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5alpha-reductase urtica open-loop lignan glycoside D inhibitor, preparation method thereof and use thereof

The technology of a reductase inhibitor and a split lignan is applied in the field of extraction of biologically active components of traditional Chinese medicine, can solve problems such as weak action, and achieve the effects of low cost and simple and easy operation.

Inactive Publication Date: 2010-06-02
DALIAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it has been reported abroad that the lignans in nettle have certain anti-BPH activity, but the effect is weak, and the split-ring nettle lignans have a special structure, and their effect is equivalent to that of the positive drug finasteride

Method used

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  • 5alpha-reductase urtica open-loop lignan glycoside D inhibitor, preparation method thereof and use thereof
  • 5alpha-reductase urtica open-loop lignan glycoside D inhibitor, preparation method thereof and use thereof
  • 5alpha-reductase urtica open-loop lignan glycoside D inhibitor, preparation method thereof and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The medicinal material of split-leaf nettle is collected from Aba Prefecture, Sichuan Province. The method steps of preparing nettle split cyclolignan C from Urtica split leaf are as follows:

[0041] (1) After crushing the dried underground part of Urtica schizophyllum, it is reflux extracted with industrial ethanol with a mass concentration of 95%, the ratio of solid to liquid (kg / l)=1:8, the extraction temperature is 90°C, the extraction time is 3h, and the extraction The number of times is 3 times, the extracts are combined, filtered and concentrated under reduced pressure until there is no alcohol smell;

[0042] (2) Suspend 200 g of the ethanol extract with 2 L of hot water, and extract with 2 L of petroleum ether, ethyl acetate, and water-saturated n-butanol successively, each extracting 3 times;

[0043] (3) 30 g of the raffinate aqueous layer extract was separated by D101 macroporous resin (1 kg), eluted with an ethanol-water gradient (water → 30% ethanol → 50...

Embodiment 2

[0047] The 5-alpha reductase inhibitory effect of Urtica schizolignanside D prepared in Example 1 was tested.

[0048] 5-α reductase inhibition experimental steps are as follows:

[0049] (1) Preparation of 5-alpha reductase:

[0050]Three male SD rats, weighing 200 ± 10 g, were provided by the Experimental Animal Center of Dalian Medical University. They were fasted and killed overnight, and the ventral prostate tissue was quickly taken out and cut into pieces on an ice table. mol L -1 , calcium chloride 1.91mmol·L -1 ) was homogenized in a glass homogenizer, centrifuged at 10,000 rpm at low temperature and high speed for 20 min at 4° C., and the supernatant was centrifuged at low temperature and high speed at 16,000 rpm for 30 min to obtain the 5α-reductase extract. The protein content was determined by the lowry method, and the total protein content in the enzyme extract was used to represent the content of the 5α-reductase extract. The extract was stored in a small cent...

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Abstract

The invention discloses an urtica open-loop lignan glycoside D serving as a 5alpha-reductase inhibitor, a preparation method thereof and use thereof. The urtica open-loop lignan glycoside D is prepared by using the underground part of urtica triangularis as a raw material, extracting the raw material with alcohol, mixing an alcohol extract with hot water to obtain a suspension, extracting the extract with petroleum ether, ethyl acetate and water-saturated n-butyl alcohol, separating the extract from a raffinate water layer with macroporous resin, eluting the extract and separating and purifying the extract by silica gel column chromatography. The urtica open-loop lignan glycoside D can obviously inhibit the generation of DHT and has the potential to be used to prevent and treat prostate diseases like finasteride which is a masculine medicament. The open-loop lignan glycoside raw material is pure natural vegetable roots and safe and readily available. The method is simple and easy to operate and avoids introducing toxic materials. The urtica open-loop lignan glycoside D is low in cost, has a remarkable effect in spite of a vegetable source and has a great significance for the researches on and development of anti-benign prostatic hyperplasia medicaments.

Description

technical field [0001] The invention belongs to the extraction field of bioactive components of traditional Chinese medicines, and relates to the preparation of effective plant components from plant nettle schizophyllum by means of a separation method of dissolving, extracting, extracting, centrifuging, absorbing and eluting. As well as potential therapeutic effects on diseases such as the prostate gland. Background technique [0002] Kraus and Wu et al. [1-2] Thirteen lignans were identified from Stinging nettle: (+)-neoliveresin, (-)-cycloisolaricin, isolaricin, pineneol, 3,4- Divanillyltetrahydrofuran, neooleoresin-4-O-β-D-glucoside, 9-acetyl-neoleoresin, 9-acetyl-neoleoresin-4-O-β- D-glucoside, 9,9'-diacetyl-neoleoresin, 9,9'-diacetyl-neoleoresin-4-O-β-D-glucoside, (-)-open Cycloisolaricesin-9-O-β-D-glucoside, (-)-secoisolarixin-4-O-β-D-glucoside, neooliveresin-9-O-β- D-glucoside. Its structural types mainly include neo-oliveresin and its glycosides, split-ring agar...

Claims

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Application Information

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IPC IPC(8): C07H15/26C07H1/08A61K31/7048A61P13/08
Inventor 鞠冠华冯宝民
Owner DALIAN UNIVERSITY
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