Extracts with liver-X-receptor modulators, compounds and their use especially in weight control

A compound, the technology of -ra, is applied in the field of one or more natural compounds alone or as an additive, as an active ingredient, and can solve problems such as unreasonable effects

Inactive Publication Date: 2010-08-04
INTERMED DISCOVERY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Even more surprisingly, these concentrated extracts did not need to contain gomisin G or benzoylgomisin Q as they showed activity (albeit weak) on NPFF (see above), whereas as in the examples As shown in , they were not expected to cross the blood / brain barrier making their effect on NPFF unreasonable

Method used

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  • Extracts with liver-X-receptor modulators, compounds and their use especially in weight control
  • Extracts with liver-X-receptor modulators, compounds and their use especially in weight control
  • Extracts with liver-X-receptor modulators, compounds and their use especially in weight control

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0176] Embodiment 1: Schisandra methanol (1), the pure change:

[0177] 1 kg of dried Schisandra fruit (Galke, Gittelde / Harz, Germany) was extracted by sonication at room temperature for 30 minutes using 1800 ml of 95% ethanol and finally crushed for 10 minutes using a high-speed disperser ultra-turrax (Janke & Kunkel, Staufen, Germany). After vacuum filtration, the remaining fruit material was extracted a second time for 30 minutes using 700 ml of 95% ethanol. The combined extract solvents were evaporated under reduced pressure. The remaining aqueous phase (about 250 ml) was extracted 3 more times with 250 ml ethyl acetate. The collected ethyl acetate extracts were evaporated to dryness under reduced pressure to obtain an extract hereinafter referred to as crude extract.

[0178] For further enrichment of pure compounds, the crude extract was subjected to a first purification step using a Nucleodur 100-5C18ec column (Macherey & Nagel, Düren, Germany) (250x20 mm) with li...

Embodiment 2

[0199] Example 2: Further enriched extract from Schisandra chinensis

[0200]The crude extract (see Example 1) was subjected to a chromatographic concentration step using a Nucleodur 100-5C18ec column (Macherey & Nagel, Düren, Germany) (130x40 mm), where a linear water (solvent A) / acetonitrile (solvent B) gradient was applied (two The solvents all contained 0.1% trifluoroacetic acid), starting from 30% acetonitrile to 100% acetonitrile in 60 minutes, followed by an isocratic period of 20 minutes. Fractions were collected every minute using a flow rate of 20ml / min. Signals were detected at 210 nm and 254 nm using a UV / VIS-155 detector (Gilson, Langenfeld, Germany). Fractions containing deoxyschisandra methanol, gomisin N and schisandrin (retention time 32-62 min) were collected and combined. The method can directly concentrate LXR active lignans and next-level LXR active compounds.

[0201] Peaks measured using various detection systems in HPLC such as figure 1 shown in . ...

Embodiment 3

[0240] Embodiment 3: Experiment in mice

[0241] The extract from Example 2 was applied as a supplement to mouse chow, and changes in body weight and body fat compared to a control group not subjected to such supplementation were measured.

[0242] By feeding a standard diet (Atromin 1324, AtrominSpezialfutterwerke GmbH, Lage, Germany) 8-week-old male mice [strain C57BL / 6 (Harlan Winkelmann GmbH, Borchen, Germany)] were acclimatized for 2 weeks.

[0243] Feeding experiment:

[0244] cc: Long-term balanced diet: after acclimatization standard food enriched with 1mg extract / 1g dry food.

[0245] cf: balanced / high-fat meal: enriched with 1mg extract / 1g dry food and 12% palm fat (Peter KGaA, Elmshorn) after acclimation to standard food.

[0246] Mice were weighed weekly (accuracy ±0.1 g) and thereafter scanned using DEXA under isoflurane (2-chloro-2-(difluoromethoxy)-1,1,1-trifluoro-ethane) anesthesia Body composition was analyzed using a PIXImus2 scanner, software version ...

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Abstract

The invention relates to the use, or methods (especially with regard to animals, especially human, that are in need of such treatment) comprising the use, of an extract and/or one or more natural compounds from plants or parts of plants, respectively, from a genus selected from the group consisting of Schisandra,Illicium, Kadsura, Steganotaenia and Magnolia, alone or as supplement, as active ingredient in the regulation of body weight and/or fat loss and/or for the management of obesity, either in humans or in animals, to the use of said extract and/or natural compound(s) or mixtures in the manufacture of a pharmaceutical or nutraceutical formulation for the regulation of body weight and/or fat loss and/or for the management of obesity either in humans or in animals. The above extract and/or compound(s) can further be used to reduce one or more adverse metabolic parameters in a subject. The invention relates also to said extract and/or compound(s) for use in the treatment or in the preparation of a medicament for the treatment of obesity, as well as their preparation. It also relates to pharmaceutical or nutraceutical formulations comprising said extract and/or natural compound(s) which are useful in the regulation of body weight and/or fat loss and/or for the management of obesity.

Description

technical field [0001] The present invention relates to extracts and / or one or more natural Use of a compound alone or as an additive (supplement), as an active ingredient, in regulating body weight and / or reducing fat and / or controlling obesity in humans or animals or methods comprising the use (especially in animals in need of such treatment, Especially for humans), relates to the use of said extract and / or natural compound or mixture in the preparation of medicaments or nutritional products for regulating human or animal body weight and / or reducing fat and / or controlling obesity. The above extracts and / or compounds can be further used for anti-inflammation. The present invention also relates to the application and preparation of the extract and / or compound in treating obesity or preparing medicine for treating obesity. The invention also relates to pharmaceutical or nutraceutical preparations comprising said extracts and / or natural compounds for regulating body weight and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/085A61K31/215A61K31/343A61K36/79A61K36/57A61P3/04A61P3/06
CPCA61K31/215A61K36/57A61K31/222A61K31/343A61K31/085A61K31/36A61K36/79A61K31/09A61P3/00A61P3/10A61P3/04A61P3/06A61P43/00A61P9/10A61P9/12
Inventor T·格罗特E·勒默尔T·亨克尔
Owner INTERMED DISCOVERY
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