WO2015022830A1 - Composition pour favoriser la sécrétion d'œstrogène, composition aromatique et outil d'arôme - Google Patents

Composition pour favoriser la sécrétion d'œstrogène, composition aromatique et outil d'arôme Download PDF

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Publication number
WO2015022830A1
WO2015022830A1 PCT/JP2014/068675 JP2014068675W WO2015022830A1 WO 2015022830 A1 WO2015022830 A1 WO 2015022830A1 JP 2014068675 W JP2014068675 W JP 2014068675W WO 2015022830 A1 WO2015022830 A1 WO 2015022830A1
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Prior art keywords
estrogen
cineole
composition
secretion
estrogen secretion
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PCT/JP2014/068675
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English (en)
Japanese (ja)
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一之 篠原
裕和 土居
正太 西谷
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株式会社 マザー＆チャイルド
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q13/00—Formulations or additives for perfume preparations

Definitions

  • the present invention relates to an estrogen secretion enhancing composition, an estrogen secretion aroma composition, and an estrogen secretion aroma device containing 1,8-cineole as an active ingredient.
  • Estrogen secretion during pregnancy is tens of times that of women who are not pregnant. Estrogen secretion levels, which have been elevated for almost 9 months, decrease rapidly within hours after delivery and fall to the point where they cannot be measured on day 7. Maternity blue occurs in about 80% of women at this time. Maternity blue, like premenstrual tension, presents unspecified complaints specific to women. Symptoms usually begin 3-5 days after delivery and disappear within 2 weeks. In addition, postpartum depression may occur due to decreased postpartum hormone secretion.
  • Estrogen secretion levels change throughout life. It begins to rise in puberty and reaches its peak in the 20s. Later, ovarian function gradually declined, estrogen decreased, and menopause. Menopause usually occurs between the ages of 45 and 55 and may be early or late. Menopause is seen in 60-70% of women at this time. Symptoms of menopause are mainly women's unspecified complaints similar to premenstrual tension or maternity blue.
  • Patent Document 1 discloses amplet seed oil as a fragrance composition as a secretion promoter for 17 ⁇ -estradiol, which is a main component of estrogen (a group of female hormones). The use of an amblet lid is disclosed.
  • Patent Document 2 discloses the use of an extract of fungal Cordyceps as a treatment for female hormone deficiency.
  • Patent Document 3 is based on the present inventors, and discloses the effect of aroma component of ⁇ -caryophyllene on women.
  • Non-Patent Documents 1 to 3 show that the presentation of odor changes the secretion frequency of luteinizing hormone (LH) controlled by the hypothalamus, and conventional aromatherapy and the like are oral, intravenous, and transdermal.
  • LH luteinizing hormone
  • the possibility of changing hypothalamic function only through the action via the olfactory nerve was shown.
  • estrogen secretion is caused by the secretion of LH
  • LH secretion is caused by the activity of the hypothalamus. Therefore, the effect of increasing the activity of the hypothalamus is considered to cause the increase of estrogen secretion. .
  • estrogen secretion which is 1,8-cineole and the female hormone.
  • Estrogens have been shown to have the following anti-aging effects (or disease risk reduction effects associated with reduced estrogen in menopause and menopausal women).
  • ⁇ Promoting the production of collagen (beautifying skin effect, preventing firmness / shininess)
  • Promoting absorption of calcium into bone reducing risk of osteoporosis
  • Promoting hair renewal (promoting hair growth)
  • Increased basic metabolism prevention of apple-type obesity
  • Cognitive enhancement reducing dementia risk
  • Promoting vasodilation reducing the risk of arteriosclerosis
  • Immune function enhancement reducing risk of autoimmune diseases such as collagen disease and rheumatism
  • Promoting the development of the mammary gland (beauty effect by maintaining the elasticity and elasticity of the breast)
  • Increased good cholesterol (HDL) (reduced risk of arteriosclerosis)
  • the route of action is not limited to the route through the olfactory nerve, but also includes the oral, intravenous, and transdermal routes.
  • the limbic system which is the center of emotion
  • hypothalamus which is the center of instinct (feeding, sleep) hormone
  • An object of the present invention is to provide a composition for enhancing estrogen secretion and the method for enhancing secretion.
  • the present inventors have found that the odor of 1,8-cineole particularly enhances estrogen secretion in late-luteal females.
  • the present invention has been completed based on the above findings, and is an estrogen secretion enhancing composition containing 1,8-cineole as an active ingredient, its fragrance composition, and its fragrance tool.
  • the first aspect of the present invention is the invention according to claim 1, wherein estrogen secretion containing 1,8-cineole synthesized or purified from natural product as an active ingredient is synthesized. It is a composition for enhancing estrogen secretion, characterized by enhancing.
  • the invention of claim 2 is the composition for enhancing estrogen secretion according to claim 1, wherein the estrogen is 17 ⁇ -estradiol.
  • the invention of claim 3 is the composition for enhancing estrogen secretion according to claim 1 or 2, wherein the administration means of the composition is administered so as to be transmitted to the brain via the olfactory nerve by a fragrance, essential oil, or cosmetics. It is characterized by that.
  • the invention of claim 4 is characterized in that, in the composition for enhancing estrogen secretion according to claim 3, the administration means of the composition is administered so as to be transmitted to the brain via the olfactory nerve by food and drink.
  • the invention according to claim 5, which is the second aspect of the present invention comprises synthesized 1,8-cineol or 1,8-cineole isolated and purified from a natural product as an active ingredient to inhibit estrogen secretion.
  • An estrogen-secreting fragrance composition characterized in that it is enhanced.
  • the invention of claim 6 is the estrogen secretion fragrance composition of claim 5, wherein the estrogen is 17 ⁇ -estradiol.
  • the invention according to claim 7, which is the third aspect of the present invention, comprises 1,8-cineole synthesized or 1,8-cineole isolated and purified from a natural product as an active ingredient to inhibit estrogen secretion. It is an estrogen fragrance tool characterized by improving it.
  • the invention of claim 8 is the estrogen-secreting fragrance device according to claim 7, wherein the estrogen is 17 ⁇ -estradiol.
  • Estrogen secretion enhancing composition, estrogen secretion fragrance composition, and estrogen fragrance composition containing 1,8-cineole isolated and purified from the synthesized 1,8-cineol or natural product of the present invention as an active ingredient Can be used to enhance estrogen secretion, and in particular, estrogen secretion can be further enhanced in the late corpus luteum. For this reason, estrogen is effective in alleviating female-specific indefinite complaints (including illness) such as premenstrual tension, menstrual symptoms, maternity blue, postpartum depression, and menopause, which are caused by decreased estrogen secretion in women. Anti-aging effect due to increased secretion can be expected.
  • composition of the present invention can be administered by a method via the olfactory nerve, it can exert its effect in a short time, and since it does not involve blood, it has the advantage of having no side effects on organs such as the liver and kidney. There is also.
  • 1,8-cineole is particularly estrogen in a woman in the late luteal phase (in the late luteal phase, estrogen decreases and premenstrual tension develops). We found an action to enhance secretion.
  • This 1,8-cineole is a naturally occurring organic compound called eucalyptol (also synthesizable), which is a kind of monoterpenoid with a cyclic ether structure, and is 1,8-cineole. It is also called limonene oxide and cajeptol, and has a fragrance and taste that makes it suitable for food additives, fragrances, and cosmetics, and has the following structural formula.
  • 1,8-cineole has the effect of promoting estrogen secretion in late luteinous women, but has come up with the idea that it can be used for the following novel uses.
  • 1,8-cineole can be presumed to be effective in improving discomfort caused by decreased estrogen secretion in women in the late corpus luteum (including menstrual periods) and in women after childbirth . Discomfort caused by decreased estrogen secretion is seen not only in women in the late corpus luteum (including menstrual periods), but also in women after childbirth and women in menopause. It can be assumed that 1,8-cineole is effective. Moreover, it can be estimated that the above-mentioned anti-aging effect is obtained.
  • composition for enhancing estrogen secretion contains 1,8-cineole as an active ingredient.
  • the 1,8-cineole to be used may be extracted from natural products (for example, tea tree, peppermint, eucalyptus, rosemary, etc.) or may be artificially synthesized.
  • 1,8-cineole is already sold as a reagent and may be used.
  • the composition for enhancing estrogen secretion of the present invention is prepared in various compositions depending on the use mode, and is usually prepared in the same composition as the estrogen secreting fragrance composition described later.
  • the estrogen-secreting fragrance composition of the present invention is prepared in various compositions depending on the use mode, but usually the 1,8-cineole concentration is 0.3 to 3.75%, preferably 1.5. %
  • a suitable solvent such as dipropylene glycol, propylene glycol, butylene glycol, mineral oil, triethyl citrate, ethanol, benzyl benzoate.
  • the aroma is inhaled as an aromatic bath using an aroma pot or a diffuser.
  • other components can be added and used as cosmetics (skin care products, perfumes, etc.), bathing agents, fragrances, sprays, massage oils, shampoos, laundry detergents and the like.
  • Estrogen secretion fragrance tool has a portion containing synthesized 1,8-cineole or 1,8-cineole isolated and purified from natural products.
  • the 1,8-cineole to be used is synthesized or isolated from a natural product and purified in the same manner as the fragrance composition.
  • the food is usually smelled before it is put into the mouth or during mastication. Therefore, 1,8-cineole can exert its effect even in the form of food or beverage, and 1,8-cineole can also be used as a food or drink for improving indefinite complaint symptoms of women.
  • the types of food and drink are not limited, and examples include flavor tea, flavor coffee, flavor beer, rice cake, gum, breath care, seasoning and the like.
  • the food of the present invention is produced by adding a process of adding 1,8-cineole to the normal food production process, and the content of 1,8-cineole in the food depends on the type of food. Normally, the appropriate amount is about 0.3-3.75%.
  • the fragrance device may be any device or tool used for fragrance, sanitary products, paper, textile products (underwear, stocking, etc.), patch medicine, soap, candle, pillow, futon, Etc. can be illustrated.
  • the fragrance tool of the present invention can be produced in the same manner as a general fragrance tool, except that 1,8-cineole is used instead of plant essential oil.
  • the use target and the administration method of the composition for enhancing estrogen secretion of the present invention are characterized in that 1,8-cineole is administered to a person who shows a decrease in estrogen. It is.
  • the administration method of 1,8-cineole is not particularly limited, and it may be administered orally, intravenously, or transdermally in the same manner as ordinary pharmaceuticals, etc., but preferably stimulated by 1,8-cineole. It is administered by a means that is transmitted to the brain via the olfactory nerve.
  • a means for allowing a person who shows a decrease in estrogen secretion to air containing 1,8-cineole can be exemplified.
  • the amount of 1,8-cineole in the air at this time cannot be measured strictly, but the content of 1,8-cineole used in the solution that emits a fragrance is, for example, when propylene glycol is used as a solvent. Is preferably in the range of 0.3 to 3.75%, more preferably about 1.5%.
  • Example 1 We examined hormonal changes that occurred when 1,8-cineole was sniffed in non-smoking women in their twenties who were healthy and mentally healthy who returned to the normal menstrual cycle (26th to 34th).
  • the enzyme immunoassay used above was a salivary component quantification kit (measurement kit) manufactured by SALIMETRICS, whose model number was 1-3702 Estradiol, EIA Kit, High Sensitivity, Salivary, and the measurement method was (A ) “A saliva sample containing an unknown concentration of 17 ⁇ -estradiol” is reacted with an antibody that binds to it (coated on a hole in a plastic plate called a 96-well plate). The known concentration of 17 ⁇ estradiol ” was also reacted at the same time, and a competitive reaction was carried out between (A) and (B) (antibodies were exchanged between (A) and (B)).
  • “Horseradish peroxidase” which is an enzyme used in the enzyme immunoassay has the following physical properties. Peroxidase (Hydrogen peroxidase, Horseradish peroxidase, HRP) Reaction Chromogenic substrate + H 2 O 2 Oxidized dye + 2H 2 O Origin Horseradish Molecular weight, 40,000, optimum pH: pH 6.5 Substrate specificity There is no specificity for chromogenic substrates (hydrogen donors).
  • Example 1 A comparative experiment was conducted using 1.5% of 1,8-cineole dissolved in propylene glycol and Comparative Example 1: only propylene glycol (PG) as a control.
  • the test subjects are 11 persons in total of 6 persons in the follicular phase and 5 persons in the late luteal phase (Late Luteal Phase), and the experimental results of Comparative Example 1 and Example 1 are shown.
  • Example 1 The comparison results of Example 1 and Comparative Example 1 before and after the experiment showed that the concentration of 17 ⁇ estradiol (E2) secreted in Example 1 was significantly increased from 3.1 pg / ml to 3.4 pg / ml ( In contrast to the paired t-test, P ⁇ 0.05), Comparative Example 1 showed no difference in concentration from 3.0 pg / ml to 3.0 pg / ml. When these changes (after sniffing-before sniffing) were compared (PG vs 1,8-Cineole), the concentration of 17 ⁇ estradiol (E2) was significantly increased compared to propylene glycol (PG) in the control (corresponding to A t test, P ⁇ 0.05).
  • PG propylene glycol
  • ANT attention network task
  • the subject's task is to answer the direction of the center arrow among the five arrows as quickly and accurately as possible using the numeric keypad buttons (RT: reaction time).
  • the central arrow is called a target stimulus, and the other four arrows are called distractor stimuli.
  • a total of four cue stimulus conditions are presented.
  • the cue stimulus is not displayed.
  • a cue stimulus is presented at the position of the gazing point, that is, at the center of the screen.
  • the cue stimulus is presented at the position where the target stimulus is presented. That is, when the arrow is presented above the gazing point, the cue stimulus is also presented above the gazing point.
  • a cue stimulus is presented at a position symmetrical to the target stimulus with respect to a horizontal line crossing the center of the screen. That is, when the target stimulus is presented above the gazing point, the cue stimulus is presented at a position opposite to the target stimulus across the gazing point.
  • the Unconscious Dot Probe task is a cognitive task by PC operation, and the change in the index that seems to reflect the libido before and after smelling 1,8-cineole (1.5%) and the case of PG (control)
  • the comparison was performed on six subjects in the late luteal phase.
  • the Unconscious Dot Probe task is a verification tool developed to assess human attention bias. In the experiment in this example, a male nude image was used as the visual stimulus used for the task, and how much attention (bias) to the image is considered as an index reflecting sexual desire was measured. However, the stimulus image presentation time was 17 ms (below the perceptible threshold), and the measurement was performed using the Dot Probe task under the threshold (Uncoscious).
  • PANAS The Positive and Negative Affect Schedule
  • PANAS is a test that answers emotional question items from two scales of “positive emotion” and “negative emotion”.
  • the results of these experiments are the graphs of FIG. 5, and before and after sniffing 1,8-cineole of the example of the present invention, positive emotions increased and negative emotions decreased compared to control (PG).
  • STAI Staize and Trait Anxiety Inventry
  • STAI is a test that answers questions about anxiety status and characteristics from two scales of “state anxiety” and “characteristic anxiety”. Explaining these experimental results with the graph of FIG. 14, before and after sniffing 1,8-cineole, state anxiety decreased compared to control (PG). As can be seen from the results of each of these tests, anxiety can be reduced.
  • a composition for enhancing estrogen secretion containing 1,8-cineole synthesized or isolated from natural products and purified as an active ingredient.
  • the estrogen secretion fragrance composition and the estrogen fragrance device can be used on women to enhance estrogen secretion. For this reason, the effects of alleviating women-specific indefinite complaints (including illness) such as premenstrual tension, menstrual symptoms, maternity blue, postpartum depression, and menopause, which are associated with decreased estrogen secretion, increased estrogen secretion, especially The anti-aging effect can be expected due to the enhanced estrogen secretion in the late corpus luteum.
  • composition of the present invention can be administered by a method via the olfactory nerve, it can exert its effect in a short time, and since it does not involve blood, it has the advantage of having no side effects on organs such as the liver and kidney. There is also.

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Abstract

La présente invention vise à fournir une composition qui est conçue pour favoriser la sécrétion d'œstrogène et qui peut favoriser la sécrétion d'œstrogène; une composition aromatique de sécrétion d'œstrogène; et un outil d'arôme d'œstrogène. Selon l'invention, au moyen d'un procédé induit par le nerf olfactif, la composition pour favoriser la sécrétion d'œstrogène favorise la sécrétion d'œstrogène et contient, comme principe actif, 1,8-cinéole synthétique ou 1,8-cinéole qui a été isolé et purifié à partir d'un produit naturel.
PCT/JP2014/068675 2013-08-10 2014-07-14 Composition pour favoriser la sécrétion d'œstrogène, composition aromatique et outil d'arôme WO2015022830A1 (fr)

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JP2013167197A JP5923468B2 (ja) 2013-08-10 2013-08-10 エストロジェン分泌増進用組成物、及びその芳香組成物、並びにその芳香用具。
JP2013-167197 2013-08-10

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Cited By (1)

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JP2015036367A (ja) * 2013-08-10 2015-02-23 株式会社マザー＆チャイルド エストロジェン分泌増進用組成物、及びその芳香組成物、並びにその芳香用具。

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JP2018104378A (ja) * 2016-12-27 2018-07-05 株式会社マザー＆チャイルド 女性月経周期における各月経ステージに対応する集中力向上・衝動性低下の作用を有する芳香用組成物。

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JP5923468B2 (ja) * 2013-08-10 2016-05-24 株式会社マザー＆チャイルド エストロジェン分泌増進用組成物、及びその芳香組成物、並びにその芳香用具。

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WO2011152007A1 (fr) * 2010-05-31 2011-12-08 株式会社資生堂 Neurodépresseur sympathique, agent de réduction de la température de la peau, et composition cosmétique, produit alimentaire, et article divers contenant ledit neurodépresseur ou ledit agent

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PERRY NS ET AL.: "In-vitro activity of S. lavandulaefolia ( Spanish sage) relevant to treatment of Alzheimer's disease.", J PHARM PHARMACOL, vol. 53, no. 10, 2001, pages 1347 - 56, XP009027602, DOI: doi:10.1211/0022357011777846 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015036367A (ja) * 2013-08-10 2015-02-23 株式会社マザー＆チャイルド エストロジェン分泌増進用組成物、及びその芳香組成物、並びにその芳香用具。

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