A kind of doxorubicin and annexin V conjugate, its preparation method and application

An annexin and doxorubicin technology, which is applied to the conjugate of doxorubicin and annexin V and the field of preparation thereof, can solve the problems of large side effects of the drug, poor tumor targeting of doxorubicin, and achieve enhanced anti-tumor effects. Tumor activity, inhibition of tumor angiogenesis and tumor growth

Active Publication Date: 2011-12-28
NANJING UNIV
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Problems solved by technology

Due to the poor targeting of doxorubicin to tumors, the side effects of the drug are large

Method used

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  • A kind of doxorubicin and annexin V conjugate, its preparation method and application
  • A kind of doxorubicin and annexin V conjugate, its preparation method and application

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Experimental program
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Embodiment

[0023] 1. Activate the carboxyl group on the surface of Annexin V: Dissolve 2 mg of Annexin V freeze-dried powder in 2 ml of 0.05 mM 2-(N-morpholino)ethanesulfonic acid (MES), 0.5 M NaCl, pH=6.0 solution, adjust the concentration to 1 mg / ml, add 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC) to make the final concentration 6 mM. Add N-hydroxysulfosuccinimide (Sulfo-NHS) to a final concentration of 5 mM, mix well and react at room temperature for 15 minutes, then add 2.8 μl 2-mercaptoethanol to a concentration of 20 mM, and react for 10 minutes , to neutralize unreacted EDC.

[0024] 2. Coupling of activated Annexin V with doxorubicin: Use an ultrafiltration tube with a molecular weight cut-off of 10KD to centrifuge and concentrate the intermediate product solution to minimize the volume of the solution to reduce the impact on the pH value of the coupling reaction buffer. Add 3 mg of doxorubicin hydrochloride to 0.1M sodium phosphate solution (pH=7.5) to for...

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Abstract

The invention belongs to the field of biological technology, and specifically relates to the coupling, preparation method and application of annexin V with the ability to bind to phosphatidylserine and its variant molecules and the anticancer drug doxorubicin. (3-Dimethylaminopropyl) carbodiimide hydrochloride and N-hydroxysulfosuccinimide are used as a crosslinking agent to couple with doxorubicin, and a method for preparing a soluble conjugate. The prepared conjugates have better anti-tumor activity, which lays the foundation for further research on targeted anti-tumor drugs and their applications.

Description

technical field [0001] The invention belongs to the field of biological technology, and in particular relates to a conjugate of doxorubicin and annexin V, a preparation method and application thereof. Background technique [0002] Doxorubicin is an anthracycline antibiotic used to treat acute leukemia, malignant lymphoma, breast cancer, osteosarcoma, soft tissue sarcoma, lung cancer and other cancers, and has a broad anticancer spectrum. Zhou Mi et al. (Zhou, M. et al., 2008, Fudan Journal * Medical Edition, 35:793-798) found that doxorubicin induces apoptosis of liver cancer cells through the endogenous caspase-3 pathway. Doxorubicin also acts on normal cells, causing serious side effects, mainly manifested as myocardial toxicity, bone marrow suppression and neurotoxicity. Doxorubicin has a significantly higher affinity to myocardial tissue than other tissues, causing myocardial toxicity. Because doxorubicin has poor tumor targeting, the side effects of the drug are large...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61K31/704A61P35/00
Inventor 华子春谢德
Owner NANJING UNIV
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