Application of Pt (1-oxidopyridin-2-thione) 2

A drug, tumor technology, applied in the new application field of Pt2 in medicine

Active Publication Date: 2015-08-19
GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Thus, cancer cells resistant to cisplatin are also resistan

Method used

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  • Application of Pt (1-oxidopyridin-2-thione) 2
  • Application of Pt (1-oxidopyridin-2-thione) 2
  • Application of Pt (1-oxidopyridin-2-thione) 2

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: The case of PtPT interacting with DNA molecules

[0054] Fixed concentration of PtPT (8.96*10 -6 M, dissolved in DMSO), gradually increasing the solubility of DNA [0(a), 1.42(b), 2.85(c), 4.27(d)*10 -5 M, dissolved in Tris-HCl buffer, 0.05M, pH=7.40], taking Tris-HCl buffer solution containing the same concentration of DMSO as reference, scan the absorption spectra of different mixed systems in the range of 200-600nm. The results showed that after mixing with DNA, the absorption intensity and peak position at the characteristic peak (323 nm) of PtPT were basically unaffected. It was speculated that there was no interaction between PtPT and DNA. See the results figure 1 (a).

[0055] Concentration of immobilized EB-DNA system [c(EB)=2 μM, c(DNA)=1.4*10 -5 M, dissolved in Tris-HCl buffer, 0.05M, pH=7.40], to which was added different concentrations of PtPT [1.2(A), 3.1(B), 6.4(C)*10 -5 M], the excitation wavelength was 514 nm, and its fluorescence spectrum...

Embodiment 2

[0056] Example 2: The effect of PtPT on DNA damage effector molecules in tumor cells

[0057] K562 and A549 cells were treated with different concentrations of PtPT (2.5, 5, 10uM) and CDDP (2.5, 5, 10uM) for 6h, respectively, and the cells were collected to extract total protein. Expression of p-ATM, p-chk2, p-chk1 and PARP. The results showed that PtPT did not produce DNA damage effects with increasing concentration in tumor cells. See the results figure 2 (a).

[0058] Western Blot method: 1. Configure the gel required for SDS-PAGE. First, configure the lower layer of separating glue according to the formula. After the configuration is completed, slowly add it to the equipped two-layer glass splint, and add an appropriate amount of double-distilled water to seal the pressure line; after the lower layer of separation glue is solidified, pour out the upper layer of water in the previous step, and add the configuration Insert the comb after the good stacking gel and wait f...

Embodiment 3

[0061] Example 3: The effect of PtPT on DNA damage effector molecules in non-transformed normal cells

[0062] After treating 16HBE and LO2 cells with PtPT (2.5uM) and CDDP (2.5uM) for 6h, 12h, and 18h, respectively, the cells were collected to extract total protein, and the DNA damage-related protein γ-H2AX was detected by Western Blot method (see Example 2). , p-ATM, p-chk2, p-chk1 and PARP expression. The results showed that PtPT did not produce DNA damage effects over time in non-transformed normal cells. See the results image 3 .

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Abstract

The present invention discloses application of Pt (1-oxidopyridin-2-thione) 2 in the manufacture of anti-tumor medicament, and application of Pt (1-oxidopyridine-2-thione)2 as a de-ubiquitination enzyme inhibitor in the manufacture of medicaments for control of inflammation, tissue ischemia-reperfusion injury and myocardial hypertrophy. The invention provides the medicaments with Pt (1-oxidopyridine-2-thione) 2 as an active ingredient for the control of inflammation, tissue ischemia-reperfusion injury and myocardial hypertrophy and provides more clinic choices.

Description

technical field [0001] The present invention relates to the technical field of medicinal chemistry, in particular to Pt (1-oxidopyridine-2-thione) which is a deubiquitinase inhibitor 2 New applications in medicine. Background technique [0002] Due to the great success of cisplatin in the treatment of ovarian cancer, head and neck cancer, testicular cancer and other cancers, the research and application of platinum-based anticancer drugs have developed rapidly. This platinum-based chemotherapeutic drug binds covalently to DNA mainly through guanine and adenine N7 sites, forming cisplatin-DNA complexes in intra- and inter-strand modes, interfering with DNA replication and transcription, causing cell death, and therefore damage DNA is a key molecular event in cisplatin-induced cell death. [0003] Although cisplatin is clinically effective, its severe renal toxicity and other toxic side effects and drug resistance limit its wide application. To overcome the shortcomings of ...

Claims

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Application Information

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IPC IPC(8): A61K31/555A61P35/00A61P35/02A61P29/00A61P9/00A61P9/10
Inventor 刘金保赵冲陈鑫师宪平杨昌山蓝晓莹廖四燕
Owner GUANGZHOU MEDICAL UNIV
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