Application of 11beta-hydroxysteroid dehydrogenase 1 selective inhibitor in preparation of drug for treating polycystic ovarian syndrome

A technology for hydroxysteroid and polycystic ovary, which is applied in the field of 11β-hydroxysteroid dehydrogenase type 1 enzyme selective inhibitor, medicine for the treatment of polycystic ovary syndrome, and preparation of medicine for the treatment of polycystic ovary syndrome, and can solve the problem of polycystic ovary syndrome. The drug effect of cystic ovary syndrome is not good enough to achieve the effect of improving ovarian polycystic lesions, obvious technical effect, and correcting estrous cycle disorder.

Pending Publication Date: 2020-03-17
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide the purposes of the selective inhibitor of 11β-hydroxysteroid dehydrogenase typ...

Method used

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  • Application of 11beta-hydroxysteroid dehydrogenase 1 selective inhibitor in preparation of drug for treating polycystic ovarian syndrome
  • Application of 11beta-hydroxysteroid dehydrogenase 1 selective inhibitor in preparation of drug for treating polycystic ovarian syndrome
  • Application of 11beta-hydroxysteroid dehydrogenase 1 selective inhibitor in preparation of drug for treating polycystic ovarian syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Modeling: 3-week-old female SD rats were divided into three groups: control group, PCOS model group and PCOS+BVT model group. The PCOS model group was subcutaneously injected with DHEA (6mg / 100g body weight) for 21 days. The PCOS+BVT model group received subcutaneous injection of DHEA (6 mg / 100 g body weight) and intragastric administration of 11β-HSD1 selective inhibitor BVT2733 (10 mg / 100 g body weight) for 21 days. Eight days before the end of modeling, vaginal smears were taken every day to observe the estrous cycle to judge whether the modeling was successful or not, and then they were killed.

[0023] Experimental result 1: Compared with the control group, the ovarian cortisol concentration and 11β-HSD1 protein expression level of rats in the PCOS group were significantly increased (pfigure 1 shown. It shows that 11β-HSD1 selective inhibitor can improve the abnormal expression of 11β-HSD1 in PCOS rat ovary.

[0024] Experimental result 2:

[0025] 1) Compared w...

Embodiment 2

[0030] Glucose tolerance test: Fast for 16 hours (17:00-9:00) after successful modeling, and inject glucose (2g / 1000g body weight) intraperitoneally. Blood glucose levels in rats were measured at 0, 15, 30, 60, 90 and 120 minutes after glucose injection.

[0031] Insulin tolerance test: Fast for 4 hours (9:00-13:00) after successful modeling, and inject Lilly Humulin insulin (1U / 1000g body weight) intraperitoneally. Blood glucose levels in rats were measured at 0, 15, 30, 45 and 60 minutes after insulin injection.

[0032] Experimental results:

[0033] 1) Compared with the control group, the rats in the PCOS group had abnormal glucose tolerance and insulin tolerance, and peripheral insulin resistance. The glucose tolerance and insulin tolerance of the rats in the PCOS+BVT model group were significantly improved compared with those in the PCOS group (p figure 2 shown. showed that a selective inhibitor of 11β-HSD1 ameliorates insulin resistance in PCOS rats.

[0034] 2) Com...

Embodiment 3

[0036] 1. Detection of serum steroid hormones: Blood was collected from the abdominal aorta of rats, centrifuged at 3500 rpm, and the upper layer of serum was absorbed for 10 minutes, and stored at -80°C. Rat follicle stimulating hormone (FSH) and luteinizing hormone (LH) were detected by ELISA kit (Nanjing Jiancheng), and testosterone (T) was detected by ELISA kit (R&D).

[0037] 2. Western Blot detection of protein expression: the tissue was lysed on ice with protein lysate (RIPA extracts total cell protein), the protein concentration was determined with a BCA protein quantification kit, and 30 μg of the sample was separated by SDS-PAGE electrophoresis, and then the protein was transferred to PVDF On the membrane, block with 5% skimmed milk-TBST on a shaker at room temperature for 2 hours, apply the primary antibody on a shaker at 4°C overnight, and incubate the secondary antibody at room temperature for 1 hour, and the ECL luminescent agent excites fluorescence. Chemilumine...

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Abstract

The invention provides application of 11beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) inhibitor in preparation of a drug for treating polycystic ovarian syndrome (PCOS). The molecular formula of the 11 beta-HSD1 is as follows: C17H21ClN4O3S2 and the structural formula is shown in the specification. According to the invention, the 11 beta-HSD1 selective inhibitor can inhibit the activity and expression of 11 beta-HSD1 in the ovary part of a PCOS rat and a phenomenon that the concentration of ovarian local cortisol of a PCOS rat is increased is avoided. Meanwhile, with the 11 beta-HSD1 selective inhibitor, the peripheral insulin resistance of the PCOS rat can be improved and ovulation dysfunction such as follicle growth and development and hormone synthesis can be treated. Therefore, the11 beta-HSD1 selective inhibitor has important significance in treating metabolic disorder and reproductive dysfunction of PCOS.

Description

technical field [0001] The invention belongs to the field of biomedicine, and relates to a medicine for treating polycystic ovary syndrome, specifically, the 11β-hydroxysteroid dehydrogenase type 1 selective inhibitor used in the preparation of medicine for treating polycystic ovary syndrome use. Background technique [0002] Polycystic ovary syndrome (PCOS) is the most common reproductive endocrine abnormality and metabolic disorder in women, with an incidence rate of 9% to 18% in women of childbearing age, and is the cause of anovulatory infertility in more than 75% of women. cause of disease. PCOS is characterized by rare ovulation or anovulation, clinical or biochemical hyperandrogenism, and polycystic ovarian changes. The main clinical manifestations are infertility, obesity, and insulin resistance, which affect female fertility and metabolic abnormalities. [0003] Glucocorticoids are mainly secreted by the adrenal glands and have the functions of regulating glucose ...

Claims

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Application Information

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IPC IPC(8): A61K31/63A61P15/00
CPCA61K31/63A61P15/00
Inventor 孙贇
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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