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Uses of theaflavin-3,3'-digallate

A bigallate and theaflavin technology is applied to medical preparations containing active ingredients, pharmaceutical formulas, bone diseases, etc. It can solve the problem of unclear relationship between aseptic loosening of prostheses and achieve concentration-dependent inhibition. sex, number reduction, reduction of periosteum thickening degree

Inactive Publication Date: 2019-01-08
THE FIRST AFFILIATED HOSPITAL OF SOOCHOW UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The relationship between TF3 and wear particles-induced periprosthetic osteolysis and aseptic loosening of prostheses is still unclear

Method used

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  • Uses of theaflavin-3,3'-digallate
  • Uses of theaflavin-3,3'-digallate
  • Uses of theaflavin-3,3'-digallate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 establishes the application model of medicine described in the present invention

[0027] 1. Main drugs and reagents

[0028] Theaflavin-3,3'-digallate (TFDG), tartrate-resistant acid phosphatase (TRAP) staining kit, ethylenediaminetetraacetic acid disodium salt dihydrate (EDTA), and mounting medium were purchased from the United States Sigma Company; RANKL and m-CSF were purchased from American R&D Company, section paraffin was purchased from German Lecia Company, and RT-PCR kit was purchased from American Invitrogen Company.

[0029] 2. Main instruments and equipment

[0030] Micro-CT (SkyScan 1176, Belgium), paraffin slicer (Leica 2135, Germany), slicer (Leica 1120, Germany), paraffin embedding machine (BMJ-Ⅱ, Changzhou, China), upright microscope Axio Imager. M1 (Zeiss, Germany), microplate reader (Biotec, U.S.), autoclave (Sanyo, Japan), enzyme-linked immunoassay (Bio-Rad, U.S.), PCR instrument (TAKARATP800, TAKARA, Japan).

[0031] 3. Experimental ...

Embodiment 2

[0048] Example 2 Effect of TF3 on the number of lacuna, lacuna area, bone density and bone volume fraction in mouse skull

[0049] The high-resolution micro-CT SkyScan 1076 produced by Belgium SkyScan Company was used to scan and analyze the mouse skull. Remove the specimen from the fixative and allow to dry before scanning. Place each skull in a micro-CT test tube cup, 5 at a time, and separate each skull with a foam sheet; the skulls should be placed neatly to avoid touching the wall of the test tube. The scanning parameters were set as follows: scanning resolution 18 μm, rotation angle 180°, rotation angle increment 0.9°, voltage 80 kV, current 100 μA, exposure time 100 ms. After scanning, the SkyScan 1076 built-in software was used for 3D reconstruction of the skull. According to the method established by Wedemeyer (Wedemeyer C, et al. Particle-induced osteolysis in three-dimensional micro-computed tomography. Calcif Tissue Int. 2007; 81 (5): 394-402.), using CTAnalyzer ...

Embodiment 3

[0051] Example 3 Effect of TF3 on osteolysis area, periosteum thickness and number of osteoclasts in mouse skull

[0052] After the skull was decalcified with 10% EDTA, it was routinely embedded in paraffin. The skull was taken horizontally, and sliced ​​continuously at the sagittal suture of the skull, with a thickness of 5 μm. HE and TRAP staining were performed respectively.

[0053] 1. HE staining steps

[0054] H&E staining is the most commonly used staining method. In this study, H&E staining was used to observe the general changes of the skull surface, and to analyze the degree of inflammatory cell infiltration and bone destruction. The specific operation steps are as follows:

[0055] (1) Select 5 consecutive slices for each sample, put them in an oven (60°C) and bake for 30 minutes;

[0056] (2) Paraffin sections were dewaxed with xylene (15 min×2 times), then passed through absolute ethanol, absolute ethanol, 95% ethanol, 95% ethanol, 90% ethanol, 80% ethanol, an...

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Abstract

The invention discloses application of theaflavin-3, 3'-digallate, and particularly relates to application of theaflavin-3, 3'-digallate in preparing a periprosthetical osteolysis drug. Compared with the prior art, theaflavin-3, 3'-digallate has the advantages that when the drug is adopted to treat periprosthetical osteolysis, bone surface lacuna number and lacuna area are obviously reduced, bone density and bone volume fraction are obviously increased, osteolysis degree is obviously lowered, periprosteal thickening degree is lowered, and mature osteoclast number is reduced; the drug can inhibit RANKL-induced osteoclast activation, and inhibition effect is dependent on concentration; the drug can obviously inhibit activation of an ERK signal path, can inhibit expression of ERK downstream target factors C0fos and NFATc1 and has no influence on activity of ERK upstream regulated kinase MEK1 / 2.

Description

technical field [0001] The invention belongs to the field of new application of medicines, and relates to a medicine for periprosthetic osteolysis, in particular to the use of theaflavin-3,3'-digallate in preparing medicine for periprosthetic osteolysis. Background technique [0002] Total joint arthroplasty (TJA) is one of the most successful orthopedic surgeries in the 20th century. It can effectively relieve joint pain, reconstruct joint function and improve the quality of life of patients. In 2007, a review article was published in "Lancet", calling TJA "the operation of the century". At present, TJA has become the first choice for the treatment of severe osteoarthritis, rheumatoid arthritis and end-stage lesions of femoral head necrosis. According to statistics, in the United States, about 700,000 patients receive TJA each year, and it is estimated that by 2030, more than 4 million patients will receive TJA each year. However, with the wide application of this technol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/353A61P19/08
CPCA61K31/353
Inventor 耿德春胡宣洋平子川朱雪松毛海青徐耀增杨惠林
Owner THE FIRST AFFILIATED HOSPITAL OF SOOCHOW UNIV
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