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Application of chiral nano-selenium materials loaded with siRNA in the preparation of antitumor drugs

An anti-tumor drug, nano-selenium technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulas, etc., can solve undiscovered problems, achieve the effects of reducing efflux, convenient and quick storage and use, and increasing drug intake

Active Publication Date: 2017-11-21
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] So far, no reports have been found about chiral nano-selenium fluorescent composite materials loaded with siRNA for the preparation of anti-tumor drugs

Method used

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  • Application of chiral nano-selenium materials loaded with siRNA in the preparation of antitumor drugs
  • Application of chiral nano-selenium materials loaded with siRNA in the preparation of antitumor drugs
  • Application of chiral nano-selenium materials loaded with siRNA in the preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: [(phen) 2 Ru(bpibp)Ru(phen) 2 ] 4+ -L-arginine modified nano-selenium (Ru@L-SeNPs) and ((phen) 2 Ru(bpibp)Ru(phen) 2 ] 4+ -D-arginine modified nano-selenium (Ru@D-SeNPs) preparation

[0054] (1)((phen) 2 Ru(bpibp)Ru(phen) 2 ](ClO 4 ) 4 And [(bpy) 2 Ru(bpibp)Ru(bpy) 2 ](ClO 4 ) 4 Preparation method

[0055] ①cis-[Ru(phen) 2 Cl 2 ]·2H 2 Synthesis of O

[0056] Weigh RuCl 3 ·NH 2 O (0.78g, 3mmol), o-phenanthroline (1.2g, 6mmol) and lithium chloride (0.84g, 14mmol) were put in a three-necked flask, 5mL DMSO was added, and heated to reflux at 140°C under argon protection for 8 hours. After cooling to room temperature, add 25 mL of acetone, shake well and freeze overnight. Suction filtration, washing with ice water and cold acetone for 3 times, and drying in a vacuum dryer to obtain purple-black microcrystals. The crude product was recrystallized with ethanol and water (V / V=1:1), and the yield was 0.96 g (67%, calculated based on o-phenanthroline).

[0057] cis-[Ru(bpy) ...

Embodiment 2

[0068] Example 2: [(phen) 2 Ru(bpibp)Ru(phen) 2 ] 4+ -L-cysteine ​​modified nano-selenium and [(phen) 2 Ru(bpibp)Ru(phen) 2 ] 4+ -D-cysteine ​​modified nano-selenium preparation

[0069] (1) Ruthenium complex stock solution, Na 2 SeO 3 The preparation and concentration of the solution are the same as in Example 1;

[0070] (2) Dissolve L-cysteine ​​and D-cysteine ​​in purified water to prepare a 1 mol / L solution, and store it at 4°C for later use;

[0071] (3) Take 1mL Na respectively 2 SeO 3 The solution was mixed with 8mL ultrapure water to obtain solution A; 1mL of L-cysteine ​​solution was added dropwise to solution A under constant stirring, and the pH value was maintained at 9-11 during the process; the stirring was continued for 10-30 minutes to obtain wine red Nanosol; centrifuge, discard the supernatant, wash, and dry to obtain red L-cysteine ​​modified selenium nanoparticles. The obtained nano-selenium was resuspended to obtain 10 mL of 1 mM nano-selenium solution, and 2 m...

Embodiment 3

[0073] Example 3: [(bpy) 2 Ru(bpibp)Ru(bpy) 2 ] 4+ -L-Ascorbic acid modified nano-selenium and [(bpy) 2 Ru(bpibp)Ru(bpy) 2 ] 4+ -D-ascorbic acid modified nano-selenium preparation

[0074] (1) Ruthenium complex stock solution, Na 2 SeO 3 The preparation and concentration of the solution are the same as in Example 1;

[0075] (2) Dissolve L-ascorbic acid and D-ascorbic acid in purified water to prepare a 1mol / L solution, and store it at 4°C for later use;

[0076] (3) Take 1mL Na respectively 2 SeO 3 Mix the solution with 8 mL ultrapure water to obtain solution A; add 1 mL of L-ascorbic acid solution dropwise to solution A under constant stirring, maintaining the pH value of 3 to 5 during the process; continue stirring for 10 to 30 minutes to obtain wine red nano sol; Centrifuge, discard the supernatant, wash, and dry to obtain red nano-selenium particles. Resuspend the obtained nano-selenium to obtain 10 mL of 1 mM nano-selenium solution, and add 2 mL of [(bpy) under constant stirri...

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Abstract

The invention belongs to the technical field of tumor targeted imaging and discloses an application of chiral nano-selenium material supported siRNA in preparation of an antitumor drug. According to the invention, both a chiral nano-selenium composite material and the chiral nano-selenium composite material supported MDR-siRNA have tumor inhibiting activities. The functional nano-selenium prepared according to the invention is not only used as an active component for inhibiting tumors, but also used as a carrier for supporting the MDR-siRNA and has an efficient antitumor effect because of the MDR-siRNA capable of inhibiting the growth of multidrug-resistant tumor cells under a synergic effect. In addition, a modifier adopted according to the invention can be used for effectively controlling the shape and size of the nano-selenium and is beneficial to increasing of intake of the cells to the drug and reduction of excretion, so that the drug in the cells is kept at the relatively-high level. Meanwhile, the chiral nano-selenium material supported siRNA prepared according to the invention has a fluorescence characteristic, and can be used as a fluorescent nanomaterial to be applied to targeted imaging.

Description

Technical field [0001] The invention belongs to the technical field of tumor targeted imaging, and particularly relates to the application of chiral nano-selenium composite materials loaded with siRNA in the preparation of anti-tumor drugs and targeted imaging. Background technique [0002] Cancer has become the number one killer threatening human health and lives, and its danger should not be underestimated. In addition, in the past 20 years, cancer has shown a trend of younger age and higher morbidity and mortality. The development of high-efficiency, low-toxicity, broad-spectrum, and highly selective anti-cancer drugs has always been an important topic in the field of cancer treatment and the direction of the efforts of scientists. [0003] Tumors are new organisms formed by the abnormal proliferation of cells in local tissues under the action of various tumor-causing factors. They often appear as local masses. They grow vigorously and often show continuous growth. At present,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/04A61K33/24A61K48/00A61K49/00A61P35/00
Inventor 刘杰陈庆昌刘亚楠于倩倩郑文静
Owner JINAN UNIVERSITY
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