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Preparation and application of human serum albumin-ruthenium inorganic drug complex

A human serum albumin, inorganic drug technology, applied in the field of antitumor drugs, can solve problems such as toxic and side effects, achieve the effects of reducing toxicity, high vascular permeability and retention rate, and improving targeting

Inactive Publication Date: 2016-04-13
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, we have to face a reality: anti-tumor inorganic drugs are still a double-edged sword. While treating diseases, they will inevitably produce many side effects, and they have very toxic side effects

Method used

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  • Preparation and application of human serum albumin-ruthenium inorganic drug complex
  • Preparation and application of human serum albumin-ruthenium inorganic drug complex
  • Preparation and application of human serum albumin-ruthenium inorganic drug complex

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of human serum albumin-Ru(ind) ruthenium inorganic drug complex

[0024] Ru(ind) was prepared according to the literature: at 60-70°C, 0.2g, 1.7mmol of indazole was dissolved in 1ml of 2N HCl, and 2ml of Ru(Ⅲ) solution was added to the hot solution, and a reddish-brown solid appeared immediately. Filtration, washing with ethanol and ether, and vacuum drying yielded 1.82 g of the product, with a yield of 50%. The prepared Ru(ind) drug was weighed and prepared into a 100mM solution with DMSO, and human serum albumin (HSA) was prepared into a 1.5mM solution with secondary deionized water. The DMSO solution of RIC and the aqueous solution of HSA were mixed at a ratio of 1:1, and the content of DMSO was not more than 5%, and incubated at 4°C for 24 hours. Concentrate the mixture of HSA and ruthenium inorganic anticancer drugs, wash it repeatedly with deionized water twice, so that the content of DMSO does not exceed 0.01%, and then concentrate to the ...

Embodiment 2

[0025] Example 2: Structural Determination of Human Serum Albumin-Ru(ind) Ruthenium Inorganic Drug Complex

[0026] Mix HSA (1.5mM, 100μL), saturated hexadecanoic acid (2.5mM, 960μL), and drug (100mM, 1.5μL), incubate for 24 hours, centrifuge to remove the precipitate, then concentrate, wash repeatedly with deionized water twice, and finally Concentrate to 100 μL and incubate albumin suitable for X-ray diffraction by gas phase diffusion method (26-30% PEG3350, 5% glycerol, 5% 2-methyl-1,3-propanediol) in a sitting drop plate - Fatty acid-metal drug complex crystals. Crystal data were collected using the Shanghai Synchrotron Radiation Facility. After processing the data with HKL2000, use the molrep program of ccp4 to use the protein with strong homology with the amino acid sequence of the protein in the protein database as a template, quickly rotate and translate the function to find a suitable template, and integrate it. If there is no protein with strong homology in the exi...

Embodiment 3

[0028] Example 3: Effect of ruthenium inorganic drug / human serum albumin-Ru(ind) ruthenium inorganic drug complex on tumor cell proliferation in vitro

[0029] Digest the confluent monolayer cells with trypsin, collect the cells into the serum-containing medium, add 200 μl of cell suspension to each well of the tenth row in the middle of a flat-bottomed 96-well plate, and add 0.5×10 3 -10×10 3 cells, place the culture plate in CO 2 In the incubator, incubate in a humid environment at 37°C. After the cells adhere to the wall, add the above-mentioned different concentrations of ruthenium inorganic drugs prepared above and albumin carrier ruthenium inorganic drugs for 48 hours, and then add MTT (3-(4, 5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide), after continuing to cultivate for 4 hours, discard the supernatant, add 100ml of DMSO, and measure the optical density at 570nm on a microplate reader. Repeat 3 times in a row. The half inhibitory rate value of the ruthenium...

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Abstract

The invention discloses a preparation and application of a human serum albumin-Ru(ind) ruthenium inorganic drug complex. After incubating Ru(ind) with human serum albumin, concentrating the mixture, and using it twice Washing with deionized water repeatedly until the DMSO content is less than 0.01%, concentrating to obtain the human serum albumin-Ru(ind) ruthenium inorganic drug complex, and then making the complex into injections, tablets, pills, capsules, suspensions or emulsion for the treatment of breast cancer, stomach cancer, lung cancer, colon cancer or liver cancer. The compound of the invention has high blood vessel permeability and retention rate, and the drug is selectively accumulated in tumor cells without any influence on normal cells, and the targeting property of the ruthenium inorganic drug is obviously improved, and the toxicity is greatly reduced.

Description

technical field [0001] The invention relates to anti-tumor drugs, in particular to the preparation of human serum albumin-Ru(ind) ruthenium inorganic drug complex and its application in anti-tumor diseases. Background technique [0002] In recent years, ruthenium complexes have been extensively studied as new anticancer drugs. Due to the unique physical and chemical properties of ruthenium complexes, it is generally believed internationally that ruthenium complexes are low-toxic, easy to absorb and excreted quickly in the body. At present, hundreds of ruthenium complexes have been synthesized. However, we have to face a reality: anti-tumor inorganic drugs are still a double-edged sword. While treating diseases, they will inevitably produce many side effects, and they are very toxic. Obviously, how to improve the intelligence of anti-tumor drugs is a problem that people really need to overcome. Compared with normal tissue, tumor tissue has rich blood vessels and special st...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/555A61P35/00
Inventor 杨峰梁宏李梅张耀
Owner GUANGXI NORMAL UNIV
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