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1. CN110452374 - Three-dimensional spherical alpha-helix cationic polypeptide with high-efficiency gene delivery capability, and preparation method and application thereof

Office
China
Application Number 201910817961.4
Application Date 30.08.2019
Publication Number 110452374
Publication Date 15.11.2019
Publication Kind A
IPC
C08G 69/48
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
69Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
48Polymers modified by chemical after-treatment
C08G 69/16
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
69Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
02Polyamides derived from amino carboxylic acids or from polyamines and polycarboxylic acids
08derived from amino carboxylic acids
14Lactams
16Preparatory processes
A61K 47/42
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
42Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
A61K 48/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 47/42
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
42Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
A61K 48/0008
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
48Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
0008characterised by an aspect of the 'non-active' part of the composition delivered, e.g. wherein such 'non-active' part is not delivered simultaneously with the 'active' part of the composition
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C08G 69/16
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
69Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
02Polyamides derived from amino-carboxylic acids or from polyamines and polycarboxylic acids
08derived from amino-carboxylic acids
14Lactams
16Preparatory processes
C08G 69/48
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
69Macromolecular compounds obtained by reactions forming a carboxylic amide link in the main chain of the macromolecule
48Polymers modified by chemical after-treatment
Applicants SUZHOU UNIVERSITY
苏州大学
Inventors YIN LICHEN
殷黎晨
YE HUAN
叶桓
DANG JUANJUAN
党娟娟
HOU MENGYING
侯梦滢
ZHU RONGYING
朱蓉英
Agents 苏州创元专利商标事务所有限公司 32103
苏州创元专利商标事务所有限公司 32103
Title
(EN) Three-dimensional spherical alpha-helix cationic polypeptide with high-efficiency gene delivery capability, and preparation method and application thereof
(ZH) 具有高效基因递送能力的三维球形α螺旋阳离子聚多肽及其制备方法与应用
Abstract
(EN)
The invention provides a three-dimensional star-shaped alpha-helix polypeptide with high-efficiency gene delivery capability, and a preparation method and application thereof. Dendritic molecules areused as an initiator and dichloromethane is used as a reaction solvent to initiate high-speed ring-opening polymerization of different types of N-carboxylic anhydride monomers, and groups with different electric properties are introduced at the tail ends through a click chemical reaction. Rich amino groups on the surfaces of the dendrimers provide enough polymerization sites, so that the polypeptide forms a three-dimensional spherical topological structure, and meanwhile, the topological structure provides an opportunity for acceleration of the initial stage of a ring-opening polymerization reaction. The polypeptide side chain modified guanidino/amino groups and the like bring higher positive charge density, high-efficiency gene loading capacity can be obtained through electrostatic interaction between positive charges and negative charges, and an alpha spiral rigid structure on a secondary structure is enhanced, so that the polypeptide has higher membrane penetrating capacity. The polypeptide has a great development prospect in the field of biomedical materials, particularly gene delivery through properties of the polypeptide.

(ZH)
本发明提供了一种具有高效基因递送能力的三维星型α螺旋聚多肽及其制备方法与应用,以树枝状分子为引发剂,二氯甲烷为反应溶剂,引发不同类型的N‑羧酸酐单体的高速开环聚合,并通过点击化学反应在末端引入不同电性的基团。树枝状分子表面丰富的氨基提供了足够的聚合位点,使聚多肽形成了三维球形拓扑结构,同时拓扑结构为开环聚合反应初期的加速作用提供了契机。聚多肽侧链修饰的胍基/氨基等带来了较高的正电荷密度,可以通过正负电荷间的静电作用获得高效的基因负载能力,且增强了二级结构上的α螺旋刚性结构进而使聚多肽拥有更强的穿膜能力;该类聚多肽的这些性能使其在生物医用材料尤其是基因递送领域中具有巨大的开发前景。

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