Platinum-containing compound and composition and application thereof

A platinum compound and composition technology, applied in the field of tumor treatment, can solve the problems of poor effect, easy generation of drug resistance, hidden dangers of adverse reactions, etc., and achieve the effects of expanding the drug spectrum, improving the poor therapeutic effect and improving the prognosis.

Active Publication Date: 2021-11-30
SUN YAT SEN UNIV CANCER CENT
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] In view of the above-mentioned problems and deficiencies, the present invention provides a platinum-containing compound and its composition and application, to solve the lo

Method used

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  • Platinum-containing compound and composition and application thereof
  • Platinum-containing compound and composition and application thereof
  • Platinum-containing compound and composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0044] Example 1 Cell in vitro killing experiment

[0045] (1) Take the H1975, H23, PC9, H1299, H460, and H228 cells of several long-term periods, inoculated in a 96-well plate in a 96-well plate in a certain density (3000-5000 / well);

[0046] (2) After 24 hours, the old medium was discarded, and the cells were treated with a medium containing different concentration drugs; wherein the drugs employed are the above formula II compound (TRI-Ligand). , Mixture of cisplatin (DDP), double thiollen (DSF), and DDP and DSF (the molar concentration ratio of 1: 1), the drug concentration gradient is 100 μm, 20 μm, 4 μm, 0.8 μm, 0.16 μm, 0.032 μm, respectively. 0.0064 μm, 0.00128 μm and 0 μm, and a blank group is not vaccinated;

[0047] (3) After 48 hours, 20 μl of 5 mg / ml MTT solution was added to each well, and the incubator was placed in a 37 ° C incubator for 4 hours, carefully discarded the medium, try not to suck the body of the hole, add DMSO瓒 瓒 解, placed in the shaker low speed ...

Example Embodiment

[0053] Example 2 combined with drug experiment

[0054] (1) Take a few long-term A549, H2228 cells inoculated in a 96-well plate according to a certain density (3000-5000 / well);

[0055] (2) After 24 hours, the old medium was discarded, and the cells were treated with a medium containing different concentration drugs, respectively; the drugs used were Tri-Ligand, Cisplatin (DDP), and Tri-Ligand. The mixture of DDP (two molar concentration ratios is 1: 1), the drug concentration gradient is 100 μm, 20 μm, 4 μm, 0.8 μm, 0.16 μm, 0.032 μm, 0.0064 μm, 0.00128 μm, and 0 μm, and the blank group is not inoculated. cell;

[0056] (3) After 48 hours, 20 μl of 5 mg / ml MTT solution was added to each well, and the incubator was placed in a 37 ° C incubator for 4 hours, carefully discarded the medium, try not to suck the body of the hole, add DMSO瓒 瓒 解, placed in the shaker low speed oscillated for 10 minutes, and the OD value of the 490 nm wavelength was detected by the enzyme label.

[0...

Example Embodiment

[0059] Example 3 Effect of platinum compound on different NSCLC cloning formation capacity

[0060] (1) It is paved in about 500 to 2000 cells (H460 and HCC827) per well in the six-hole plate, and different densities are selected according to the purpose of the experimental purpose;

[0061] (2) After 24 hours, it is appropriately treated (after 12 hours after 12 hours), it is continued for 10 to 14 days, and it is stopped when the single cell clone grows to greater than 50 cells. nourish;

[0062] (3) Removal of the medium supernatant, use 1 x PBS solution, washed once, stained with 0.5% crystalline hydrol methanol solution, observe the number of clones formed by each group, take photos and statistics and calculate the clonal formation rate: Cloning formation Rate = (Total number of plate clones / total number of layers) × 100%.

[0063] The result is as follows figure 2 Indicated. The results showed that the platinum-containing compounds of the present invention produced signifi...

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Abstract

The invention provides a pharmaceutical composition for treating cancer, especially lung cancer. The pharmaceutical composition comprises a platinum-containing compound. Through a large number of long-term researches, it is found that the platinum-containing compound, especially Tri-ligand, can generate a remarkable growth inhibition effect on lung cancer cells in vivo and in vitro; and the effect of the compound is obviously superior to that of a drug (cisplatin) suggested by a first-line treatment scheme for clinically treating lung cancer, even a DDP+DSF combined medication scheme which is newly researched and used for improving the drug resistance of the cisplatin, and besides, the in-vivo safety shown by Tri-ligand is also superior to that of the DDP+DSF combined medication scheme. Therefore, a new treatment strategy is provided for the lung cancer, especially non-small cell lung cancer, the medication spectrum of the lung cancer can be effectively expanded, and the current situations that the first-line treatment medicine cisplatin for the lung cancer is poor in effects, prone to drug resistance and the like are improved. The invention plays an important role in improving the prognosis of lung cancer, and has very important clinical significance and social significance.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment, and specifically relates to a platinum-containing compound and its composition and application. Background technique [0002] Lung cancer is a common malignant tumor of the respiratory system, and it is one of the most common tumors with the highest discovery rate in the world. In the past 50 years, many countries have reported that the incidence and mortality of lung cancer have increased significantly. The incidence and mortality of lung cancer in men account for the first of all malignant tumors, and the incidence and mortality of lung cancer occupy the second place in women. The etiology of lung cancer is still not completely clear. [0003] Clinically, there are mainly chemotherapy, radiotherapy, and surgery for lung cancer. Chemotherapy is the most common treatment for lung cancer. More than 90% of lung cancers require chemotherapy. The curative effect of chemotherapy on small c...

Claims

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Application Information

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IPC IPC(8): A61K31/282A61K45/06A61P35/00
CPCA61K31/282A61K45/06A61P35/00A61K2300/00
Inventor 刘然义袁雪霞岳欣段有发
Owner SUN YAT SEN UNIV CANCER CENT
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