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Medical application of ethane dimethane sulfonate (EDS)

A technology of ethane dimethanesulfonate and medicine, applied in the field of medicine, can solve the problems of narrow treatment range of EDS, limited application of EDS, etc., and achieve the effect of high safety and no systemic side effects

Inactive Publication Date: 2013-10-09
HANGZHOU YIHAIXUAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, EDS applications are limited by the
One of the limitations of EDS application: the range of EDS treatment is relatively narrow, at high doses EDS can not only kill Leydig cells, it also kills other cells

Method used

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  • Medical application of ethane dimethane sulfonate (EDS)
  • Medical application of ethane dimethane sulfonate (EDS)
  • Medical application of ethane dimethane sulfonate (EDS)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: EDS was injected into the testicular artery to kill Leydig cells in rats

[0037] 1. 36 adult SD male rats. Grouped and randomly divided into 6 groups. In the first group, 6 rats were injected with 0.05ml vehicle (DMSO:H2O, 1:4, V / V) into the testicular artery. EDS was dissolved in vehicle, and the second group of 6 rats injected 0.05ml of 0.5mg / kg (mg / kg) EDS into the testicular artery; the third group of 6 rats injected 0.05ml of 2mg / kg EDS into the testicular artery; Four groups of 6 rats were injected with 0.05ml of 5mg / kg EDS into the testicular artery; 6 rats of the fifth group were injected with 0.05ml of 10mg / kg EDS into the testicular artery; 6 rats of the sixth group were injected with 0.05ml of testicular artery 15 mg / kg EDS; one EDS injection.

[0038] 2. After 7 days of intra-arterial injection of EDS, the rats were sacrificed by inhaling carbon dioxide.

[0039] 3. Immunohistochemical staining was performed on one testis of each animal after ...

Embodiment 2

[0044] Example 2: Rat intraperitoneal injection of EDS and testicular intraarterial injection of EDS potency comparison

[0045] 1. The other 36 adult SD male rats. Grouped and randomly divided into 6 groups. In the first group, 6 rats were intraperitoneally injected with 0.5ml vehicle (DMSO:H2O, 1:4, V / V). EDS was dissolved in vehicle, and 6 rats in the second group were injected intraperitoneally with 0.5ml of 10mg / kg EDS; 6 rats in the third group were injected intraperitoneally with 0.5ml of 20mg / kg EDS; 6 rats in the fourth group were injected intraperitoneally 0.5ml of 30mg / kg EDS; 6 rats in the fifth group were injected intraperitoneally with 0.5ml of 50mg / kg EDS; 6 rats in the sixth group were injected intraperitoneally with 0.5ml of 75mg / kg EDS; one EDS injection.

[0046] 2. Seven days after EDS injection, the rats were sacrificed by inhaling carbon dioxide. Blood samples were collected, centrifuged at 500 g, and serum was stored at -20°C for testosterone radioimmu...

Embodiment 3

[0049] Example 3: Comparison of the Sensitivity of EDS to Human and Rat Mesenchymal Cells

[0050] 1. The sensitivity of EDS to kill Leydig cells is species-dependent. For example, rat Leydig cells are sensitive to EDS but mouse Leydig cells are not sensitive (Rommerts F F. et al. 2004. J Endocrinol.181 :169-78). The sensitivity of human Leydig cells to EDS has not been tested. For our comparison the sensitivity of Leydig cells to EDS in human and rat testis.

[0051] 2. We established an in vitro culture system of seminiferous tubules, and human seminiferous tubules were derived from biopsy. Rat seminiferous tubules were taken from 90-day-old SD rats, and mouse seminiferous tubules were taken from 90-day-old C57BL / 6 mice. Human, mouse, and rat Leydig cells on the surface of the seminiferous tubules. We cultured human, mouse and rat seminiferous tubules in vitro according to the literature (Stanley E, et al. Endocrinology. 2012 Oct; 153(10):5002-10), and treated them with ...

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Abstract

The invention relates to medical application of ethane dimethane sulfonate (EDS). EDS can be used for eliminating leydig cells and preparing a medicine for treating and / or preventing leydig cell dependent diseases. When low-dosage EDS is injected into testicular arteries, the concentration of testosterone can achieve and be kept below a castrating level; furthermore, systemic side reaction nearly does not exist; health is not influenced; toxicity is also not generated; EDS is sensitive on human leydig cells and has high safety.

Description

technical field [0001] The present invention relates to the medical use of the compound ethanesulfonate (Ethane Dimethane Sulfonate, EDS), which can eliminate Leydig cells at low doses, and is used to prepare and treat and / or prevent Leydig cells from relying on Leydig cells. A medicine for a disease belongs to the technical field of medicine. Background technique [0002] EDS can specifically eliminate Leydig cells within 1-4 days to reduce the serum testosterone concentration to castration level. Reducing the serum testosterone concentration is an important strategy for the treatment of male prostate cancer. A serum testosterone concentration of less than 0.5 ng / ml was once considered castration level, but now new data suggest that the new castration level for either surgical or chemical castration is a serum testosterone concentration of less than 0.2 ng / ml, thereby maximizing to improve the efficacy of prostate cancer treatment. The acute and chronic effects of testost...

Claims

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Application Information

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IPC IPC(8): A61K31/255A61P35/00A61P15/00
Inventor 葛仁山郭晶晶葛海芳陈冰冰
Owner HANGZHOU YIHAIXUAN BIOTECH
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