Compound and application in anti-tumor medicine thereof

A composition and anti-tumor technology, which is applied in the direction of anti-tumor drugs, drug combinations, medical preparations of non-active ingredients, etc., can solve the problems of drug resistance and serious adverse reactions, so as to improve the anti-tumor effect and reduce the Nephrotoxicity, high safety effect

Active Publication Date: 2019-08-02
广东健尔圣医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of this, the present invention provides a composition and its application in antitumor drugs, which are used to solve the problem of serious adverse reactions and easy drug resistance in the prior art when platinum-containing antitumor drugs are used. technical flaws

Method used

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  • Compound and application in anti-tumor medicine thereof
  • Compound and application in anti-tumor medicine thereof
  • Compound and application in anti-tumor medicine thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] This example is a specific example of preparing an anti-tumor composition.

[0039] 1000 μmol of chelating agent was mixed with 50 μmol of cisplatin in a pharmaceutically acceptable solvent to obtain composition 1.

[0040] 1000 μmol of the chelating agent was mixed with 50 μmol of oxaliplatin in a pharmaceutically acceptable solvent to obtain composition 2.

[0041] 1000 μmol of the chelating agent was mixed with 50 μmol of carboplatin with a pharmaceutically acceptable solvent to obtain composition 3.

Embodiment 2

[0043] This example is a specific example of determining the complexation effect of the combination of the chelating agent and the platinum-containing anti-tumor compound.

[0044] In this embodiment, the assay method used is HPLC assay; wherein, the stationary phase is a C18 column (250mm×4.6mm, particle size 5 μm); the gradient mobile phase is: 0-8min, H 2 The volume ratio of O / acetonitrile is 77:23 (+0.1%H 3 PO 4 ), 8-13min, H 2 The volume ratio of O / acetonitrile is 68:32 (+0.1% H 3 PO 4 ), at 13-16min, H 2 The volume ratio of O / acetonitrile is 23:77 (+0.1%H 3 PO 4 ), 16-40min, H 2 The volume ratio of O / acetonitrile is 77:23 (+0.1%H 3 PO4 ); flow rate: 1.0 mL / min; 10 μL sample loading, DAD detector, UV350nm complex.

[0045] Identify and quantify chemical substances in analytical chemistry by ultraviolet-visible (UV / Vis) spectroscopy, use NanodropOne to scan the UV spectrum, cisplatin dissolved in water has a peak UV absorbance at 210nm, and chelating agent aqueous...

Embodiment 3

[0048] This example is a specific example of determining how a chelating agent slows down the toxic effect of a platinum-containing anti-tumor compound at the cellular level in vitro.

[0049] 3.1 Cell Culture

[0050] The cells used include: human kidney proximal tubular cell line HK2 (ATCCCRL2190), porcine proximal tubular cell line LLC-PK1 (ATCCCL101) and mouse breast cancer cell line 4T1 (ATCCCRL2539), all purchased from AmericanTypeCultureCollection.

[0051] LLC-PK1 cells were cultured in Dulbecco's modified Eagle medium (DMEM), HK2 cells were cultured in DMEM / F12 medium, and 4T1 cells were cultured in RPMI1640 medium. All cell culture media were supplemented with 10% FBS, 100 units / mL penicillin and 100 units / mL streptomycin. The cell lines were incubated at 37°C in a 5% CO2 atmosphere and subcultured twice a week.

[0052] 3.2 In vitro cell viability assay

[0053] HK2 and LLC-PK1 cells were trypsinized and seeded at a density of 10,000 cells / well in 100 μL medium i...

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Abstract

The invention belongs to the field of medicine research and development, and particularly relates to a compound and application in an anti-tumor medicine thereof. The compound is prepared from a platiniferous anti-tumor compound and a chelating agent, wherein the chelating agent is sodium(S)-2-(dithiocarboxylic acid((2S,3R,4R,5R)-2,3,4,5,6-pentacarbonyl hexyl)amino)-4-(methylmercapto)butyrate. Theinvention further provides application of the compound in the anti-tumor medicine. Through experiment examination, the chelating agent in the compound can effectively chelate heavy metal in the platiniferous anti-tumor compound, so that multiple adverse reaction during exclusive use of the platiniferous compound is effectively reduced, the dosage of the platiniferous anti-tumor compound can be improved, and an anti-tumor effect is optimized; meanwhile, the chelating agent is non-toxic, and has no toxic effects on normal cells; and the technical defects that in the prior art, when the platiniferous anti-tumor compound is used for medication, adverse reaction is large, and medicine resistance is liable to be generated are solved.

Description

technical field [0001] The invention belongs to the field of drug research and development, in particular to a composition and its application in antitumor drugs. Background technique [0002] Platinum-containing antineoplastic drugs are very effective and powerful chemotherapy agents. Among them, cisplatin, also known as the penicillin in cancer, is used to treat many different cancers. According to statistics, nearly 50% of cancer patients have been treated with platinum-based substances, and cisplatin combined therapy has become the cornerstone of many cancer treatments. [0003] However, platinum-containing antitumor drugs have certain adverse reactions, especially nephrotoxicity and ototoxicity, which limit their use; Drugs are often used in lower doses, which also leads to patients' resistance to platinum-containing antineoplastic drugs. Meanwhile, about one-third of patients developed acute kidney injury after receiving cisplatin. [0004] Therefore, a composition ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/243A61K31/555A61K47/20A61P35/00
CPCA61K33/24A61K31/555A61K47/20A61P35/00A61K33/243C07C333/20C07C333/04
Inventor 唐小江任雪峰葛怡琛钟志勇卢肖宇胡伟
Owner 广东健尔圣医药科技有限公司
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