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Method for biologic preparing 4, 4 dihydric bowel lactone from burdock glycoside

A technology of hydroxyenterolactone and arctiin, which is applied in the direction of drug combination, diseases, bone diseases, etc., can solve the problems of low conversion rate and unsuitable enterolactone, etc., and achieve high theoretical value and economic benefits

Inactive Publication Date: 2007-05-09
CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, arctigenin is not suitable as a prodrug of enterolactone due to the low conversion rate of arctigenin to enterolactone in intestinal bacteria

Method used

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  • Method for biologic preparing 4, 4 dihydric bowel lactone from burdock glycoside
  • Method for biologic preparing 4, 4 dihydric bowel lactone from burdock glycoside

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] 1. Strain cultivation:

[0022] Add 0.2 mg of arctiin to 20 mL of GAM broth medium, and then add 0.02 g of healthy 35°C anaerobic culture for 24 hours to obtain a culture solution. 10 mL of the culture solution was added to 90 mL of GAM broth medium containing 1.0 mg arctiin, and anaerobically cultured at 35° C. for 24 hours to obtain a bacterial culture solution, which was used as a strain.

[0023] 2. Preparation of 4,4'-dihydroxyenterolactone:

[0024] Add 50 mg of arctiin to 900 mL of GAM broth medium, then add 100 mL of the strain prepared in the above step (1), and culture anaerobically at 35° C. for 1 day. Extract with ethyl acetate, concentrate the extract under reduced pressure, separate and purify through a silica gel column to obtain 20 mg of 4,4'-dihydroxyenterolactone.

Embodiment 2

[0026] 1. Strain cultivation:

[0027] Add 2 mg of arctiin to 10 mL of GAM broth medium, then add 1.0 g of fresh feces from a healthy person, and culture it anaerobically at 37° C. for 24 hours to obtain a culture solution. 10 mL of this culture solution was added to 100 mL of GAM broth medium containing 20 mg arctiin, and cultured anaerobically at 37° C. for 36 hours. Then 100 mL of the culture solution was added to 400 mL of GAM broth medium containing 100 mg of arctiin, and anaerobically cultured at 37° C. for 36 hours to obtain 500 mL of a bacterial culture solution with enhanced activity. This bacterial culture solution was used as a strain.

[0028] 2. Preparation of 4,4'-dihydroxyenterolactone:

[0029] Add 500 mg of arctiin to 500 mL of GAM broth medium, then add 500 mL of the strain prepared in the above step (1), and culture anaerobically at 37° C. for 5 days. Extract with ethyl acetate, concentrate the extract under reduced pressure, separate and purify through a...

Embodiment 3

[0031] 1. Strain cultivation:

[0032] Add 10 mg of arctiin to 10 mL of GAM broth medium, then add 2.0 g of fresh feces from healthy people, and culture at 40° C. for 24 hours to obtain a culture solution.

[0033] 10 mL of the culture solution was added to 40 mL of GAM broth medium containing 40 mg arctiin, and cultured anaerobically at 40° C. for 48 hours. Then 50 mL of the culture solution was added to 50 mL of GAM broth medium containing 50 mg of arctiin, and cultured anaerobically at 37° C. for 48 hours. Then 100 mL of the culture solution was added to 100 mL of GAM broth medium containing 100 mg arctiin, and cultured anaerobically at 37° C. for 48 hours. Then 200 mL of the culture solution was added to 200 mL of GAM broth medium containing 200 mg of arctiin, and cultured anaerobically at 37° C. for 48 hours. Then 400 mL of the culture solution was added to 400 mL of GAM broth medium containing 400 mg arctiin, and anaerobically cultured at 37° C. for 48 hours to obtain ...

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Abstract

This invention relates to a method for preparing 4, 4'-dihydroxy enterolactone from arctiin. The method comprises: utilizing arctiin as the precursor compound, and converting arctiin into 4, 4'-dihydroxy enterolactone by intestinal bacteria in an anaerobic condition. 4, 4'-dihydroxy enterolactone is lignin compound, and can be converted into phytoestrogen (enterolactone) in human intestinal canals. The method simplifies the synthesis process of 4, 4'-dihydroxy enterolactone, widens the pharmaceutical applications of arctiin, and provides a new healthcare food for preventing and treating climacteric syndrome, osteoporosis, hyperlipemia, breast cancer and endometritis.

Description

technical field [0001] The invention relates to a method for biologically preparing 4,4'-dihydroxy enterolactone from arctiin. Background technique [0002] Phytoestrogens are a class of non-steroidal compounds, including isoflavones and lignans. Soybean isoflavones are the most thoroughly researched at present, and lignans were discovered late. The known lignans plants include linseed, Eucommia, Arctium, Acanthopanax, Magnolia officinalis, etc. The secoisolaricine diglycoside in flaxseed is used as adjuvant drug for cancer, and its metabolites enterodiol and enterolactone have a structure similar to that of estradiol, which can competitively bind with estrogen receptors to play a similar role. It has estrogen-like effects and has protective effects on menopausal syndrome, osteoporosis, and cardiovascular diseases. Hutchins et al. found that the excretion of lignans in urine of postmenopausal women is directly proportional to the dose-dependence of administration, and the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P17/04A61P15/12A61P19/10A61P35/00
Inventor 刘淑莹赵宇峰刘志强宋凤瑞
Owner CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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