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Use of nitazoxanide and in-vivo metabolite tizoxanide thereof in resisting psoriasis and psoriasis-like dermatitis

A technology of nitazoxanide and tizoxanide, which is applied to the application of anti-psoriasis and psoriasis-like skin inflammation In the field of structural modification of nitazoxanide and tizoxanide, it can solve the problems of less adverse reactions and undetectable prototype drug nitazoxanide, and achieve the effect of less adverse reactions, good oral absorption and improved effect.

Pending Publication Date: 2022-01-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Nitazoxanide is an antiparasitic drug for the treatment of Cryptosporidium. It is well absorbed orally and has few adverse reactions. After being absorbed in the body, it is completely metabolized into tizoxanide to play a role. The prototype drug nitazoxanide cannot be detected in the body

Method used

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  • Use of nitazoxanide and in-vivo metabolite tizoxanide thereof in resisting psoriasis and psoriasis-like dermatitis
  • Use of nitazoxanide and in-vivo metabolite tizoxanide thereof in resisting psoriasis and psoriasis-like dermatitis
  • Use of nitazoxanide and in-vivo metabolite tizoxanide thereof in resisting psoriasis and psoriasis-like dermatitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Effect of Nitazoxanide on Western Diet-Induced Psoriasis in ApoE(- / -) Mice

[0028] 1 Materials and methods

[0029] 1.1 Experimental animals:

[0030] ApoE(- / -) mice, male, 8 weeks old, body weight: 19-21 g; C57BL / 6 mice, male, 8 weeks old, body weight: 19-21 g, were purchased from Beijing Huafukang Biotechnology Co., Ltd.

[0031]1.2 Feed:

[0032] Normal standard feed (Normal Diet) was purchased from Beijing Keao Xieli Feed Co., Ltd.

[0033] Western diet (Western Diet, H10141) was purchased from Beijing Huafukang Biotechnology Co., Ltd., containing (g) per kilogram: casein 195.00; methionine 3.00; corn starch 50.00; maltodextrin 100.00; sucrose 341.00; cellulose 50.00; Corn Oil 10.00; Anhydrous Cream 200.00; Mineral Blend M1001 35.00; Calcium Carbonate 4.00; Vitamin Blend V1001 10.00; Choline Bitartrate 2.00; Cholesterol 1.50; Antioxidant TBHQ 0.04.

[0034] 1.3 Reagents:

[0035] Nitazoxanide: Shanghai Adamas reagent, CAS number: 55981-09-4.

[0036] Sodium c...

Embodiment 2

[0049] Effects of tizoxanide and nitazoxanide on the proliferation of human immortalized epidermal HaCaT cells

[0050] 1 Materials and methods

[0051] 1.1 cells

[0052] HepG2 human liver cancer cells were purchased from Shanghai Zhongqiao Xinzhou Biotechnology Co., Ltd., article number: ZQ0022

[0053] 1.2 Reagents

[0054] Tizoxanide, purchased from MedChemExpress, product number: HY-12687 / CS-3893

[0055] EdU-488 (BeyoClick TM ), purchased from Biyuntian.

[0056] 1.3 Experimental method

[0057] Cell proliferation by EdU-488 (BeyoClick TM ) Cell Proliferation Detection Kit.

[0058] step:

[0059] a. Inoculate 9000 cells / well in a 96-well plate. The cells were cultured for 24 hours, and after the cells reached 60%, the corresponding concentration of nitazoxanide or tizoxanide was added for drug treatment for 24 hours.

[0060] b. Dilute EdU to 20 μM working solution with cell culture medium.

[0061] c. Add an equal volume of 37°C preheated EdU working solutio...

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Abstract

The invention discloses use of nitazoxanide and an in-vivo metabolite tizoxanide thereof in resisting psoriasis and psoriasis-like dermatitis. A research finds that nitazoxanide (formula I) has an effect of inhibiting psoriasis-like dermatitis change of ApoE (- / -) mouse skin induced by western diet feed and obviously alleviates symptoms of unhairing and skin ulcer. After being absorbed, the nitazoxanide is rapidly and completely metabolized into the tizoxanide (formula II) in vivo to play a role. Further, cytological experiments prove that both the nitazoxanide and the tizoxanide have an effect of inhibiting proliferation of human immortalized epidermal cells HaCaT. Therefore, the nitazoxanide and the in-vivo metabolite tizoxanide thereof can be used in preparing a medicine for resisting psoriasis and psoriasis-like dermatitis. The invention provides a new effective technical means for treating psoriasis and psoriasis-like dermatitis and has a wide use prospect.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to nitazoxanide and its structural modification, nitazoxanide metabolite tizoxanide and the structural modification of tizoxanide in anti-psoriasis and psoriasis-like skin Application in inflammation. Background technique [0002] Psoriasis, commonly known as psoriasis, is a chronic inflammatory skin disease caused by a variety of factors. It has a long course of disease and is prone to recurrence, which seriously affects the quality of life. The pathological manifestations of psoriasis include epidermal hyperplasia, epidermal acanthosis, parakeratosis, and inflammatory cell infiltration. At present, mild to moderate psoriasis is usually treated with topical glucocorticoids, and moderate to severe psoriasis usually requires systemic treatment. These treatments have side effects of hormones and drug toxicity of systemic treatment, so it is urgent to develop new anti-psoriasis Diseases an...

Claims

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Application Information

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IPC IPC(8): A61K31/426A61P17/06A61P17/00
CPCA61K31/426A61P17/06A61P17/00
Inventor 董德利孙志洁
Owner CHINA PHARM UNIV
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