Extract enriched in benzopyran lactone as well as preparation method and medical application of extract

A benzopyran lactone and extract technology, applied in the field of medicine, can solve the problems of increasing the difficulty of monomer purification and high cost, and achieve the effects of reducing nephrotoxicity, low cost and easy industrialization

Active Publication Date: 2018-05-04
南京道尔医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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

Method used

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  • Extract enriched in benzopyran lactone as well as preparation method and medical application of extract
  • Extract enriched in benzopyran lactone as well as preparation method and medical application of extract
  • Extract enriched in benzopyran lactone as well as preparation method and medical application of extract

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0034] Example 1: Preparation of extract 1

[0035] Including the following steps:

[0036] Step S1: pulverize the dried roots of Ligularia gracilis, extract with 75% ethanol, collect the extract, filter, and collect the filtrate;

[0037] Step S2, the filtrate is placed on a macroporous resin column, the model of the macroporous resin is D101, first eluted with 40% ethanol aqueous solution for 8 column volumes, and then with 60% ethanol aqueous solution to collect the 5-6 column volume eluate , Concentrated to obtain crude benzopyran lactone;

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

[0039] Step S4, acidic loop closure: after the pH of the filtrate is adjusted to 6.5, the filtrate is immediately filtered to obtain the second filtrate, and the second filtrate is allowed to stand at 4°C for cry...

Example Embodiment

[0042] Example 2: Preparation of extract 2

[0043] Including the following steps:

[0044] Step S1: pulverize the dried roots of Ligularia gracilis, extract with 75% ethanol, collect the extract, filter, and collect the filtrate;

[0045] Step S2, the filtrate is placed on a macroporous resin column, the model of the macroporous resin is D101, first eluted with 40% ethanol aqueous solution for 8 column volumes, and then eluted with 60% ethanol aqueous solution, collecting the 5-7th column volume eluate , Concentrated to obtain crude benzopyran lactone;

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

[0047] Step S4, acidic loop closure: after the pH of the filtrate is adjusted to 6.5, the filtrate is immediately filtered to obtain the second filtrate, and the second filtrate is allowed to stand at 4...

Example Embodiment

[0050] Example 3: Protective effect of the above extract 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 the Chinese 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 immunosorbent assay, Thermofisher, USA; Flow cytometer, BD, USA.

[0056] 2. Experimental method

[0057] 1. Cell culture and grouping

[0058] Take the well-growing HK-2 cells and suspend them in DMEM: HamsF-12 medium containing 10% FCS and 1% penicillin + streptomycin, to 6×10 7 / L cell suspension was seeded in 96-well plate, 100μL per well, at 37℃, 5% CO 2 After the cells are cultured for 24 hours in an environment of 100% humidity to adhere to the...

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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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IPC IPC(8): C07D493/04A61K31/37A61P39/02A61P13/12
CPCA61K31/37A61K36/28C07D493/04
Inventor 赵腾骅林溪王倩付俊毅
Owner 南京道尔医药科技有限公司
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