Shape-variable polypeptide-dye conjugate as well as preparation method and application thereof

A conjugate and dye technology, applied in the field of biomedicine, can solve the problems of low photothermal conversion efficiency and poor photothermal dye stability, and achieve the effects of improving delivery efficiency, enhancing residence time, and improving photothermal performance.

Active Publication Date: 2021-06-22
SOUTHWEST JIAOTONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the technical problems of low stability of photothermal dyes and low photothermal conversion efficiency in the prior art, the present invention provides a polypeptide-crotonate cyanine dye conjugate with variable morphology, its preparation method and application, The self-assembly of polypeptide-crotonate cyanine dye con

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  • Shape-variable polypeptide-dye conjugate as well as preparation method and application thereof
  • Shape-variable polypeptide-dye conjugate as well as preparation method and application thereof
  • Shape-variable polypeptide-dye conjugate as well as preparation method and application thereof

Examples

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Example Embodiment

[0038] Example 1

[0039] This embodiment provides a variable polypeptide-dye conjugate that is identified by CR-KLA, the polypeptide-dye conjugate comprising hydrophilic processed polypeptide sequence, hydrophobic glycinoctine dye derived Substrate molecules AHX for connecting two fragments, forming a two-projection-based photothermal dye conjugate, wherein the hydrophobicol-hydrophizone dye derivative comprises a glyphocyanine dye CR and a reaction thereof by an amide reaction thereof. The KLVffGFLG sequence, the KLVffGFLG sequence can cut the GFLG sequence from the phenylalanine F and the leucine L site to cut the GFLG sequence into two parts from the phenylalanine F and the leucine L site. The hydrophilic segment and hydrophobic segment of the sexual photothermal dye conjugate are separated to perform structural recombination, producing morphological changes.

[0040] Specifically, the polypeptide-dye conjugate CR-KLA is a linear structure, as shown in Formula 1:

[0041]

...

Example Embodiment

[0048] Example 2

[0049] This example provides a method of preparing a variable polypeptide-dye conjugate CR-KLA, a specific process, such as a specification figure 1 As shown, the specific preparation process is as follows:

[0050] S1, Synthesis of KLVffGFLG-AHX-KLCKLAKLCKLAK sequence based on FMOC solid phase synthesis method;

[0051] First, 300 mg RINK resin is first we use N, N-dimethylformamide DMF for 30 min, configure the deprotection (70% morphine, 30% DMF) and add it to the RINK resin FMOC protection. The group, exposed N-terminal amino group, which was subsequently cleaned with DMF and DCM. The desired amino acid and HATU were proved and added DMF was added to the resin, and the reaction was added, each amino acid reaction 2 times, 2 hours each time.

[0052] S2, weigh 1.5 equivalents of glyphocyanine dyes and 0- (7-nitroza-benzotriazole) -N, N, N ', N'-tetramethylurea hexafluorophosphate Hatu, After the DMF dissolution followed the method in the first step, it was ad...

Example Embodiment

[0057] Example 3

[0058] To verify the photothermography of CR-KLA in two different nano-assembled topography, the prepared Cr-KLA nanoparticles and nanofibers are nearly 808 nm near-infrared light at 1W / cm. 2 The power of the power is irradiated by 10min, and each temperature value is recorded. Figure 5 The temperature rise curve shown. The inventors have been creatively found that the Cr-KLA nanopartic formation group Δt is stable at 15.5 ° C, and the CR-KLA nanofibrosis group ΔT is stable at 23.5 ° C, while the PBS group did not show the heating ability. Since the nanofibers formed by the oxyl ketaric acid crystal hyperthermithic peptide material increased by 8 ° C at the same illumination time and the light intensity at the same illumination time and the light intensity, the optical change of the morphology is demonstrated. The thermal performance is significantly improved, and the possible reason is that the dye molecules are different in the arrangement of both nanopartic...

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Abstract

The invention discloses a shape-variable polypeptide-croconic acid cyanine dye conjugate as well as a preparation method and the application thereof. The polypeptide-dye conjugate comprises a hydrophilic functional peptide fragment, a hydrophobic croconic acid cyanine dye fragment and a spacer molecule Ahx for connecting the hydrophilic functional peptide fragment and the hydrophobic dye fragment, the hydrophobic dye segment comprises a morphology adaptation unit capable of realizing morphology transformation, and the polypeptide-dye conjugate can generate morphology transformation through specific recognition or action of a morphology transformation driving unit and the morphology adaptation unit; a polypeptide-croconic acid cyanine dye conjugate is self-assembled under a polar condition to form nanoparticles with a stable structure, the nanoparticles are transformed into nanofiber morphology under the specific action of a morphology transformation driving unit, and the photothermal conversion performance of the croconic acid cyanine dye can be effectively improved through morphology transformation; the synergistic treatment of photothermal and chemotherapy is realized, the tumor inhibition effect is further improved, and a good tumor treatment application prospect is achieved.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a polypeptide-dye conjugate with variable morphology, its preparation method and application. Background technique [0002] Utilizing the Enhanced Permeability and Retention Effect (EPR) to achieve targeted delivery of anti-tumor drug nanoparticles has become a common method for targeted tumor therapy. Through the EPR effect, the nanoparticles circulating in the body can be abnormally grown. The tumor blood vessel wall enters the tumor lesion site, thereby achieving the tumor killing effect. The abnormal growth of blood vessels in the tumor tissue leads to the increase of the vascular space. Usually, the tumor vascular space can increase to 380-780nm. Therefore, in order to effectively exert the EPR effect and realize the enrichment of nanoparticles in tumor sites, it is necessary to fine-tune the particle size of nanoparticles. When the particle size of the nanoparticle ...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/64A61K9/51A61P35/00
CPCA61K41/0052A61K47/645A61K9/5169A61P35/00
Inventor 周绍兵张凌田原
Owner SOUTHWEST JIAOTONG UNIV
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