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Trivalent arsenic complex and preparation method and application thereof

A complex, trivalent arsenic technology, applied in the fields of drug combination, organic chemistry, anti-tumor drugs, etc., can solve the problems of poor and toxic malignant tumor treatment effect, and achieve the effect of strong anti-tumor effect and controllable biological toxicity

Pending Publication Date: 2019-08-06
SHANGHAI NINTH PEOPLES HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to provide a trivalent arsenic complex and its preparation method and application, so as to overcome the defects in the prior art that arsenic trioxide is toxic and has poor therapeutic effect on malignant tumors

Method used

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  • Trivalent arsenic complex and preparation method and application thereof
  • Trivalent arsenic complex and preparation method and application thereof
  • Trivalent arsenic complex and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of pyrrolidine dithiocarbamate-arsenic complex aqueous preparation:

[0030] Take 1 g of commercially available ammonium pyrrolidine dithiocarbamate, add deionized water, and dissolve to a volume of 10 ml to obtain a 100 mg / L ammonium pyrrolidine dithiocarbamate solution, which is airtight and stored at 4°C for later use.

[0031] Take 10 mg of commercially available arsenic trioxide and sodium chloride solution to obtain a 1 mg / ml arsenic trioxide solution, seal it, and store it at 4°C for later use.

[0032] Take a 15ml volume sterilized centrifuge tube, first add 10ml of arsenic trioxide solution, then add the ammonium pyrrolidine dithiocarbamate solution according to the molar ratio of arsenic trioxide: ammonium pyrrolidine dithiocarbamate = 1:6, mix well, and prepare pyrrole Aqueous preparation of alkane dithiocarbamate-arsenic complex.

[0033] Ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (electrospray ioniz...

Embodiment 2

[0035] Anti-tumor activity assay cell experiment:

[0036] Human pancreatic cancer Mia-Paca2 cells were cultured in 1640+10% FBS medium, 5% CO 2 , Routine culture at 37°C. 96-well culture plate, 5000 cells were implanted in each well, pre-cultured for 12 hours, after the cells adhered to the wall, the culture medium containing 1 μM arsenic trioxide (ATO), 6 μM ammonium pyrrolidine dithiocarbamate (APDC), 1 μM arsenic trioxide + 6 μM pyrrole Ammonium alkanedithiocarbamate (APDC-ATO) water-soluble preparation (according to the concentration indicated by the equivalent of arsenic trioxide) in 1640+10% FBS culture medium for 48 hours after conventional culture, using CCK-8 reagent, microplate reader 450nm wavelength to detect the absorbance of each well Value (OD), using the following formula to calculate tumor cell growth inhibition rate and cell viability, to evaluate the inhibitory effect of drugs on tumor cells.

[0037] Tumor cell growth inhibition rate = (OD 空白 -OD 实验 ) / ...

Embodiment 3

[0041] Determination of anti-tumor activity in animal experiments:

[0042] The molar ratio of arsenic trioxide: ammonium pyrrolidine dithiocarbamate = 1:6 temporarily prepares a water-soluble preparation of pyrrolidine dithiocarbamate-arsenic complex (APDC-ATO), and the concentration of the compound preparation is indicated by the concentration of arsenic trioxide. 5-week-old BCLB / C thymic immunodeficient nude mice, male or female, were raised in SPF environment. Six nude mice were firstly taken, and 1×10 Mia-Paca2 human pancreatic cancer cells were subcutaneously injected into the right scapula. 7 / mouse, after 3 weeks, the tumor grew to ~500mm 3, the nude mice were routinely sacrificed, and the tumors were taken. Two vigorously growing tumors were selected, cut into 1mm×1mm×1mm square pieces, and implanted under the scapula skin of the other 6 nude mice. When the nude mouse tumor grows to ~150mm 3 After 2 weeks, they were randomly divided into control group (n=6) and tre...

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Abstract

The invention relates to a trivalent arsenic complex and a preparation method and application thereof. The structural formula of the complex is shown as (I). The preparation method comprises mixing apyrrolidine dithiocarbamate aqueous solution with an arsenic trioxide aqueous solution, and performing complexation reaction. The complex is in a water soluble state, has controllable biological toxicity and strong anti-tumor effect, and can be used for preparing anti-tumor drugs.

Description

technical field [0001] The invention belongs to the field of arsenic complex and its preparation method and application, in particular to a trivalent arsenic complex and its preparation method and application. Background technique [0002] Tumor drug therapy is one of the three basic methods for treating malignant tumors. Arsenic trioxide (chemical formula: As 2 o 3 ) is the main component of traditional Chinese medicine arsenic or arsenite. The treatment of acute myelocytic leukemia (APL) has received widespread attention both domestically and internationally, and has become a model for the study of traditional Chinese medicine for tumor treatment. In my country, arsenic trioxide is not only approved for the treatment of acute myeloid leukemia, but also for the treatment of advanced liver cancer. In addition, some researchers have also explored the use of arsenic trioxide in the treatment of other malignant tumors such as pancreatic cancer. However, the current laborator...

Claims

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Application Information

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IPC IPC(8): C07D295/21A61P35/00
CPCC07D295/21A61P35/00
Inventor 韩尽斌
Owner SHANGHAI NINTH PEOPLES HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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