Application of tetrahydroxanthone dimer compound to preparing alpha1-AR adrenergic receptor antagonist medicine

A technology of xanthone dimers, receptor antagonists, applied in the field of new uses of known compounds

Active Publication Date: 2015-10-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Tetrahydroxanthone dimer compounds dicerandrol A, dicerandrol B and deacetylphomoxanthone B were isolated from secondary ...

Method used

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  • Application of tetrahydroxanthone dimer compound to preparing alpha1-AR adrenergic receptor antagonist medicine
  • Application of tetrahydroxanthone dimer compound to preparing alpha1-AR adrenergic receptor antagonist medicine
  • Application of tetrahydroxanthone dimer compound to preparing alpha1-AR adrenergic receptor antagonist medicine

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Experimental program
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Embodiment 1

[0017] The tetrahydroxanthone dimer compound phomoxanthones of the present invention can be extracted and isolated from the fermentation and culture cells of the endophytic fungus Phomopsis sp.HNY29-2B of South China Sea mangrove, and its structure is shown in formula (I).

[0018]

[0019] The separation method of the above-mentioned tetrahydroxanthone dimer compound comprises the following steps:

[0020] S1. Seed culture of the fungus Phomopsis sp.HNY29-2B (the depository unit of the marine fungus Phomopsis sp.HNY29-2B is the China Center for Type Culture Collection CCTCC, the preservation number is CCTCC NO: M 2014395, and the preservation date is September 2014 On the 3rd, the preservation address is: China. Wuhan. Wuhan University; the classification is named Phomopsis HNY29-2B Phomopsis sp.HNY29-2B) The composition of the PDA medium is: glucose 2g, potato 20g (clarified liquid obtained from filter residue), crude Sea salt 0.3g, agar 1-1.5g, water 100mL; make a test t...

Embodiment 2

[0029] Tetrahydroxanthone dimer compounds dicerandrol A, dicerandrol B and deacetylphomoxanthone B on alpha 1 -Study on selective inhibition of AR subtypes:

[0030] 1. Strain cultivation and plasmid extraction: the corresponding plasmids (pGL4.29[luc2P / CRE / Hygro], pGL4.74[hRluc / TK], EX-A0967-M29, EX-Y3321-M29, EX-Y2008-M29 ) strains were added to LB liquid medium and cultured overnight; plasmids were extracted using a plasmid extraction kit (QIAprep Spin Miniprep Kit). And the plasmid concentration was measured with a miniature nucleic acid protein quantifier (Gene Company Limited, ND-100).

[0031] 2. Preparation of drug compound samples to be screened: Dissolve 1-2 mg of the pure compound in an appropriate amount of dimethyl sulfoxide to prepare a stock solution with a concentration of 2 mmol / L, take 0.5 uL to act on 99 uL containing transient cells In the culture medium, the final drug concentration was 10 μmol / L.

[0032] 3. Cell culture and plating: Take out HEK293 ce...

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Abstract

The invention relates to the field of new application of known compounds, and particularly discloses an application of a tetrahydroxanthone dimer compound to preparing an alpha1-AR adrenergic receptor antagonist medicine. On the basis of researches, the antagonism effect of the tetrahydroxanthone dimer compound on three adrenoreceptor alpha1-AR subtypes (alpha1A, alpha1B and alpha1D) is found for the first time, wherein the tetrahydroxanthone dimer compound dicerandrol B has the selective antagonism on the adrenoreceptor alpha1B-AR, and can be used for preparing a medicine for blood pressure reduction or benign prostatic hyperplasia treatment.

Description

technical field [0001] The present invention relates to the field of new uses of known compounds, more specifically, to tetrahydroxanthone dimer compounds in the preparation of alpha 1 -Application of AR adrenoceptor antagonist drugs. Background technique [0002] Since the discovery of cephalosporin antibiotics in the 1960s from Cephalosporium fungi off the coast of Sardinia, Italy, marine natural products have increasingly become a rich source of drugs. In 2012, Gerwick William H reported in "Chemistry & Biology" that there are currently 7 drugs from marine natural products, which were screened from 22,000 compounds, and an average of 1 drug was obtained from 3,142 marine natural product compounds, while the entire pharmaceutical industry field One drug is obtained from an average of 5,000-10,000 compounds. It can be seen that obtaining drugs from marine natural products has very important research value and significance. Marine fungi are an important source of marine na...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P9/12A61P13/08
Inventor 佘志刚丁博许芳陆勇军陈洪何磊
Owner SUN YAT SEN UNIV
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