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Anti-cancer drug as well as preparation method and specific application thereof

An anti-cancer drug and drug technology, applied in the direction of antibodies, anti-tumor drugs, drug combinations, etc., can solve the problems of immature preparation of chiral nanostructures and insufficient bioavailability, and achieve good pharmaceutical properties, safe and effective side effects, and avoidance of side effects. effect of pain

Active Publication Date: 2022-01-21
苏州迪拉纳生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention aims at the ineffective uptake of chiral molecules in cells in the prior art, which limits the application of chiral molecules in cells. There are corresponding problems in microinjection and cell penetrating peptides. The chiral molecules in PEGylated liposomes Low load, fine liposome manufacturing process and rapid discharge from the liver and spleen cannot meet the technical problems of cell uptake and targeting activity of chiral molecules. The invention provides an anticancer drug and its preparation method and specific application to solve Although chirality is ubiquitous in biomolecules in the prior art, chiral nanomedicines, especially oral chiral nanomedicines, are extremely rare, the preparation of chiral nanostructures is immature, and the technical problems of insufficient bioavailability

Method used

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  • Anti-cancer drug as well as preparation method and specific application thereof
  • Anti-cancer drug as well as preparation method and specific application thereof
  • Anti-cancer drug as well as preparation method and specific application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1: Engineered chiral polypeptide-derived exosomes and preparation method

[0076] This example uses a p53 activator - D-peptide, which can specifically degrade MDM2, the most important p53 negative regulatory protein in cancer cells. Such as figure 1 As shown in A, the chiral polypeptide of this example is named chiral MVP (MDM2 and VHL bridging peptide).

[0077] In this example, MVP is a targeted chimeric protein consisting of three functional parts: a dextro-dodecamer motif that binds to MDM2 with high affinity D MBP (MDM2 bind D-peptide), a flexible tripolyethylene glycol linker chain, and a motif VHL (Von Hippel Lindau factor) that binds to the E3 ubiquitin convener.

[0078] In this example, in order to couple Au 3+ With the D-peptide, an additional sulfhydryl chiral Cys residue and a hydrophilic chiral Arg residue were introduced at the C-terminus of the chiral MVP.

[0079] In this embodiment, compared with the natural MVP constructed, D The motif o...

Embodiment 2

[0083] Example 2: Preparation method of engineered chiral polypeptide-derived exosomes

[0084] The difference from Example 1 is that in this example, the D-peptide is replaced with a polypeptide molecule targeting inhibition of beta-catenin, a polypeptide molecule targeting activation of p53 ~ a polypeptide molecule targeting inhibition of PD-L1, etc. Polypeptide molecules of disease-causing proteins.

[0085] In this example, bovine milk exosomes were replaced with exosomes extracted from human bone marrow stem cells, mesenchymal stem cells, umbilical cord stem cells or edible plant extracts.

[0086] Example 2: Stability verification experiment of engineered chiral polypeptide-derived exosome drug

[0087] After the engineered chiral polypeptide-derived exosomes were constructed, their colloidal stability at neutral and acidic pH values ​​was tested through this example. Such as figure 2 As shown in A, the engineered chiral peptide-derived exosomes remained monodisperse...

Embodiment 3

[0088] Example 3: Oral administration of engineered chiral polypeptide-derived exosomes to verify the tumor accumulation effect

[0089] In this example, in order to verify tumor targeting, 5×10 5 tumor cells to establish a B16F10 melanoma homograft mouse model. After oral administration of engineered chiral polypeptide-derived exosomes or CPAICP at a dose of 2 mg / Kg, ICP-MS was used to analyze the 197 Au was quantified. Such as figure 2 As shown in E, the time-dependent accumulation ratio of engineered chiral polypeptide-derived exosomes in tumors versus normal organs or tissues shows a trend towards tumor accumulation. More importantly, the tumor accumulation of engineered chiral peptide-derived exosomes was nearly ten times that of CPAICP without ME ( figure 2 F). Furthermore, although engineered chiral peptide-derived exosomes, CPAICP and LPAICP@ME exhibit liver, spleen, kidney, and lung accumulation, engineered chiral peptide-derived exosomes increased tumor accumu...

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Abstract

The invention provides an anti-cancer drug as well as a preparation method and specific application thereof, a chiral polypeptide gold infinite covalent polymer is coated with cow milk exosome, and the anti-cancer drug is prepared through a method that chiral peptide oligomerization and a nanostructure grow along with fusion of an exosome membrane. According to the engineered chiral polypeptide exosome and the preparation method thereof, a feasible strategy is provided for constructing an oral chiral polypeptide derived nanostructure, and development of chiral nano-drugs for wider diseases including cancers is possibly promoted.

Description

technical field [0001] The invention belongs to the technical field of medicines, and specifically the invention relates to the technical field of chiral polypeptides. Background technique [0002] Chiral molecules are ubiquitous in our world, and they mainly exhibit left-handed and right-handed optical rotations, also known as enantiomers. However, in the biological world, life molecules including carbohydrates, nucleic acids, and proteins basically have only one chirality, resulting in enantioselectivity in biological reactions. Interestingly, the chiral structures of enantiomers directly affect their biological and pharmaceutical activities, resulting in different physiological effects. Moreover, natural polypeptides are composed of L-enantiomer amino acids, which only provide binding sites that can be specifically recognized by natural L-proteases. Therefore, the essential changes in the main chain-side chain connectivity and geometric configuration make the D-peptide ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/46A61K47/60A61K38/10A61K39/395A61K9/00A61P35/00A61P37/04
CPCA61K9/5176A61K9/0053A61K47/60A61K38/10A61K39/39558A61P35/00A61P37/04A61K2300/00
Inventor 闫瑾何旺骁刘文佳
Owner 苏州迪拉纳生物科技有限公司
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