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Use of icariside Ⅱ in the preparation of products for preventing and treating reproductive dysfunction

A technology for icariside and reproductive function, which is applied in the field of application of icariside II in the preparation of products for preventing and treating reproductive dysfunction, and can solve problems such as unclear mechanism of action, limited pharmacological effects, and lack of

Active Publication Date: 2019-08-30
北京东方百奥医药开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is a lack of safe and effective drugs to prevent and treat reproductive dysfunction clinically. Some drug animal experiments have reported that Lycium barbarum polysaccharide can promote testosterone secretion, increase testicular and The quality of the epididymis and the purpose of repairing testicular tissue damage; garlic and onion plant extracts can improve the antioxidant capacity of sperm, improve spermatogenesis and protect the normal structure of sperm by inhibiting lipid peroxidation, repairing sperm antioxidant function; taking fermented papaya, vitamin C. Tablets of vitamin E, lactoferrin, and dextran can protect sperm through anti-oxidation, and can improve the normal sperm rate and sperm motility to a certain extent, but their pharmacological effects are limited, and the mechanism of action is unclear. to be further studied
[0005] Although some Chinese patent medicines are used in the treatment of reproductive dysfunction, it is difficult to study and confirm their pharmacological and pharmacodynamic mechanisms due to their complex components.
Icariside Ⅱ is a metabolite of icariin. There are currently some related animal experimental research reports on the effect of icariin on reproductive dysfunction, but there is no research on the improvement of testicular reproduction by icariin Ⅱ. Dysfunction and its pathological changes, research reports of increased sperm count and / or sperm motility

Method used

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  • Use of icariside Ⅱ in the preparation of products for preventing and treating reproductive dysfunction
  • Use of icariside Ⅱ in the preparation of products for preventing and treating reproductive dysfunction
  • Use of icariside Ⅱ in the preparation of products for preventing and treating reproductive dysfunction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The preparation of embodiment 1 icariin and icariin II

[0050] Refer to Xia Q et al. (2010) literature (Xia Q, Xu D, Huang Z, Liu J, Wang X, Wang X, LiuS. Preparation of icariside II from icariin by enzymatic hydrolysis method. Fitoterapia.2010; 81(5): 437- 442.) to prepare icariin and icariin II.

[0051] Preparation of icariin: extracting with ethanol, purifying with macroporous resin, extracting and separating icariin from Epimedium, and purifying according to the literature method. A large amount of icariin (Icariin, ICA) can be obtained. Its purity was 98.0% by HPLC analysis.

[0052] Preparation of Icariside II:

[0053] In vitro, the icariin in Epimedium was converted into icariside Ⅱ (Icariside Ⅱ, ICA Ⅱ) by glycosidase (β-glucosidase) fermentation, and purified according to the literature method. Utilize HPLC to analyze its purity to be 98.0% (as figure 1 ).

[0054] The prepared icariin and icariin II were used in the following examples.

Embodiment 2

[0055] Example 2 Effect of icariside II on reproductive function

[0056] Intraperitoneal injection of streptozotocin not only damages islet cells to induce diabetes animal models, but also damages testicular seminiferous epithelium to induce reproductive dysfunction animal models. Bose R (2012) found that this model is an effective animal model of testicular reproductive dysfunction (Bose R, Adiga SK, D'Souza F, Salian SR, Uppangala S, Kalthur G, Jain N, Radhakrishnan RA, Bhat N, Krishnamurthy H, Kumar P. Germ cell abnormalities instreptozotocin induced diabetic mice do not correlate with blood glucose level. J Assist Reprod Genet. 2012; 29(12):1405-1413.).

[0057] 24 male Sprague-Dawley rats, 8w old, 200-250 grams. After fasting for 16 hours, intraperitoneal injection of streptozotocin (streptozocin, STZ), 60 mg / kg, to prepare animal models of reproductive dysfunction, 24 rats were randomly divided into 4 groups, normal control group (NC group), STZ group group (STZ group...

Embodiment 3

[0069] Example 3 Effect of Icariside II on the Histopathological Changes of the Testis in a Rat Model of Reproductive Dysfunction

[0070] Get the testicular tissue of embodiment 2 model rats and carry out testicular histopathological detection: prepare bouin's solution by picric acid saturated solution (1.22%) 75ml, formalin 25ml, glacial acetic acid 5ml to fix testicular tissue, the consumption of Bouin's solution is about 10 times that of the tissue, the fixation time is 24h. After the tissue was removed from the bouin solution, it was directly rinsed in 70% alcohol. Routine paraffin embedding, section thickness 5 μm, HE staining. It was observed that the thickness of the seminiferous epithelium of SD rats in the normal control group was 5.0±1.1 layers of cells, but the thickness of the seminiferous epithelium of the STZ group was significantly lower than that of the normal control group (2.7±0.8 layers, p=0.000). Compared with STZ group, the thickness of seminiferous epi...

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Abstract

The present invention relates to uses of icariside II, particularly to uses of icariside II in preparation of products for prevention or treatment of reproduction dysfunction, prevention and / or treatment of abnormal semen quality, prevention and / or treatment of sterility caused by clinical oligospermia, asthenospermia, teratozoospermia or oligospermia-asthenospermia-teratozoospermia triad, or improvement of sperm amount and / or sperm motility.

Description

technical field [0001] The present invention relates to the use of icariside II, in particular to the use of icariside II or a pharmaceutically acceptable salt thereof in the preparation of prevention and / or treatment of reproductive dysfunction, prevention and / or treatment of abnormal semen quality, prevention and treatment of / or treatment of infertility caused by one or more of oligospermia, asthenospermia, teratospermia, or for improving testicular reproductive dysfunction and its pathological changes, increasing sperm count and / or sperm Uses in Active Products. Background technique [0002] The International Health Organization (WHO) defines reproductive dysfunction as a couple who have had regular sex for more than one year without taking contraceptive measures, and the spouse is not pregnant, also known as infertility. The causes of male infertility include semen output disorder, testicular spermatogenesis dysfunction and abnormal semen quality caused by various rea...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61P15/08
Inventor 辛钟成田贞姬辛华
Owner 北京东方百奥医药开发有限公司
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