Aza-BODIPY-Biotin Conjugates DPR2a and DPR2b as Theranostic Agents
- Overview
Brief Description: Novel 2,6-Diiodo-aza-BODIPY-Biotin Conjugates (DPR2a, DPR2b) act as third-generation photosensitizers for cancer theranostics (imaging and photodynamic therapy). They selectively target cancer cells and exhibit excellent photophysical properties and PDT activity.
Development Stage: Preclinical stage, with detailed synthesis, photophysical characterization, and in vitro photobiological evaluation, showing promising results in laboratory settings.
- Key Features
- NIR Absorption and Emission: Strong Near-Infrared absorption (550-750 nm) and emission (640-850 nm) enable deep tissue penetration for both imaging and PDT.
- High Singlet Oxygen Generation Quantum Yield: High yields (0.72 for DPR2a, 0.75 for DPR2b) indicate potent photodynamic therapy efficacy.
- Cancer Cell Targeting (Biotin Conjugation): Biotin conjugation ensures specific targeting of cancer cells, potentially reducing side effects on healthy tissues.
- Benefits:
- Economic Impact: Potential to reduce overall cancer treatment costs through more effective and targeted therapies.
- Social Impact: Offers more precise diagnosis and treatment, minimizing damage to healthy tissues and improving patient quality of life.
- Applications:
- Healthcare (Cancer Treatment and Diagnostics): Primarily used as theranostic agents for cancer.
- Photodynamic Therapy (PDT): DPR2a and DPR2b can be used as photosensitizers to generate reactive oxygen species that kill cancer cells upon light activation. They have shown significant photocytotoxicity against various cancer cell lines, including breast, colon, liver, cervical, pancreatic, and oral cancer.
- Bioimaging: Their strong NIR absorption and emission properties make them suitable for in vivo imaging applications, allowing for real-time monitoring and localization of cancer cells.
- Research Opportunities: The compound has potential for clinical trials and further commercialization. Further studies could explore their efficacy in diverse cancer types and in vivo models.
- Case Studies:
- Case Study 1 (In Vitro Photobiological Evaluation): In vitro studies on human breast cancer cell line MDA-MB-231 demonstrated that DPR2a and DPR2b are non-cytotoxic in the dark but exhibit remarkable photocytotoxicity under light exposure. The IC50 values were 3 µM for DPR2a and 7 µM for DPR2b in MDA-MB-231 cells. Cellular uptake was observed within 15 minutes of incubation, with localization in the cytoplasm.
- Case Study 2 (Synergistic Effect): The conjugates showed excellent photocytotoxic effects across various cancer cell lines, with IC50 values ranging from 3.5 µM to 15 µM depending on the cell type. Furthermore, synergistic effects were observed in combination assays, leading to decreased cell viability, elevated reactive oxygen species (ROS), increased apoptotic induction, and G2/M arrest in cancer cells after PDT treatment with DPR2a and DPR2b.
- IP Status:
- Intellectual Property: An Indian patent application has been filed jointly by Council of Scientific & Industrial Research and RGCB vide application Number
202111015510 dated March 31 2021.
- Support Offered:
- Licensing Options: Exclusive, non-exclusive licensing options are available.
- Technical Support: Experimental protocols and optimization guidance will be provided.
- Collaboration Opportunities: Co‑development of therapeutic applications, Research collaborations and Industry partnerships.
- Contact Information:
Contact Person: :Dr. S Asha Nair, Scientist, BRIC-RGCB
Email Address: sasha@rgcb.res.in,techventures@rgcb.res.in
Phone Number: +91-471-2529-501