Ah receptor antagonists

A preparation and filter technology, applied in the field of aromatic hydrocarbon receptors (Ah receptors, can solve problems such as enhancement

Active Publication Date: 2009-06-24
SYMRISE GMBH & CO KG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

All-trans retinoic acid also has obvious disadvantages: enhanced TCDD-induced MMP-1 expression (Murphy et al. (2004) J. Biol. Chem. 279, 25284-25293) and photostability

Method used

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  • Ah receptor antagonists
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Examples

Experimental program
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Effect test

Embodiment 6

[0363] Embodiment 6 (decolorization)

[0364] B16V mouse melanoma cells were divided into 5×10 3 Cells / well were seeded into 96-well microtiter plates. at 37°C and 5% CO 2 After 24 hours of incubation in RPMI matrix enhanced with 10% fetal bovine serum, different concentrations of test substances, 0.3 mM tyrosine and 10 nM α-MSH (α-melanocyte stimulating hormone) were added and incubation was continued for 96 hours. Standards were incubated with kojic acid at concentrations of 0.01 mM, 0.1 mM and 1 mM with tyrosine and α-MSH. Only tyrosine and α-MSH were added to the control. After incubation, sodium lauryl sulfate and sodium hydroxide solutions (final concentrations of 1 mM and 1 M, respectively) were added to the medium, and the absorbance (A) was measured at 400 nm after 3 hours.

[0365] Staining inhibition in the presence of test compound or kojic acid was calculated using the following equation:

[0366] Coloring inhibition (%)=100-[(A 试验化合物 / A 对照 )×100]

[036...

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PUM

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Abstract

The invention relates to the field of aryl hydrocarbon receptor (Ah receptor; AhR) antagonists and their uses.

Description

technical field [0001] The present invention relates to the field of aryl hydrocarbon receptor (Ah receptor; AhR) antagonists and uses thereof. Background technique [0002] The skin is the largest organ of the human body. Its most important function is to prevent the uncontrollable loss of water from the body on the one hand, and the intrusion of harmful chemicals or bacteria and solar radiation on the other. [0003] Prolonged exposure of human skin to solar radiation can cause various damages. Examples that may be mentioned here are sun damage, photoaging of the skin and skin cancer. This detrimental effect of sunlight is due in particular to the UVB radiation (280 to 320 nm) contained in the sunlight spectrum. Especially since the recent ongoing ozone depletion has greatly increased the intensity of the UVB component of the sunlight spectrum, it is imperative to protect the skin from UVB radiation as comprehensively as possible. [0004] In order to form a protective...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K8/35C07C49/755A61P17/00A61P17/16A61P35/00
CPCA61Q19/004A61K31/122A61Q19/00A61K8/046A61K8/35A61Q17/04A61Q19/08A61Q5/02A61Q5/12A61P17/00A61P17/16A61P35/00
Inventor 马丁纳·赫尔曼奥斯卡·科吉加布里埃莱·菲尔哈伯让·克鲁特曼
Owner SYMRISE GMBH & CO KG
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