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Application of salidroside in prevention and/or treatment of skin inflammation caused by abnormal increase of COX-2 activity through inhibition of cyclooxygenase-2(COX-2)

A technology of COX-2 and salidroside, applied in skin diseases, organic active ingredients, drug combinations, etc.

Inactive Publication Date: 2016-07-13
史飞
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, clinical studies have shown that selective COX-2 inhibitors have cardiovascular toxicity (BresalierRS, SandlerRS, QuanH, BologneseJA, OxeniusB, HorganK, et al. FowlerR, FinnP, et al. Cardiovascular risk associated with celecoxibinaclinicaltrial for colorectal adenoma prevention. NEnglJMed2005;352:1071-80)

Method used

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  • Application of salidroside in prevention and/or treatment of skin inflammation caused by abnormal increase of COX-2 activity through inhibition of cyclooxygenase-2(COX-2)
  • Application of salidroside in prevention and/or treatment of skin inflammation caused by abnormal increase of COX-2 activity through inhibition of cyclooxygenase-2(COX-2)
  • Application of salidroside in prevention and/or treatment of skin inflammation caused by abnormal increase of COX-2 activity through inhibition of cyclooxygenase-2(COX-2)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Salidroside can directly bind to COX-2.

[0060] Traditional Chinese medicine has special pharmacological effects. Finding a natural and non-toxic drug can provide us with new methods and new ideas for clinical treatment of diseases. Therefore, we applied structure-based virtual screening in traditional Chinese medicine to identify novel COX-2 inhibitors. We identified salidroside, which is extracted from Rhodiola rosea, as a COX-2 inhibitor. Molecular modeling showed that the sugar groups of Rhodiola can form hydrogen bonds with the protein amino acid residues ARG106 and TYR341 of COX-2. Therefore, it can be said that salidroside can bind to COX-2. To test this prediction, we performed an in vitro protein binding assay to investigate whether salidroside could bind COX-2 in HaCaT cell lysates. The results showed that COX-2 could bind to salidroside-Sepharose 4B beads, but not to Sepharose 4B beads. Experimental data confirmed that salidroside can directly ...

Embodiment 2

[0067] Example 2 Salidroside inhibits the activation of COX-2 and its downstream p38 or JNKs activation, and reduces the secretion of inflammatory factors in HaCaT and JB6CL41 cells.

[0068] Because Rhodiola can directly bind to COX-2, we next explored whether it can inhibit the activity of COX-2. First, we use Rhodiola rosea (400μM), 40KJ / m 2 , were irradiated for 15 minutes (HaCaT cells) and 60 minutes (JB6CL41 cells), respectively, to observe the inhibitory effect of salidroside on COX-2 levels in the two cells under different pretreatment times, and observed that after 12 hours of pretreatment, red Sedroside has an inhibitory effect on it. Secondly, we use Rhodiola rosea (400μM), 40KJ / m 2 , were irradiated for 15 minutes (HaCaT cells) and 60 minutes (JB6CL41 cells), respectively, and observed the effect of different salidroside pretreatment doses on them. It was observed that 400 μM pretreatment salidroside had an inhibitory effect on COX-2. PGE2 represents the activit...

Embodiment 3

[0073] Example 3 Increased expression of COX-2 in actinic dermatosis caused by UV.

[0074] 1) The phosphorylation levels of COX-2, P38, or JNKs are all elevated in human actinic dermatosis (chronic actinic dermatitis).

[0075] Ultraviolet (UVB) irradiation can cause oxidative damage and inflammation in the body, and ultimately increase the risk of skin cancer, and COX-2, p38, and JNKs signaling pathways are involved in this process. Actinic dermatosis is closely related to UV radiation. Therefore, we detected the phosphorylation levels of COX-2, p38 and JNKs signaling pathways in skin lesions of 5 patients with actinic dermatosis and skin samples of 2 normal individuals. . Histopathological H&E staining of actinic dermatosis compared with normal skin lesions showed epidermal hyperkeratosis, epidermal hyperplasia, spinous process elongation, intercellular edema, superficial dermal vascular dilation, and lymphocyte infiltration in the superficial dermis and around blood vesse...

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Abstract

The invention discloses a novel pharmacological effect and a molecular mechanism of salidroside. The inhibition function of the salidroside on UV induced photodermatoses such as sunburn and chronic actinic dermatitis is realized through binding with cyclooxygenase-2(COX-2), inhibition activity of cyclooxygenase-2(COX-2) and blockage of a COX-2 signal pathway. The immunopathogenesis prompts that expression of COX-2, P38 and JNK in skin lesions caused by photodermatoses is increased. The COX-2 activity affects phosphorylation of UV induced P38 and JNK in a cell experiment. The in-vitro protein binding experiment shows that the salidroside can be directly bound with COX-2 so as to inhibit COX-2 activation and inhibit phosphorylation of P38, JNK and H2AX and secretion of IL-6 and TNF-alpha. A cell experiment result is also verified by an animal experiment.

Description

[0001] The invention belongs to the fields of new pharmacological effects and disease prevention and treatment of natural medicines. It specifically relates to the biological activity of salidroside (Salidroside) inhibiting cyclooxygenase-2 (COX-2), and the application of salidroside in preventing and / or treating inflammation and tumor by inhibiting the abnormal increase of COX-2 activity, including Ultraviolet (UV)-induced actinic dermatoses such as sunburn and chronic actinic dermatitis. Background technique [0002] Many environmental and genetic factors lead to the occurrence of skin cancer, and ultraviolet (UV) in sunlight is the most important risk factor (NicholsJA, KatiyarSK. Skinphotoprotectionbynaturalpolyphenols: anti-inflammatory, antioxidantandDNA repair mechanisms. ArchDermatolRes. 2010; 302: 71-83. [ PubMed: 19898857]; ZhengD, BodeAM, ZhaoQ, ChoYY, ZhuF, MaWY, et al. The cannabinoid receptors are required for ultraviolet-induced inflammation and skin cancer deve...

Claims

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Application Information

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IPC IPC(8): A61K31/7032A61P17/00
CPCA61K31/7032
Inventor 史飞
Owner 史飞
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