Use of CPT-1 modulators and compositions thereof

A CPT-1, stimulant technology, which can be used in drug combinations, cosmetic preparations, skin care preparations, etc., and can solve problems such as limited methods

Inactive Publication Date: 2014-10-29
AVON PROD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these ways of fighting cellulite or subcutaneous fat are limited and additional approaches are still needed

Method used

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  • Use of CPT-1 modulators and compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0183] Example 1: Determination of CPT-1 Gene Expression

[0184] Human preadipocytes were differentiated into adipocytes in adipocyte differentiation medium for 7 days. On day 8, the adipocyte differentiation medium was replaced with adipocyte maintenance fluid containing potential CPT-1 modulating compounds for an additional 7 days, as described above. The indicated weight percent of the test compound was added every other day. At the end of treatment, RNA was extracted from adipocytes using the RNA Easy mini kit (Qiagen, CA). 20 microliters of cDNA were generated from 200 ng of total RNA using the High Capacity cDNA Reverse Transcription Kit (Applied Biosystem: Cat #4368814). Dilute reverse transcriptase, buffer, dNTPs, random primers, and RNase inhibitor with RNA according to the manufacturer's instructions. Use 1 microliter of cDNA in a 20 microliter RTq-PCR reaction. Briefly, 10 μl of TaqMan Gene Expression Master Mix (Applied Biosystem; Cat#4369016), 8 μl of H 2 O,...

Embodiment 2

[0187] Example 2: Assay for regulation of intracellular triglycerides

[0188] Cryopreserved human primary preadipocytes collected from subcutaneous adipose tissue of healthy females were obtained from Zen-Bio (Research Triangle Park, NC). Preadipocytes were cultured in preadipocyte medium containing DMEM / Ham's F-12 (1:1, v / v), HEPES (pH 7.4), fetal calf serum, penicillin, streptomycin and amphotericin B (Zen-Bio). After reaching 90% confluency, preadipocytes were differentiated into adipocytes by adding Adipocyte Differentiation Medium containing DMEM / Ham's F-12 (1:1, v / v), HEPES pH 7.4 , fetal bovine serum, biotin pantothenate, human insulin, dexamethasone, isobutylmethylxanthine, penicillin, streptomycin, and amphotericin B (Zen-Bio).

[0189]To treat adipocytes with potential CPT-1 modulating compounds, test compounds are dissolved in adipocyte differentiation medium and then added to cell culture medium for 7 days. Untreated adipocytes were used as controls. After cu...

Embodiment 3

[0191] Example 3: Procollagen-I ELISA assay

[0192] at 37°C in 10% CO 2 Human epidermal fibroblasts were plated at 5000-7000 cells / well in supplemented medium (DMEM, 10% fetal bovine serum, 1% penicillin / streptomycin and 1% L-glutamine) in a humidified atmosphere. 24 hours in a 96-well culture dish. The medium was replaced with fresh medium (DMEM, 10% fetal bovine serum, 1% penicillin / streptomycin, and 1% L-glutamine) the next day, and concentrations of 0.01% and 0.1% Carambola (Carambola) leaf extract in triplicate. Water was used as vehicle control. After 72 hours of incubation, the plates were removed from the incubator, and the conditioned medium from each well was collected for procollagen-I ELISA.

[0193] Collagen production was measured using procollagen type I C-peptide (PIP) EIA kit (Takara Bio, Inc., Japan). Briefly, conditioned medium was diluted 1:25 in sample diluent. 20 μl of diluted conditioned medium and 100 μl of antibody-POD conjugate solution were ad...

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Abstract

The present invention describes methods for improving the appearance of skin, particularly, treating, ameliorating, preventing, delaying, and / or improving one or more signs of excess accumulation and / or production of subcutaneous fat, such as cellulite, and conditions related thereto, by topically applying compositions comprising Carnitine Palmitoyl Transferase-1 (CPT-1) modulators, optionally with other anti-lipid agents; and also describes compositions and methods for treating, preventing and improving the appearance of skin, particularly, treating, preventing, ameliorating, reducing and / or eliminating loss of subcutaneous fat in the skin, wherein the compositions include natural plant constituents that stimulate lipid synthesis.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Patent Application Serial No. 61 / 604,631 filed in the US Patent and Trademark Office on February 29, 2012, which is hereby incorporated by reference in its entirety for all purposes. technical field [0003] The present invention generally relates to compositions comprising modulators of carnitine palmitoyltransferase-1 (CPT-1 ) expression, for topical application to the skin. The composition of the present invention comprises at least one CPT-1 modulator for conferring benefits to the skin, in particular for: (1) stimulating the expression of CPT-1, which is an oxidized fat and thus improves cellulite Enzymes important to the condition and appearance of the skin affected by the tissue; (2) impart anti-aging benefits to the skin, and / or improve the aesthetic appearance of the skin; and / or (3) inhibit the expression of CPT-1, thereby stimulating lipids in the skin Adipog...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61Q19/00A61Q17/04A61K8/97
CPCA61K8/18A61Q19/00A61Q19/06A61K8/97A61Q19/08A61K8/9771A61K8/9789A61P17/00A61P17/08A61P17/10
Inventor C·S·黄S·殷U·桑塔纳姆J·W·利加
Owner AVON PROD INC
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