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H2S (hydrogen sulfide) releasing agent HA-ADT as well as preparation method and application thereof

A release agent, hydrogen sulfide technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems of short circulation time in the body, lack of targeting, and difficulty in becoming

Active Publication Date: 2019-04-26
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

in relation to H 2 In the early studies of S, the small molecular hydrogen sulfide release source was usually used as the H 2 S donors are used for biological research, but due to the disadvantages of poor water solubility, short circulation time in the body, and lack of targeting, it is difficult to become an ideal H donor. 2 S donor

Method used

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  • H2S (hydrogen sulfide) releasing agent HA-ADT as well as preparation method and application thereof
  • H2S (hydrogen sulfide) releasing agent HA-ADT as well as preparation method and application thereof
  • H2S (hydrogen sulfide) releasing agent HA-ADT as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The synthesis of HA-ADT, first synthesizes ADT through the reaction of anethole and sulfur in dimethylacetamide; then uses pyridine hydrochloride to perform ADT demethylation reaction to form ADT-OH; finally, under the appropriate amount of EDC·HCl and DMAP, HA and ADT-OH are reacted to synthesize HA-ADT.

[0038] The specific process is as follows:

[0039] Hyaluronic acid was purchased from Shandong Freda Company and used without further purification. All other reagents during the synthesis were purchased from Sigma Chemical Co. (St. Louis, MO) or Aladin Chemical Reagent Inc. of Shanghai. Distilled water was used in all experiments.

[0040] Synthesis of (p-methoxyphenyl)-3H-1,2-dithiolane-3-thione (compound 2, ADT)

[0041] Anethole (compound 1, 8 g, 54 mmol) and sulfur (96.93 g, 377.2 mmol) were reacted in dimethylacetamide (30 mL) at 145 °C for 6 h; the mixture was then cooled to room temperature and 100 mL of H 2 O, the product was extracted with diethyl ether...

Embodiment 2

[0062] h 2 S concentration detection

[0063] Human breast cancer cells MCF-7 and MDA-MB-231 were divided into negative control group, positive control group NaHS group, positive control group GYY4137 group, HA-ADT group, MCF-7 cells were treated with RPMI of 10% fetal bovine serum Cultured in 1640 medium, MDA-MB-231 was cultured in DMEM (H) medium with 10% fetal bovine serum. After the cells grew to the logarithmic growth phase, each group was replaced with the same volume of serum-free medium with different drugs: negative control Normal saline was added to the positive control group, and 200 µmol / L NaHS was added to the NaHS group of the positive control group (5.6 mg of NaHS was dissolved in 5 mL of serum-free medium, and then diluted 100 times with the medium to obtain 200 µmol / L NaHS), positive Add 200 μmol / L GYY4137 to the control group GYY4137 (weigh 3.76 mg of GYY4137 and dissolve it in 5 mL of serum-free medium, then dilute it 10 times with the medium to obtain 200 ...

Embodiment 3

[0067] In order to detect the effect of HA-ADT on the proliferation of human breast cancer cells, the inventors conducted further detection experiments, and the related process is introduced as follows.

[0068] (1) First, the MTT method was used to determine the effect of HA-ADT on the survival of tumor cells. The specific process was as follows:

[0069] Collect the cells in the logarithmic phase and make a single cell suspension with culture medium containing 10% fetal bovine serum. After counting with a counting plate, adjust the cell concentration to the required cell number at 5×10 per well. 3 cells / 100 µL were inoculated in 96-well plates and placed in 5% CO 2 Incubate in an incubator at 37°C. After the cells adhere to the wall, add 100 μL / well of drug-containing medium (the negative control group is added with normal saline, the positive control group is added with 200 μmol / L NaHS, and the positive control group is added with 200 μmol / L NaHS. µmol / L GYY4137, 200 µmol / ...

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Abstract

The invention provides a H2S (hydrogen sulfide) releasing agent HA-ADT as well as a preparation method and an application thereof. The H2S releasing agent HA-ADT has the structural formula as followsin the description, wherein p is 4-6 and q is 16-22. By enzyme-linked immunosorbent assay, the concentration change of H2S in cell supernatant within 48 h and the concentration of H2S in the cell andthe supernatant in 24 h after cell administration are detected. Detection by Western blotting, MTT, EDU and Tunel methods shows that 200 mu mol / L of HA-ADT can promote cell apoptosis and inhibit cellgrowth when acting on human breast cancer cells MCF-7 and MDA-MB-231; detection by scratch, transwell method and invasion method shows that the HA-ADT can inhibit cell migration; tumor-forming experiments in nude mice show that the HA-ADT can inhibit growth of human breast cancer cells.

Description

technical field [0001] The application belongs to the technical field of biopharmaceuticals, and in particular relates to a hydrogen sulfide releasing agent HA-ADT, its preparation method and application. Background technique [0002] Breast cancer (breast cancer) is one of the most common malignant tumors in women, accounting for 7-10% of all kinds of malignant tumors in the whole body. It is second only to uterine cancer in women and has become the main cause of threat to women's health. In recent years, the morbidity and mortality of breast cancer have been increasing. According to statistics, at least one out of nine women suffers from it. About 1.4 million patients are newly diagnosed with breast cancer every year in the world, and about 500,000 of them die from the disease in China. Therefore, scholars from various countries pay close attention to breast cancer. At present, chemotherapy is the main method in the comprehensive treatment of breast cancer. However, chem...

Claims

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Application Information

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IPC IPC(8): C08B37/08A61K31/728A61P35/00
CPCA61K31/728A61P35/00C08B37/0072
Inventor 段少峰吴东栋董茜韩举国杨波余海兰姬新颖胡玉荣张梦梦张欣刘玮张师慧
Owner HENAN UNIVERSITY
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