Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe

<b>Background:</b> Atherosclerotic diseases, including coronary heart disease and cerebrovascular disease, are leading causes of morbidity and mortality worldwide. Atherosclerosis is a chronic vascular condition marked by the accumulation of lipid plaque within arterial walls. These plaq...

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Main Authors: Tingting Gao, Siqi Gao, Maolin Qiao, Chuanlong Lu, Heng Wang, Hongjiu Zhang, Lizheng Li, Shule Wang, Ruijing Zhang, Honglin Dong
Format: Article
Language:English
Published: MDPI AG 2025-03-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/4/444
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author Tingting Gao
Siqi Gao
Maolin Qiao
Chuanlong Lu
Heng Wang
Hongjiu Zhang
Lizheng Li
Shule Wang
Ruijing Zhang
Honglin Dong
author_facet Tingting Gao
Siqi Gao
Maolin Qiao
Chuanlong Lu
Heng Wang
Hongjiu Zhang
Lizheng Li
Shule Wang
Ruijing Zhang
Honglin Dong
author_sort Tingting Gao
collection DOAJ
description <b>Background:</b> Atherosclerotic diseases, including coronary heart disease and cerebrovascular disease, are leading causes of morbidity and mortality worldwide. Atherosclerosis is a chronic vascular condition marked by the accumulation of lipid plaque within arterial walls. These plaques can become unstable and rupture, leading to thrombosis and subsequent cardiovascular events. Therefore, early identification of vulnerable plaque is critical for preventing such events. <b>Objectives:</b> This study aims to develop a novel imaging platform for atherosclerotic plaque by designing a molecular imaging probe based on fluorescent molecules that target lipid necrotic cores. The goal is to specifically detect high-risk plaque, enabling early diagnosis and intervention. <b>Methods:</b> Bioinformatic analysis and immunofluorescence were used to detect CD36 expression in human carotid plaque. CD36pep-ICG was synthesized using the Fmoc solid-phase peptide method. A series of experiments was conducted to characterize the probe’s properties. To assess imaging performance, probe concentration gradients were tested using FLI equipment. Ex vivo imaging was performed on atherosclerotic mice and treatment models to evaluate the probe’s targeting ability and effectiveness in monitoring disease progression. <b>Results:</b> The CD36 expression was significantly elevated in the core of plaque compared to distal regions. The CD36pep-ICG probe, specifically designed to target lipids, was successfully synthesized and exhibited excellent fluorescence properties. In animal models, FLI imaging demonstrated that the CD36pep-ICG probe selectively accumulated in atherosclerotic plaque, enabling precise plaque detection. Moreover, the probe was used to monitor the therapeutic efficacy of anti-atherosclerotic drugs. <b>Conclusions:</b> The CD36pep-ICG probe developed in this study is an effective molecular imaging tool for the specific identification of vulnerable atherosclerotic plaque, offering a novel approach for early diagnosis and treatment. Additionally, the probe shows promise in tracking the therapeutic effects of the drug, potentially advancing the precision treatment of cardiovascular diseases.
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spelling doaj-art-b55f2f9d37ec4fe890af83ce656af80d2025-08-20T02:18:15ZengMDPI AGPharmaceutics1999-49232025-03-0117444410.3390/pharmaceutics17040444Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core ProbeTingting Gao0Siqi Gao1Maolin Qiao2Chuanlong Lu3Heng Wang4Hongjiu Zhang5Lizheng Li6Shule Wang7Ruijing Zhang8Honglin Dong9The Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, ChinaThe Second Clinical Medical College, Shanxi Medical University, Taiyuan 030000, China<b>Background:</b> Atherosclerotic diseases, including coronary heart disease and cerebrovascular disease, are leading causes of morbidity and mortality worldwide. Atherosclerosis is a chronic vascular condition marked by the accumulation of lipid plaque within arterial walls. These plaques can become unstable and rupture, leading to thrombosis and subsequent cardiovascular events. Therefore, early identification of vulnerable plaque is critical for preventing such events. <b>Objectives:</b> This study aims to develop a novel imaging platform for atherosclerotic plaque by designing a molecular imaging probe based on fluorescent molecules that target lipid necrotic cores. The goal is to specifically detect high-risk plaque, enabling early diagnosis and intervention. <b>Methods:</b> Bioinformatic analysis and immunofluorescence were used to detect CD36 expression in human carotid plaque. CD36pep-ICG was synthesized using the Fmoc solid-phase peptide method. A series of experiments was conducted to characterize the probe’s properties. To assess imaging performance, probe concentration gradients were tested using FLI equipment. Ex vivo imaging was performed on atherosclerotic mice and treatment models to evaluate the probe’s targeting ability and effectiveness in monitoring disease progression. <b>Results:</b> The CD36 expression was significantly elevated in the core of plaque compared to distal regions. The CD36pep-ICG probe, specifically designed to target lipids, was successfully synthesized and exhibited excellent fluorescence properties. In animal models, FLI imaging demonstrated that the CD36pep-ICG probe selectively accumulated in atherosclerotic plaque, enabling precise plaque detection. Moreover, the probe was used to monitor the therapeutic efficacy of anti-atherosclerotic drugs. <b>Conclusions:</b> The CD36pep-ICG probe developed in this study is an effective molecular imaging tool for the specific identification of vulnerable atherosclerotic plaque, offering a novel approach for early diagnosis and treatment. Additionally, the probe shows promise in tracking the therapeutic effects of the drug, potentially advancing the precision treatment of cardiovascular diseases.https://www.mdpi.com/1999-4923/17/4/444atherosclerosislipid necrotic corefluorescence imagingCD36targeting probe
spellingShingle Tingting Gao
Siqi Gao
Maolin Qiao
Chuanlong Lu
Heng Wang
Hongjiu Zhang
Lizheng Li
Shule Wang
Ruijing Zhang
Honglin Dong
Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe
Pharmaceutics
atherosclerosis
lipid necrotic core
fluorescence imaging
CD36
targeting probe
title Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe
title_full Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe
title_fullStr Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe
title_full_unstemmed Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe
title_short Advanced Detection and Therapeutic Monitoring of Atherosclerotic Plaque Using CD36-Targeted Lipid Core Probe
title_sort advanced detection and therapeutic monitoring of atherosclerotic plaque using cd36 targeted lipid core probe
topic atherosclerosis
lipid necrotic core
fluorescence imaging
CD36
targeting probe
url https://www.mdpi.com/1999-4923/17/4/444
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