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Application of icariin or derivatives and compositions thereof to prevention and treatment of kidney diseases

A technology of icariin and derivatives, applied in the field of icariin derivatives or their pharmaceutically acceptable salts, icariin, can solve polycythemia, side effects of drugs, aggravation of sleep apnea syndrome, etc. question

Inactive Publication Date: 2020-02-28
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this therapy may bring many side effects at the same time, such as inducing endometrial cancer, breast cancer, ovarian cancer and other cancers, causing thromboembolic events and cholecystitis, etc., which bring certain risks to the treatment; although testosterone replacement therapy It can bring many benefits to patients with hypogonadism, but in recent years clinicians have paid more and more attention to the possible risks and adverse reactions of long-term treatment to patients, including acne / oily skin, exacerbation of male pattern baldness, gynecomastia, Or aggravate sleep apnea syndrome, promote prostatic hyperplasia, aggravate lower urinary tract symptoms, accelerate the progression of existing prostate cancer, breast cancer and promote the growth of prostate metastatic cancer, inhibit sperm production, cause polycythemia, liver toxicity, lipid metabolism disorders and cardiovascular events
For the curative effect of long-term hormone replacement, the alternative dosage form, dosage, choice of administration method, combined drug use, maintenance time, etc., the results of various studies are also inconsistent, and long-term observation studies with large samples are still needed to solve the problem.
In addition, there is currently no new drug officially approved for the treatment of diabetic nephropathy clinically. Most commonly used clinical drugs have side effects of varying degrees and unclear indications, and sex hormone replacement therapy is even more risky. unknown

Method used

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  • Application of icariin or derivatives and compositions thereof to prevention and treatment of kidney diseases
  • Application of icariin or derivatives and compositions thereof to prevention and treatment of kidney diseases
  • Application of icariin or derivatives and compositions thereof to prevention and treatment of kidney diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1: Effect of icariin on renal function protection of STZ (streptozotocin)-induced type 1 diabetic nephropathy rats

[0076] 1 Experimental materials

[0077] 1.1 Experimental animals

[0078] Male Sprague-Dawley rats, weighing 180-200 g, were provided by the Experimental Animal Center of Zhejiang Province. Animals were kept in separate cages, free to drink water, fed with standard pellet feed, controlled at room temperature of 24±2°C, and relative humidity of 40-70%.

[0079] 1.2 Experimental methods and detection indicators

[0080] Establishment of STZ-induced diabetic rat model and administration regimen

[0081] Healthy male SD rats, 70, weighing 180-200g, were given ordinary standard pellet feed for adaptive feeding at room temperature 24±2°C for 1 week, then randomly selected 10 as normal control group, and the rest were used for modeling. Modeling method: All rats were fasted without food and water for 12 hours. The model group was intraperitoneally i...

Embodiment 2

[0181] Example 2: Study on the protective effect of icariin on renal function in rats with type 2 diabetic nephropathy induced by high sugar and high fat combined with small doses of STZ

[0182] 1 Experimental materials

[0183] 1.1 Experimental animals

[0184] Male Sprague-Dawley rats, weighing 160-180 g, were provided by the Experimental Animal Center of Zhejiang Province. Animals were kept in separate cages, free to drink water, fed with standard pellet feed, controlled at room temperature of 24±2°C, and relative humidity of 40-70%.

[0185] 2 Experimental methods and detection indicators

[0186] 2.1 Establishment of high-sugar and high-fat diet plus low-dose STZ-induced type 2 diabetes rat model and dosing regimen

[0187]Healthy male SD rats were fed with common standard pellet feed for 1 week and then randomly selected as normal control group, and the rest were used for modeling. Modeling method: After the adaptive feeding, the model rats were fed with high-sugar ...

Embodiment 3

[0286] Example 3: Effect of icariin on expression of type IV collagen and fibronectin induced by high glucose in mesangial cells

[0287] 1 Experimental materials

[0288] Improved RPMI-1640 medium: HyClone (Thermo Scientific) product;

[0289] 0.25% trypsin solution: HyClone (Thermo Scientific) product;

[0290] Fetal bovine serum: HyClone (Thermo Scientific) product;

[0291] Penicillin-streptomycin 100X solution: HyClone (Thermo Scientific) product;

[0292] Dimethyl sulfoxide (DMSO): Nanjing Shengxing Biotechnology Co., Ltd.;

[0293] Type IV collagenase: Gibco;

[0294] Icariin (98% HPLC): Nanjing Zelang Pharmaceutical Technology Co., Ltd.;

[0295] Fulvestrant Fulvestrant: Sigma-Aldrich product;

[0296] G-15: Tocris products;

[0297] U0126: Cell Signaling products;

[0298] Recombinant Transforming Growth Factor-β1 (TGF-β1): R&D Systems product;

[0299] RIPA lysate: Biyuntian Institute of Biotechnology;

[0300] Cocktail protease inhibitor: Sigma-Aldrich pro...

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Abstract

The invention discloses application of icariin, icariin derivatives or pharmaceutically-acceptable salts of icariin to preparation of products for prevention and / or treatment of kidney diseases, particularly to preparation of products for treatment of diabetic nephropathy, renal impairment, renal fibrosis, kidney inflammation and glomerular hypertrophy.

Description

technical field [0001] The present invention relates to the use of icariin, icariin derivatives or pharmaceutically acceptable salts thereof, in particular to the use of icariin, icariin derivatives or pharmaceutically acceptable salts thereof in the prevention and treatment of kidney diseases the use of. Background technique [0002] Diabetes mellitus (DM) is a chronic, systemic metabolic disease characterized by hyperglycemia caused by insulin secretion defects and (or) biological action disorders. Diabetic Nephropathy (Diabetic Nephropathy, DN) refers to glomerulosclerosis caused by diabetic microangiopathy, also known as diabetic glomerulosclerosis. According to epidemiological statistical research, it is estimated that by 2030, the number of diabetic patients worldwide will reach 366 million, while the number of diabetic nephropathy patients will exceed 100 million. The prevalence of diabetes is on the rise. Among many diabetic patients, about 35% to 40% develop diabe...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K45/06A61K31/565A61P13/12A61P3/10
CPCA61K31/565A61K31/7048A61K45/06A61P3/10A61P13/12A61K2300/00
Inventor 丁选胜王凯吴正红
Owner CHINA PHARM UNIV
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