DOI
https://doi.org/10.1248/cpb.c24-00728
Primary Topic
Natural product bioactivities and synthesis
Type
article
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0.00
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article

Identification of a Novel Retinoid X Receptor Agonist from Boenninghausenia albiflora var. japonica

Ayaka Murase, Tomoki Mizoguchi, Ken‐ichi Nakashima, Yasuharu Nakama et al.
Chemical and Pharmaceutical Bulletin
Natural product bioactivities and synthesis
article

Identification of a Novel Retinoid X Receptor Agonist from Boenninghausenia albiflora var. japonica

Ayaka Murase, Tomoki Mizoguchi, Ken‐ichi Nakashima, Yasuharu Nakama, Makoto Inoue, Ryura Tateiwa
article en

Abstract

Retinoid X receptors (RXRs) are nuclear receptors involved in various crucial biological processes, such as gene regulation, metabolism, and cell differentiation. They predominantly function as heterodimers with other nuclear receptors and modulate gene expression in response to ligand binding. Additionally, they act as therapeutic targets for different conditions, such as cancer and metabolic disorders. Although synthetic RXR agonists, such as bexarotene, are used in clinical settings, they exert adverse side effects. In this study, to explore insights into potential natural RXR agonists as alternatives to existing drugs, we isolated 14 coumarins, including 1 new compound from Boenninghausenia albiflora var. japonica (Rutaceae). Among them, daphnoretin methyl ether (14), a known biscoumarin, was found to exhibit subtype-nonspecific RXR agonist activity.

Chemical and Pharmaceutical BulletinVol. 73(3)
Aichi Gakuin University (JP)
Openalex Percentile: Top 96%
Natural product bioactivities and synthesis
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Identification of a Novel Retinoid X Receptor Agonist from <i>Boenninghausenia albiflora</i> var. <i>japonica</i> — Ayaka Murase, Tomoki Mizoguchi, et al. · Chemical and Pharmaceutical Bulletin (2025) | TGRS Research Map | TGRS