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An extract rich in benzopyranolactone, its preparation method and its medicinal use

A technology of benzopyranolactone and extract, which is applied in the field of medicine, can solve the problems of high cost and increase the difficulty of monomer purification, and achieve the effects of low cost, reduced nephrotoxicity and high content

Active Publication Date: 2018-09-04
南京道尔医药研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, from the above chemical structure, it can be known that petrogastrodin A, petrogastrodin B, and petrogastrodin C are isomers, and this structural similarity increases the difficulty of purification of monomers, and the cost of making monomers into medicines is too high. high

Method used

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  • An extract rich in benzopyranolactone, its preparation method and its medicinal use
  • An extract rich in benzopyranolactone, its preparation method and its medicinal use
  • An extract rich in benzopyranolactone, its preparation method and its medicinal use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1: the preparation of extract 1

[0035] Including the following steps:

[0036] Step S1, pulverizing the dried roots of Ligularia laminae, extracting with 75% ethanol, collecting the extract, filtering, and collecting the filtrate;

[0037] Step S2, put the filtrate on a macroporous resin column, the type of the macroporous resin is D101, first elute with 40% ethanol aqueous solution for 8 column volumes, then elute with 60% ethanol aqueous solution, and collect the eluate of the 5th to 6th column volume , concentrated to obtain crude benzopyranolactone;

[0038] Step S3, basic ring opening: the crude benzopyranolactone obtained in step S2 is ultrasonically suspended in a sodium hydroxide solution with a pH value of 8.0, filtered through a 0.45 μm filter membrane, and the filtrate is collected;

[0039] Step S4, acidic closed loop: after the pH of the filtrate is adjusted to 6.5, the second filtrate is obtained by filtering immediately, and the second filt...

Embodiment 2

[0042] Embodiment 2: the preparation of extract 2

[0043] Including the following steps:

[0044] Step S1, pulverizing the dried roots of Ligularia laminae, extracting with 75% ethanol, collecting the extract, filtering, and collecting the filtrate;

[0045] Step S2, put the filtrate on a macroporous resin column, the type of the macroporous resin is D101, first elute with 40% ethanol aqueous solution for 8 column volumes, then elute with 60% ethanol aqueous solution, and collect the eluate of the 5th to 7th column volume , concentrated to obtain crude benzopyranolactone;

[0046] Step S3, basic ring opening: the crude benzopyranolactone obtained in step S2 is ultrasonically suspended in a sodium hydroxide solution with a pH value of 8.0, filtered through a 0.45 μm filter membrane, and the filtrate is collected;

[0047] Step S4, acidic closed loop: after the pH of the filtrate is adjusted to 6.5, the second filtrate is obtained by filtering immediately, and the second filt...

Embodiment 3

[0050] Example 3: The protective effect of the above extracts on human renal tubular epithelial cell damage caused by aristolochic acid

[0051] 1. Experimental materials

[0052] Human renal tubular epithelial cell line (HK-2) was purchased from China Type Culture Collection;

[0053] Aristolochic acid-I (AA-I) was purchased from China Institute for the Control of Pharmaceutical and Biological Products;

[0054] Fetal calf serum (FCS), Gibico company; DMEM: HamsF-12 medium (Hyclone); Annexin-V kit, Invitrogen company;

[0055] Enzyme-linked immunoassay instrument, American Thermofisher Company; flow cytometer, American BD Company.

[0056] 2. Experimental method

[0057] 1. Cell culture and grouping

[0058] Well-grown HK-2 cells were taken, suspended in DMEM: HamsF-12 medium containing 10% FCS and 1% penicillin + streptomycin, and 6×10 7 / L cell suspension was inoculated in a 96-well plate, inoculated 100 μL per well, at 37°C, 5% CO 2 1. After culturing for 24 hours in...

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Abstract

The invention discloses an extract enriched in benzopyran lactone as well as a preparation method and medical application of the extract. The extract provided by the invention is enriched in gastrodinA, gastrodin B and gastrodin C, wherein the sum of contents of the three is not lower than 90%; or the extract is enriched in gastrodin A, gastrodin B, gastrodin C and gastrodin D, and the sum of contents of the four is not lower than 85%. The extract is clear in monomer composition, high in content and capable of easily controlling the quality, the renal toxicity of aristolochic acid can be reduced, and the extract can be used for preparing a single Chinese herb containing aristolochic acid or a traditional Chinese medicine tract or an attenuated drug of a traditional Chinese medicine compound preparation. According to the preparation method of the extract, disclosed by the invention, separation methods that are difficult to operate on a large scale in a factory, such as column chromatography on silica gel, do not need to be repeatedly used, the extract with the total content 85% or higher of effective monomer composition can be prepared by only passing through a primary macroporousresin and combining with pH regulation and control, and the preparation method is capable of easily realizing industrialization, simple in operation and low in cost.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to an extract rich in benzopyranolactone, a preparation method and a medical application. Background technique [0002] Ligastrodin A, Ligastrodin B, Ligastrodin C, and Ligastrodin are the first benzopyranolactone compounds isolated from the root of Ligusticum sativa, and their chemical structures are shown in the table below. [0003] [0004] The applicant has found that peturogastrodin A, peturogastrodin B, peturogastrodin C, and peturogastrodin can reduce the nephrotoxicity of aristolochic acid, and can be used to prepare single Chinese medicine or Chinese medicine extract containing aristolochic acid or Attenuated drugs of traditional Chinese medicine compound preparations (see the invention patent application submitted by the applicant, the application number is 2017112638286). [0005] However, from the above chemical structure, it can be known that petrogastrodin A, petrogastrodin ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61K31/37A61P39/02A61P13/12
CPCA61K31/37A61K36/28C07D493/04
Inventor 赵腾骅林溪王倩付俊毅
Owner 南京道尔医药研究院有限公司
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