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New use of hemin and compound thereof to medicines

A technology of hemin and compound, which is applied in the direction of medical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problems of joint damage prevention, high price, loss of benefit, etc.

Pending Publication Date: 2019-12-20
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The first category is non-steroidal anti-inflammatory drugs (Non-steroid anti-inflammatory drugs, NSAIDs), by inhibiting cyclooxygenase, inhibiting the transformation of arachidonic acid into prostaglandins, thereby playing the role of anti-inflammatory and analgesic, in the present invention The control drug used in this category is celecoxib (celecoxib), which is a highly selective and reversible COX-2 inhibitor, but this type of drug can only relieve symptoms, and cannot prevent and alleviate cartilage and bone damage
[0015] The second category is anti-rheumatic drugs (Disease-modifying antirheumatic drugs, DMARDs), which mainly exert a certain anti-RA effect through cytotoxicity and immunosuppression, and can delay but not prevent joint damage. Loss of benefit over time
[0016] The third category is glucocorticoids, which have powerful anti-inflammatory effects, but have a short half-life, are massively metabolized in the body, and have a series of side effects such as excessive immunosuppression, osteoporosis, and even osteonecrosis. For the treatment of rheumatoid arthritis, which itself has bone and joint pathological changes, its side effects on the body's bones are particularly unfavorable
However, compared with traditional DMARDS, these drugs are very expensive, which limits their clinical application and has certain side effects, including serious and opportunistic infections.

Method used

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  • New use of hemin and compound thereof to medicines
  • New use of hemin and compound thereof to medicines
  • New use of hemin and compound thereof to medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The preparation of the stable compound of embodiment 1 Hemin

[0044] In this example, a stable complex of hemin and albumin or amino acids was prepared.

[0045] (1) Complex with albumin

[0046] Hemin with 5mg / ml Na 2 CO 3 The solution was dissolved, and the albumin was dissolved in PBS with a pH of 7.4, and an equimolar amount of albumin was added to the hemin solution, stirred while adding, and reacted overnight to obtain a hemin-albumin complex. The albumin is bovine serum albumin (bovine serum albumin, BSA) or human serum albumin (human serum albumin, HSA).

[0047] (2) Complex with amino acids

[0048] Take arginine that is 3 times the mole number of hemin and dissolve it in 10% ethanol: 40% ethylene glycol: water mixed solvent (v / v), add hemin under stirring, and react overnight to obtain the compound of hemin and arginine thing (hemin arginate). The amino acid may also be lysine or histidine.

[0049] (3) Soluble salts of hemin

[0050] Dissolve hemin i...

Embodiment 2

[0051] Example 2 In vitro evaluation of the anti-inflammatory effect of Hemin and the stable complex of hemin

[0052] In this example, the Raw264.7 cell inflammation model stimulated by LPS+IFN-γ was established to investigate the in vitro anti-inflammatory effect of hemin and hemin stable complex. Raw264.7 cells in the logarithmic growth phase were inoculated into 12-well plates, and after 24 hours of culture, 500ng / ml lipopolysaccharide (LPS) and 20ng / ml γ-interferon (interferon gamma, IFN-γ) were added to stimulate 6 hours to establish macrophages Inflammation model (M1 macrophage), add 1 μM, 5 μM, 10 μM, 20 μM, 30 μM, 40 μM, 50 μM, 60 μM, 80 μM, 100 μM, 150 μM, 200 μM hemin or hemin-albumin complex and hemin arginate with corresponding hemin content , hemin sodium salt, after cultivating for 16 hours, extract RNA, detect the mRNA expressions of inflammatory factors TNFα, IL-1β and IL-6 in each group by PCR, and screen the hemin concentration with the best anti-inflammator...

Embodiment 3

[0054] Example 3 Evaluation of anti-inflammatory effect of Hemin arginate and hemin sodium salt used for preventive administration of rat adjuvant arthritis model

[0055] In this embodiment, by establishing the rat arthritis model induced by Freund's complete adjuvant, prophylactic administration was given 1 h before the inflammation on the 0th day, and the administration was continued until 28 days after the inflammation, by measuring the hind paw thickness (mm ) and observe and evaluate the arthritis index score, and examine the preventive and therapeutic effects of hemin arginate and hemin sodium salt on rat adjuvant arthritis.

[0056] 1. Experimental animals: healthy Sprague-Dawley (SD) rats, male, weighing 250-300 g.

[0057] 2. The establishment of AIA:

[0058] Rats were injected with 0.1ml of complete Freund's adjuvant into the skin of the right hind paw of rats to induce inflammation and induce arthritis in rats.

[0059] 3. Grouping and administration of experime...

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PUM

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Abstract

The invention provides an application of hemin and / or hemin compounds thereof to preparation of medicines for preventing and treating rheumatoid arthritis. The hemin or the hemin compounds have remarkable effect of resisting inflammation when being used for performing in vitro action on macrophages, can effectively restrain vola swelling for a rat arthritis model, and can notably reduce expressionof metapodium inflammatory factor mRNA and mRNA expression of liver and spleen tissue autoimmunity correlation factors. The application explains that the hemin or the hemin compounds have good effectof preventing and treating rheumatoid arthritis.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to the new application of hemin and its compound in medicine. Background technique [0002] Hemin (Hemin), also known as hemin or hemin (Haemin or FerricChloride Heme). Hemin is a porphyrin compound containing ferric ions. Hemin can be oxidized from natural heme, the chemical properties of the former and the latter are similar. Heme is ubiquitous in animal blood, muscle and some plant tissues. It is the key prosthetic group of many biologically active macromolecules (such as hemoglobin, muscle protein, cytochrome and peroxidase, etc.), so heme is the key prosthetic group of organisms. One of the most important compounds in [0003] [0004] Hemin CAS No. 16009-13-5, molecular formula C 34 h 32 ClFeN 4 o 4 , the relative molecular mass is 651.94. The chemical structure of hemin is shown above. Since the chemical structural formula of hemin contains a large hydrophob...

Claims

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Application Information

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IPC IPC(8): A61K31/555A61K47/62A61K47/54A61P29/00A61P19/02A61P37/02
CPCA61K31/555A61K47/62A61K47/542A61K47/545A61P29/00A61P19/02A61P37/02Y02A50/30
Inventor 冯敏孙冰之
Owner SUN YAT SEN UNIV
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