Composition, for preventing, remedying or treating female climacteric syndrome, containing loganin or derivative of same as active ingredient

一种活性成分、组合物的技术，应用在有机活性成分、含有效成分的医用配制品、药物组合等方向，能够解决有副作用、效果有限、骨密度降低等问题

Pending Publication Date: 2018-12-21
NINE B CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Regarding treatment, estrogen therapy is used, but side effects have been reported, and there are some cases where bone density continues to decrease and osteoporosis treatment is required
On the other hand, health functional foods such as Baishouwu (cynanchi wilfordii radix) compound extract and pomegranate concentrate or bone-healthy calcium, vitamin D and isoflavones are also used to relieve menopausal symptoms, but their effects are limited

Method used

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  • Composition, for preventing, remedying or treating female climacteric syndrome, containing loganin or derivative of same as active ingredient
  • Composition, for preventing, remedying or treating female climacteric syndrome, containing loganin or derivative of same as active ingredient
  • Composition, for preventing, remedying or treating female climacteric syndrome, containing loganin or derivative of same as active ingredient

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Summary of embodiment 1 menopausal animal model experiment

[0043] The single test compound used in the animal experiments of the present invention was loganin. Loganin is an iridoid glycoside, its name is derived from the family of Loganaceae, and its chemical formula is C 17 h 26 o 10 ( Figure 5 ). Loganin is a naturally occurring single compound that is abundant in nux vomica and Cornus officinalis.

[0044] 10-week-old ovariectomized ddY female mice (OVX mice) were used as an animal model of menopause to evaluate the in vivo efficacy of loganin (ovariectomized after 8 weeks and fed for an additional 2 weeks for recovery). A sham-operated group of mice whose abdomen was incised but not ovariectomized (normal control group) was used as a control group, and an OVX mouse group (in which the ovariectomized mice were given physiological saline alone, negative control group) and SrCl 2 Group of mice (in which a single compound strontium chloride (SrCl 2 ), the con...

Embodiment 2

[0045] Example 2 Effect of Loganin on Improving Blood Estrogen Reduction in Menopausal Female Model

[0046] Typical estrogen menopause symptoms result in a marked drop in female hormones (ie, estrogen and progesterone). The amounts of estradiol (17β-estradiol, E2) and progesterone (both of which are estrogens) in blood were measured by ELISA 12 weeks after loganin was administered to the female climacteric mouse model. In ovariectomized OVX mice, the estrogen estradiol ( Figure 6a ) and progesterone ( Figure 6b ) was significantly reduced. The comparison group SrCl given the non-effective compound 2 Mice did not differ from OVX mice. However, in the loganin-administered group, the decreased levels of estradiol and progesterone in blood were significantly suppressed ( Figure 6a and Figure 6b ). Statistical analysis also showed significance of efficacy (*: P2 There was no significant difference between the group of mice and the group of mice given loganin ( Figure ...

Embodiment 3

[0047] Example 3 Effect of Loganin on Improving the Decreased Expression of Estrogen Receptor α in Uterine Tissue in the Female Climacteric Mouse Model

[0048] Typical estrogen menopause symptoms lead to a marked decrease in estrogen receptors in uterine tissue cells due to a decrease in estrogen. Estrogen receptors are activated by estradiol (17β-estradiol, E2) and have two types, estrogen receptor alpha and estrogen receptor beta. In the uterus, estrogen receptor α plays a more important role than estrogen receptor β, and during menopause, a marked decrease in estrogen receptor α leads to contraction and regression of the uterus. The mRNA expression level of estrogen receptor α gene and the expression level of estrogen receptor α protein were analyzed by immunohistochemistry of uterine sections after loganin was administered to a menopausal mouse model for 12 weeks, followed by uterine excision. When compared with normal sham-operated mice without ovariectomy, estrogen rec...

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Abstract

The present invention relates to a composition, for preventing, remedying or treating female climacteric syndrome, containing loganin, a derivative of same or pharmaceutically acceptable salts of sameas an active ingredient. Loganin, according to the present invention, enables an increase in the estradiol (17beta-estradiol, E2) concentration in the blood of a menopausal mouse model and has showneffects such as: an increase in the estrogen receptor alpha expression in the uterus; remedying of uterine contraction and degeneration; a decrease in the size and accumulation of adipocytes in the abdominal adipose tissues and the liver; and weight loss. Therefore, loganin enables remedying of symptoms in menopausal women such as loss of estrogen, weight gain, and size increase in adipocytes andfat accumulation in the abdominal adipose tissues and the liver. Therefore, loganin and a composition comprising same as an active ingredient, according to the present invention, are expected to be utilized as a pharmaceutical preparation for preventing and remedying climacteric symptoms.

Description

technical field [0001] The present invention relates to a composition for preventing, improving or treating climacteric syndrome in females. The composition contains loganin, its derivatives or a pharmaceutically acceptable salt thereof as an active ingredient. Background technique [0002] Estrogen, a representative hormone that is a symbol of femaleness, is an important female hormone that regulates the lifespan of women through menstruation, pregnancy, and menopause. Estrogen is a well-known female hormone, which is mainly secreted by follicles, corpus luteum and placenta in the ovary, and is a general term for estrone (E1), estradiol (E2) and estriol (E3). Among them, estradiol (E2) shows the strongest activity among estrogens. [0003] Female sex hormones are mainly related to reproductive activities, and their secretion is regulated by the menstrual cycle. These are controlled by follicle stimulating hormone (FSH). When estrogen is secreted, the feedback action redu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A23L33/10
CPCA23L33/10A61K36/56A61K31/7048A61P5/30Y02A50/30A61P15/12A23V2002/00
Inventor 郑善容朴恩国金彣昶金定炫
Owner NINE B CO LTD
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