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Application of pyridine carboxamide derivative AMSP-30m in preparation of medicine for preventing and treating rheumatoid arthritis

A technology of picolinamide and amsp-30m, which can be applied in drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., and can solve the problems that the pharmacological effects of rheumatoid arthritis have not yet been reported.

Inactive Publication Date: 2021-03-02
ANHUI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The abnormal proliferation and high invasiveness of RAFLS are similar to tumor cells. It is reasonable to speculate that AMSP-30m may exert its potential anti-rheumatic effect by inhibiting the expression of HIF-1α protein in RA hypoxic synovial tissue, but AMSP-30m prevents rheumatoid The pharmacological effect of arthritis has not been reported yet, the present invention derives from it

Method used

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  • Application of pyridine carboxamide derivative AMSP-30m in preparation of medicine for preventing and treating rheumatoid arthritis
  • Application of pyridine carboxamide derivative AMSP-30m in preparation of medicine for preventing and treating rheumatoid arthritis
  • Application of pyridine carboxamide derivative AMSP-30m in preparation of medicine for preventing and treating rheumatoid arthritis

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Embodiment 1

[0032] Pharmacodynamic study of picolinamide derivative AMSP-30m in the treatment of adjuvant arthritis in rats

[0033] 1. Experimental method

[0034] 1.1 Establishment and experimental grouping of adjuvant-induced arthritis (AIA) rats:

[0035] After BCG was inactivated at 80°C for 1 hour, it was fully ground and mixed with high-pressure sterilized liquid paraffin to make a 10g / L emulsion (that is, Freund's complete adjuvant), and SD rats were intradermally injected with Freund's complete adjuvant on the left hind foot The AIA rat model was prepared by injecting 0.1 mL of it into inflammation. Rats in the normal control group were intradermally injected with an equal volume of normal saline on the left hind paw. On the 12th day of modeling (d12), the rats without secondary side joint swelling symptoms were discarded, and the rats showing AIA symptoms were randomly divided into model group, AMSP-30m (30, 60mg / kg) group and positive drug methylamine group. Pterin (MTX, 0.5...

Embodiment 2

[0066] Effects of picolinamide derivative AMSP-30m on the biological characteristics of human fibroblast-like synoviocytes cultured in hypoxia MH7A in vitro

[0067] 1. Experimental method

[0068] 1.1 MTT method to detect cell proliferation:

[0069] Cells were grouped as follows: Hypoxia (1% O 2 ) group, hypoxia+DMSO solvent control group, hypoxia+AMSP-30m (10μM) group. Inoculate the suspension of human fibroblast-like synoviocytes (MH7A) in a 96-well culture plate (100 μL / well) at a cell density of about 4000 cells / well at 37°C, 5% CO 2 The culture was adherent, the original culture medium was discarded, and 100 μL of DMEM culture medium containing AMSP-30m (final concentration 10 μM) was added, and a non-medicated treatment group and a DMSO solvent control group were set up. Place in an anoxic incubator for 48 hours, add 10 μL of MTT (5 g / L) to each well and continue to incubate for 4 hours, discard the supernatant, add 100 μL of dimethyl sulfoxide to each well, shake, ...

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Abstract

The invention discloses an application of a pyridine carboxamide derivative AMSP-30m in preparation of a medicine for preventing and treating rheumatoid arthritis, and the chemical structural formulaof the AMSP-30m is shown in the specification. The invention provides the application of the AMSP-30m in preventing and treating rheumatoid arthritis, explores a new medicinal prospect of the AMSP-30m, and opens up a new medicinal field,in-vivo pharmacodynamic experiments and in-vitro cell experiments prove that AMSP-30m has the purpose of efficiently preventing and treating rheumatoid arthritis,shows a good rheumatoid arthritis treatment effect, does not have obvious side effects, and provides a strong basis for preparing AMSP-30m into an innovative drug for preventing and treating rheumatoid arthritis.

Description

technical field [0001] The invention relates to a pyridine carboxamide derivative, in particular to the application of a pyridine carboxamide derivative AMSP-30m in the preparation of drugs for preventing and treating rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis (RA) is a common chronic, systemic, and progressive autoimmune disease characterized by extensive and persistent joint synovial inflammation and irreversible cartilage / bone destruction, eventually leading to Patients suffer from joint deformity and loss of function, with a high morbidity rate. The global incidence of RA is about 1%, which seriously endangers human health and reduces the quality of life. At present, RA treatment mainly focuses on relieving pain, controlling inflammation, and improving joint function. Clinically, RA treatment measures are mainly based on drug therapy, including glucocorticoids, non-steroidal anti-inflammatory drugs, antirheumatic drugs that improve the cond...

Claims

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Application Information

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IPC IPC(8): A61K31/4418A61P19/02A61P37/02
CPCA61K31/4418A61P19/02A61P37/02
Inventor 李荣刘明明蔡莉沐玉荣周梦媛孟博刘方园
Owner ANHUI MEDICAL UNIV
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