Application of neauline in preparation of medicine for treating arthritis

An arthritic and neorline technology, applied in the field of medicine and biology, can solve the problems of little NE pharmacological activity and application research, no NE rheumatoid arthritis research report, etc., and achieve high oral bioavailability and good medicinal use. Prospects, the effect of enriching treatment methods

Pending Publication Date: 2022-04-12
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0003] Neoline (NE) is a C-19 type aconitum alkaloid extracted and separated from the traditional Chinese medicine Aconite. At present, the research on NE at home and abroad is mainly focused on the extraction, separation and structure identification. The pharmacological activity and application of NE There are very few studies. The known studies have shown that NE has the effects of strengthening the heart, dilating blood vessels, and anti-tumor in vitro. It has applications in anti-arrhythmia, anti-heart failure, and analgesia. Research Report on the Treatment of Rheumatoid Arthritis

Method used

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  • Application of neauline in preparation of medicine for treating arthritis
  • Application of neauline in preparation of medicine for treating arthritis
  • Application of neauline in preparation of medicine for treating arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1: The treatment experiment of NE to RA

[0042] This example focuses on the treatment experiment of Niolin (NE) on adjuvant arthritis in rats to investigate the therapeutic effect of NE on rheumatoid arthritis.

[0043]Adopt 30 male SD rats of 120 ± 20g, take 6 as a group, divide into 5 groups at random, namely normal group, model group, indomethacin group (positive drug), 4mg / kg NE group (high dose NE group) and 2mg / kg NE group (low dose NE group). After the rats were fixed, the hair near the base of the tail was shaved, wiped and disinfected with 75% alcohol, and 0.1 mL of normal saline was subcutaneously injected at about 1 cm from the base of the tail of the rats in the normal group, and the rats in the other groups were injected with the same volume of Freund's complete adjuvant. After the rats were injected with Freund's complete adjuvant, the disease began on the 9th day. From the ninth day, rats in the normal group, model group, indomethacin group...

Embodiment 2

[0070] Example 2: Experiments related to the pharmacological and pharmacological effects of NE in the treatment of RA

[0071] The main clinical features of RA are joint inflammation and swelling, local joint pain, and systemic mild or moderate fever. Therefore, anti-inflammation, analgesia and antipyretic are the key to relieve RA symptoms, which can effectively eliminate joint swelling, relieve pain and restore body temperature. This example demonstrates the anti-inflammatory, analgesic and antipyretic pharmacological activities of NE through experimental verification.

[0072] (1) Anti-inflammatory activity of NE

[0073] In this example, the classic carrageenan-induced paw swelling and inflammation model in mice was used to investigate the anti-inflammatory activity of NE. Twenty-four male 8-week-old C57 mice were randomly divided into 4 groups with 6 mice in each group, and the thickness of the right hind foot of each mouse was measured with a vernier caliper. The mice...

Embodiment 3

[0083] Example 3: Oral bioavailability and absorption and transport characteristics of NE

[0084] In this implementation, by investigating the oral bioavailability and absorption and transport characteristics of NE, it preliminarily evaluates its druggability.

[0085] (1) Oral bioavailability of NE

[0086] Ten male 8-week-old C57 mice were randomly divided into 2 groups, 5 in each group. The mice in the two groups were given 15 mg / kg NE intragastrically and 1.5 mg / kg NE intravenously, respectively, at time points of 0, 3, 7, 10, 15, 20, 30, 50, 80, 120, 240, 360 and 480 min from Tail vein blood collection. After the blood sample was centrifuged to obtain plasma, it was processed by organic solvent precipitation protein, and 2uL was taken into the UHPLC-MS / MS system to quantitatively detect the concentration of NE in the plasma, draw the blood drug concentration-time curve, and calculate the pharmacokinetic parameters, and follow the formula below Calculation of oral bioa...

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Abstract

The invention discloses an application of Neole in preparation of a medicine for treating arthritis, and the Neole can also be applied to preparation of a medicine for treating arthritis and having anti-inflammatory and analgesic activity effects, rat experiments verify that Neole has a remarkable treatment effect on rheumatoid arthritis, can remarkably reduce the concentration of MMP3 in serum, and can be used for preparing medicines for treating rheumatoid arthritis. The treatment effect is obviously better than that of indometacin, and no side effect exists; experiments prove that the pharmaceutical composition has the characteristics of remarkable anti-inflammatory and analgesic activity and the like, also has the advantages of high permeability, good absorption, high oral bioavailability and the like, has good druggability and good medicinal prospects, and can enrich treatment means for rheumatoid arthritis.

Description

technical field [0001] The invention relates to the field of medical biotechnology, and specifically relates to the use of an active ingredient of a traditional Chinese medicine, that is, Niolin can be used for treating rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis (RA) is a chronic, inflammatory, systemic autoimmune disease. The clinical features are symmetrical swelling of the joints, morning stiffness, local joint pain, dysfunction, and systemic mild or moderate fever. RA has a high disability rate, and multi-articular cartilage and bone erosions will occur if the treatment is not timely, seriously affecting the quality of life of patients. The etiology and pathogenesis of RA have not been fully clarified, and the current treatment of RA mainly focuses on controlling symptoms and delaying the disease. Western medicine mainly treats RA with non-steroidal anti-inflammatory drugs, glucocorticoids, and immunosuppressants, which can delay the disea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/439A61K36/714A61P19/02A61P29/00
Inventor 朱丽君刘中秋李小翠倪家栋许仪红傅愉区晓君
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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