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Human serum albumin-drug complex and its synthesis method and application

A technology of human serum albumin and drug complexes, which is applied in the field of medicine to achieve the effects of low toxicity, improved targeting, and improved therapeutic effects

Inactive Publication Date: 2018-04-10
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are no related reports on the complexes of 5-fluorouracil, G-rich oligonucleotide (AS1411) and copper complexes simultaneously transported using human serum albumin (HSA) as a carrier

Method used

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  • Human serum albumin-drug complex and its synthesis method and application
  • Human serum albumin-drug complex and its synthesis method and application
  • Human serum albumin-drug complex and its synthesis method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Synthesis of BpT complexes

[0044] a) Dissolve 10mmol of 2-benzoylpyridine in 20ml of ethanol (concentration of solvent ethanol is 50v / v%), stir at 60°C for 15min to obtain a solution, drop the above solution into 20ml and add 10mmol In the ethanol solution of thiosemicarbazide (the concentration of solvent ethanol is 50v / v%), reflux and stir at 60°C for 24h to obtain a light yellow precipitate, filter the above obtained light yellow precipitate and wash with absolute ethanol and ether three times respectively , after drying, the ligand 2-benzoylpyridine thiosemicarbazone was obtained;

[0045] b) will contain CuBr 2 (223.35mg, 1mmol) 20ml of methanol (concentration of solvent methanol is 60v / v%) solution, added dropwise to 20ml ethanol containing 1mmol 2-benzoylpyridine thiosemicarbazone ligand (concentration of solvent ethanol is 50v / v%) v%) solution, reflux and stir at 60°C for 2h, filter the reacted solution into a 50ml beaker, seal it with plastic wra...

Embodiment 2

[0051] Example 2: Synthesis of BpT complexes

[0052] a) Dissolve 10mmol of 2-benzoylpyridine in 10ml of methanol (concentration of solvent methanol is 80v / v%), stir at 50°C for 15min to obtain a solution, drop the above solution into 20ml and add 10mmol In the ethanol solution of thiosemicarbazide (the concentration of solvent ethanol is 20v / v%), reflux and stir at 80°C for 18h to obtain a light yellow precipitate, filter the light yellow precipitate obtained above, wash with water 3 times, and dry to obtain the compound Body 2-benzoylpyridinethiosemicarbazone;

[0053] b) will contain CuBr 2 (223.35mg, 1mmol) 20ml of ethanol (the concentration of solvent ethanol is 40v / v%) solution, add dropwise to 20ml ethanol containing 1mmol 2-benzoylpyridine thiosemicarbazone ligand (the concentration of solvent ethanol is 70v / v%) v%) solution, reflux and stir at 50°C for 2h, filter the reacted solution into a 50ml beaker, seal it with plastic wrap, prick 30 holes and volatilize at 8°C...

Embodiment 3

[0054] Example 3: Synthesis of BpT complexes

[0055] a) Dissolve 10mmol of 2-benzoylpyridine in 10ml of methanol (concentration of solvent methanol is 80v / v%), stir at 50°C for 15min to obtain a solution, drop the above solution into 20ml and add 10mmol In the methanol solution of thiosemicarbazide (the concentration of solvent methanol is 60v / v%), stir at 35°C for 48h to obtain a light yellow precipitate, filter the light yellow precipitate obtained above, wash it with methanol three times, and dry it. Obtain ligand 2-benzoylpyridine thiosemicarbazone;

[0056] b) will contain CuBr 2 (223.35mg, 1mmol) 20ml of ethanol (the concentration of solvent ethanol is 30v / v%) solution, add dropwise to 20ml ethanol containing 1mmol 2-benzoylpyridine thiosemicarbazone ligand (the concentration of solvent ethanol is 20v / v%) v%) solution, stirred at 40°C for 36h, filtered the reacted solution into a 50ml beaker, sealed it with plastic wrap, pricked 20 holes and volatilized at 2°C for sev...

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Abstract

The invention discloses a human serum albumin-drug complex as well as its synthesis method and application. The human serum albumin-drug complex is based on human serum albumin as a carrier, and 5-fluorouracil is jointly combined at two sites of tyrosine 161 and histidine 146 in the IB subdomain of human serum albumin. A copper (II) metal complex is bound to the histidine 242 position in the II A subdomain of serum albumin, and a G-rich oligonucleus is bound to the cysteine ​​34 position of human serum albumin through a cross-linking agent glycosides. The applicant conducted an in vivo anti-tumor activity study on the obtained complex, and the results showed that the albumin-based multi-drug delivery system has improved targeting and therapeutic effects compared with the three drugs alone, and has lower toxicity.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a complex of three kinds of medicines and human serum albumin, a synthesis method thereof, and an application thereof. Background technique [0002] Cancer is a complex disease involving multiple pathways, characterized by successive mutations in cells along a single line leading to disease progression. In addition, tumors also face the challenge of endogenous and acquired resistance to chemotherapeutic agents due to the increased survival rate of tumor cell gene mutations caused by chemotherapy. Clearly, inhibition by a single agent is not sufficient to achieve tumor regression. Therefore, multi-target combination therapy is becoming an increasingly important strategy for cancer treatment. Multiple drugs can be used to regulate different signaling pathways in disease cells to maximize the resistance and improve the therapeutic effect. [0003] In fact, there is a lot of evide...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/64A61K31/7088A61P35/00A61K31/513A61K31/555
Inventor 杨峰张振雷齐金旭苟峄张耀王俊
Owner GUANGXI NORMAL UNIV