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Targeted tracing noble metal fluorescence probe and anti-tumor prodrug

A nano-fluorescent probe, targeting technology, used in anti-tumor drugs, drug combinations, luminescent materials, etc., can solve the problems of long targeting time to the tumor site, increasing the complexity of the method, lack of targeting molecules, etc. Achieve the effect of reducing toxic and side effects, achieving cell-level imaging, and improving the cure rate

Inactive Publication Date: 2012-10-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since different probes are investigated at the cell level and animal level, it is not consistent to a certain extent and increases the complexity of the method
Xu et al. synthesized fluorescent gold nanoclusters (Au-BSA) modified on the surface of bovine serum albumin. Due to the lack of targeting molecules, Au-BSA took a long time to target the tumor site, and the contrast between the tumor site and other tissue sites was not high. (Wu X, He X, Wang K, Xie C, Zhou BQing Z. Nanoscale. 2010, 2, 2244-2249)

Method used

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  • Targeted tracing noble metal fluorescence probe and anti-tumor prodrug
  • Targeted tracing noble metal fluorescence probe and anti-tumor prodrug
  • Targeted tracing noble metal fluorescence probe and anti-tumor prodrug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation of Au NCs-2DG-MPA:

[0034] Take 1ml of gold nanocluster solution, 11.5mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), mix the two together in the dark and stir for reaction, and then add N- Hydroxysuccinimide (NHS) continued to avoid light and stirred for reaction, the reaction time should not be too long, EDC is easy to hydrolyze. After reacting for 2 hours, 24 mg of 2-DG was added, and the reaction was stirred overnight in the dark. The clear red-brown solution (Au-2-DG) was purified by a Sephadex column (G-25) to remove unreacted starting material. Take 1 mg of organic near-infrared dye MPA, dicyclohexylcarbodiimide (DCC), N-hydroxysuccinimide (NHS) and stir in the dark for 3 hours. Take 1ml of the purified Au-2DG solution and 200μl of the activated MPA solution, mix and stir in the dark for 12 hours, and then purify with Sephadex (G-25) to obtain the final product.

[0035] Its absorption and fluorescence spectra are shown in...

Embodiment 2

[0037] Preparation of Au NCs-FA-MPA:

[0038] Take 22mg of folic acid, 12mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (DCC), and N-hydroxysuccinimide (NHS) and mix them in the dark and stir to react. The reaction time should not be too long, as EDC is easily hydrolyzed. After 3 hours of reaction, 24 mg of FA was added, and the reaction was stirred overnight in the dark. The clear red-brown solution (Au-FA) was purified by a Sephadex column (G-25) to remove unreacted starting material. Take 1 mg of organic near-infrared dye MPA, dicyclohexylcarbodiimide (DCC), and N-hydroxysuccinimide (NHS) and stir in the dark for 3 hours. Take 1ml of the purified Au-FA solution and 200μl of the activated MPA solution, mix well and stir in the dark to react overnight, and then purify it with Sephadex (G-25) to obtain the final product.

Embodiment 3

[0040] Preparation of Au NCs-2-DG-DOX:

[0041] Take 1ml of gold nanocluster solution, 11.5mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), mix the two together in the dark and stir for reaction, and then add N- Hydroxysuccinimide (NHS) continued to avoid light and stirred for reaction, the reaction time should not be too long, EDC is easy to hydrolyze. After 2 hours of reaction, 15 mg of methionine (also known as methionine) was added, and the reaction was stirred overnight in the dark. The clear red-brown solution (Au-Met) was purified by a Sephadex column (G-25) to remove unreacted starting material. Take 1 mg of organic near-infrared dye DOX, dicyclohexylcarbodiimide (DCC), N-hydroxysuccinimide (NHS) and stir for 3 hours in the dark. Take 1ml of the purified Au-2-DG solution and 200μl of the activated DOX solution, mix well and stir in the dark to react overnight, and then purify it with Sephadex (G-25) to obtain the final product.

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Abstract

The invention relates to a bio-assay reagent for early diagnosis of tumor and a prodrug for the targeted therapy of tumor, in particular to a targeted tracing noble metal fluorescence probe and an anti-tumor prodrug. Through experiment, the synthesized probe does not have cytotoxicity and is safe and effective, can realize the level imaging of cells and the imaging of in-vivo tumor, and has good prospect when used as the targeted fluorescence probe or the prodrug.

Description

technical field [0001] The invention relates to a living body detection reagent for early tumor diagnosis and a prodrug for tumor targeting therapy. It specifically relates to a targeted near-infrared fluorescent probe and a prodrug. Background technique [0002] Tumor is a major disease that threatens human health at present. The mortality rate caused by malignant tumors is second only to cardiovascular diseases, and it is becoming the first killer of human beings, seriously endangering human health and survival. Its incidence rate has remained high, and it has shown a clear trend of younger people. The number of new cancer patients in mainland China alone reaches 2 million every year. Therefore, improving the diagnosis rate and cure rate of cancer is an important means to improve human health and quality of life. [0003] At present, the conventional means for tumor diagnosis are computed tomography (CT), magnetic resonance imaging (MRI), ultrasound (US) and so on. How...

Claims

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Application Information

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IPC IPC(8): C09K11/06A61K49/00A61K47/48A61K45/00A61K31/704A61K31/407A61P35/00
Inventor 陈海燕顾月清杨林张鑫崔思思
Owner CHINA PHARM UNIV
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