A kind of hydrogen sulfide releasing agent ha-adt, its preparation method and application
A release agent, hydrogen sulfide technology, used in pharmaceutical formulations, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of short circulation time in the body, poor water solubility, and difficulty in becoming
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
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 ether (2×80 m...
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 Add normal saline to the positive control group, and add 200 µmol / L NaHS to the NaHS group in the positive control group (weigh 5.6 mg of NaHS and dissolve it in 5 mL of serum-free medium, then dilute 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 μmol / L GY...
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 / ...
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More