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Pterostilbene (PTER) for use in the prevention and/or treatment of skin diseases, damages or injures

A skin disease, skin disease technology, applied in the field of pharmacy

Inactive Publication Date: 2012-08-15
GREEN MOLECULAR
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the prior art has disclosed orally administered drugs that may be useful in the treatment of inflammatory conditions, however, these orally administered drugs have never exerted their potential therapeutic effect on distant target tissues such as the skin

Method used

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  • Pterostilbene (PTER) for use in the prevention and/or treatment of skin diseases, damages or injures
  • Pterostilbene (PTER) for use in the prevention and/or treatment of skin diseases, damages or injures
  • Pterostilbene (PTER) for use in the prevention and/or treatment of skin diseases, damages or injures

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0205] Example 1: Experimental animal model.

[0206] The SKH-1 strain mice provided by Charles River Company were used as experimental animals. They are hairless immune competent mice. As shown in Table 2, the experimental group was formed with female mice aged 3 to 4 weeks. Each light protection experimental group consists of 5 to 6 animals. In these studies, each experimental group consisted of 20 mice.

[0207] Table 2

[0208] Group

Name

Treatment

UVB exposure

I

Negative control

Liposome carrier

No

IIt

UVBa

Liposome carrier

20min after treatment

IIa

UVBb

Liposome carrier

20min before treatment

IIIt

RESa

RES liposome

20min after treatment

IIIa

RESb

RES liposome

20min before treatment

IVt

PTERa

PTER liposome

20min after treatment

IVa

PTERb

PTER liposome

20min before treatment

Vt

QUERa

QUER liposome

20min after treatment

Va

QUERb

QUER liposome

20min before treatment

VIt

(PTER+QUER)a

PTER+QUER liposome

20min after treatmen...

Embodiment 2

[0218] Example 2: Preparation of liposomes.

[0219] Regardless of polyphenols, the method of preparing liposomes is also used: soybean lecithin; dichloromethane is used as an organic solvent in the case of PTER and / or QUER, and ether is used for resveratrol because it cannot dissolve dichloromethane Of organic solvents. The organic solvent was evaporated using a rotary evaporator connected to a vacuum and a temperature of 40°C. After removing the organic solvent, the liposomes were resuspended in PBS diluted to 1 mM. In the final liposome concentration, the concentration of each polyphenol was 20 μM polyphenol as determined by HPLC / MS-MS before adding Carbopol.

[0220] The steps used to prepare liposomes can be summarized as follows:

[0221] 1. Weigh polyphenols and lecithin

[0222] PTER

QUER

RESV

Lecithin

0,512g

0,676g

0,458g

2,376

[0223] 2. Dissolve polyphenols and lecithin in 40 ml of dichloromethane (in the case of PTER and / or QUER) or 140 ml of ether (in...

Embodiment 3

[0248] Example 3: Measurement of skinfold thickness 24h after irradiation.

[0249] The thickness of the skinfold was measured by forming a fold of the skin from the back of the mouse (from the armpit to the hip); the fold was measured with a vernier caliper.

[0250] The increase in fold thickness is calculated from the difference between the initial point (before the reaction) and the thickness of each point.

[0251] figure 1 The results obtained when measuring the thickness of the skin of the mouse's hind legs and buttocks (where various treatments have been applied) are shown. These results were statistically analyzed by ANOVA and compared by Tukey's test, and grouped according to significant differences. Standard deviation is added to figure 1 in. Such as figure 1 As shown, when applied before UVB exposure, the combination of PTER+QUER and PTER alone as a photoprotectant are more effective than commercially available creams (Vichy, Heliocare, and Isdin) and RESV. Therefore, ...

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Abstract

The present invention refers to the use of PTER, or any acceptable salt thereof, optionally in combination with QUER, or any acceptable salt thereof, for the manufacture of pharmaceutical compositions for preventing and / or treating skin diseases, damages or injuries. Those methods of prevention and / or treatment comprise the administration of an effective amount of a composition comprising PTER as active compound, or any acceptable salt thereof, optionally in combination with QUER, or any acceptable salt thereof, to the subject. The present invention also refers to the compositions, per se, comprising PTER as active compound, or any acceptable salt thereof, optionally in combination with QUER, or any acceptable slat thereof, characterized by being formulated in the form of liposomes, and to the method for preparing said liposome formulations.

Description

Technical field [0001] The present invention can be covered in the field of pharmaceutical technology. Background technique [0002] High intake of fruits and vegetables is associated with a healthy lifestyle. This correlation is due to the presence of natural antioxidants in food, mainly polyphenol compounds. One of the polyphenols that has generated greater interest in the scientific community is resveratrol (3,4',5-trihydroxy-trans-stilbene; RESV), which is abundant in wine The small (molecule) polyphenols of serotonin have potential beneficial effects attributable to them in different chronic diseases (especially cancer, cardiovascular disease, type II diabetes and neurodegenerative diseases). The anti-cancer properties of RESV were first proposed by Jang et al. (Jang M, CaiL, Udeani GO, Slowing KV, Thomas CF, Beecher CW, Fong HH, Farnsworth NR, Kinghorn AD, Mehta RG, Moon RC, Pezzuto JM. (1997) Science 275(5297):218-20), has an effect on the three stages (initiation, prom...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05
CPCA61K8/14A61K8/347A61K8/498A61K9/0014A61K9/127A61K31/352A61Q19/00A61K31/09A61P17/00A61P17/02A61P17/06A61P17/16A61P35/00A61P43/00A61K2300/00C07C43/166C07D311/30A61Q17/04A61K31/353A61K2800/74
Inventor 何塞·马里亚·埃斯特雷拉阿里奎尔米格尔·A·阿森西米拉莱斯
Owner GREEN MOLECULAR
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