DNA tetrahedron-resveratrol compound as well as preparation method and application thereof

A technology of resveratrol and tetrahedron, which is applied in the field of medicine, can solve problems such as the undiscovered therapeutic effect of tFNAs, achieve good application prospects, improve insulin resistance, reduce body weight and blood sugar levels

Active Publication Date: 2021-05-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, tFNAs have not been found to have a therapeutic effect on insulin resistance

Method used

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  • DNA tetrahedron-resveratrol compound as well as preparation method and application thereof
  • DNA tetrahedron-resveratrol compound as well as preparation method and application thereof
  • DNA tetrahedron-resveratrol compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1, Preparation and Characterization of DNA Tetrahedral Framework Nucleic Acid

[0036] 1. Preparation of DNA tetrahedral framework nucleic acid

[0037] DNA tetrahedral framework nucleic acids (tFNAs) are synthesized by self-assembly of four uniquely designed DNA single strands (S1, S2, S3, S4) through a PCR program (maintain at 95°C for 10 min, rapidly cool down to 4°C for more than 20 min). The specific preparation method is as follows:

[0038] Four DNA single strands S1, S2, S3 and S4 (the specific sequences are shown in Table 1) were dissolved in TM buffer (10mM Tris-HCl, 50mM MgCl 2 , pH 8.0), so that the final concentrations of the four DNA single strands were 1000nM, mixed well, heated to 95°C and maintained for 10min, then rapidly cooled to 4°C and maintained for more than 20min, that is, the DNA tetrahedral framework was obtained by self-assembly synthesis Nucleic acids (tFNAs).

[0039] Table 1. Concrete sequences of four DNA single strands of the ...

Embodiment 2

[0044] Example 2, Preparation and Characterization of DNA Tetrahedron-Resveratrol Complex of the Present Invention

[0045] 1. Preparation of DNA tetrahedron-resveratrol complex of the present invention

[0046]Preparation of tFNAs-RSV: The tFNAs and resveratrol (RSV) solution synthesized in Example 1 were added to the TM buffer and mixed so that the concentration of tFNAs in the mixed solution was 250 nM, and the concentration of RSV in the mixed solution was 80 μM, stirred on a magnetic stirrer at 4°C for 6h, and ultrafiltered at 4°C under 6000g centrifugal force for 5min to obtain the DNA tetrahedron-resveratrol complex (tFNAs-RSV) of the present invention. The solvent of the resveratrol solution was DMSO with a concentration of 10 mM.

[0047] 2. Characterization of the DNA tetrahedron-resveratrol complex of the present invention

[0048] The successfully synthesized tFNAs-RSV was measured by UV spectrophotometer for absorption spectrum, and TEM for shape and size.

[0...

Embodiment 3

[0050] Example 3, the screening of the preparation process of the DNA tetrahedron-resveratrol complex of the present invention

[0051] The method described in Example 2 was used to prepare tFNAs-RSV, only the concentration of RSV in the mixed solution was changed (the concentrations of RSV in the mixed solution were 20 μM, 40 μM, 80 μM, 120 μM and 160 μM, respectively). The concentrations of tFNAs and RSV in each tFNAs-RSV were measured by NanoPhotometer N60, and the drug loading (LE) and encapsulation efficiency (EE) were calculated. Calculated as follows:

[0052] LE = (amount of total RSV substances – amount of remaining RSV substances) / (amount of total tFNAs substances)

[0053] EE (%) = (the amount of total RSV substances - the amount of remaining RSV substances) / (the amount of total RSV substances) × 100%

[0054] The result is as image 3 It shows that because the drug loading and encapsulation efficiency need to be high, comprehensive consideration, when the RSV ...

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Abstract

The invention provides a DNA tetrahedron-resveratrol compound as well as a preparation method and application thereof, and belongs to the technical field of medicines. The compound is a compound formed by mixing DNA tetrahedral framework nucleic acid and resveratrol. The DNA tetrahedron-resveratrol compound can effectively reduce body weight and blood sugar content and improve tolerance to glucose and insulin, so that obesity is effectively treated, and insulin resistance caused by obesity is improved and even treated; the compound can also be used for treating metabolic syndrome, type 2 diabetes mellitus, hypertension, hyperuricemia, dyslipidemia, cardiovascular and cerebrovascular diseases, polycystic ovarian syndrome, Alzheimer's disease or tumor and other diseases caused by insulin resistance. Meanwhile, the compound disclosed by the invention can be used for effectively treating adipose tissue inflammation. Compared with single use of DNA tetrahedral framework nucleic acid or resveratrol, the compound disclosed by the invention plays a synergistic effect and has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a DNA tetrahedron-resveratrol complex and a preparation method and application thereof. Background technique [0002] Metabolic syndrome is a common metabolic disease with glucose intolerance, hypertension and dyslipidemia as the main symptoms. Insulin resistance caused by obesity is a key cause of metabolic syndrome and an important risk factor for diseases such as type 2 diabetes and atherosclerosis. Chronic low-grade tissue inflammation is an important cause of insulin resistance in obesity. [0003] Resveratrol (resveratrol), a non-flavonoid polyphenol traditional Chinese medicine monomer, is an antitoxin produced by many plants when stimulated. In vitro experiments and animal experiments have shown that resveratrol has antioxidant, anti-inflammatory, anti-cancer and cardiovascular protection effects. However, resveratrol monomer has unstable properties, poor ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7088A61K31/05A61K47/26A61K47/54A61P3/04A61P3/10A61P5/50A61P9/12A61P19/06A61P9/00A61P15/08A61P25/28A61P35/00
CPCA61K31/7088A61K31/05A61K47/26A61K47/549A61P3/04A61P3/10A61P5/50A61P9/12A61P19/06A61P9/00A61P15/08A61P25/28A61P35/00
Inventor 林云锋李彦静蔡潇潇
Owner SICHUAN UNIV
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