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Application of psoralen to preparation of medicinal composition and medicinal composition

A technology of psoralen and composition, applied in the directions of drug combination, active ingredient of heterocyclic compound, bone disease, etc., to achieve the effect of promoting secretion and inhibiting inflammatory response

Inactive Publication Date: 2018-08-21
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no better specific drug for the treatment of osteoarthritis. The drug for the treatment of osteoarthritis needs to have two effects. On the one hand, it must activate and protect chondrocytes; on the other hand, it must inhibit the synovial cells in the joint tissue. The dual role of secreting inflammatory factors

Method used

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  • Application of psoralen to preparation of medicinal composition and medicinal composition
  • Application of psoralen to preparation of medicinal composition and medicinal composition
  • Application of psoralen to preparation of medicinal composition and medicinal composition

Examples

Experimental program
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Effect test

preparation example Construction

[0031] The psoralen is mixed with other components by conventional preparation methods in the art to prepare the desired dosage form.

[0032] The important pathogenesis of osteoarthritis is the degeneration of chondrocytes in the joint cavity and the inflammation of the surrounding synovial tissue. The present inventors found that human synoviocytes and rat chondrocytes induced by TNF-α were treated with psoralen, and found that psoralen could inhibit the inflammatory response of synoviocytes, protect and regulate the function of chondrocytes.

[0033] According to another specific embodiment of the present invention, a use of psoralen in the preparation of a pharmaceutical composition for treating osteoarthritis is provided.

[0034] The aforementioned osteoarthritis is preferably knee arthritis.

[0035] Preferably, the daily dose of psoralen is 0.1 mg / kg to 10 mg / kg, preferably 0.5 mg / kg to 8 mg / kg, more preferably 1 mg / kg to 5 mg / kg, expressed as psoralen.

Embodiment 1

[0037] Example 1 The Function of Psoralen Inhibiting the Inflammatory Response of Human Synovial Fibroblasts

[0038] Human synovial fibroblasts were induced by TNF-α, and uninduced human synovial fibroblasts were set as a control group. Human synovial fibroblasts induced by TNF-α were treated with 1 μM, 10 μM and 20 μM psoralen for 24 hours, and matrix metalloproteinase (MMP)-1, -2, -3, -9, - 12 and -13 and the expression of interleukin (IL)-1β, -6 and -12. Then, the treated human synovial fibroblasts were immunostained, and the fluorescence intensity of IL-1β and MMP-13 in the synovial fibroblasts was detected. The experiment was repeated 3 times. The results are shown in figure 1 a-e in.

[0039] see figure 1 a-e, psoralen significantly inhibited the expression of MMP-1, -2, -3, -9, -12, -13 and IL-1β, -6, -12 induced by TNF-α, and inhibited Synthesis of MMP-13 and IL-1β proteins induced by TNF-α. This confirms that psoralen has the effect of inhibiting the inflammat...

Embodiment 2

[0040] Example 2 The function of psoralen in protecting chondrocytes

[0041] Rat chondrocytes were induced by TNF-α, and TNF-α-induced chondrocytes were treated with 10 μM psoralen for 24 hours and 48 hours, respectively. The expression of matrix metalloproteinase MMP-13, the expression of chondrocyte proliferation genes MAPK1, CDK1, Ki67, P21, MYC, and the synthesis of type II collagen Col II and aggrecan AGG in the treated chondrocytes were measured respectively. The experiment was repeated 3 times. The results are shown in figure 2 a-f in.

[0042] see figure 2 a-f, psoralen significantly inhibited the expression of MMP-13, promoted the expression of chondrocyte proliferation genes MAPK1, CDK1, Ki67, P21, MYC, and promoted the synthesis of Col II and AGG. This confirms that psoralen can effectively protect chondrocytes and promote the secretion of cartilage matrix.

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Abstract

The invention provides a medicinal composition comprising psoralen as an active component, and the application of the psoralen to preparation of the medicinal composition for treating osteoarthritis.The medicinal composition comprises a therapeutically effective amount of psoralen and a pharmacologically acceptable excipient or carrier. The medicinal composition comprising the psoralen can promote secretion of a cartilage matrix, protect chondrocytes and maintain a normal cartilage tissue structure, so that the medicinal composition can effectively treat the osteoarthritis.

Description

technical field [0001] The present invention relates to the application of psoralen in preparing a pharmaceutical composition for treating osteoarthritis, and the pharmaceutical composition for treating osteoarthritis comprising psoralen as an active ingredient. Background technique [0002] Psoralen (Psoralen, PSO) is mainly derived from the leguminous plant psoralen, known to have photosensitizing effect, can promote the increase of pigment after application, and also has anticancer effect. [0003] Osteoarthritis is a degenerative disease, which is caused by various factors such as aging, obesity, strain, trauma, joint deformity, etc. arthritis. [0004] The current treatment for osteoarthritis is generally to reduce the load on the joints and excessive large-scale activities to delay the progress of the disease. If necessary, use auxiliary equipment such as splints, braces and canes, or take anti-inflammatory and analgesic drugs such as: non-steroidal Anti-inflammatory...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/37A61P19/02A61P19/08
CPCA61K31/37
Inventor 许康朱鹏邱雪峰董念国
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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