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New lignan compounds, and preparation method and medical application thereof

A compound and drug technology, applied in the field of lignan compounds and their preparation, can solve the problems such as no medicinal records of Magnolia officinalis

Inactive Publication Date: 2015-12-16
WENZHOU HONGCHENGXIANG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no record of the medicinal use of Magnolia officinalis leaves in ancient and modern pharmacy monographs, and it is only used in folks to a certain extent.

Method used

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  • New lignan compounds, and preparation method and medical application thereof
  • New lignan compounds, and preparation method and medical application thereof
  • New lignan compounds, and preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0023] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0024] Preparation method: (a) crush the dry bark (8kg) of Magnolia officinalis, extract with 85% ethanol under heat reflux (25L×3 times), combine the extracts, concentrate to no alcohol smell (6L), and use petroleum ether ( 6L×3 times), ethyl acetate (6L×3 times) and water-saturated n-butanol (6L×3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract (355g) and n-butanol extract (b) In the step (a), the ethyl acetate extract is removed with AB-8 type macroporous resin, first eluted with 15% ethanol for 6 column volumes, then with 75% ethanol for 10 column volumes, and collected 75% ethanol e...

Embodiment 2

[0026] Embodiment 2: compound (I) pharmacological action test

[0027] 1. Materials and Instruments

[0028] Vascular endothelial cells (ECV-304) were donated by the Department of Immunology, School of Medicine, Shandong University. Compound (I) is self-made, the preparation method is shown in Example 1, and the HPLC normalized purity is greater than 98%. RPMI-1640 dry powder medium and trypsin were purchased from Gibeo, USA. Fetal bovine serum was purchased from Tianjin TBD Company. MTT, agarose, and AnnexinV-FITC were purchased from Sigma, USA. LDH, MDA, SOD, GSH-Px assay kits were purchased from Nanjing Jiancheng Bioengineering Institute. DMSO was purchased from China Pharmaceutical (Group) Shanghai Chemical Reagent Co., Ltd. Hematoxylin was purchased from Fuzhou Maixin Biotechnology Co., Ltd. Rhodamine123 was purchased from Solarbic Corporation of the United States. The positive drug ligustrazine was purchased from Shanghai Yuanye Biotechnology Co., Ltd.

[0029] I...

Embodiment 3

[0064] Preparation of tablets: firstly prepare compound (I) according to the method of Example 1, and utilize organic acids such as tartaric acid, or citric acid, formic acid or oxalic acid, etc., inorganic acids such as hydrochloric acid or sulfuric acid or phosphoric acid to make salts, according to its The weight ratio of the excipient to the excipient is 1:9, and the excipient is granulated and compressed into tablets.

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PUM

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Abstract

The invention discloses new lignan compounds, and a preparation method and medical application thereof. The lignan compounds are reported for the first time, have novel structure, and can be extracted, separated and purified from dry bark of Mangnolia officinalis. The in-vitro test proves that the compounds have a protective action on H2O2 oxidation damaged ECV-304 cells. The determination on cell supernatant MDA (malondialdehyde) content, SOD (superoxide dismutase) activity and GSH-Px (glutathione peroxidase) activity proves that the compounds (I) have the antioxidation characteristic of removing free radicals and active oxygen and can be used for developing vessel-protecting drugs.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a lignan compound with blood vessel protection effect isolated from the dry bark of Magnolia officinalis and a preparation method thereof. Background technique [0002] Magnolia officinalis, derived from the dry bark, bark and root bark of Magnolia officinalis Rehdet Wils. and Magnolia officinalis Rehd.et Wils.var.bilobaRehd.etWils. of Magnoliaceae Magnolia, mainly produced in Sichuan, Hubei, Zhejiang, Fujian and Anhui and so on. It was first recorded in "Shen Nong's Materia Medica", and was listed as a middle grade. Magnolia officinalis is a commonly used traditional Chinese medicine. It has the effects of aromatizing dampness, promoting qi and eliminating accumulation, drying dampness and eliminating fullness, reducing adverse events and relieving asthma. , chest fullness, wheezing and coughing and other symptoms. Magnolia officinalis is used as medicine in man...

Claims

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Application Information

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IPC IPC(8): C07C41/36C07C43/23A61K31/09A61P9/00
CPCC07C41/36C07C43/23
Inventor 叶澄
Owner WENZHOU HONGCHENGXIANG TECH
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