Photosensitizer with tumor targeting and preparation method thereof

A photosensitizer and targeting technology, which is applied in the field of new targeted photosensitizer and its preparation, can solve the problems of poor water solubility and poor selectivity of tumor cells, and achieve the effect of simple preparation, clear compound structure and high selectivity

Inactive Publication Date: 2012-01-18
FUJIAN INST OF RES ON THE STRUCTURE OF MATTER CHINESE ACAD OF SCI
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  • Abstract
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  • Application Information

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Problems solved by technology

[0009] The invention mainly aims at the defects of metal phthalocyanine photosensitizers such as poor water solubility and poor selectivity to tumor cells, and provides a new photosensitizer with good water solubility and tumor targeting

Method used

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  • Photosensitizer with tumor targeting and preparation method thereof
  • Photosensitizer with tumor targeting and preparation method thereof
  • Photosensitizer with tumor targeting and preparation method thereof

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Embodiment Construction

[0022] Synthesis of zinc phthalocyanine-luteinizing hormone-releasing hormone analog (ZnPc-LHRH):

[0023] Dissolve 13.4mg (0.0215mmol) of β-monocarboxyl substituted zinc phthalocyanine and 24mg (0.0633mmol) of benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate (HBTU) Add 93.3 μL N,N-diisopropylethylamine (DIEA) to 1.5 mL N,N-dimethylformamide (DMF), and stir for 30 min at room temperature in the dark. Add 50 mg (0.015 mmol) of luteinizing hormone-releasing hormone (LHRH) analogue with the N-terminus exposed and resin-connected C-terminus to the above reaction system, and stir overnight at room temperature in the dark. After the reaction was completed, the residual reactant was washed away with N,N-dimethylformamide (DMF), and then washed several times with methanol until the methanol was colorless.

[0024] After the reaction, the resin was freeze-dried, reacted with 95% trifluoroacetic acid (TFA) for 4 hours, filtered off the solid, collected the filtrate, added...

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Abstract

The invention relates to a photosensitizer with the tumor targeting and a preparation method thereof. The photosensitizer preparation method is mainly characterized in that a peptides solid-phase synthesis method is utilized, carboxylic groups of beta-monocarboxyl substituted phthalocyanine zinc is firstly activated at normal temperature, then, the beta-monocarboxyl substituted phthalocyanine zinc is coupled with gonadotropin releasing hormone analogs under the effect of coupling agents, and finally, products are obtained through separation and purification by efficient liquid phase chromatographic columns. The preparation method is fast and simple, generated products have single structures, and high selectivity on specific tumor cells is realized. Therefore, the photosensitizer can be used as photodynamic specific tumor treatment candidate drug and has good application prospects.

Description

technical field [0001] The invention relates to a novel targeted photosensitizer and a preparation method thereof. The photosensitizer can be used for photodynamic targeted therapy of specific tumors. Background technique [0002] A report from the American Cancer Society points out that cancer has become the world's number one "economic killer" because of its economic loss and death toll surpassing AIDS, malaria, influenza and other human-to-human diseases, and it may also become the leading cause of death. According to the report: In 2008, the economic loss caused by cancer was as high as 895 billion US dollars, equivalent to 1.5% of global GDP. This loss only refers to the loss caused by the disability and life-year reduction caused by cancer, and does not include the cost of cancer treatment. Due to the low level of treatment and the lack of popularization of cancer knowledge, the cancer situation in my country is more serious than that in developed countries. Amon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/23C07K1/04A61K47/48A61K41/00A61P35/00
Inventor 黄明东徐芃陈卓陈锦灿周山勇胡萍陈学元
Owner FUJIAN INST OF RES ON THE STRUCTURE OF MATTER CHINESE ACAD OF SCI
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