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Flavones-containing medicine, preparation method thereof, medicine composition and application

A technology of drugs and flavones, which is applied in the field of its preparation and flavone-containing drugs, can solve the problems of difficult to ensure the target group, influence, connection and non-toxic degradation.

Active Publication Date: 2020-05-01
BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cationic liposomes have high transfection activity in vivo and in vitro, however, because the positive charge on the surface affects their normal distribution in vivo, at the same time, cationic lipids can cause immunogenicity and inflammatory responses in animal experiments
The development of polycationic gene carriers has been relatively mature. However, it is difficult to ensure that the targeting group is on the surface of the structure in the structural design, and there is a self-design contradiction between toxicity and transfection activity. At the same time, its connection is difficult to achieve non-toxic degradation in vivo.
[0006] Therefore, how to improve the delivery reliability of the existing small molecule drug flavonoids is one of the difficulties in solving the current limited clinical application of flavonoid drugs

Method used

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  • Flavones-containing medicine, preparation method thereof, medicine composition and application
  • Flavones-containing medicine, preparation method thereof, medicine composition and application
  • Flavones-containing medicine, preparation method thereof, medicine composition and application

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preparation example Construction

[0153] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned flavone-containing drug, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; Loaded on nucleic acid nanoparticles to obtain flavonoid-containing drugs.

[0154] When physically linked, flavonoids usually form intercalations between GC base pairs by physical intercalation. In the case of covalent linkage, flavones usually react with the amino group outside the G ring to form a covalent linkage. The flavonoid-containing drug prepared by the above method can have better targeting after the target head is modified, can stably deliver the flavone, and has high reliability.

[0155] In a preferred embodiment, the step of mounting flavonoids through physical connection includes: mixing and stirring flavones, nucleic acid nanoparticles and the first solvent to obtain a premixed system; precipitating th...

Embodiment 1

[0179] 1. RNA and DNA nanoparticle carriers:

[0180] (1) The base sequences of the three polynucleotides that make up the RNA nanoparticles are shown in Table 1:

[0181] Table 1:

[0182]

[0183] (2) Three polynucleotide base sequences of DNA nanoparticles

[0184] The DNA uses the same sequence as the above RNA, except that T is substituted for U. Among them, the molecular weight of chain a is 8802.66, the molecular weight of chain b is 8280.33, and the molecular weight of chain c is 9605.2.

[0185] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0186] 2. Self-assembly experimental steps:

[0187] (1) RNA or DNA single strands a, b, and c are simultaneously mixed and dissolved in DEPC water or TMS buffer at a molar ratio of 1:1:1;

[0188] (2) Heat the mixed solution to 80°C / 95°C (the RNA assembly temperature is 80°C, and the DNA assembly temperature is 95°C)...

Embodiment 2

[0199] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0200] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:

[0201] Table 2: R-1

[0202]

[0203]

[0204] Table 3: R-2

[0205]

[0206] Table 4: R-3

[0207]

[0208] Table 5: R-4

[0209]

[0210]

[0211] Table 6: R-5

[0212]

[0213] Table 7: R-6

[0214]

[0215] Table 8: R-7

[0216]

[0217]

[0218] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0219] 2. Self-assembly experimental steps:

[0220] (1) RNA single strands a, b, and c are simultaneously mixed and dissolved in DEPC water or TMS buffer at a molar ratio of 1:1:1;

[0221] (2) Heat the mixed solution to 80°C, keep it for 5min and then cool down slowly to room temperature at a rate of 2°C / min;

[0222] (3) Load the pro...

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Abstract

The invention provides a flavones-containing medicine, a preparation method thereof, a medicine composition and application. The medicine comprises nucleic acid nanoparticles and flavones, wherein theflavones are hung on the nucleic acid nanoparticles; the nucleic acid nanoparticles comprise a nucleic acid structure domain; the nucleic acid structure domain comprises a sequence a, a sequence b and a sequence c; the sequence a comprises a sequence a1 or a sequence that at least one base group is inserted, deleted or replaced in the sequence a1; the sequence b comprises a sequence b1 or a sequence that at least one base group is inserted, deleted or replaced in the sequence b1; and the sequence comprises a sequence c1 or a sequence that at least one base group is inserted, deleted or replaced in the sequence c1. After target head modification on the nucleic acid structure domain, the flavones-containing medicine provided by the invention has good targeting performance, is capable of stably delivering the flavones and is high in reliability.

Description

technical field [0001] The application relates to the field of medicine, in particular, to a flavonoid-containing medicine, its preparation method, pharmaceutical composition and application. Background technique [0002] Flavones refer to a series of compounds in which two benzene rings (A- and B-rings) with phenolic hydroxyl groups are connected to each other through the central three carbon atoms, and the basic core is 2-phenylchromone. Functional groups such as phenolic hydroxyl group, methoxyl group, methyl group and isopentenyl group are often connected in the structure of flavonoids. In addition, it is often combined with sugars to form glycosides. The efficacy of flavonoids is multifaceted. It is a strong antioxidant that can effectively remove oxygen free radicals in the body. For example, anthocyanins can inhibit the full-stage overflow of oily peroxides. This ability to prevent oxidation is More than ten times that of vitamin E, this antioxidant effect can preve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K47/55A61K47/69A61K9/51A61K47/26A61K31/352A61P35/00A61P9/10A61P3/10A61P9/14A61P27/02
CPCA61K47/549A61K47/55A61K47/6929A61K9/5123A61K31/352A61P35/00A61P9/10A61P3/10A61P9/14A61P27/02
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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