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Cis-platinum ligand and application thereof in preparation of nano-agent for tumor diagnosis and treatment

A ligand and cisplatin technology, applied in the field of medicine, can solve the problems of cells prone to drug resistance, high toxicity and side effects, and poor targeting of drug therapy

Active Publication Date: 2021-04-27
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, tumor is one of the diseases that pose the greatest threat to human health. Traditional drug therapy is the first choice for tumor treatment, but drug therapy has poor targeting, high toxicity and side effects; poor solubility and stability of drugs; cells are prone to drug resistance ; and the shortcomings of drug delivery and treatment in the body are difficult to detect. Due to its dynamic reversible characteristics, supramolecular chemistry can well solve the above problems
[0003] As a typical supramolecular carrier, Pt(II) coordination assembly has also made some progress in supramolecular tumor therapy. Toxic and side effects (stability of internal circulation), and a supramolecular intelligent tumor treatment system that integrates chemotherapy and photothermal / photodynamic therapy and other synergistic treatments has not been systematically carried out, which seriously restricts the development of supramolecular chemistry and tumor treatment research

Method used

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  • Cis-platinum ligand and application thereof in preparation of nano-agent for tumor diagnosis and treatment
  • Cis-platinum ligand and application thereof in preparation of nano-agent for tumor diagnosis and treatment
  • Cis-platinum ligand and application thereof in preparation of nano-agent for tumor diagnosis and treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Preparation of tetraphenylethylene porphyrin cisplatin ligand

[0020] Weigh 63.78mg monopyridine tetraphenylethylene, 61.5mg monopyridine porphyrin, 145.8mg 90°Pt, 93.49mg glycol chain isophthalic acid, add to a 10mL round bottom flask, add 4mL acetone and 1mL water, heat to React overnight at 60°C, monitor by TLC until the reactant disappears, remove insoluble substances by filtration, dry the solvent with nitrogen, redissolve in 0.5mL acetone, add 8mL anhydrous ether for recrystallization three times, and obtain tetraphenylethylene porphyrin cisplatin complex body. Yield: 83%.

[0021] H NMR spectra of cisplatin ligands as figure 1 shown.

[0022] 1 H NMR (400MHz, Acetone-d 6 )δ:9.50(s,1H),8.78(d,J=4.00Hz,2H),8.71(d,J=4.00Hz,2H),8.38(s,1H),8.10(s,2H),7.70( d,J=4.00Hz,2H),7.60-7.53(m,18H),7.46-7.41(m,20H),7.38-7.31(m,10H),7.04(s,2H),6.65(s,2H) ,6.44(s,2H),6.11(s,2H),6.00(d,J=4.00Hz,2H),5.11(s,2H),4.17(t,J=4.00Hz,6H),3.81(t, J=4.00Hz, 6H), 3.60(t, J=4.00Hz, 30H...

Embodiment 2

[0026] Preparation of cisplatin ligand nano-diagnostic agent

[0027] Add 180mg of cisplatin ligand and 0.1mL DMF to a 10mL round-bottomed flask, add 10mL of water dropwise within 1 hour under vigorous stirring, stir for 1 hour, centrifuge and dialyze to remove DMF to obtain cisplatin ligand nano-therapeutic agent . The prepared nano-diagnostic agent was characterized by scanning electron microscope after vacuum drying.

[0028] The result is as figure 2 As shown, it can be seen from the figure that the finally prepared nano-medicine is spherical, with a diameter of about 250nm.

Embodiment 3

[0030] Anti-tumor effect test of nano-therapeutic agent

[0031] 1. Mitochondria targeted cell imaging. Human cervical cancer cells (HeLa cells) were seeded in 6-well plates (5×10 4 mL –1 , 2mL per well), at 37°C, 5% CO 2 Incubate for 24 hours in the incubator. Cells were incubated in the corresponding solutions for 4 hours. The medium was then removed, and the cells were washed 3 times with phosphate buffered saline. Finally, cells were visualized by confocal laser scanning microscopy.

[0032] The result is as image 3 As shown, the nano-therapeutic agents all enter into the mitochondria in the cells. Since the nano-therapeutic agent contains tetraphenylethylene units, it will produce strong fluorescence emission in the aggregated state, and triethylphosphine has the effect of targeting mitochondria, so when the nano-therapeutic agent enters the cell, it will "point" the mitochondria in the cell. Bright", thus playing the role of cell imaging.

[0033] 2. Cytotoxici...

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Abstract

The invention discloses a cis-platinum ligand and application thereof in preparation of a nano-agent for tumor diagnosis and treatment, and belongs to the technical field of medicines. Fluorescent elements and elements generating singlet oxygen are connected to a molecule through metal coordination, the exterior of an assembly is protected by a glycol chain, so that the assembly stably exists in an in-vivo circulation process, meanwhile, dense packing between porphyrins is inhibited by the metal coordination, and the capacity of generating the singlet oxygen through illumination is greatly improved, thus the anti-tumor efficiency is improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a cisplatin ligand and its application in the preparation of nano-diagnosis and treatment agents for tumors. Background technique [0002] At present, tumor is one of the diseases that pose the greatest threat to human health. Traditional drug therapy is the first choice for tumor treatment, but drug therapy has poor targeting, high toxicity and side effects; poor solubility and stability of drugs; cells are prone to drug resistance ; and the shortcomings of drug delivery and treatment in vivo are difficult to detect. Due to its dynamic reversible characteristics, supramolecular chemistry can well solve the above problems. [0003] As a typical supramolecular carrier, Pt(II) coordination assembly has also made some progress in supramolecular tumor therapy. Toxicity and side effects (stability of internal circulation), and a supramolecular intelligent tumor treatment...

Claims

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Application Information

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IPC IPC(8): A61K33/243A61K47/69A61K41/00A61K47/54A61K47/55A61K49/00C07F15/00A61P35/00B82Y5/00B82Y20/00B82Y30/00B82Y40/00
CPCA61K41/0052A61K41/0071A61K49/0021A61K49/0052A61K49/0082A61K47/54A61K47/55A61K47/6907A61P35/00A61K33/243B82Y5/00B82Y20/00B82Y30/00B82Y40/00C07F15/0093A61K2300/00
Inventor 张越时令姚勇汪洋
Owner NANTONG UNIVERSITY
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