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A kind of small interfering nucleic acid and pharmaceutical composition and application thereof

A composition and drug technology, applied in the field of biomedicine, can solve the problems of being easily degraded by nucleases, poor stability of siRNA, differences between target nucleic acid species, etc., and achieve the effect of preventing and/or treating dyslipidemia and inhibiting content

Active Publication Date: 2021-05-28
SUZHOU RIBO LIFE SCIENCE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are species differences in target nucleic acids, which increases the difficulty in the development of siRNA drugs targeting target nucleic acids. At the same time, the stability of siRNA is poor, and systemic drug delivery has the disadvantage of being easily degraded by nucleases.

Method used

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  • A kind of small interfering nucleic acid and pharmaceutical composition and application thereof
  • A kind of small interfering nucleic acid and pharmaceutical composition and application thereof
  • A kind of small interfering nucleic acid and pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0106] The sequence of siRNA is shown in Table 2, and the positive-sense strand nucleotide sequence numbered as siAP-1 is shown in SEQ ID NO.6, wherein the 1-19 nucleotide sequence is as shown in the human APOC3mRNA sequence (NM_000040.1) The target nucleic acid shown in SEQ ID NO.1 is identical; the antisense strand nucleotide sequence of the siRNA is shown in SEQ ID NO.7, wherein the 1-19 nucleotide sequence is the same as that of SEQ ID NO.1 in Table 1 The indicated target nucleic acids are complementary. The positive-sense strand nucleotide sequence numbered as siAP-2 is shown in SEQ ID NO.8, wherein the 1-19 nucleotide sequence is identical to the target nucleic acid shown in SEQ ID NO.2 in the APOC3 mRNA sequence; the siRNA The nucleotide sequence of the antisense strand is shown in SEQ ID NO.9, wherein the nucleotide sequence at positions 1-19 is complementary to the target nucleic acid shown in SEQ ID NO.2 in Table 1. The positive-sense strand nucleotide sequence numb...

Embodiment 1

[0114] This example is used to detect the inhibitory rate of the siRNA obtained in Preparation Example 1 on the expression level of APOC3 mRNA in vitro.

[0115] The human liver cancer cell line Huh7 was inoculated in 24-well plates with DMEM complete medium containing 10% fetal bovine serum at a seeding density of 4×10 5 Cells / well, 0.5mL culture medium per well, culture overnight at 37°C.

[0116] Aspirate the cell culture medium in the 24-well plate, and add 0.5 mL Opti-MEM serum-free medium to each well. Dilute 1.5 μL of the siRNA with a concentration of 20 μM in Preparation Example 1 with 50 μL of Opti-MEM serum-free medium; dilute 1 μL of Lipofectamine TM 2000 (Invitrogen Company) was diluted in 50 μL Opti-MEM serum-free medium, incubated at room temperature for 5 minutes after mixing; mixed diluted siRNA and diluted Lipofectamine TM 2000, mix gently, and let stand at room temperature for 20 minutes to allow complex formation. Add the above final mixed solution at 10...

preparation example 2

[0125] The siRNA obtained after the chemical modification of the sense and antisense strands of siRNA numbered siNC is shown in Table 5, and the number is siNC-M; the three groups of siRNAs obtained after the chemical modification of the sense and antisense strands of siRNAs numbered siAP-1 As shown in Table 5, they are respectively numbered siAP-1-M1, siAP-1-M2, and siAP-1-M3. The three groups of siRNA obtained after chemically modifying the siRNA sense strand and antisense strand numbered siAP-2 are shown in Table 5 and numbered siAP-2-M1, siAP-2-M2, and siAP-2-M3 respectively. The three groups of siRNA obtained after chemically modifying the siRNA sense strand and antisense strand numbered siAP-3 are shown in Table 5, and are numbered siAP-3-M1, siAP-3-M2, and siAP-3-M3 respectively. The three groups of siRNA obtained after chemical modification of the siRNA sense strand and antisense strand numbered siAP-4 are shown in Table 5 and numbered siAP-4-M1, siAP-4-M2, and siAP-4-...

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Abstract

The present disclosure relates to a small interfering nucleic acid and a pharmaceutical composition and uses thereof. The siRNA contains a complementary sense strand and an antisense strand, and the sense strand contains such as SEQ ID NO.24, SEQ ID NO.26, SEQ ID NO. 28 or the nucleotide sequence shown in SEQ ID NO.30, the antisense strand contains the nucleotide sequence shown in SEQ ID NO.25, SEQ ID NO.27, SEQ ID NO.29 or SEQ ID NO.31 and the phosphate backbone and / or nucleotide pentose in the phosphate-sugar backbone of the siRNA may or may not have a modification group. The present disclosure provides a brand-new high-efficiency siRNA and a pharmaceutical composition thereof, which can effectively prevent and / or treat dyslipidemia.

Description

technical field [0001] The present disclosure relates to the technical field of biomedicine, in particular to a small interfering nucleic acid (siRNA), a pharmaceutical composition and uses thereof. Background technique [0002] Dyslipidemia, also known as hyperlipidemia, is a systemic disease in which fat metabolism or operation is abnormal, making plasma lipids higher than normal. The clinical manifestations of hyperlipidemia mainly include two aspects: (1) xanthoma caused by lipid deposition in the dermis; (2) atherosclerosis caused by lipid deposition in the vascular endothelium, resulting in coronary heart disease and peripheral Vascular disease, etc. According to reports, approximately 35% of type 2 diabetes patients worldwide also suffer from dyslipidemia; in addition, 18 million people suffer from hypertriglyceridemia in hyperlipidemia. The prevalence of dyslipidemia among people aged 18 and over in my country is about 18.6%, and even nearly 10% of children have el...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12N15/113A61K48/00A61K31/713A61P3/06A61P9/10
CPCA61K31/713C12N15/113C12N2310/14C12N2310/315C12N2310/32C12N2320/30
Inventor 张鸿雁高山
Owner SUZHOU RIBO LIFE SCIENCE CO LTD
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