Related Experiment Video
Updated: Apr 24, 2026
Isolation of Mouse Interstitial Valve Cells to Study the Calcification of the Aortic Valve In Vitro
Published on: May 10, 2021
Hypericum monogynum extract inhibits human aortic valve interstitial cell calcification by interfering with the
Zhengfeng Fan1, Jincheng Hou1, Jiangchun Wei2
1Department of Cardiovascular Surgery, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China.
Insights
Chipericumin D inhibits calcific aortic valve disease (CAVD) by targeting the epidermal growth factor receptor (EGFR). This natural compound shows promise as a new pharmaceutical therapy for CAVD, offering a potential alternative to valve replacement surgery.
Area of Science:
- Cardiovascular Research
- Pharmacology
- Molecular Biology
Background:
- Calcific aortic valve disease (CAVD) is a prevalent heart condition with no approved pharmaceutical treatments.
- Current interventions for CAVD involve surgical or transcatheter valve replacement.
- Osteogenic differentiation of human aortic valve interstitial cells (hVICs) is a key factor in CAVD development.
Purpose of the Study:
- To identify compounds that inhibit hVIC osteogenic differentiation.
- To investigate the molecular mechanisms underlying the action of identified compounds.
- To explore novel therapeutic targets for CAVD.
Main Methods:
- Screening of an 88-compound library using dot-blotting.
- Network pharmacology, molecular docking, DARTS, CETSA, and SPR assays.
- Analysis of the EGFR/PI3K/AKT signaling pathway in hVICs.
Main Results:
- Chipericumin D, from Hypericum monogynum L., demonstrated potent inhibition of hVIC osteogenic differentiation.
- Direct binding of chipericumin D to the epidermal growth factor receptor (EGFR) was confirmed.
- Chipericumin D suppressed EGFR/PI3K/AKT pathway activation in hVICs under osteogenic conditions.
Conclusions:
- Chipericumin D is a promising therapeutic candidate for CAVD.
- EGFR represents a novel molecular target for therapeutic intervention in CAVD.
- This study provides a foundation for developing pharmaceutical treatments for CAVD.
Abstract:
Calcific aortic valve disease (CAVD) is a serious heart valve condition with increasing global prevalence. Currently, transcatheter aortic valve implantation (TAVI) or surgical aortic valve replacement (SAVR) represents the only available treatment strategy, as no pharmaceutical therapies for CAVD are approved. The aim of this study was to identify compounds capable of inhibiting osteogenic differentiation of human aortic valve interstitial cells (hVICs), a process critically implicated in CAVD pathogenesis, and to elucidate the underlying molecular mechanism. From an in-house library of 88 compounds screened via dot-blotting, we identified chipericumin D, a natural compound extracted from Hypericum monogynum L., as a candidate exhibiting potent inhibitory activity against hVIC osteogenic differentiation. Network pharmacology analysis, molecular docking, drug affinity responsive target stability (DARTS), cellular thermal shift assay (CETSA), and surface plasmon resonance (SPR) collectively demonstrated direct binding of chipericumin D to the epidermal growth factor receptor (EGFR). Furthermore, chipericumin D suppressed activation of the EGFR/phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) signaling pathway in hVICs cultured under osteogenic medium (OM) conditions. These findings indicate that chipericumin D is a promising therapeutic candidate for CAVD, and provide preliminary evidence that EGFR constitutes a novel molecular target for CAVD intervention.
Related Concept Videos
01:25Aortic Regurgitation III: Medical Management
01:26Heart Failure Drugs: Inhibitors of Renin-Angiotensin System