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Trinuclear platinum complex possessing Y type structure and its targeting for gastric adenocarcinoma cells

A technology for platinum complexes and gastric adenocarcinoma, applied in platinum group organic compounds, platinum-based organic compounds, medical preparations containing active ingredients, etc., to achieve excellent anti-human gastric adenocarcinoma cell activity and targeting effect

Inactive Publication Date: 2012-06-27
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the small molecule stabilizers of G-quadruplex DNA have made great progress, how to obtain ligands / complexes of small molecule G-quadruplex DNA with higher affinity and better selectivity is still a challenge. A great challenge for chemists and biologists

Method used

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  • Trinuclear platinum complex possessing Y type structure and its targeting for gastric adenocarcinoma cells
  • Trinuclear platinum complex possessing Y type structure and its targeting for gastric adenocarcinoma cells
  • Trinuclear platinum complex possessing Y type structure and its targeting for gastric adenocarcinoma cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the preparation of the trinuclear platinum complex with Y-type structure:

[0029] Synthetic (I) of Y-type structure trinuclear platinum complex: the cisplatin of 0.5 millimolar quantity is dissolved in 6 milliliters of water, under the protection of nitrogen, add the silver nitrate of 0.49 millimole quantity in dark place, 40 ℃ of stirring 24 hours, After the reaction is completed, centrifuge to discard the precipitate and keep it clear; add 0.15 mmol of bridging ligand to the above clear liquid, and the whole reaction is reacted under nitrogen protection at 90 degrees and protected from light for 3 days. An appropriate amount of absolute ethanol was added to precipitate a light yellow solid, which was centrifuged to obtain a light yellow solid, and the product was vacuum-dried. Yield: 83%. Elemental analysis (%), theoretical value: C 18 h 37 N 15 Cl 3 o 12.5 Pt 3 3.5H 2 O(1355.17): C, 15.95; H, 2.75; N, 15.50. Experimental values: C, 16.00; H, 2....

Embodiment 2

[0031] Embodiment 2: the experiment of antitumor activity:

[0032] Adopt the compound prepared in embodiment 1 to carry out following test:

[0033] Cell lines and culture conditions: The cell lines used in this experiment are as follows: human colorectal cancer cells (HCT-8), human gastric adenocarcinoma cells (BGC-823), human melanoma cancer cells (A375), human nasopharyngeal carcinoma cells (KB) and human rectal cancer cells (HT-29). The cells were cultured in DMEM medium containing 10% fetal bovine serum, which contained 100 units of penicillin and 100 micrograms of streptomycin per milliliter, and the cells were inoculated in a 10 cm diameter petri dish at 37 degrees, 5% CO 2 The cells were cultured in the environment, and passaged by trypsinization when the cells were confluent.

[0034] Cytotoxicity test: Cytotoxicity was measured by MTT method. The cells were digested with 0.25% trypsin into a single cell suspension, and the number of viable cells was calculated us...

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Abstract

The invention relates to a preparation method of an organic hybrid trinuclear platinum complex possessing a Y type structure synthesized by supermolecules self-assembly as well as treatment for gastric adenocarcinoma cells. The MTT experiment data shows that the compound can cross a drug resistance mechanism of cisplatin, and can specifically target to the gastric adenocarcinoma cells. A platinum ligand Pt(NH3)2Cl(NO3)] in which the chloride ion is replaced by nitrate and a bridge ligand (2,4,6-tri(pyridin-4-yl)-1,3,5-triazine) are subjected to self-assembly, thereby the novel and latent medicine for treating gastric adenocarcinoma with excellent anticancer activity and tumor targeting is obtained. Because the complex enables specific recognition of the gastric adenocarcinoma cells, and can induce the G-rich sequence of the oncogene to form a G-quadruplex structure, the activity of telomerase can be inhibited, thereby the complex possesses high gastric adenocarcinoma resistance activity. The preparation method has the advantages of simple process and low cost, can be completed in a general chemical laboratory, and the production process is environmentally-friendly. The trinuclear platinum complex possessing Y type structure can be taken as the novel and latent gastric adenocarcinoma resistance medicine.

Description

technical field [0001] The invention relates to a class of trinuclear platinum complexes that use supramolecular self-assembly to synthesize organic hybrids and have excellent anti-human gastric adenocarcinoma cell activity and targeting properties and a preparation method thereof, in particular to trinuclear platinum complexes with a Y-shaped structure The preparation method of the drug and its targeting to human gastric adenocarcinoma cells. Background technique [0002] Since G-quadruplex DNA was found to be a potential anti-tumor target, the design of new anti-cancer drugs targeting G-quadruplex DNA has become one of the important frontiers in the research of cancer targeted therapy drugs in recent years. Although the small molecule stabilizers of G-quadruplex DNA have made great progress, how to obtain ligands / complexes of small molecule G-quadruplex DNA with higher affinity and better selectivity is still a challenge. A great challenge for chemists and biologists. Be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCC07F15/00A61K31/555C07D401/14A61P35/00C07F15/0093
Inventor 毛宗万郑小辉钟毅芳黄华珍计亮年
Owner SUN YAT SEN UNIV
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