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Cell-responsive ruthenium complex anticancer drug and preparation method thereof

A technology for ruthenium complexes and anticancer drugs is applied in the field of ruthenium complex anticancer drugs and their preparation, which can solve the problems of few types and preparation methods, and achieve the effects of strong antitumor activity and enhanced binding ability.

Active Publication Date: 2019-07-19
FUJIAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, although drugs based on ruthenium complexes have shown certain anti-tumor effects, there are relatively few specific types and preparation methods disclosed, and there is still a lot of room for improvement in the protection of active drugs and the release of tumor environments.

Method used

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  • Cell-responsive ruthenium complex anticancer drug and preparation method thereof
  • Cell-responsive ruthenium complex anticancer drug and preparation method thereof
  • Cell-responsive ruthenium complex anticancer drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The synthesis of the ruthenium complex anticancer drug of embodiment 1 intracellular response

[0051] The synthesis method of the ruthenium complex anticancer drug that responds in the cell comprises:

[0052] (1) Synthesis of PN

[0053] Weigh 20 g of 1,10-phenanthroline and add it to 30 mL of concentrated sulfuric acid, stir slowly, heat the oil bath to 165 ° C, slowly add 120 mL of concentrated sulfuric acid and concentrated nitric acid mixture (volume ratio 1:1), and produce Large amounts of brown gas. After the dropwise addition, reflux for 3 hours, and naturally cool to room temperature to obtain a brownish-yellow liquid. Place it in an ice-water bath, slowly add 10mol / L ice NaOH solution dropwise, keep stirring, and adjust the pH to about 5. There is a large amount of A yellow precipitate was produced, which was filtered by suction and dried to obtain PN (5-nitro-1,10-phenanthroline).

[0054] (2) Synthesis of PNH

[0055] in N 2 Under ambient conditions, d...

Embodiment 2

[0063] Kinetic experiment of embodiment 2 RuDPH and RuDPNI binding DNA in vitro

[0064] Experimental method: use different concentrations of DNA to titrate the UV-visible spectrum changes of RuDPNI and RuDPH, and calculate the binding constants of RuDPNI and RuDPH to DNA.

[0065] Experimental results: see image 3 , a of the figure shows that RuDPNI exhibits a color reduction effect (at 346 nm and 395 nm) and a red shift at 401 nm (about 6 nm) after adding increasing amounts of ct-DNA. RuDPH binds weakly to DNA (b), and no significant color reduction effect was observed in the figure. From the UV-Vis titration spectra, it was speculated that RuDPNI binds to DNA in an intercalation mode. From the absorbance at 346nm, the RuDPNI binding constant was calculated (see Figure 6 )K b The value is 1.204×10 6 m -1 , K of RuDPH b =8.497×10 4 m -1 . By modifying the 1,8-naphthalimide group, the DNA-binding affinity of RuDPNI was enhanced about 14.17-fold.

Embodiment 3

[0066] Example 3 In Vitro Cytotoxicity Test

[0067]Experimental method: The international general MTT method is used to analyze the toxicity of materials. The full name of MTT is 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide, ThiazolylBlueTetrazolium Bromide, Chinese is 3-(4,5-dimethylthiazolyl-2)- 2,5-Diphenyl tetrazolium bromide, trade name: thiazolium blue, is a yellow dye. MTT method is a method for detecting cell survival. The detection principle is that succinate dehydrogenase in the mitochondria of living cells can reduce exogenous MTT to water-insoluble blue-purple crystal formazan (Formazan) and deposit in the cells, while dead cells have no such function. Dimethyl sulfoxide (DMSO) can dissolve formazan in cells, and its light absorption value is measured at a wavelength of 540 or 720 nm with an enzyme-linked immunosorbent assay, which can indirectly reflect the number of living cells. Within a certain cell number range, the amount of MTT cryst...

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Abstract

The invention relates to the technical field of anticancer drugs, in particular to a ruthenium complex anticancer drug and a preparation method thereof. The ruthenium complex anticancer drug is activated through redox, inserted into tumor cell DNA, and coordinated with DNA to undergo a crosslinking reaction, so as to prevent DNA replication and DNA breakage. Due to the introduction of a planar structure ligand, namely, 1,8-naphthalic anhydride, the binding capacity of the drug to DNA is enhanced by 14.17 times, and the stability and anti-tumor activity of the anticancer drug are greatly improved.

Description

technical field [0001] The invention relates to the technical field of anticancer drugs, in particular to a ruthenium complex anticancer drug and a preparation method thereof. Background technique [0002] Chemotherapy drugs are the most effective way to treat tumors, especially for tumors of hematological origin such as acute promyelocytic leukemia, the cure effect is better. However, chemotherapy drugs have weak anti-tumor targeting and large side effects, and are not effective in treating solid tumors and metastases. In addition, some cancer cell lines are prone to drug resistance, making treatment more difficult. With the increasing incidence of tumors, it is particularly urgent to study chemotherapy drugs with targeted anti-tumor effects. [0003] Platinum anticancer drugs are currently widely used in clinical practice. Platinum anticancer drugs are used in more than half of the chemotherapy regimens. Sexual drug resistance is limited. Ruthenium complexes are the mo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00A61K31/555
CPCA61P35/00C07F15/0053
Inventor 肖方南吴允昆陈方满
Owner FUJIAN NORMAL UNIV
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