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Texaphyrin-folic acid conjugate as well as preparation method and application thereof

A technology of chelate and folic acid derivatives, which can be used in drug combinations, pharmaceutical formulations, radioactive preparations in vivo, etc., and can solve the problem that there is no Texaphyrin-folate chelate.

Inactive Publication Date: 2021-08-24
弗兰克杰瑞拉罗德 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far, there is no report of Texaphyrin-folate conjugate

Method used

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  • Texaphyrin-folic acid conjugate as well as preparation method and application thereof
  • Texaphyrin-folic acid conjugate as well as preparation method and application thereof
  • Texaphyrin-folic acid conjugate as well as preparation method and application thereof

Examples

Experimental program
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Embodiment 2

[0093]Orthotopic PC3 prostate tumor model: Athymic nude male mice were purchased from Harlan Laboratories. A 5 mm long incision into the peritoneum was made in the abdomen; the bladder and seminal vesicles were partially excised from the abdominal cavity to expose the dorsal lobe of the prostate. Inject 5×105 PC-3M-luc-C6 cells (cell line expressing Lucifer, Caliper)

[0094] Use a 28-gauge needle from in situ to the dorsal lobe of the prostate. The organs were returned to the abdominal cavity, and the muscle wall and skin were sutured. Subcutaneous injection of 0.05 mg kg-1 for analgesia. Orthotopic prostate tumor growth was monitored by MRI (Biospec 70 / 30 USR, Bruker).

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Abstract

The invention belongs to the technical field of chemical compounds, and relates to a texaphyrin-folic acid conjugate as well as a preparation method and application thereof, wherein the texaphyrin-folic acid conjugate comprises texaphyrin, a texaphyrin derivative or a conjugate formed by combining a texaphyrin homolog with folic acid or an O-(alkylamino) diaminophenol derivative of a folic acid derivative through a covalent bond. The texaphyrin-folate conjugate or the texaphyrin-folate nano-particles disclosed by the invention are applied to treatment comprising radiosensitization, radiation therapy and photothermal therapy. The texaphyrin-folic acid conjugate also can be used for medical imaging comprising MRI, two-photon, SPECT, PET, CT, fluorescence and ultrasound.

Description

technical field [0001] The invention belongs to the technical field of chemical synthesis, and relates to a texaphyrin-folate chelate and a preparation method and application thereof. Background technique [0002] Oncology therapeutics and imaging agents face considerable hurdles when trying to selectively target cancerous lesions to achieve higher efficacy. So far, a variety of overexpressed receptors have been identified on cancer tumors, which provide valuable targets for the design of tumor drugs with higher selectivity and specificity. [0003] The folate receptor is a prominent target that has been shown to be overexpressed in a variety of cancer cell lines. [1] Based on this, a variety of imaging and therapeutic agents have been developed to target multiple cancer types in a single chemotherapy or imaging agent. [2] Although a worthy goal, the FDA has not approved the use of folic acid as a targeted cancer therapy or imaging agent. [0004] Texaphyrin is capable of...

Claims

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Application Information

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IPC IPC(8): C07D519/00
CPCC07D519/00A61K41/0052A61K49/0052A61K49/10A61K49/221A61K51/0451A61P35/00
Inventor 弗兰克·杰瑞·拉罗德乔瑟夫·米歇尔·凯卡顾梵陈汉杰
Owner 弗兰克杰瑞拉罗德
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