Tumor imaging and treatment probe of targeted follicle-stimulating hormone receptor as well as preparation method and application of tumor imaging and treatment probe

A follicle-stimulating hormone and tumor imaging technology, which is applied to the preparation method of peptides, preparations for in vivo experiments, anti-tumor drugs, etc., can solve the problem that near-infrared fluorescent dyes cannot specifically bind to tumor cells, and achieve improved surgical resection rate, reduce tumor burden, and improve prognosis

Active Publication Date: 2021-03-05
FUDAN UNIV +1
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Problems solved by technology

However, near-infrared fluorescent dyes cannot specifically bind to tumor cells. It has been reported in the literature that the false positive rate of indocyanine green for ovarian cancer imaging is as high as 62%.

Method used

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  • Tumor imaging and treatment probe of targeted follicle-stimulating hormone receptor as well as preparation method and application of tumor imaging and treatment probe
  • Tumor imaging and treatment probe of targeted follicle-stimulating hormone receptor as well as preparation method and application of tumor imaging and treatment probe
  • Tumor imaging and treatment probe of targeted follicle-stimulating hormone receptor as well as preparation method and application of tumor imaging and treatment probe

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Embodiment Construction

[0028]The invention provides a novel FSH receptor-targeted tumor imaging and treatment probe FSH-Rh760, which is formed by coupling FSH polypeptide and near-infrared fluorescent dye Rh760.

[0029] The specific embodiment of preparing above-mentioned near-infrared fluorescent probe is as follows:

[0030] (1) Add 0.2 mmol compound Rh760, 100 mg (0.25 mmol) Carter condensation reagent, 150 mg (1 mmol) piperazine and 10 mL dichloromethane solution into a 50 mL round-bottomed flask, and stir for 2 h at room temperature. After the reaction, the solvent was distilled off under reduced pressure, and the compound Rh760-Paz (105 mg) was purified and isolated by column chromatography using dichloromethane and methanol as eluents. Yield: 80%. 1 H NMR (400 MHz, DMSO-d6, δ) 8.99 (bs, 1H), 7.62 (m, 2H), 7.53 (d, J = 8.4 Hz, 1H), 7.35 (d, J = 8.4 Hz, 1H), 6.76 (dd, J = 9.2 Hz, J =2.4 Hz, 1H), 6.71 (d, J = 9.2 Hz, 1H), 6.62 (d, J = 2.4 Hz, 1H), 3.45 (q, J =13.6 Hz, 4H), 3.15-3...

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Abstract

The invention provides a tumor imaging and treatment probe of a targeted follicle-stimulating hormone receptor as well as a preparation method and application of the tumor imaging and treatment probe,aiming at accurately identifying a focus in an operation and increasing specific imaging on the basis of the advantage of a near-infrared fluorescent dye for imaging. The tumor imaging and treatmentprobe FSH-Rh760 of the targeted follicle-stimulating hormone receptor is formed by coupling follicle-stimulating hormone polypeptide (LYTRDLVYKDPARPKIQKTCTF) and the near-infrared fluorescent dye Rh760. The tumor imaging and treatment probe has the advantages that ovarian cancer cells are identified in a targeted manner by utilizing high expression of FSHR in ovarian cancer based on a principle ofspecific binding of the FSH polypeptide and the FSHR. The tumor imaging and treatment probe has good application prospects in fluorescent imaging and fluorescent guided operations by utilizing the advantages of deeper penetration depth and lower background signals of the near-infrared fluorescent dye Rh760. The targeted probe FSH-Rh760 can be used for photothermal therapy of the ovarian cancer, and is used as a supplement of operative treatment to improve prognosis of the ovarian cancer.

Description

technical field [0001] The invention relates to a follicle-stimulating hormone receptor-targeted tumor imaging and treatment probe as well as a preparation method and application thereof. Background technique [0002] The mortality rate of ovarian cancer ranks first among malignant tumors of the female reproductive system. 87% of the cases were detected at advanced stage (stages III and IV), and the 10-year survival rate was only 15%. Reductive surgery combined with chemotherapy is the main treatment for advanced ovarian cancer. The thoroughness of surgery is closely related to the prognosis of ovarian cancer. In order to achieve complete resection, accurate identification of the lesion during operation is the key. Existing imaging examinations such as ultrasound, X-ray, CT, and MRI are non-specific imaging of tumors, and are difficult to be used for intraoperative real-time imaging. Fluorescence-guided surgery uses tumor-targeted imaging probes to specifically bind and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/59C07K1/04C07K1/02C07K1/107C09K11/06A61K49/00A61K41/00A61P35/00
CPCC07K14/59C09K11/06A61K49/0056A61K49/0021A61K41/0052A61P35/00C09K2211/1029C09K2211/1088Y02P20/55
Inventor 石梅张晓燕周晓波刘齐雨李富友李小平徐丛剑
Owner FUDAN UNIV
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