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Application of mangiferin aglycone and its derivatives in the preparation of antiprostatic hyperplasia drugs

A prostatic hyperplasia and drug technology, applied in the field of medicine, can solve problems such as quality control difficulties, unknown material basis and active ingredients of Chinese patent medicine preparations, adverse reactions of chemical drugs, etc.

Active Publication Date: 2017-04-19
KPC PHARM INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Whether it is symptomatic, corrective or combined treatment, it can restore the urinary function of patients with benign prostatic hyperplasia to varying degrees and improve their quality of life. However, long-term use of chemical drugs has obvious adverse reactions. The status quo of unclear targets, difficult quality control, and difficult guarantee of curative effect
At present, there is no report on the obvious inhibitory effect of natural medicine on 5α-reductase and its application in anti-prostatic hyperplasia

Method used

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  • Application of mangiferin aglycone and its derivatives in the preparation of antiprostatic hyperplasia drugs
  • Application of mangiferin aglycone and its derivatives in the preparation of antiprostatic hyperplasia drugs
  • Application of mangiferin aglycone and its derivatives in the preparation of antiprostatic hyperplasia drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Inhibition of 5α-reductase in vitro

[0033] 1. Experimental materials

[0034] SD female mice, Kunming Medical University; Testosterone, Shanghai Yuanye Biotechnology Co., Ltd. (20130409); NADPH, sigma company (Lot SLBC6718V); Finasteride, Hubei Subang Pharmaceutical Co., Ltd. (20121001); Tris-base, BIOSHARP Company (Amresco0497); Sodium Chloride, Sangon Biological Company (Lot3004B220); DTT, Sigma Company (LotBCBK8875V); Absolute Ethanol, Yunnan Shandian Pharmaceutical Co., Ltd. (Lot LN70N21); Dichloromethane, Tianjin Windboat Chemical Reagent Technology Co., Ltd. (20100926); Chromatographic methanol, Beijing Bailingwei Technology Co., Ltd. (116481); Mangiferin; 1-hydroxy-3,6,7-triacetoxymangiferin; 3-hydroxy-1,6 , 7-triacetoxymangiferin; 1,3-dihydroxy-6,7-diacetoxymangiferin; 6,7-dihydroxy-1,3-diacetoxymangiferin, purity All are greater than 98%, provided by Kunming Pharmaceutical Group Drug Research Institute.

[0035] 2. Experimental equipment

[003...

Embodiment 2

[0057] Example 2: Investigation of the In Vivo Pharmacological Effects of Testosterone Propionate Replication Prostatic Hyperplasia Model Mice

[0058] 1. Test material

[0059] 1.1 Animals

[0060] SPF-grade male ICR mice, weighing 20-22 g, were provided by the Animal Department of Kunming Pharmaceutical Group Co., Ltd., license number SCXK (Dian).

[0061] 1.2 Test substance

[0062] Mangiferin, light yellow powder, purity >98%, provided by Kunming Pharmaceutical Group Research Institute, batch number 20130903; Finasteride Tablets (Guoyao Zhunzi H20070146), 5mg / tablet, Hubei Subang Pharmaceutical Co., Ltd., batch number: 0121001 ; Longbishu Capsules (Z10960007), 0.3g / capsule, Shijiazhuang Kedi Pharmaceutical Co., Ltd., batch number: 111113; use pure water to make suspensions of different concentrations for later use.

[0063] 1.3 Reagents

[0064] Testosterone Propionate Injection (Guoyao Zhunzi H12020531), 10mg / mL, Tianjin Jinyao Amino Acid Co., Ltd., batch number 12020...

Embodiment 3

[0099] Example 3: Acute Toxicity Test by Oral Gavage in Mice

[0100] Preliminary test shows that LD cannot be detected by oral administration of mangiferin in mice 50 , so the acute toxicity of the test substance is reflected by the maximum dose administered twice a day. During the test, after the animals were fasted and given water for 8 hours, 40 animals weighing 19.5 to 21.9 g, half male and half male, were randomly divided into a treatment group and a control group according to sex and body weight, with 10 male and 10 males in each group. The mice in the treatment group were given 0.27g / mL mangiferin paste by oral gavage at the maximum capacity of 40mL / kg, and then administered again after an interval of 6h. The equivalent dose was 21.6g / kg.d, and the control group was given the same volume of pure water. As a result, there were no obvious toxic reactions in the appearance, behavior, mental state, appetite, urine and stool, fur, skin color and breathing of the two group...

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Abstract

The invention belongs to the field of medicines, and discloses novel application of a mango aglycone derivative. An in-vitro test shows that the mango aglycone derivative can obviously inhibit activity of 5 alpha-reductase, can remarkably lower prostate wet weight index of a testosterone propionate replication prostate hyperplasia model mouse, can lower a ratio of E2 / T in blood serum, and can lower activity of the 5 alpha-reductase in a liver tissue, so that the mango aglycone derivative is indicated to have effect in inhibiting activity of 5 alpha-reductase, can be used for treating 5 alpha-reductase expression or superhigh-activity-associated diseases, for example testosterone propionate; moreover, the mouse stomach is filled with the drug in maximum administration dosage of 21.6g / kg, and therefore, the drug has very good clinical application prospect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of mangiferin and its derivatives in the preparation of anti-prostatic hyperplasia drugs. Background technique [0002] Benign prostatic hyperplasia (BPH) is a common disease in middle-aged and elderly men characterized by progressive urinary frequency and dysuria due to the obvious enlargement of the prostate gland. Epidemiological studies have shown that the incidence of benign prostatic hyperplasia is very low before the age of 40, accounts for 40% at the age of 50, and is close to 90% after the age of 80. By the age of 90, almost 100% of prostate hyperplasia will be found if the histological examination of the prostate is performed. With the aging of my country's population, its incidence is on the rise in recent years. [0003] The treatment of BPH is mainly divided into surgery and drug therapy. Surgical resection was once considered to be the first choic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61P13/08A61P35/00A61P17/00A61P17/10A61P17/14
Inventor 刘一丹齐美凤王萍宋立明李小英张建文张伟尚建华其他发明人请求不公开姓名
Owner KPC PHARM INC
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