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
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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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