Fluorescent Probes for Detection of Calcifications

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This invention describes novel fluorescent probes that are specifically designed to detect calcium deposits (calcifications) in biological tissues. The probes consist of a fluorescent organic core (such as porphyrin, BODIPY, or other dye cores) to which one or more metal-binding groups (like phosphonic acid or arsonic acid) are directly linked. When these probes bind to calcium-containing structures (such as hydroxyapatite in bones or pathological calcifications), their fluorescence is enhanced, enabling highly sensitive and specific imaging of such deposits in vitro and in vivo.

Use CasesContent extracted from patent full text and abstract with AI.

• Early detection of microcalcifications in breast tissue for breast cancer screening.
• Monitoring bone growth and resorption, important for bone health studies and osteoporosis tracking.
• Detecting and imaging calcifications in soft tissues (e.g., brain, eye, kidneys) for diagnosing diseases such as Alzheimer’s, age-related macular degeneration, or vascular disease.
• As contrast agents in medical imaging techniques for improved visualization of calcifications.
• Detecting and studying calcium phosphate or hydroxyapatite in cell cultures, animal models, or clinical samples.
• Potentially guiding therapies by enabling real-time monitoring of calcification regression or progression during treatment.

BenefitsContent extracted from patent full text and abstract with AI.

• Greatly increased sensitivity and specificity for detecting small or early-stage calcifications compared to traditional stains and imaging methods.
• Fluorescence signal increases upon binding, yielding high signal-to-noise ratio and more reliable imaging results.
• Broad applicability across tissues (bone and soft tissues) and diseases.
• Cost-effective synthesis using established chemical methods, allowing for scalable production.
• Some probes are cell-permeable and minimally toxic, enabling use in live-cell and in vivo animal imaging.
• May function at physiological pH and low concentrations, minimizing interference with biological samples.
• Potential improvement over existing commercial agents (e.g., lower cost, larger fluorescence range, higher efficiency).

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Inventors & Applicants

Patent Abstract

The invention relates to a fluorescent probe comprising one or more metal binding functional group, preferably selected the group comprising phosphonic acid group and an arsonic acid group, wherein the functional group is covalently linked to a fluorescent core via a sp2-carbon atom of the fluorescent core. In embodiments, the fluorescent core is an organic fluorescent compound/moiety, preferably a tetrapyrrole derivative, such as porphyrin or phthalocyanine, acridine, BODIPY, cyanine or cyanine derivatives, carbazole, coumarine or coumarine derivatives, xanthene or xanthene derivatives such as fluorescein or rhodamine. Preferably, the fluorescent probe of the invention can bind to calcium and/or a calcification, such as preferably hydroxyapatite (HAP). In a further aspect, the invention relates a fluorescent probe of the invention for use in a method of detecting calcium, preferably a calcification or HAP, in a bodily tissue. Also, the invention relates to the use of the fluorescent probe of the invention for detecting calcium, a calcification and/or HAP, preferably calcium depositions in a bodily tissue.