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EP-4285889-B1 - A COMPOSITION FOR USE IN SUPPRESSING SKIN IRRITATION

EP4285889B1EP 4285889 B1EP4285889 B1EP 4285889B1EP-4285889-B1

Inventors

  • SON, Euidong
  • KIL, Insup
  • CHO, SI YOUNG
  • PARK, WONSEOK
  • HONG, YONG DEOG

Dates

Publication Date
20260506
Application Date
20230130

Claims (7)

  1. A composition comprising a compound represented by a following Chemical Formula 1, a salt thereof, a stereoisomer thereof, a hydrate thereof or a solvate thereof as an active ingredient for use in alleviating skin irritation:
  2. The composition for use according to claim 1, wherein the composition comprises 0.001 % by weight or more to less than 2 % by weight of the active ingredient based on a total weight of the composition.
  3. The composition for use according to any one of claims 1 or 2, wherein the active ingredient is administered to a human body in an amount of 0.1 to 20000 mg/kg/day, optionally, wherein the active ingredient is administered orally or by injection in an amount of 0.1 to 15 mg/kg/day, optionally, wherein the active ingredient is applied to the skin in an amount of 10 to 20000 mg/kg/day.
  4. The composition for use according to any one of claims 1, 2 and 3, wherein the composition relieves the irritation of the skin stimulated by an ultraviolet ray, optionally, wherein the ultraviolet ray is at least one of UVA and UVB, optionally wherein the UVA is irradiated to the skin with an amount of light of 5 J/cm 2 or more to stimulate the skin, optionally wherein the UVB is irradiated to the skin with an amount of light of 9 mJ/cm 2 or more to stimulate the skin
  5. The composition for use according to any one of claims 1 to 4, wherein in a cell of the skin stimulated by the ultraviolet ray, one or more factors of the group consisting of interluekin-1 alpha (IL-1α), interleukin-8 (IL-8), and prostaglandin E2 (PEG2) have an increased expression level, compared to the cell of the skin that is not irradiated with the ultraviolet ray, and the composition is to reduce the expression level of the one or more factors, optionally, wherein the composition reduces the expression level of the one or more factors from the group consisting of the IL-1α, the IL-8, and the PEG2 by 20 % or more, based on the skin stimulated by the ultraviolet ray, or optionally, wherein the cell is a keratinocyte.
  6. The composition for use according to any one of claims 1 to 5, wherein the composition is an external preparation for the skin.
  7. The composition for use according to any one of claims 1 to 6, wherein the composition is formulated in a form of pharmaceutical composition.

Description

BACKGROUND OF THE INVENTION Field of the Invention The present disclosure relates to a composition for use in alleviating skin irritation. Description of the Related Art Skin irritation refers to a dermatologically sensitive reaction to external irritants, allergens, environmental changes, or internal causes of the human body to cause irritation or dermatitis. Generally speaking, skin irritation refers to cases where the skin feels unbearable when applying cosmetics. Here, the unbearable feeling refers to itching, stinging, burning, pulling, etc. subjectively felt in response to a stimulus. Objectively, it could be flaking, redness, rashes, blisters, etc. Recently, it is known that skin irritation is increasing due to wearing a mask in a pandemic situation due to coronavirus infection, rapid temperature change between seasons, and use of cosmetics, and in particular, it is known that skin troubles caused by ultraviolet rays increase. Skin irritation can be exacerbated by excessive UV exposure. Ultraviolet rays are classified into UVA, UVB, and UVC according to their wavelength. Among them, an UVA has a long wavelength of 320 to 400 nm, and when the skin is exposed to the UVA for a long time, the UVA can reach the dermis and cause skin irritation. UVA has a medium wavelength of 290 to 320 nm and can reach the stratum epidermal layer or the epidermis layer, thereby causing irritation to the skin in a short time. In order to alleviate skin irritation increased by the UVA and UVB stimulation, there is a need for a material that reduces the expression of inflammatory factors in skin cells related to skin irritation. Meanwhile, sebum is a secretion from the sebaceous glands in the skin, and plays a role in maintaining moisture in the skin including the scalp and face or preventing the invasion of microorganisms. During puberty, the sebaceous glands in the skin proliferate due to an increase in the amount of testosterone found in both men and female. The proliferation of these sebaceous glands produces sebum, which blocks hair follicles and provides favorable conditions for bacterial growth. Bacteria reside in hair follicles, and even if these bacteria are present on the skin of a person with normal skin condition, there is no problem at all. However, as the hair follicles are clogged and sebum accumulates in the hair follicles, bacteria eat the sebum and grow rapidly, which is the main cause of skin troubles. In particular, the grown bacteria destroy the hair follicle wall, and the detached cells at this time, sebum, and bacteria cause pus and swelling to form acne, and cause many cosmetic problems such as oily skin, makeup deterioration, and enlarged pores. This chemical change in the skin causes healthy weakly acidic skin to become alkalized as the pH balance of oil is broken, eventually leading to deterioration of the skin's own function and causing a vicious cycle in the skin. In order to prevent and alleviate such skin troubles, research on methods of suppressing sebum secretion are being actively conducted. Androgen, a male hormone produced and metabolized in the sebaceous gland, promotes the lipid synthesis pathway by increasing gene expression of transcription factors involved in lipid synthesis. These lipid metabolism-related factors commonly have a transcriptional regulatory region called sterol regulatory element (SRE), and androgens regulate these factors by regulating sterol regulatory element-binding proteins (SREBPs) that bind to SREs. The factors involved in lipid metabolism include fatty acid synthase (FAS), acetyl-CoA carboxylase (ACACA), malic enzyme, ATP-citric lyase, sterol-regulatory element binding protein (SREBP), and the like. Although the discovery of materials that suppress the production of sebum by reducing the expression of these lipid metabolic factors is being actively conducted, studies on materials that have fewer side effects such as skin irritation and can be effectively delivered are required. KR 2003 0015654 A discloses a skin composition for external application contains 0.00001 to 30% by weight of an extract of leaves or fruits of raspberry such as Rubus coreanum, Rubus idaeus and Rubus parvifolius. The composition disclosed in KR 2003 0015654 A inhibits IL-6, IL-8 and PGE2 by substance P and bradykinin, and consequently prevents skin irritation and inflammation. CN 100 389 743 C discloses a composition for external application to the skin containing a component accelerating the formation of heat shock protein, and 3,4,5-trimethoxycinnamic acid thymolester of the formula(1) as a component inhibiting the formation of melanin, as well as a component inhibiting the inflammation caused by ultraviolet rays. SUMMARY OF THE INVENTION In one aspect, the present invention is to provide a composition for use in alleviating skin irritation. In one aspect, the present invention is to alleviate skin irritation due to UV stimulation. In one aspect, the present invention is to alleviate s