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Application of gentiopicroside and gentiopicroside preparation

A technology of gentiopicroside and external preparations, which is applied in the application field of this compound, can solve the problems of adrenal cortex atrophy, long-term effects and safety that need to be further observed, secondary infection, etc., and achieves low preparation cost and is beneficial to The effect of promotion and application and wide application prospect

Inactive Publication Date: 2016-05-11
PERFECT CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Using traditional treatment methods, such as hormones, antihistamines, anti-inflammatory drugs, etc., can temporarily relieve symptoms, but often relapses after drug withdrawal, and the condition is aggravated, and even becomes chronic; However, long-term external use of such drugs may cause adverse reactions such as skin atrophy, telangiectasia, pigmentation, perioral dermatitis, and secondary infection. For a long time, there is no alternative drug with the same curative effect and less adverse reactions, so topical glucocorticoid has been widely used as the drug of choice in dermatology
At present, more than 7 million patients have used topical calcineurin inhibitors (Pimecrolimus > 5 million, Tacrolimus > 1.7 million) and shown to be safe and as effective as corticosteroids. However, many cases of skin cancer and lymphoma have been reported in recent years, so Its long-term effect and safety need to continue to be observed

Method used

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  • Application of gentiopicroside and gentiopicroside preparation
  • Application of gentiopicroside and gentiopicroside preparation
  • Application of gentiopicroside and gentiopicroside preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 The blocking effect of gentiopicroside on (CAN)-NF-AT pathway

[0021] Experimental principle

[0022] Using the cell line NFATK562ReporterStableCellLine stably transfected with NFAT reporter gene purchased from affimatrix in the United States, K562 cells were stimulated with PMA (activator of protein kinase CPKC) and A23187 (activator of calcium channel) to detect the expression of luciferase gene driven by transcription factor NFAT Level, reflecting the activation level of calcineurin (CaN) pathway.

[0023] PMA and A23187 respectively activate protein kinase C (PKC) and calcium ion channels, simulating the two signaling pathways necessary for the activation of T lymphocytes. After the intracellular calcium ion concentration increases, it binds to calmodulin (CaM) and activates calcineurin. , the activated calcineurin dephosphorylates the specific substrate transcription factor NFAT, translocates into the nucleus, and is further modified by the activated PK...

Embodiment 2

[0036] Example 2 The inhibitory effect of gentiopicroside on mouse skin allergy

[0037] experimental method

[0038] Select 110 Kunming mice weighing 18-22 g, half male and half male, and randomly divide them into 11 groups, with 10 mice in each group and 5 male and 5 mice in each group. The test sample is 50% ethanol (blank model control), compound dexamethasone acetate cream group (positive control, referred to as group A in the chart) and compound ketoconazole ointment (positive control, referred to as group B in the chart), gentianic acid Glycosides. The concentration of gentiopicroside was set to 8 gradients, which were 0.2 μM, 1 μM, 2 μM, 4 μM, 8 μM, 12 μM, 16 μM, and 20 μM. Cut off the back hair of the mouse with scissors, and then wash it with a depilatory cream to expose the skin, and then administer to the mice in 11 groups: the dosage of the compound dexamethasone acetate cream group and the compound ketoconazole ointment group The dosage of 50% ethanol group an...

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Abstract

The invention discloses application of gentiopicroside and a gentiopicroside preparation, particularly discloses non-treatment application of the gentiopicroside serving as a calcineurin (CAN)-NF-AT pathway blocker and application of the gentiopicroside to preparation of the calcineurin (CAN)-NF-AT pathway blocker, and further discloses application of the gentiopicroside to preparation of an external preparation or daily chemical product for preventing or treating skin hypersensitivity inflammatory reaction. The gentiopicroside stemming from dried roots and rhizomes of Gentiana lutea is capable of blocking a CAN-NF-AT pathway to effectively prevent or treat skin allergy symptoms such as eczema and contact dermatitis caused by excessive immune response and can be prepared into various daily chemical products or external preparations. A gentiopicroside synthetic process used herein is mature, preparation cost is low, popularization and application are benefited, and accordingly the gentiopicroside is promising in application prospect.

Description

technical field [0001] The present invention relates to the use of a compound, in particular to the non-therapeutic use of gentiopicroside as a calcineurin (CAN)-NF-AT pathway blocker and in the preparation of calcineurin (CAN)-NF- The use of the AT pathway blocker also relates to the use of gentiopicroside in the preparation of daily chemicals or external preparations for the treatment or prevention of skin allergic inflammation caused by hyperimmune response. Background technique [0002] Calcineurin (CaN), also known as protein phosphatase 2B (PP2B), is a member of the serine / threonine protein phosphatase family and is the only Ca-regulated enzyme found so far. 2+ / calmodulin (CaM)-regulated serine / threonine protein phosphatase. CaN is involved in the regulation of various cellular functions, especially in the regulation of T cell activation. CaN mainly mediates the dephosphorylation reaction of T cell nuclear factor (NF-AT), which translocates NF-AT into the nucleus, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K8/60A61P17/00A61P37/08
Inventor 胡瑞连李子安孙常磊朱丽平
Owner PERFECT CHINA
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