Application of cnidium lactone as [alpha]36 estrogen receptor activator

A technology of estrogen receptor and osthole, which is applied in the field of osthole, can solve the problems of significant side effects and abnormal activation of estrogen receptors, and achieve the effect of avoiding side effects and mild effect

Inactive Publication Date: 2017-06-23
LONGHUA HOSPITAL SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
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Problems solved by technology

Therefore, the reduction of estrogen will lead to the abnormal activation of estrogen receptors and exert biological effects, thus causing a series of diseases, including osteoporosis, premature ovarian failure, menopausal syndrome, irregular menstruation, infertility, and intervertebral disc degenerative diseases , bone and joint inflammatory and immune diseases, cardiovascular diseases, senile dementia, tumor bone metastasis, etc., there is clinically available estrogen replacement therapy, but the side effects are significant

Method used

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  • Application of cnidium lactone as [alpha]36 estrogen receptor activator
  • Application of cnidium lactone as [alpha]36 estrogen receptor activator
  • Application of cnidium lactone as [alpha]36 estrogen receptor activator

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Effect test

Embodiment 1

[0018] Osthole is a novel α36 estrogen receptor activator that has a competitive activation effect on estrogen receptors: osthole ( figure 1 ) is a natural product extracted from the traditional Chinese medicine Cnidium Fructus for warming kidney and yang. In the study, a human endometrial cancer cell line (Ishikawa cell line) was first used. After knocking out estrogen receptor β, the cells only expressed α36 estrogen receptor. The cells were intervened with different concentrations of osthole, and after the cells were lysed, the binding of the isotope-labeled ligand to the receptor was detected. It was found that osthole can competitively bind to the α36 estrogen receptor in a dose-dependent manner, and the binding rate of the isotope-labeled ligand to the α36 estrogen receptor gradually decreases with the increase of the concentration of osthole, and is close to that at 1-10 μM. at 100% inhibition. That is, when 0.01 μM osthole intervened the cells, nearly 70% of the α36 ...

Embodiment 2

[0020] Firstly, it was proved by Western Blot that the α36 estrogen receptor was mainly highly expressed in osteoclasts ( image 3 ). The osteoclast differentiation system was used in vitro to verify the biological effect of osthole after competitively binding to α36 estrogen receptor. That is, primary mononuclear-macrophage cells were isolated and cultured, osteoclast formation was induced by RANKL+MCSF, and gradient osthole was given for in vitro culture. It was found that the inhibitory effect of osthole on osteoclasts was enhanced with the increase of concentration 0.01μM osthole has a slight inhibitory effect on osteoclast formation, 0.5μM osthole can inhibit 50% osteoclast formation, and 5-10μM osthole can completely inhibit osteoclast formation. Therefore, it is proved that after osthole competitively binds to the α36 estrogen receptor, it can indeed exert a biological effect and inhibit the formation of osteoclasts ( Figure 4 ). Bone resorption experiments also pro...

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Abstract

The invention discloses an application of cnidium lactone as an [alpha]36 estrogen receptor activator, in particular an application of the cnidium lactone as the [alpha]36 estrogen receptor activator in preparing medicines or health care foods for preventing and treating osteoporosis, premature ovarian failure, climacteric syndrome, irregular menstruation, infertility, degenerative disc disease, bone joint inflammatory and immunological diseases, cardiovascular disease, alzheimer disease or bone metastases from cancer. The invention also discloses the [alpha]36 estrogen receptor activator, and cnidium lactone serves as an active ingredient of the [alpha]36 estrogen receptor activator at a concentration of 0.01-10 [mu]M.

Description

technical field [0001] The present invention relates to a new application of osthole. Background technique [0002] Estrogen receptors are expressed in a variety of cells in the body, distributed in the uterus, vagina, breast, pelvic cavity (ligament and hoof tissue), skin, bladder, urethra, bone and brain and other tissues. Therefore, the reduction of estrogen will lead to the abnormal activation of estrogen receptors and exert biological effects, thus causing a series of diseases, including osteoporosis, premature ovarian failure, menopausal syndrome, irregular menstruation, infertility, and intervertebral disc degenerative diseases , bone and joint inflammatory and immune diseases, cardiovascular diseases, senile dementia, tumor bone metastasis, etc., there is estrogen replacement therapy clinically, but the side effects are significant. Therefore, it is necessary to develop drugs or health foods that can bind to estrogen receptors, exert biological effects, and have a m...

Claims

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Application Information

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IPC IPC(8): A61K31/37A61P19/10A61P15/08A61P15/12A61P15/00A61P19/02A61P19/08A61P37/00A61P9/00A61P25/28A61P35/04A61P5/30A23L33/105
CPCA23V2002/00A61K31/37A23V2200/306A23V2200/308A23V2200/322A23V2200/324A23V2200/326A23V2250/21
Inventor 舒冰王拥军施杞赵东峰王晶唐德志李晨光薛纯纯李晓锋刘书芬赵永见卢盛
Owner LONGHUA HOSPITAL SHANGHAI UNIV OF TRADITIONAL CHINESE MEDICINE
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