The Institute of Chemistry has made a series of progress in the field of conjugated polymer design and biomedical applications

Conjugated polymers have strong light-capturing capabilities and can be used to amplify fluorescent sensing signals, playing an increasingly important role in disease diagnosis and biological detection. In recent years, the application of conjugated polymers in fluorescence imaging at the cell and animal level and in the field of biomedicine has also received great attention. With the support of the National Natural Science Foundation of China and the Ministry of Science and Technology, researchers from the Key Laboratory of Organic Solids, Institute of Chemistry, Chinese Academy of Sciences have made new progress in the field of conjugated polymer design and biomedical applications.

Changes in the methylation of cancer-related gene promoters are a potential biomarker for early diagnosis of cancer. Compared to changes in single methylation, cumulative analysis of multiple promoter methylation levels is expected to improve the accuracy and sensitivity of cancer detection. They collaborated with the relevant personnel of the First Affiliated Hospital of the PLA General Hospital to analyze the DNA methylation levels of seven related genes of colon cancer using a novel fluorescence resonance energy transfer technology based on cationic conjugated polymers. Through stepwise discriminant analysis and cumulative detection analysis, higher accuracy and sensitivity of colon cancer detection results and differential diagnosis results were obtained. Combining the cumulative analysis of promoter methylation changes with the fluorescence resonance energy transfer of cationic conjugated polymers, this technology is expected to be used in the screening and differential diagnosis of colon cancer. Related research results were published in Nature Communications 2012, 3: 1206.

After the work was published, Nature Reviews Clinical Oncology (2013, 10, 3) published a special review entitled The help of epigenetics in differential diagnosis in the form of Research Highlights. They also designed and synthesized water-soluble fluorescent conjugated polymers with different main chain and side chain structures to obtain a red-green-blue three-color polymer system. By regulating the self-assembly of different fluorescent color polymers on the same microbial template engineered, multi-color emission conjugated polymer micro-nano particles at a single excitation wavelength were obtained. The application of multi-color coded polymer micro-nano particles in cell imaging and cell coding was studied by fluorescence spectroscopy, fluorescence microscopy and flow cytometry. The research results were published in Adv. Mater. 2012, 24, 637- 641 on. The researchers also designed and synthesized a new cationic branched side chain polyfluorene molecule, which can be used as a high-efficiency gene transfection material and also has a fluorescence imaging function. The transfection material can effectively protect the DNA from nuclease hydrolysis. The green fluorescent protein particle transfection experiment showed that the transfection efficiency is 92%, and the commercial transfection agent liposome 2000 (lipo2000) and polyethyleneimine (PEI) is equivalent and can be used for real-time tracking and localization of gene transfection. The results of this study were published in Adv. Mater. 2012, 24, 5428-5432.

Photodynamic therapy (PDT) has been applied clinically as a new disease treatment method, but this method relies on the illumination of external light sources. The researchers designed and developed a new model of photodynamic therapy system that does not require external light irradiation and uses the principle of chemical molecules to generate active oxygen to achieve effective suppression of tumor and microbial infections. In this system, the bioluminescence produced by the luminol molecule in the presence of peroxide oxidase and hydrogen peroxide can be efficiently transferred to the cationic oligomeric paraphenylene vinylene molecule (OPV) through the energy transfer (BRET) process, and the excited state OPV molecule Oxygen molecules sensitizing the surrounding environment produce reactive oxygen species (ROS), which in turn kills adjacent tumor cells and pathogenic microorganisms. This system can overcome the shortcomings of the light source that cannot penetrate deep tissues in classic photodynamic therapy, and provides new ideas for designing a new model of photodynamic therapy system. The research results are published in J. Am. Chem. Soc. 2012, 134, 13184- 13187. Most molecular-targeted anti-tumor systems rely on antibodies for cell-surface targeted recognition, and because the system cannot enter the cell, the system cannot recognize proteins in the cell. To this end, they designed and synthesized a multifunctional polymer-drug (polythiophene-tamoxifen) binary system, which can target and recognize specific signaling proteins (estrogen receptors) in MCF-7 cancer cells, Under light irradiation, the conjugated polymer can sensitize oxygen molecules to produce ROS and further inactivate signaling proteins, thereby inhibiting tumor cell growth. In addition, the fluorescent properties of the polymer endow this system to be used for intracellular fluorescence imaging tracking at the same time. The research results are published in Scientific Reports 2012, 2: 766.

Recently, researchers published a review article in the Journal of the American Chemical Society "Chem. Rev. 2012, 112, 4687-4735", focusing on the field of fluorescent imaging, disease diagnosis and treatment in the past five years. Important progress, and prospects for the future development direction of the field, as well as the challenges and opportunities.

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