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Compounds and compositions for treating polycystic ovary syndrome

A polycystic ovary and compound technology, which is applied in the field of compounds and compositions for the treatment of polycystic ovary syndrome, can solve the problems of large side effects, application restrictions, and restrictions on the selection of drugs for PCOS insulin resistance, and achieve obvious therapeutic effects

Active Publication Date: 2021-06-08
诸城市林家村中心卫生院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Metformin has a significant therapeutic effect on hyperandremia and insulin resistance in PCOS patients, and thiazolidinedione is better than metformin in treating insulin resistance, but these drugs have relatively large side effects (hepatotoxicity, heart failure, etc.), especially It has a certain inducing effect, which leads to certain limitations in its application in PCOS patients.
[0005] It can be seen that since PCOS patients mostly occur in unmarried women, it is necessary to consider the future impact on the patient's pregnancy while treating PCOS, which greatly limits the drug selection of PCOS insulin resistance.

Method used

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  • Compounds and compositions for treating polycystic ovary syndrome
  • Compounds and compositions for treating polycystic ovary syndrome
  • Compounds and compositions for treating polycystic ovary syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Effect of Example 1 Compound on 3T3-L1 Cellular Insulin Resistance Model

[0019] The following compound standard products were purchased from Beijing Laiyao Biotechnology Co., Ltd., and the specific structural formula is as follows:

[0020]

[0021]

[0022] The above-mentioned compounds are all isolated from the plant Epimedium, and the structure has been reported by the prior art, and those skilled in the art can also extract and separate Epimedium according to the relevant literature.

[0023] Model preparation: the cultured 3T3-L1 cells were mixed with 1×10 5 Individuals / ml were inoculated in 6-well plates, and cultured with low-sugar DMEM medium containing 10% FBS. After culturing for 48 hours, induction medium (10% FBS, 1.0umol / L dexamethasone, 0.5mmol / L IBMX , 10ug / L insulin, low-sugar DMEM medium), the medium was changed every 72 hours after induction, and the cells were digested and harvested after 6 days of induction. Wash 3 times with PBS at 1 x 10...

Embodiment 2

[0034] Example 2 Effect of pharmaceutical composition on 3T3-L1 cell insulin resistance model

[0035] On the basis of the above experiments, we continued to investigate the therapeutic effect of compound 1 in combination with a compound (berberine) known in the prior art to treat insulin resistance. The investigation method was the same as in Example 1, and the specific dosage regimen was as follows:

[0036] Administration group 1 was given compound 1 with a final concentration of 5umol / L; administration group 2 was given berberine with a final concentration of 5umol / L; administration group 3 was given compound 1 with a final concentration of 5umol / L and berberine with a final concentration of 5umol / L ; Administration group 4 was given metformin with a final concentration of 10umol / L; the control group and the model group were given the same amount of medium, and relevant measurements were carried out after 48 hours of culture.

[0037] The specific results are as follows:...

Embodiment 3

[0042] Effect of Example 3 compound and pharmaceutical composition on DHEA-induced polycystic ovary syndrome insulin resistance model ring

[0043] Modeling method: 21-day-old female wistar rats were taken, and after being adaptively fed for one week, they were randomly divided into groups of 10 rats. On the day of grouping, except the control group, other groups of rats were injected with 0.2ml (6mg / 100g) of DHEA was injected once a day for 20 consecutive days, and the control group was injected with the same amount of normal saline. After 20 days of injection, the model rats were fasted, and blood was collected 12 hours later to detect fasting blood glucose (glucose meter) and fasting insulin (insulin ELISA kit). According to the calculation method of insulin resistance index, HOMA-IR=fasting blood glucose (mmol / L)×fasting insulin (mU / L) / 22.5. Model rats with HOMA-IR>2.8 were used for subsequent experiments.

[0044] Dosing method: After successful modeling, each drug ...

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Abstract

The invention relates to a compound and composition for treating polycystic ovary syndrome (PCOS), in particular to insulin resistance caused by PCOS, and belongs to the field of medicine. The compound of formula I provided by the present invention has obvious therapeutic effect on treating PCOS insulin resistance. Further, the present invention provides a pharmaceutical composition comprising the compound of formula I.

Description

technical field [0001] The invention relates to a compound and composition for treating polycystic ovary syndrome (PCOS), in particular to insulin resistance caused by PCOS, and belongs to the field of medicine. Background technique [0002] Polycystic ovary syndrome (PCOS), also known as Stein-leventhal syndrome, is a common gynecological endocrine disease characterized by hyperandrogenism, ovulation disorders, and ovarian hyperplasia. Cystic state is a characteristic manifestation, and with the development of the disease, the incidence of long-term complications such as diabetes, endometrial cancer, hypertension, and heart disease increases, which is a major challenge in gynecological clinical practice. Insulin resistance is an important clinical feature of PCOS, and more than 60% of patients have different degrees of insulin resistance. Modern studies have shown that insulin resistance is associated with hyperandremia, follicular development and ovulation disorders, endom...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04C07H17/04A61K31/352A61K31/7048A61K31/4375A61P15/08A61P5/50
CPCA61K31/352A61K31/4375A61K31/7048A61P5/50A61P15/08C07D493/04C07H17/04A61K2300/00
Inventor 王坤芳丁伟王亮德
Owner 诸城市林家村中心卫生院