Cinobufagin Directly Targets PDE4D to Disrupt Fibroblast–Dendritic Cell Crosstalk in Atopic Dermatitis

Atopic dermatitis (AD) is a chronic inflammatory skin disease driven by immune dysregulation and Th2-dominant inflammation. This study identifies phosphodiesterase 4D (PDE4D) as a key regulator of AD pathogenesis and a potential therapeutic target. Single-cell RNA sequencing (scRNA-seq) revealed activation of the macrophage migration inhibitory factor (MIF) signaling pathway in lesional tissues, with inflammatory fibroblasts mediating MIF-driven interactions with myeloid cells. Elevated PDE4D expression in lesional tissues suppressed cyclic adenosine monophosphate (cAMP) signaling, promoting inflammation. Cinobufagin, a bufadienolide compound, is identified as a potent PDE4D inhibitor. Compared to other PDE4 inhibitors used in clinical cases, cinobufagin demonstrated superior efficacy in improving AD in mice while effectively regulating the MIF pathway. It directly bound to PDE4D, restored cAMP signaling, suppressed MIF secretion in inflammatory fibroblasts, and disrupted fibroblast-dendritic cell interactions via the cAMP/protein kinase A (PKA)/cAMP-response element binding protein (CREB) pathway, thereby significantly reducing the clinical and histological features of AD. Notably, PDE4D knockout mice exhibited diminished inflammation, mimicking the effects of cinobufagin and confirming a role for PDE4D in AD progression. These findings establish PDE4D as a critical driver of AD and demonstrate that cinobufagin effectively targets this pathway, offering a promising therapeutic approach for AD and related inflammatory skin disorders.

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Publication Details

Journal
Advanced Science
Published
2025-10-08
DOI
https://doi.org/10.1002/advs.202501670
Citations
1
Primary Topic
Asthma and respiratory diseases
Type
article
Field-Weighted Citation Impact
1.16
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article

Cinobufagin Directly Targets PDE4D to Disrupt Fibroblast–Dendritic Cell Crosstalk in Atopic Dermatitis

Dihui Xu, Jiaojiao Wang, Yang Sun, Yuyu Zhu et al.
1 citations
Advanced Science
Asthma and respiratory diseases
1.16
article

Cinobufagin Directly Targets PDE4D to Disrupt Fibroblast–Dendritic Cell Crosstalk in Atopic Dermatitis

Dihui Xu, Jiaojiao Wang, Yang Sun, Yuyu Zhu, Chunxiu Xiao, Shicong Li, Min Hong, Hongyue Ma, Chenyang Zhang, Liang Zhang, Xiang Lv, Jing Zhou, Wenyuan Wu, Meng Yu, Dongping Yuan
article en
1 citations

Abstract

Atopic dermatitis (AD) is a chronic inflammatory skin disease driven by immune dysregulation and Th2-dominant inflammation. This study identifies phosphodiesterase 4D (PDE4D) as a key regulator of AD pathogenesis and a potential therapeutic target. Single-cell RNA sequencing (scRNA-seq) revealed activation of the macrophage migration inhibitory factor (MIF) signaling pathway in lesional tissues, with inflammatory fibroblasts mediating MIF-driven interactions with myeloid cells. Elevated PDE4D expression in lesional tissues suppressed cyclic adenosine monophosphate (cAMP) signaling, promoting inflammation. Cinobufagin, a bufadienolide compound, is identified as a potent PDE4D inhibitor. Compared to other PDE4 inhibitors used in clinical cases, cinobufagin demonstrated superior efficacy in improving AD in mice while effectively regulating the MIF pathway. It directly bound to PDE4D, restored cAMP signaling, suppressed MIF secretion in inflammatory fibroblasts, and disrupted fibroblast-dendritic cell interactions via the cAMP/protein kinase A (PKA)/cAMP-response element binding protein (CREB) pathway, thereby significantly reducing the clinical and histological features of AD. Notably, PDE4D knockout mice exhibited diminished inflammation, mimicking the effects of cinobufagin and confirming a role for PDE4D in AD progression. These findings establish PDE4D as a critical driver of AD and demonstrate that cinobufagin effectively targets this pathway, offering a promising therapeutic approach for AD and related inflammatory skin disorders.

Advanced ScienceVol. 12(48)
Nanjing University of Chinese Medicine (CN), Xuzhou Medical College (CN), Nanjing Drum Tower Hospital (CN)
Openalex Percentile: Top 17%
Asthma and respiratory diseases
1.16
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