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COMPOSITIONS COMPRISING AN NFkB-INHIBITOR AND A TROPOELASTIN PROMOTER

a technology of nfkb-inhibitor and promoter, which is applied in the direction of biocide, plant/algae/fungi/lichens ingredients, drug compositions, etc., can solve the problems that the skin can be aging and affect the elasticity and strength of the skin,

Inactive Publication Date: 2011-04-07
JOHNSON & JOHNSON CONSUMER COPANIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0008]The inventors have now surprisingly discovered surprising benefits of a particular class of anti-inflammatory compounds, agents that inhibit the cell transcription factor nuclear kappa-B (NFκB). The inventors have found that while NFκB-inhibitors do not themselves necessarily enhance tropoelastin activity, when NFκB-inhibitors are combined with tropoelastin promoters, the resulting combinations exhibit a surprisingly large, unexpected and synergistic boost in tropoelastin promotion efficacy. Even more surprisingly, the inventors have identified certain compounds such as resorcinol derivatives, previously unknown for their inhibitory activity on NFκB, as particularly suitable to dramatically boost the tropoelastin activity of tropoelastin promoters.

Problems solved by technology

Aging of the skin can adversely affect elasticity and strength of the skin through changes in the two main constituents of the dermal extracellular matrix, the fibrous proteins collagen and elastin.

Method used

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  • COMPOSITIONS COMPRISING AN NFkB-INHIBITOR AND A TROPOELASTIN PROMOTER
  • COMPOSITIONS COMPRISING AN NFkB-INHIBITOR AND A TROPOELASTIN PROMOTER
  • COMPOSITIONS COMPRISING AN NFkB-INHIBITOR AND A TROPOELASTIN PROMOTER

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0086]The NFκB-INHIBITION TEST described above was performed on test samples of Bay 11-7082 (Sigma-Aldrich, St. Louis, Mo.), Tetrahydrocurcuminoids CG (Sabinsa Corporation, Piscataway, N.J.), as well as various concentrations of 4-hexylresorcinol. The results are shown in Table 1, in which NF-kB Gene Reporter Activation (Luminescence, L) is reported for the test samples and a control sample. Percent NF-kB Inhibition is also reported.

TABLE 1NF-kB Gene ReporterPercentActivationNF-kB(Luminescence, L)InhibitionUntreated 1.2 ± 0.3—TNFα (100 ng / ml) Stimulated,108.2 ± 8.5 —“Lcontrol”TNFα + 4-Hexylresorcinol 9.3 ± 0.991.4%(50 ug / ml)TNFα + 4-Hexylresorcinol29.3 ± 9.272.9%(10 ug / ml)TNFα + 4-Hexylresorcinol55.1 ± 1.750.9%(5 ug / ml)TNFα + 4-Hexylresorcinol106.1 ± 1.9  1.9%(1 ug / ml)TNFα + Tetrahydrocurcuminoids CG37.8 ± 2.665.1%(10 ug / ml)Bay 11-7082 (25 uM)11.3 ± 5.689.5%

[0087]Bay 11-7082 and Tetrahydrocurcuminoids CG showed strong NF-kB inhibition. Unexpectedly, 4-hexylresorcinol also resulted i...

example 2

[0088]The NFκB-INHIBITION TEST described above was performed on a series of substituted resorcinols each having a concentration of 10 ug / ml. The results are shown in Table 2.

TABLE 2Percent NF-kBStructureInhibition4-Octylresorcinol99.5%4-Hexylresorcinol92.4%β-Zearalenol CAS#71030-11-087.1%β-Zearalanol CAS#42422-68-476.56%2,4-Dinitrosorcinol51.78%4-Chlororesorcinol51.63%2,6-Dichlororesorcinol51.54%Zearalanone50.95%Phenethylresorcinol31.8%4-Dodecylresorcinol20.87%4-Caproylresorcinol10.25%C-Undecylcalix[4]- resorcinarene 4.87%3-Methoxyphenol  0%2′4′- Dihydroxypropiophenone−0.7%2,4- DIHYDROXYCINNAMIC Acid−1.7%1,3-Dimethoxybenzene−1.7%

[0089]It can be seen from the data in Table 2 that superior NFκB inhibition is provided by substituted resorcinols containing only substituents free of phenyl functionalities, substituted resorcinols containing only substituents free of ketone functionalities, and substituted resorcinols comprising a substituent having 5 to 11 carbon atoms.

example 3

[0090]The TROPOELASTIN PROMOTER ASSAY was performed on the following compounds: Tanacetum parthenium (parthenolide-free feverfew extract from Integrated Botanical Technologies of Ossining, N.Y.), Rubus fruticosus (SymMatrix, from Symrise), cells treated with various preparations of Phyllanthus niruri (Raintree Nutrition, Inc., Carson City, Nev.) subsequently extracted with water and fractionated to include only species with molecular weight less than 100,000 daltons, and 4-hexylresorcinol (Synovea HR, Sytheon Ltd).

[0091]The compounds were diluted in cell culture media (DMEM Media of Invitrogen, San Diego Calif.) to the concentration of “active” indicated in Table 3 below. The compounds were added to the transfected H9C2 cells and were incubated for 24 hours. Test samples were compared to a DMSO vehicle.

[0092]The results are shown in Table 3.

TABLE 3RespectivePercentRatio ofConcentrationsTropoelastinChangeNFκB-Inhibitor:of ActivesPromoterOverTropoelastinCompound / Extract(on active basi...

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Abstract

The present invention relates to a composition comprising an NFκB-inhibitor and a tropoelastin promoter, and methods of treating signs of skin aging using said compositions.

Description

FIELD OF THE INVENTION[0001]A composition comprising an NFκB-inhibitor and a tropoelastin promoter is provided. The composition is useful, for example, for topical application to the skin.BACKGROUND OF THE INVENTION[0002]The aging of skin may be understood as being influenced by intrinsic factors and extrinsic factors. Intrinsic factors include natural changes to the skin, which are regulated by genetic makeup. Extrinsic factors include exogenous influences such as UV damage, environmental factors, and the like.[0003]Aging of the skin can adversely affect elasticity and strength of the skin through changes in the two main constituents of the dermal extracellular matrix, the fibrous proteins collagen and elastin. For example, elastin is a large fibrous protein formed by the crosslinking of elastin precursor protein molecules (e.g., tropoelastin) into spiral filaments. Collagen, more ubiquitous than elastin, is another fibrous protein that forms the structural network of skin.[0004]Ce...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K8/41A61K8/35A61K8/34A61Q19/08A61K8/97
CPCA61K8/347A61K8/35A61Q19/08A61K8/97A61K8/466A61K8/9789A61P17/00A61K31/05A61K36/45
Inventor KAUR, SIMARNASOUTHALL, MICHAELTUCKER-SAMARAS, SAMANTHA
Owner JOHNSON & JOHNSON CONSUMER COPANIES
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